Identification

Name
Amitriptyline
Accession Number
DB00321  (APRD00227)
Type
Small Molecule
Groups
Approved
Description

Amitriptyline hydrochloride is a dibenzocycloheptene-derivative tricyclic antidepressant (TCA) and analgesic. TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, amitriptyline does not affect mood or arousal, but may cause sedation. In depressed individuals, amitriptyline exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Tertiary amine TCAs, such as amitriptyline, are more potent inhibitors of serotonin reuptake than secondary amine TCAs, such as nortriptyline. TCAs also down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine-H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. Amitriptyline may be used to treat depression, chronic pain (unlabeled use), irritable bowel syndrome (unlabeled use), diabetic neuropathy (unlabeled use), post-traumatic stress disorder (unlabeled use), and for migraine prophylaxis (unlabeled use).

Structure
Thumb
Synonyms
  • 10,11-dihydro-5-(gamma-Dimethylaminopropylidene)-5H-dibenzo(a,D)cycloheptene
  • 10,11-dihydro-N,N-Dimethyl-5H-dibenzo(a,D)heptalene-delta(5),gamma-propylamine
  • 3-(10,11-dihydro-5H-Dibenzo(a,D)cyclohepten-5-ylidene)-N,N-dimethyl-1-propanamine
  • 3-(10,11-dihydro-5H-Dibenzo[a,D]cyclohepten-5-ylidene)-N,N-dimethylpropan-1-amine
  • 5-(3-Dimethylaminopropylidene)-10,11-dihydro-5H-dibenzo(a,D)cycloheptatriene
  • 5-(3-Dimethylaminopropylidene)-10,11-dihydro-5H-dibenzo(a,D)cycloheptene
  • 5-(gamma-Dimethylaminopropylidene)-5H-dibenzo[a,D][1,4]cycloheptadiene
  • Amitriptilina
  • Amitriptylin
  • Amitriptyline
  • Amitriptylinum
External IDs
MK 230 / N 750 / Ro 4-1575
Product Ingredients
IngredientUNIICASInChI Key
Amitriptyline Hydrochloride26LUD4JO9K549-18-8KFYRPLNVJVHZGT-UHFFFAOYSA-N
Amitriptyline PamoateYX6VNM127F17086-03-2HBFZQWHVSYYTGA-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AmitriptylineTablet10 mgOralSivem Pharmaceuticals Ulc2016-02-11Not applicableCanada
AmitriptylineTablet50 mgOralSivem Pharmaceuticals Ulc2016-02-11Not applicableCanada
AmitriptylineTablet25 mgOralSivem Pharmaceuticals Ulc2016-02-11Not applicableCanada
Amitriptyline 10 TabTablet10 mgOralDuchesnay Inc.1981-12-312003-07-18Canada
Amitriptyline 25 TabTablet25 mgOralDuchesnay Inc.1981-12-312003-07-18Canada
Amitriptyline HCl Tab 25mgTablet25 mgOralD.C. Labs Limited1977-12-312003-07-11Canada
Amitriptyline HCl Tab 50mgTablet50 mgOralD.C. Labs Limited1977-12-312003-07-11Canada
Amitriptyline Tablets B.p 25mgTablet25 mgOralClonmel Healthcare Limited1992-12-311996-09-09Canada
Amitriptyline-10Tablet10 mgOralPro Doc Limitee1976-12-31Not applicableCanada
Amitriptyline-25Tablet25 mgOralPro Doc Limitee1976-12-31Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amitriptyline HydrochlorideTablet, film coated10 mg/1OralRebel Distributors1977-11-21Not applicableUs
Amitriptyline HydrochlorideTablet, film coated50 mg/1OralStat Rx USA1997-09-112018-02-08Us
Amitriptyline HydrochlorideTablet, film coated10 mg/1OralRed Pharm Drug, Inc.1977-11-21Not applicableUs
Amitriptyline HydrochlorideTablet, film coated75 mg/1OralLake Erie Medical Dba Quality Care Produts Llc2010-08-242017-01-25Us
Amitriptyline HydrochlorideTablet, film coated75 mg/1OralRemedy Repack2015-03-072017-12-22Us
Amitriptyline HydrochlorideTablet, film coated75 mg/1OralAidarex Pharmaceuticals LLC1997-09-11Not applicableUs
Amitriptyline HydrochlorideTablet, film coated50 mg/1OralZydus Pharmaceuticals Usa, Inc.2017-12-26Not applicableUs
Amitriptyline HydrochlorideTablet, film coated100 mg/1OralAccord Healthcare Limited2014-12-05Not applicableUs16729 0175 01 nlmimage10 933fc98e
Amitriptyline HydrochlorideTablet, film coated100 mg/1OralAmerincan Health Packaging2015-03-312017-02-09Us
Amitriptyline HydrochlorideTablet, film coated100 mg/1OralPreferreed Pharmaceuticals Inc.2011-06-09Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Apo Peram Tab 2-25Amitriptyline Hydrochloride (25 mg) + Perphenazine (2 mg)TabletOralApotex Corporation1977-12-312011-08-05Canada
Apo Peram Tab 3-15Amitriptyline Hydrochloride (15 mg) + Perphenazine (3 mg)TabletOralApotex Corporation1977-12-312011-08-05Canada
Chlordiazepoxide and Amitriptyline HClAmitriptyline Hydrochloride (25 mg/1) + Chlordiazepoxide (10 mg/1)TabletOralPar Pharmaceutical1988-05-09Not applicableUs
Chlordiazepoxide and Amitriptyline HClAmitriptyline Hydrochloride (12.5 mg/1) + Chlordiazepoxide (5 mg/1)TabletOralPar Pharmaceutical1988-05-09Not applicableUs
Chlordiazepoxide and Amitriptyline HydrochlorideAmitriptyline Hydrochloride (27.98 mg/1) + Chlordiazepoxide (10 mg/1)Tablet, film coatedOralMylan Pharmaceuticals1986-12-10Not applicableUs00378 0277 01 nlmimage10 74133a79
Chlordiazepoxide and Amitriptyline HydrochlorideAmitriptyline Hydrochloride (14 mg/1) + Chlordiazepoxide (5 mg/1)Tablet, film coatedOralMylan Pharmaceuticals1986-12-10Not applicableUs
Elavil Plus TabAmitriptyline Hydrochloride (25 mg) + Perphenazine (2 mg)TabletOralTriton Pharma Inc1973-12-312003-03-08Canada
Etrafon 2 10Amitriptyline Hydrochloride (10 mg) + Perphenazine (2 mg)TabletOralSchering Plough1970-12-312006-08-01Canada
Etrafon A TabAmitriptyline Hydrochloride (10 mg) + Perphenazine (4 mg)TabletOralSchering Plough1963-12-312007-08-03Canada
Etrafon D TabAmitriptyline Hydrochloride (25 mg) + Perphenazine (2 mg)TabletOralSchering Plough1963-12-312007-08-03Canada
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Equipto - Amitriptyline External Cream Compounding KitAmitriptylineKitTopicalAlvix Laboratories2015-01-202018-03-14Us
Sentravil PM-25Amitriptyline Hydrochloride + CholineKitPhysician Therapeutics Llc2011-07-072016-10-13Us
International/Other Brands
Adepril (Teofarma) / Amitryp (Raza) / Conmitrip (Condrugs) / Endep (Alphapharm) / Fiorda (Driburg) / Kamitrin (Saga) / Laroxyl (Deva) / Latilin (La Pharmaceuticals) / Maxitrip (Invision) / Redomex (Lundbeck) / Saroten (Lundbeck) / Sarotex (Lundbeck) / Sarotex Retard (Lundbeck) / Syneudon (Krewel Meuselbach) / Tryptanol (Merck Sharp & Dohme) / Tryptanol (Square) / Tryptizol (Algorithm) / Uxen Retard (Sanofi-Aventis)
Categories
UNII
1806D8D52K
CAS number
50-48-6
Weight
Average: 277.4033
Monoisotopic: 277.183049741
Chemical Formula
C20H23N
InChI Key
KRMDCWKBEZIMAB-UHFFFAOYSA-N
InChI
InChI=1S/C20H23N/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20/h3-6,8-12H,7,13-15H2,1-2H3
IUPAC Name
dimethyl(3-{tricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,11,13-hexaen-2-ylidene}propyl)amine
SMILES
CN(C)CCC=C1C2=CC=CC=C2CCC2=CC=CC=C12

Pharmacology

Indication
  • Indicated for the treatment of major depressive disorder in adults
  • Indicated for the management of neuropathic pain in adults
  • Indicated for the prophylactic treatment of chronic tension type headache (CTTH) in adults
  • Indicated for the prophylactic treatment of migraine in adults
  • Indicated for the the treatment of nocturnal enuresis in children aged 6 years and above when organic pathology, including spina bifida and related disorders, have been excluded and no response has been achieved to all other non-drug and drug treatments, including antispasmodics and vasopressin-related products. This medicinal product should only be prescribed by a healthcare professional with expertise in the management of persistent enuresis. -Other off-label uses include irritable bowel syndrome, sleep disorders, diabetic neuropathy, agitation and insomnia
Structured Indications
Pharmacodynamics

Amitriptyline, a tertiary amine tricyclic antidepressant, is structurally related to both the skeletal muscle relaxant cyclobenzaprine and the thioxanthene antipsychotics such as thiothixene. It is extremely sedating, and thus improvement of sleep patterns can be the first benefit of treatment. Amitriptyline exhibits strong anticholinergic activity, cardiovascular effects including orthostatic hypotension, changes in heart rhythm and conduction, and a lowering of the seizure threshold. As with other antidepressants, several weeks of therapy may be required in order to realize the full clinical benefit of amitriptyline. Although not a labelled indication, amitriptyline is widely used in the management of chronic nonmalignant pain (e.g., post-herpetic neuralgia, fibromyalgia).

Mechanism of action

Amitriptyline has anticholinergic and sedative properties. It is metabolized to nortriptyline which inhibits the reuptake of norepinephrine and serotonin almost equally. Amitriptyline inhibits the membrane pump mechanism responsible for uptake of norepinephrine and serotonin in adrenergic and serotonergic neurons [FDA Label]. Pharmacologically this action may potentiate or prolong neuronal activity since reuptake of these biogenic amines is important physiologically in terminating transmitting activity. This interference with the reuptake of norepinephrine and/or serotonin is believed by some to underlie the antidepressant activity of amitriptyline. There is some evidence in literature that neuronal and glial plasticity may be a critical action mediated by antidepressants via production of neurotrophic factors, such as GDNF, that promote neurogenesis, gliogenesis, development, plasticity, and survival [2]. In a study involving C6 glioma cells and normal human astrocytes, amitriptyline may activate the FGFR/FRS2α/ERK/CREB signaling cascade, thus resulting in GDNF production [2].

Amitriptyline displays affinity for muscarinic and histamine H1 receptors [FDA Label]. At both central and spinal cord level, amitriptyline exhibits ion-channel blocking effects on sodium, potassium and NMDA channel [FDA Label]. The noradrenaline, sodium and the NMDA effects are mechanisms known to be involved in the maintenance of neuropathic pain, chronic tension type headache prophylaxis and migraine prophylaxis [FDA Label]. In cultured rat cortical neurons, amitriptyline blocked sodium channel current (I(Na)) in a concentration-dependent, not voltage-dependent manner and reduced mRNA expression of sodium channels [3]. This may explain the actions of amitriptyline leading to migraine prophylaxis.

TargetActionsOrganism
ASodium-dependent noradrenaline transporter
inhibitor
Human
ASodium-dependent serotonin transporter
inhibitor
Human
A5-hydroxytryptamine receptor 2A
antagonist
Human
U5-hydroxytryptamine receptor 1A
inhibitor
Human
UDelta-type opioid receptor
agonist
Human
UKappa-type opioid receptor
agonist
Human
UHigh affinity nerve growth factor receptor
agonist
Human
UBDNF/NT-3 growth factors receptor
agonist
Human
NAlpha-1A adrenergic receptor
antagonist
Human
NAlpha-1D adrenergic receptor
antagonist
Human
NAlpha-2A adrenergic receptor
antagonist
Human
NHistamine H1 receptor
antagonist
Human
NMuscarinic acetylcholine receptor M1
antagonist
Human
NMuscarinic acetylcholine receptor M2
antagonist
Human
NMuscarinic acetylcholine receptor M3
antagonist
Human
NMuscarinic acetylcholine receptor M4
antagonist
Human
NMuscarinic acetylcholine receptor M5
antagonist
Human
NPotassium voltage-gated channel subfamily KQT member 2
inhibitor
Human
NPotassium voltage-gated channel subfamily A member 1
inhibitor
Human
NPotassium voltage-gated channel subfamily D member 2
inhibitor
Human
NPotassium voltage-gated channel subfamily D member 3
inhibitor
Human
UHistamine H2 receptor
blocker
Human
UHistamine H4 receptor
binder
Human
USigma non-opioid intracellular receptor 1
agonist
Human
U5-hydroxytryptamine receptor 2C
binder
Human
UAlpha-1B adrenergic receptor
antagonist
Human
U5-hydroxytryptamine receptor 7
antagonist
Human
U5-hydroxytryptamine receptor 1D
binder
Human
UMu-type opioid receptor
binder
Human
U5-hydroxytryptamine receptor 1B
binder
Human
U5-hydroxytryptamine receptor 6
antagonist
Human
UPotassium voltage-gated channel subfamily KQT member 3Not AvailableHuman
UBeta adrenergic receptor
binder
Human
Absorption

Rapidly and well absorbed following oral administration (bioavailability is 30-60% due to first pass metabolism). Peak plasma concentrations occur 2-12 hours following oral or intramuscular administration. Amitriptyline and the main metabolite nortriptyline pass across the placental barrier and small amounts can be excreted with the breast milk [FDA Label].

Volume of distribution

The apparent volume of distribution (Vd)β estimated after intravenous administration is 1221 L±280 L; range 769-1702 L (16±3 L/kg) [FDA Label].

Protein binding

Very highly protein bound (95%) in plasma and tissues [FDA Label].

Metabolism

Amitriptyline undergoes hepatic metabolism that mainly involves demethylation. Demethylation leads to the formation of its primary active metabolite, nortriptyline. This secondary amine retains a pharmacological activity. It can further undergo hydroxylation (mediated by CYP2D6) followed by conjugation with glucuronic acid. Other isozymes involved are CYP1A2 and CYP2C9. The metabolism is subject to genetic polymorphism [FDA Label].

Other metabolites such as cis- and trans-10-hydroxyamitriptyline and cis- and trans-10-hydroxynortriptyline have the same profile as nortriptyline but is considerably weaker.Demethylnortriptyline and amitriptyline N oxide are only present in plasma in minute amounts; the latter is almost inactive. All the metabolites are less anticholinergic than amitriptyline and nortriptyline. In plasma the amount of total 10-hydroxynortriptyline dominates but most of the metabolites are conjugated [FDA Label].

Route of elimination

Amitriptyline and its metabolites are mainly excreted in the urine. Virtually the entire dose is excreted as glucuronide or sulfate conjugate of metabolites, with about 2% of unchanged drug appearing in the urine [FDA Label]. 25-50% of a single orally administered dose is excreted in urine as inactive metabolites within 24 hours. Small amounts are excreted in feces via biliary elimination.

Half life

The elimination half-life (t1⁄2 β) amitriptyline after peroral administration is about 25 hours (24.65 ± 6.31 hours; range 16.49-40.36 hours) [FDA Label].

Clearance

The mean systemic clearance (Cls) is 39.24 ± 10.18 L/h, range 24.53-53.73 L/h [FDA Label].

Toxicity

LD50=350 mg/kg (in mice). Symptoms of overdose include abnormally low blood pressure, confusion, convulsions, dilated pupils and other eye problems, disturbed concentration, drowsiness, hallucinations, impaired heart function, rapid or irregular heartbeat, reduced body temperature, stupor, and unresponsiveness or coma. Side effects include: sedation, hypotension, blurred vision, dry mouth, constipation, urinary retention, postural hypotension, tachycardia, hypertension, ECG changes, heart failure, impaired memory and delirium, and precipitation of hypomanic or manic episodes in bipolar depression. Withdrawal symptoms include gastrointestinal disturbances, anxiety, and insomnia.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 2D6CYP2D6*4(A;A)A AlleleEffect Directly StudiedPatients with this genotype have reduced metabolism of amitriptyline.Details
Multidrug resistance protein 1---(C;C) / (C;T)C AlleleEffect Directly StudiedPatients with this genotype have an increased likelihood of remission when using amitriptyline to treat major depressive disorderDetails
Cytochrome P450 2C19CYP2C19*2(A;A) / (A;G)G > ADirectly Studied EffectPatients with this genotype have reduced metabolism of amitriptyline.Details
Multidrug resistance protein 1---(C;C) / (C;T)T > CEffect Directly StudiedPatients with this genotype have increased risk of adverse events with amitriptylineDetails
Cytochrome P450 2D6CYP2D6*3Not Available2549delAEffect Directly StudiedThe presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of amitriptyline.Details
Cytochrome P450 2D6CYP2D6*4Not AvailableA alleleEffect Directly StudiedThe presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of amitriptyline.Details
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole-gene deletionEffect Directly StudiedThe presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of amitriptyline.Details
Cytochrome P450 2D6CYP2D6*6Not Available1707delTEffect Directly StudiedThe presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of amitriptyline.Details
Cytochrome P450 2C19CYP2C19*2Not Available681G>AEffect Directly StudiedThe presence of this polymorphism in CYP2C19 is associated with poor metabolism of amitriptyline.Details
Cytochrome P450 2C19CYP2C19*3Not Available636G>AEffect Directly StudiedThe presence of this polymorphism in CYP2C19 is associated with reduced or poor metabolism of amitriptyline.Details
Cytochrome P450 2D6CYP2D6*7Not Available2935A>CEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*8Not Available1758G>TEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*11Not Available883G>CEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*12Not Available124G>AEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*13Not AvailableCYP2D7/2D6 hybrid gene structureEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*14ANot Available1758G>AEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*15Not Available137insT, 137_138insTEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*19Not Available2539_2542delAACTEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*20Not Available1973_1974insGEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*21Not Available2573insCEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*31Not Available-1770G>A / -1584C>G  … show all Effect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*36Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*38Not Available2587_2590delGACTEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*40Not Available1863_1864ins(TTT CGC CCC)2Effect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*42Not Available3259_3260insGTEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*44Not Available2950G>CEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*47Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*51Not Available-1584C>G / -1235A>G  … show all Effect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*56Not Available3201C>TEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*57Not Available100C>T / 310G>T  … show all Effect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*62Not Available4044C>TEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*68ANot Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*68BNot AvailableSimilar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4.Effect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*69Not Available2988G>A / -1426C>T  … show all Effect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*92Not Available1995delCEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*100Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*101Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer. For individual with two non-functional alleles, alternative drug or dose reduction recommended.Details
Cytochrome P450 2C19CYP2C19*2ANot Available681G>AEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, dose reduction recommended.Details
Cytochrome P450 2C19CYP2C19*2BNot Available681G>AEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, dose reduction recommended.Details
Cytochrome P450 2C19CYP2C19*4Not Available1A>GEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, dose reduction recommended.Details
Cytochrome P450 2C19CYP2C19*5Not Available1297C>TEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, dose reduction recommended.Details
Cytochrome P450 2C19CYP2C19*6Not Available395G>AEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, dose reduction recommended.Details
Cytochrome P450 2C19CYP2C19*7Not Available19294T>AEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, dose reduction recommended.Details
Cytochrome P450 2C19CYP2C19*22Not Available557G>C / 991A>GEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, dose reduction recommended.Details
Cytochrome P450 2C19CYP2C19*24Not Available99C>T / 991A>G  … show all Effect InferredPoor drug metabolizer. For individual with two non-functional alleles, dose reduction recommended.Details
Cytochrome P450 2C19CYP2C19*35Not Available12662A>GEffect InferredPoor drug metabolizer. For individual with two non-functional alleles, dose reduction recommended.Details
Cytochrome P450 2D6CYP2D6*3Not AvailableC alleleEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole-gene deletionEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*6Not Available1707delTEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*7Not Available2935A>CEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*8Not Available1758G>TEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*11Not Available883G>CEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*12Not Available124G>AEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*13Not AvailableCYP2D7/2D6 hybrid gene structureEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*14ANot Available1758G>AEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*15Not Available137insT, 137_138insTEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*19Not Available2539_2542delAACTEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*20Not Available1973_1974insGEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*21Not Available2573insCEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*31Not Available-1770G>A / -1584C>G  … show all Effect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*36Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*38Not Available2587_2590delGACTEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*40Not Available1863_1864ins(TTT CGC CCC)2Effect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*42Not Available3259_3260insGTEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*44Not Available2950G>CEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*47Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*51Not Available-1584C>G / -1235A>G  … show all Effect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*56Not Available3201C>TEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*57Not Available100C>T / 310G>T  … show all Effect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*62Not Available4044C>TEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*68ANot Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*68BNot AvailableSimilar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4.Effect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*69Not Available2988G>A / -1426C>T  … show all Effect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*92Not Available1995delCEffect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*100Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2D6CYP2D6*101Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, lower dose requirements, higher risk for adverse side effectsDetails
Cytochrome P450 2C19CYP2C19*2ANot Available681G>AADR InferredThose with the AA or AG genotype are poor metabolizers of amitriptylineDetails
Cytochrome P450 2C19CYP2C19*2BNot Available681G>AADR InferredThose with the AA or AG genotype are poor metabolizers of amitriptylineDetails
Cytochrome P450 2C19CYP2C19*3Not Available636G>AADR InferredThose with the AA or AG genotype are poor metabolizers of amitriptylineDetails
Cytochrome P450 2C19CYP2C19*4Not Available1A>GADR InferredThose with the AA or AG genotype are poor metabolizers of amitriptylineDetails
Cytochrome P450 2C19CYP2C19*5Not Available1297C>TADR InferredThose with the AA or AG genotype are poor metabolizers of amitriptylineDetails
Cytochrome P450 2C19CYP2C19*6Not Available395G>AADR InferredThose with the AA or AG genotype are poor metabolizers of amitriptylineDetails
Cytochrome P450 2C19CYP2C19*7Not Available19294T>AADR InferredThose with the AA or AG genotype are poor metabolizers of amitriptylineDetails
Cytochrome P450 2C19CYP2C19*22Not Available557G>C / 991A>GADR InferredThose with the AA or AG genotype are poor metabolizers of amitriptylineDetails
Cytochrome P450 2C19CYP2C19*24Not Available99C>T / 991A>G  … show all ADR InferredThose with the AA or AG genotype are poor metabolizers of amitriptylineDetails
Cytochrome P450 2C19CYP2C19*35Not Available12662A>GADR InferredThose with the AA or AG genotype are poor metabolizers of amitriptylineDetails
Cytochrome P450 2D6CYP2D6*3Not AvailableG alleleEffect Directly StudiedThe presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of amitriptyline.Details
Cytochrome P450 2D6CYP2D6*4Not Available3877G>AEffect Directly StudiedThe presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of amitriptyline.Details

Interactions

Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe serum concentration of Amitriptyline can be increased when it is combined with 1,10-Phenanthroline.Experimental
2,5-Dimethoxy-4-ethylamphetamineAmitriptyline may increase the stimulatory activities of 2,5-Dimethoxy-4-ethylamphetamine.Experimental, Illicit
2,5-Dimethoxy-4-ethylthioamphetamineAmitriptyline may increase the stimulatory activities of 2,5-Dimethoxy-4-ethylthioamphetamine.Experimental
3,4-DichloroisocoumarinThe serum concentration of Amitriptyline can be increased when it is combined with 3,4-Dichloroisocoumarin.Experimental
3,4-MethylenedioxyamphetamineAmitriptyline may increase the stimulatory activities of 3,4-Methylenedioxyamphetamine.Experimental, Illicit
4-(2-Aminoethyl)Benzenesulfonyl FluorideThe serum concentration of Amitriptyline can be increased when it is combined with 4-(2-Aminoethyl)Benzenesulfonyl Fluoride.Experimental
4-Bromo-2,5-dimethoxyamphetamineAmitriptyline may increase the stimulatory activities of 4-Bromo-2,5-dimethoxyamphetamine.Experimental, Illicit
4-MethoxyamphetamineAmitriptyline may decrease the antihypertensive activities of 4-Methoxyamphetamine.Experimental, Illicit
7-NitroindazoleThe risk or severity of adverse effects can be increased when Amitriptyline is combined with 7-Nitroindazole.Experimental
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the serotonergic activities of Amitriptyline.Experimental
AbirateroneThe serum concentration of Amitriptyline can be increased when it is combined with Abiraterone.Approved
AcenocoumarolAmitriptyline may increase the anticoagulant activities of Acenocoumarol.Approved, Investigational
AcepromazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Aceprometazine.Approved
AcetophenazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Acetophenazine.Approved
AdipiplonThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Adipiplon.Investigational
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Amitriptyline.Approved
AgmatineAmitriptyline may decrease the antihypertensive activities of Agmatine.Experimental, Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Agomelatine.Approved, Investigational
AlaproclateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Alaproclate.Experimental
AlfaxaloneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Amitriptyline.Approved, Illicit
AllopregnanoloneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Allopregnanolone.Investigational
AlmotriptanThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Almotriptan.Approved, Investigational
AlogliptinThe serum concentration of Amitriptyline can be increased when it is combined with Alogliptin.Approved
Alpha-1-proteinase inhibitorThe serum concentration of Amitriptyline can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Alphaprodine.Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Amitriptyline.Approved, Illicit, Investigational
AltretamineAltretamine may increase the orthostatic hypotensive activities of Amitriptyline.Approved
AmiodaroneThe metabolism of Amitriptyline can be decreased when combined with Amiodarone.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Amisulpride.Approved, Investigational
AmobarbitalThe metabolism of Amitriptyline can be increased when combined with Amobarbital.Approved, Illicit
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Amitriptyline.Approved, Investigational
AmoxapineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Amperozide.Experimental
AmphetamineAmphetamine may increase the serotonergic activities of Amitriptyline.Approved, Illicit, Investigational
AmprenavirThe serum concentration of Amitriptyline can be increased when it is combined with Amprenavir.Approved, Investigational
AnagrelideAmitriptyline may increase the QTc-prolonging activities of Anagrelide.Approved
Antithrombin III humanThe serum concentration of Amitriptyline can be increased when it is combined with Antithrombin III human.Approved
ApalutamideThe serum concentration of Amitriptyline can be decreased when it is combined with Apalutamide.Approved, Investigational
ApixabanThe serum concentration of Amitriptyline can be increased when it is combined with Apixaban.Approved
ApomorphineAmitriptyline may decrease the antihypertensive activities of Apomorphine.Approved, Investigational
ApraclonidineAmitriptyline may decrease the antihypertensive activities of Apraclonidine.Approved
AprepitantThe serum concentration of Amitriptyline can be increased when it is combined with Aprepitant.Approved, Investigational
AprotininThe serum concentration of Amitriptyline can be increased when it is combined with Aprotinin.Approved, Investigational, Withdrawn
ArbutamineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Arbutamine.Approved
ArformoterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Arformoterol.Approved, Investigational
ArgatrobanThe serum concentration of Amitriptyline can be increased when it is combined with Argatroban.Approved, Investigational
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Amitriptyline.Approved, Investigational
ArmodafinilThe metabolism of Amitriptyline can be decreased when combined with Armodafinil.Approved, Investigational
Arsenic trioxideAmitriptyline may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherAmitriptyline may increase the QTc-prolonging activities of Artemether.Approved
ArticaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Articaine.Approved
AsenapineAmitriptyline may increase the QTc-prolonging activities of Asenapine.Approved
AsunaprevirThe serum concentration of Amitriptyline can be increased when it is combined with Asunaprevir.Approved, Investigational, Withdrawn
AtazanavirThe metabolism of Amitriptyline can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Amitriptyline can be decreased when combined with Atomoxetine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Azaperone.Investigational, Vet Approved
AzelastineAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzithromycinThe metabolism of Amitriptyline can be decreased when combined with Azithromycin.Approved
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Amitriptyline.Approved
BambuterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Bambuterol.Approved, Investigational
BarbexacloneThe metabolism of Amitriptyline can be increased when combined with Barbexaclone.Experimental
BarbitalThe metabolism of Amitriptyline can be increased when combined with Barbital.Illicit
BatimastatThe serum concentration of Amitriptyline can be increased when it is combined with Batimastat.Experimental
BedaquilineAmitriptyline may increase the QTc-prolonging activities of Bedaquiline.Approved
BenazeprilThe serum concentration of Amitriptyline can be increased when it is combined with Benazepril.Approved, Investigational
BenmoxinBenmoxin may increase the serotonergic activities of Amitriptyline.Withdrawn
BenperidolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Benperidol.Approved, Investigational
BenzamidineThe serum concentration of Amitriptyline can be increased when it is combined with Benzamidine.Experimental
BenzocaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Benzocaine.Approved, Investigational
BenzphetamineAmitriptyline may decrease the antihypertensive activities of Benzphetamine.Approved, Illicit
Benzyl alcoholThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Benzyl alcohol.Approved
BetaxololThe metabolism of Amitriptyline can be decreased when combined with Betaxolol.Approved, Investigational
BethanidineAmitriptyline may decrease the antihypertensive activities of Bethanidine.Approved
BifeprunoxThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Bifeprunox.Investigational
BivalirudinThe serum concentration of Amitriptyline can be increased when it is combined with Bivalirudin.Approved, Investigational
BoceprevirThe metabolism of Amitriptyline can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Amitriptyline can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Amitriptyline can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Amitriptyline.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Amitriptyline.Approved, Investigational
BrexpiprazoleThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Brexpiprazole.Approved, Investigational
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.Approved
BrofaromineBrofaromine may increase the serotonergic activities of Amitriptyline.Experimental
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Amitriptyline.Approved, Illicit, Investigational
BromisovalThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Bromisoval.Experimental
BromocriptineAmitriptyline may decrease the antihypertensive activities of Bromocriptine.Approved, Investigational
BromperidolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Bromperidol.Approved, Investigational
BrompheniramineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Brompheniramine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Brotizolam.Approved, Investigational, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Bupivacaine.Approved, Investigational
BuprenorphineAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Amitriptyline can be decreased when combined with Bupropion.Approved
BuspironeThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Buspirone.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Amitriptyline.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Butalbital is combined with Amitriptyline.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Butamben.Approved, Withdrawn
ButaperazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Butaperazine.Experimental
ButethalThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Butethal.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Amitriptyline.Approved, Illicit, Vet Approved
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Amitriptyline.Approved
CaffeineThe metabolism of Amitriptyline can be decreased when combined with Caffeine.Approved
CamostatThe serum concentration of Amitriptyline can be increased when it is combined with Camostat.Experimental
CandoxatrilThe serum concentration of Amitriptyline can be increased when it is combined with Candoxatril.Experimental
CandoxatrilatThe serum concentration of Amitriptyline can be increased when it is combined with Candoxatrilat.Experimental
CanertinibThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Canertinib.Investigational
CapecitabineThe metabolism of Amitriptyline can be decreased when combined with Capecitabine.Approved, Investigational
CaptoprilThe serum concentration of Amitriptyline can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Amitriptyline can be increased when combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Carbinoxamine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Carfentanil.Illicit, Investigational, Vet Approved
CariprazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Cariprazine.Approved, Investigational
CarisoprodolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Carisoprodol.Approved
CaroxazoneCaroxazone may increase the serotonergic activities of Amitriptyline.Withdrawn
CelecoxibThe metabolism of Amitriptyline can be decreased when combined with Celecoxib.Approved, Investigational
CeliprololThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Celiprolol.Approved, Investigational
CeritinibThe serum concentration of Amitriptyline can be increased when it is combined with Ceritinib.Approved
CetirizineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Cetirizine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Chloral hydrate.Approved, Illicit, Investigational, Vet Approved
ChloramphenicolThe metabolism of Amitriptyline can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Amitriptyline.Approved, Illicit, Investigational
ChlormezanoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Chlormezanone.Approved, Investigational, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Chloroprocaine.Approved
ChloroquineThe metabolism of Amitriptyline can be decreased when combined with Chloroquine.Approved, Investigational, Vet Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Chlorphenamine.Approved
ChlorphentermineAmitriptyline may increase the stimulatory activities of Chlorphentermine.Illicit, Withdrawn
ChlorproethazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Chlorproethazine.Experimental
ChlorpromazineThe metabolism of Amitriptyline can be decreased when combined with Chlorpromazine.Approved, Investigational, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Chlorprothixene.Approved, Investigational, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Chlorzoxazone.Approved
CholecalciferolThe metabolism of Amitriptyline can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholesterolThe serum concentration of Amitriptyline can be increased when it is combined with Cholesterol.Approved, Experimental, Investigational
ChymostatinThe serum concentration of Amitriptyline can be increased when it is combined with Chymostatin.Experimental
CilastatinThe serum concentration of Amitriptyline can be increased when it is combined with Cilastatin.Approved, Investigational
CilazaprilThe serum concentration of Amitriptyline can be increased when it is combined with Cilazapril.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Amitriptyline.Approved, Investigational
CimetidineThe metabolism of Amitriptyline can be decreased when combined with Cimetidine.Approved, Investigational
CinacalcetThe serum concentration of Amitriptyline can be increased when it is combined with Cinacalcet.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Cinchocaine.Approved, Vet Approved
CiprofloxacinAmitriptyline may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CirazolineAmitriptyline may increase the vasopressor activities of Cirazoline.Experimental
CisaprideAmitriptyline may increase the arrhythmogenic activities of Cisapride.Approved, Investigational, Withdrawn
CitalopramThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Citalopram.Approved
ClarithromycinThe metabolism of Amitriptyline can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Amitriptyline can be decreased when combined with Clemastine.Approved, Investigational
ClenbuterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Clenbuterol.Approved, Investigational, Vet Approved
ClidiniumThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Clidinium.Approved
ClobazamThe metabolism of Amitriptyline can be decreased when combined with Clobazam.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when Amitriptyline is combined with clomethiazole.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Clomipramine.Approved, Investigational, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Clonazepam.Approved, Illicit
ClonidineAmitriptyline may decrease the antihypertensive activities of Clonidine.Approved
ClopenthixolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Clopenthixol.Experimental
ClopidogrelThe metabolism of Amitriptyline can be decreased when combined with Clopidogrel.Approved
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Amitriptyline.Approved, Illicit
ClorindioneAmitriptyline may increase the anticoagulant activities of Clorindione.Experimental
ClothiapineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Clothiapine.Experimental
ClotrimazoleThe metabolism of Amitriptyline can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Amitriptyline can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Amitriptyline can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Amitriptyline can be decreased when combined with Cocaine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Amitriptyline.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Amitriptyline.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Amitriptyline.Approved, Investigational
CrisaboroleThe metabolism of Amitriptyline can be decreased when combined with Crisaborole.Approved, Investigational
CrizotinibThe metabolism of Amitriptyline can be decreased when combined with Crizotinib.Approved
CyamemazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Cyamemazine.Approved
CyclizineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Cyclizine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Cyclobenzaprine.Approved
CyclopropaneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Cyclopropane.Experimental
CyclosporineThe metabolism of Amitriptyline can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Cyproheptadine.Approved
Cyproterone acetateThe serum concentration of Amitriptyline can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Amitriptyline.Approved
DabrafenibThe serum concentration of Amitriptyline can be decreased when it is combined with Dabrafenib.Approved, Investigational
DantroleneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dantrolene.Approved, Investigational
DapiprazoleThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dapiprazole.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Amitriptyline.Investigational
DarexabanThe serum concentration of Amitriptyline can be increased when it is combined with Darexaban.Investigational
DarifenacinThe metabolism of Amitriptyline can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Amitriptyline can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Amitriptyline can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Amitriptyline can be decreased when it is combined with Deferasirox.Approved, Investigational
DelanzomibThe serum concentration of Amitriptyline can be increased when it is combined with Delanzomib.Investigational
DelaprilThe serum concentration of Amitriptyline can be increased when it is combined with Delapril.Experimental
DelavirdineThe metabolism of Amitriptyline can be decreased when combined with Delavirdine.Approved
DeramciclaneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Amitriptyline.Approved
DesipramineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Desipramine.Approved, Investigational
DesloratadineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Desloratadine.Approved, Investigational
DesmopressinThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Desmopressin.Approved
DesvenlafaxineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Desvenlafaxine.Approved, Investigational
DetomidineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Detomidine.Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dexbrompheniramine.Approved
DexmedetomidineAmitriptyline may decrease the antihypertensive activities of Dexmedetomidine.Approved, Vet Approved
DexmethylphenidateThe risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with Amitriptyline.Approved, Investigational
DextroamphetamineAmitriptyline may increase the stimulatory activities of Dextroamphetamine.Approved, Illicit
DextromethorphanThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dextromethorphan.Approved
DextromoramideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dezocine.Approved, Investigational
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Amitriptyline.Approved, Illicit, Investigational, Vet Approved
DicoumarolAmitriptyline may increase the anticoagulant activities of Dicoumarol.Approved
Diethyl etherThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Diethyl ether.Experimental
DiethylpropionAmitriptyline may increase the stimulatory activities of Diethylpropion.Approved, Illicit
DifenoxinThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Amitriptyline.Approved, Illicit
DihydroergotamineAmitriptyline may decrease the antihypertensive activities of Dihydroergotamine.Approved, Investigational
DihydroetorphineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dihydromorphine.Experimental, Illicit
DiltiazemThe metabolism of Amitriptyline can be decreased when combined with Diltiazem.Approved, Investigational
DimenhydrinateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dimenhydrinate.Approved
DiphenadioneAmitriptyline may increase the anticoagulant activities of Diphenadione.Experimental
DiphenhydramineThe metabolism of Amitriptyline can be decreased when combined with Diphenhydramine.Approved, Investigational
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Amitriptyline.Approved, Illicit
DipivefrinAmitriptyline may decrease the antihypertensive activities of Dipivefrin.Approved
DisopyramideAmitriptyline may increase the QTc-prolonging activities of Disopyramide.Approved
DixyrazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dixyrazine.Experimental
DobutamineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dobutamine.Approved
DofetilideAmitriptyline may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
DolasetronAmitriptyline may increase the QTc-prolonging activities of Dolasetron.Approved, Investigational
DomperidoneAmitriptyline may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DoramectinThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Doramectin.Vet Approved
DosulepinThe metabolism of Amitriptyline can be decreased when combined with Dosulepin.Approved
DoxepinThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Doxepin.Approved, Investigational
DoxofyllineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Doxofylline.Approved, Investigational
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Amitriptyline.Approved, Investigational
DoxorubicinThe metabolism of Amitriptyline can be decreased when combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Amitriptyline can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Amitriptyline is combined with DPDPE.Experimental
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.Approved, Illicit
DronedaroneAmitriptyline may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Drotebanol.Experimental, Illicit
DroxidopaAmitriptyline may decrease the antihypertensive activities of Droxidopa.Approved, Investigational
DuloxetineDuloxetine may increase the serotonergic activities of Amitriptyline.Approved
DyclonineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Dyclonine.Approved
EcabetThe serum concentration of Amitriptyline can be increased when it is combined with Ecabet.Approved, Investigational
EcgonineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ecgonine.Experimental, Illicit
EcopipamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ecopipam.Investigational
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Amitriptyline.Approved
EfavirenzThe metabolism of Amitriptyline can be decreased when combined with Efavirenz.Approved, Investigational
ElafinThe serum concentration of Amitriptyline can be increased when it is combined with Elafin.Investigational
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Amitriptyline.Approved, Investigational
EliglustatAmitriptyline may increase the QTc-prolonging activities of Eliglustat.Approved
EltanoloneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Eltanolone.Investigational
EnalaprilThe serum concentration of Amitriptyline can be increased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe serum concentration of Amitriptyline can be increased when it is combined with Enalaprilat.Approved
EnalkirenThe serum concentration of Amitriptyline can be increased when it is combined with Enalkiren.Experimental
EnfluraneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Enflurane.Approved, Investigational, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Entacapone.Approved, Investigational
EnzalutamideThe serum concentration of Amitriptyline can be decreased when it is combined with Enzalutamide.Approved
EphedraAmitriptyline may decrease the antihypertensive activities of Ephedra.Approved, Nutraceutical, Withdrawn
Epigallocatechin GallateThe serum concentration of Amitriptyline can be increased when it is combined with Epigallocatechin Gallate.Investigational
EpinephrineAmitriptyline may decrease the antihypertensive activities of Epinephrine.Approved, Vet Approved
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ergoloid mesylate.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ergonovine.Approved
ErgotamineAmitriptyline may decrease the antihypertensive activities of Ergotamine.Approved
ErythromycinThe metabolism of Amitriptyline can be decreased when combined with Erythromycin.Approved, Investigational, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe metabolism of Amitriptyline can be decreased when combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Amitriptyline can be decreased when combined with Esomeprazole.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Amitriptyline.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Amitriptyline.Approved, Investigational
EthanolAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ethchlorvynol.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ethotoin.Approved
Ethyl biscoumacetateAmitriptyline may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ethyl carbamateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ethyl carbamate.Withdrawn
Ethyl chlorideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ethyl chloride.Approved, Experimental, Investigational
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ethyl loflazepate.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ethylmorphine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Etifoxine.Investigational, Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Etizolam.Approved
EtomidateAmitriptyline may decrease the antihypertensive activities of Etomidate.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Etoperidone.Withdrawn
EtorphineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Etorphine.Illicit, Vet Approved
EtravirineThe metabolism of Amitriptyline can be decreased when combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Amitriptyline.Approved
EzogabineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ezogabine.Approved, Investigational
FaldaprevirThe serum concentration of Amitriptyline can be increased when it is combined with Faldaprevir.Investigational
FelbamateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Felbamate.Approved
FelodipineThe metabolism of Amitriptyline can be decreased when combined with Felodipine.Approved, Investigational
FencamfamineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fencamfamine.Approved, Illicit, Withdrawn
FenoterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fenoterol.Approved, Investigational
FentanylThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Amitriptyline.Approved
FexofenadineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fexofenadine.Approved, Investigational
FlecainideAmitriptyline may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FlibanserinThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Flibanserin.Approved, Investigational
FloxuridineThe metabolism of Amitriptyline can be decreased when combined with Floxuridine.Approved
FluanisoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fluanisone.Experimental
FluconazoleAmitriptyline may increase the QTc-prolonging activities of Fluconazole.Approved, Investigational
FludiazepamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fludiazepam.Approved, Illicit
FluindioneAmitriptyline may increase the anticoagulant activities of Fluindione.Approved, Investigational
FlunarizineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Flunitrazepam.Approved, Illicit
FluorouracilThe metabolism of Amitriptyline can be decreased when combined with Fluorouracil.Approved
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Amitriptyline.Approved, Vet Approved
FlupentixolAmitriptyline may increase the QTc-prolonging activities of Flupentixol.Approved, Investigational, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Amitriptyline.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Amitriptyline.Approved, Illicit, Investigational
FluspirileneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fluspirilene.Approved, Investigational
Fluticasone propionateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fluticasone propionate.Approved
FluvastatinThe metabolism of Amitriptyline can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Amitriptyline.Approved, Investigational
FormoterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Formoterol.Approved, Investigational
FosamprenavirThe serum concentration of Amitriptyline can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Amitriptyline can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe serum concentration of Amitriptyline can be increased when it is combined with Fosinopril.Approved
FosphenytoinThe metabolism of Amitriptyline can be increased when combined with Fosphenytoin.Approved, Investigational
FospropofolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fospropofol.Approved, Illicit, Investigational
FrovatriptanThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Frovatriptan.Approved, Investigational
FurazolidoneFurazolidone may increase the serotonergic activities of Amitriptyline.Approved, Investigational, Vet Approved
Fusidic AcidThe serum concentration of Amitriptyline can be increased when it is combined with Fusidic Acid.Approved, Investigational
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Amitriptyline.Approved, Investigational
Gabapentin EnacarbilThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Gabapentin Enacarbil.Approved, Investigational
GabexateThe serum concentration of Amitriptyline can be increased when it is combined with Gabexate.Investigational
Gadobenic acidAmitriptyline may increase the QTc-prolonging activities of Gadobenic acid.Approved, Investigational
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Amitriptyline.Approved, Illicit, Investigational
GeldanamycinThe serum concentration of Amitriptyline can be increased when it is combined with Geldanamycin.Experimental, Investigational
GemfibrozilThe metabolism of Amitriptyline can be decreased when combined with Gemfibrozil.Approved
GemifloxacinAmitriptyline may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GepefrineAmitriptyline may increase the stimulatory activities of Gepefrine.Experimental
GepironeThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Glutethimide.Approved, Illicit
GM6001The serum concentration of Amitriptyline can be increased when it is combined with GM6001.Experimental
GoserelinAmitriptyline may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronAmitriptyline may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
GuanabenzAmitriptyline may decrease the antihypertensive activities of Guanabenz.Approved, Investigational
GuanfacineAmitriptyline may decrease the antihypertensive activities of Guanfacine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Halazepam.Approved, Illicit, Withdrawn
HaloperidolThe metabolism of Amitriptyline can be decreased when combined with Haloperidol.Approved
HalothaneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Halothane.Approved, Vet Approved
HarmalineHarmaline may increase the serotonergic activities of Amitriptyline.Experimental
HeroinThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Heroin.Approved, Illicit, Investigational
HexobarbitalThe metabolism of Amitriptyline can be increased when combined with Hexobarbital.Approved
HydracarbazineHydracarbazine may increase the serotonergic activities of Amitriptyline.Experimental
HydrocodoneAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Amitriptyline.Approved, Illicit
HydroxyamphetamineAmitriptyline may increase the stimulatory activities of Hydroxyamphetamine.Approved
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.Approved
IbutilideAmitriptyline may increase the QTc-prolonging activities of Ibutilide.Approved
IdelalisibThe metabolism of Amitriptyline can be decreased when combined with Idelalisib.Approved
IdraparinuxThe serum concentration of Amitriptyline can be increased when it is combined with Idraparinux.Investigational
IloperidoneAmitriptyline may increase the QTc-prolonging activities of Iloperidone.Approved
ImatinibThe metabolism of Amitriptyline can be decreased when combined with Imatinib.Approved
ImidaprilThe serum concentration of Amitriptyline can be increased when it is combined with Imidapril.Investigational
ImipramineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Imipramine.Approved
IndacaterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Indacaterol.Approved
IndalpineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Indalpine.Investigational, Withdrawn
IndinavirThe metabolism of Amitriptyline can be decreased when combined with Indinavir.Approved
IndiplonThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Indiplon.Investigational
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Amitriptyline.Approved, Investigational
Iofetamine I-123Amitriptyline may increase the stimulatory activities of Iofetamine I-123.Approved
IproclozideIproclozide may increase the serotonergic activities of Amitriptyline.Withdrawn
IproniazidIproniazid may increase the serotonergic activities of Amitriptyline.Withdrawn
IrbesartanThe metabolism of Amitriptyline can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoleThe serum concentration of Amitriptyline can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Amitriptyline can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidThe therapeutic efficacy of Amitriptyline can be increased when used in combination with Isocarboxazid.Approved
IsoetarineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Isoetarine.Approved
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Amitriptyline.Approved, Vet Approved
IsoflurophateThe serum concentration of Amitriptyline can be increased when it is combined with Isoflurophate.Approved, Investigational, Withdrawn
IsoniazidThe metabolism of Amitriptyline can be decreased when combined with Isoniazid.Approved, Investigational
IsoprenalineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Isoprenaline.Approved, Investigational
IsradipineThe metabolism of Amitriptyline can be decreased when combined with Isradipine.Approved, Investigational
ItraconazoleThe metabolism of Amitriptyline can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Amitriptyline can be increased when it is combined with Ivacaftor.Approved
IxazomibThe serum concentration of Amitriptyline can be increased when it is combined with Ixazomib.Approved, Investigational
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Amitriptyline.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ketazolam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ketobemidone.Approved, Investigational
KetoconazoleThe metabolism of Amitriptyline can be decreased when combined with Ketoconazole.Approved, Investigational
L-TryptophanL-Tryptophan may increase the serotonergic activities of Amitriptyline.Approved, Nutraceutical, Withdrawn
LamotrigineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Lamotrigine.Approved, Investigational
LapatinibThe metabolism of Amitriptyline can be decreased when combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Amitriptyline.Approved
LeflunomideThe metabolism of Amitriptyline can be decreased when combined with Leflunomide.Approved, Investigational
LenvatinibAmitriptyline may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
LepirudinThe serum concentration of Amitriptyline can be increased when it is combined with Lepirudin.Approved
LetaxabanThe serum concentration of Amitriptyline can be increased when it is combined with Letaxaban.Investigational
LeuprolideAmitriptyline may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Levobupivacaine.Approved, Investigational
LevocabastineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Levocabastine.Approved, Investigational
LevocetirizineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Levodopa.Approved
LevofloxacinAmitriptyline may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Levomethadyl Acetate.Approved, Investigational
LevomilnacipranThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Levomilnacipran.Approved, Investigational
LevonordefrinAmitriptyline may decrease the antihypertensive activities of Levonordefrin.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Amitriptyline.Approved
LevosalbutamolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Levosalbutamol.Approved, Investigational
LevothyroxineLevothyroxine may increase the arrhythmogenic activities of Amitriptyline.Approved
LidocaineThe metabolism of Amitriptyline can be decreased when combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Amitriptyline can be increased when it is combined with Linagliptin.Approved
LinezolidLinezolid may increase the serotonergic activities of Amitriptyline.Approved, Investigational
LiothyronineLiothyronine may increase the arrhythmogenic activities of Amitriptyline.Approved, Vet Approved
LiotrixLiotrix may increase the arrhythmogenic activities of Amitriptyline.Approved
LisdexamfetamineAmitriptyline may increase the stimulatory activities of Lisdexamfetamine.Approved, Investigational
LisinoprilThe serum concentration of Amitriptyline can be increased when it is combined with Lisinopril.Approved, Investigational
LithiumLithium may increase the neurotoxic activities of Amitriptyline.Approved
LobeglitazoneThe metabolism of Amitriptyline can be decreased when combined with Lobeglitazone.Approved, Investigational
LofentanilThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Lofentanil.Illicit
LofexidineAmitriptyline may decrease the antihypertensive activities of Lofexidine.Approved, Investigational
LopinavirThe metabolism of Amitriptyline can be decreased when combined with Lopinavir.Approved
LoprazolamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Loprazolam.Experimental
LoratadineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Loratadine.Approved, Investigational
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Amitriptyline.Approved
LorcaserinThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Lorcaserin.Approved
LormetazepamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Lormetazepam.Approved
LorpiprazoleThe serum concentration of Amitriptyline can be increased when it is combined with Lorpiprazole.Approved
LosartanThe metabolism of Amitriptyline can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Amitriptyline can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Amitriptyline.Approved
LuliconazoleThe serum concentration of Amitriptyline can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Amitriptyline can be increased when it is combined with Lumacaftor.Approved
LumefantrineAmitriptyline may increase the QTc-prolonging activities of Lumefantrine.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Amitriptyline.Approved, Investigational
Magnesium sulfateThe therapeutic efficacy of Amitriptyline can be increased when used in combination with Magnesium sulfate.Approved, Investigational, Vet Approved
ManidipineThe metabolism of Amitriptyline can be decreased when combined with Manidipine.Approved, Investigational
MaprotilineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Maprotiline.Approved, Investigational
MebanazineMebanazine may increase the serotonergic activities of Amitriptyline.Withdrawn
MebicarThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Mebicar.Experimental
MeclizineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Meclizine.Approved
MedazepamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Medazepam.Experimental
MedetomidineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Medetomidine.Vet Approved
MelagatranThe serum concentration of Amitriptyline can be increased when it is combined with Melagatran.Experimental
MelatoninThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Melatonin.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Melperone.Approved, Investigational
MephedroneAmitriptyline may increase the stimulatory activities of Mephedrone.Investigational
MephentermineAmitriptyline may increase the vasopressor activities of Mephentermine.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Mepivacaine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Amitriptyline.Approved, Illicit
MeptazinolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Meptazinol.Experimental
MesoridazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Mesoridazine.Approved, Investigational
MetaraminolAmitriptyline may increase the vasopressor activities of Metaraminol.Approved, Investigational
MetaxaloneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Metaxalone.Approved
MethadoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Methadyl Acetate.Approved, Illicit
MethamphetamineAmitriptyline may decrease the antihypertensive activities of Methamphetamine.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Methaqualone.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Methocarbamol.Approved, Vet Approved
MethohexitalThe metabolism of Amitriptyline can be increased when combined with Methohexital.Approved
MethotrimeprazineAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved, Investigational
MethoxamineAmitriptyline may increase the vasopressor activities of Methoxamine.Approved, Investigational
MethoxyfluraneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Methoxyflurane.Approved, Investigational, Vet Approved
MethoxyphenamineAmitriptyline may increase the stimulatory activities of Methoxyphenamine.Experimental
MethsuximideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Methsuximide.Approved
MethylecgonineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Methylecgonine.Experimental
Methylene blueAmitriptyline may increase the serotonergic activities of Methylene blue.Approved, Investigational
MethylphenidateThe risk or severity of adverse effects can be increased when Methylphenidate is combined with Amitriptyline.Approved, Investigational
MethylphenobarbitalThe metabolism of Amitriptyline can be increased when combined with Methylphenobarbital.Approved
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Amitriptyline.Approved, Investigational
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Amitriptyline.Approved, Investigational
MetyrosineThe risk or severity of adverse effects can be increased when Metyrosine is combined with Amitriptyline.Approved
MexiletineThe metabolism of Amitriptyline can be decreased when combined with Mexiletine.Approved, Investigational
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Amitriptyline.Approved, Illicit
MidodrineAmitriptyline may increase the vasopressor activities of Midodrine.Approved
MidomafetamineAmitriptyline may increase the stimulatory activities of Midomafetamine.Experimental, Illicit, Investigational
MidostaurinThe metabolism of Amitriptyline can be decreased when combined with Midostaurin.Approved, Investigational
MifepristoneThe serum concentration of Amitriptyline can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Milnacipran.Approved, Investigational
MinaprineMinaprine may increase the serotonergic activities of Amitriptyline.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.Approved, Investigational
MirabegronThe metabolism of Amitriptyline can be decreased when combined with Mirabegron.Approved
MirtazapineAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MitotaneThe serum concentration of Amitriptyline can be decreased when it is combined with Mitotane.Approved
MMDAAmitriptyline may increase the stimulatory activities of MMDA.Experimental, Illicit
MoclobemideMoclobemide may increase the serotonergic activities of Amitriptyline.Approved, Investigational
ModafinilThe metabolism of Amitriptyline can be decreased when combined with Modafinil.Approved, Investigational
MoexiprilThe serum concentration of Amitriptyline can be increased when it is combined with Moexipril.Approved
MolindoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Molindone.Approved
MoperoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Moperone.Experimental
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Amitriptyline.Approved, Investigational
MosapramineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Mosapramine.Experimental
MoxifloxacinAmitriptyline may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
MoxonidineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Amitriptyline.Approved, Investigational
N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-ProlineThe serum concentration of Amitriptyline can be increased when it is combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline.Experimental
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.Approved, Investigational
NafamostatThe serum concentration of Amitriptyline can be increased when it is combined with Nafamostat.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Amitriptyline.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Amitriptyline.Approved
NaphazolineAmitriptyline may decrease the antihypertensive activities of Naphazoline.Approved
NaratriptanThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Naratriptan.Approved, Investigational
NefazodoneThe metabolism of Amitriptyline can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Amitriptyline can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Amitriptyline can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Amitriptyline can be increased when combined with Nevirapine.Approved
NialamideNialamide may increase the serotonergic activities of Amitriptyline.Withdrawn
NicardipineThe metabolism of Amitriptyline can be decreased when combined with Nicardipine.Approved, Investigational
NicorandilAmitriptyline may increase the hypotensive activities of Nicorandil.Approved, Investigational
NicotineThe metabolism of Amitriptyline can be decreased when combined with Nicotine.Approved
NilotinibAmitriptyline may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Amitriptyline.Approved
NitroaspirinThe serum concentration of Amitriptyline can be increased when it is combined with Nitroaspirin.Investigational
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Amitriptyline.Approved, Vet Approved
NorepinephrineAmitriptyline may decrease the antihypertensive activities of Norepinephrine.Approved
NorfluraneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Norflurane.Approved, Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Normethadone.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Nortriptyline.Approved
OctamoxinOctamoxin may increase the serotonergic activities of Amitriptyline.Withdrawn
OfloxacinAmitriptyline may increase the QTc-prolonging activities of Ofloxacin.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Amitriptyline.Approved, Investigational
OlaparibThe metabolism of Amitriptyline can be decreased when combined with Olaparib.Approved
OlodaterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Olodaterol.Approved
OlopatadineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Olopatadine.Approved
OmapatrilatThe serum concentration of Amitriptyline can be increased when it is combined with Omapatrilat.Investigational
OmeprazoleThe metabolism of Amitriptyline can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronAmitriptyline may increase the QTc-prolonging activities of Ondansetron.Approved
OpiumThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Opium.Approved, Illicit
OrciprenalineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Orciprenaline.Approved
OrphenadrineAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Amitriptyline can be increased when it is combined with Osimertinib.Approved
OtamixabanThe serum concentration of Amitriptyline can be increased when it is combined with Otamixaban.Investigational
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Amitriptyline.Approved
OxethazaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Oxethazaine.Approved, Investigational
OxprenololThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Oxprenolol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Oxybuprocaine.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Amitriptyline.Approved, Illicit, Investigational
OxymetazolineAmitriptyline may decrease the antihypertensive activities of Oxymetazoline.Approved, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Amitriptyline.Approved, Investigational, Vet Approved
OxypertineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Oxypertine.Experimental
PalbociclibThe serum concentration of Amitriptyline can be increased when it is combined with Palbociclib.Approved, Investigational
PaliperidoneAmitriptyline may decrease the antihypertensive activities of Paliperidone.Approved
PalonosetronPalonosetron may increase the serotonergic activities of Amitriptyline.Approved, Investigational
PanobinostatThe serum concentration of Amitriptyline can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Amitriptyline can be decreased when combined with Pantoprazole.Approved
ParaldehydeAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved, Investigational
PargylinePargyline may increase the serotonergic activities of Amitriptyline.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Amitriptyline.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Amitriptyline.Approved
Peginterferon alfa-2bThe serum concentration of Amitriptyline can be decreased when it is combined with Peginterferon alfa-2b.Approved
PenfluridolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Penfluridol.Experimental
PentamidineAmitriptyline may increase the QTc-prolonging activities of Pentamidine.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Amitriptyline.Approved, Vet Approved
PentobarbitalThe metabolism of Amitriptyline can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.Approved
PerazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Perazine.Approved, Investigational
PerflutrenAmitriptyline may increase the QTc-prolonging activities of Perflutren.Approved
PergolideAmitriptyline may decrease the antihypertensive activities of Pergolide.Approved, Investigational, Vet Approved, Withdrawn
PerindoprilThe serum concentration of Amitriptyline can be increased when it is combined with Perindopril.Approved
PerospironeThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Amitriptyline.Approved
PethidineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Pethidine.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Phenazocine.Experimental
PhenelzinePhenelzine may increase the serotonergic activities of Amitriptyline.Approved
PhenibutThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Phenibut.Experimental
PhenindioneAmitriptyline may increase the anticoagulant activities of Phenindione.Approved, Investigational
PheniprazinePheniprazine may increase the serotonergic activities of Amitriptyline.Withdrawn
PhenobarbitalThe metabolism of Amitriptyline can be increased when combined with Phenobarbital.Approved, Investigational
PhenoperidineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Phenoperidine.Experimental
PhenoxyethanolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Phenoxyethanol.Approved
PhenoxypropazinePhenoxypropazine may increase the serotonergic activities of Amitriptyline.Withdrawn
PhenprocoumonAmitriptyline may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhentermineAmitriptyline may increase the stimulatory activities of Phentermine.Approved, Illicit
PhenylephrineAmitriptyline may increase the vasopressor activities of Phenylephrine.Approved
PhenylpropanolamineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Phenylpropanolamine.Approved, Vet Approved, Withdrawn
PhenytoinThe metabolism of Amitriptyline can be increased when combined with Phenytoin.Approved, Vet Approved
PhosphoramidonThe serum concentration of Amitriptyline can be increased when it is combined with Phosphoramidon.Experimental
PimozideAmitriptyline may increase the QTc-prolonging activities of Pimozide.Approved
PioglitazoneThe metabolism of Amitriptyline can be decreased when combined with Pioglitazone.Approved, Investigational
PipamperoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Pipamperone.Approved, Investigational
PipotiazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Pipotiazine.Approved, Investigational
PirbuterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Pirbuterol.Approved
PiritramideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Piritramide.Approved, Investigational
PirlindolePirlindole may increase the serotonergic activities of Amitriptyline.Approved
PitolisantThe serum concentration of Pitolisant can be increased when it is combined with Amitriptyline.Approved, Investigational
PivhydrazinePivhydrazine may increase the serotonergic activities of Amitriptyline.Withdrawn
PizotifenThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Pomalidomide.Approved
PosaconazoleThe metabolism of Amitriptyline can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PramipexoleAmitriptyline may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Pramocaine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Prazepam.Approved, Illicit
PregabalinThe therapeutic efficacy of Amitriptyline can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Prilocaine.Approved
PrimaquineAmitriptyline may increase the QTc-prolonging activities of Primaquine.Approved
PrimidoneThe metabolism of Amitriptyline can be increased when combined with Primidone.Approved, Vet Approved
PrinomastatThe serum concentration of Amitriptyline can be increased when it is combined with Prinomastat.Investigational
ProcainamideAmitriptyline may increase the QTc-prolonging activities of Procainamide.Approved
ProcaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Procaine.Approved, Investigational, Vet Approved
ProcarbazineProcarbazine may increase the serotonergic activities of Amitriptyline.Approved, Investigational
ProcaterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Procaterol.Approved, Investigational
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Amitriptyline.Approved, Vet Approved
PromazineThe metabolism of Amitriptyline can be decreased when combined with Promazine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Promethazine.Approved, Investigational
PropafenoneAmitriptyline may increase the QTc-prolonging activities of Propafenone.Approved
PropanididThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Propanidid.Experimental
ProparacaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Proparacaine.Approved, Vet Approved
PropericiazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Propericiazine.Approved, Investigational
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Amitriptyline.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Propoxycaine.Approved
ProthipendylThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Prothipendyl.Investigational
ProtokylolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Protokylol.Approved, Vet Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Protriptyline.Approved
ProxibarbalThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Proxibarbal.Experimental
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Amitriptyline.Approved
PSD502The risk or severity of adverse effects can be increased when Amitriptyline is combined with PSD502.Investigational
PseudoephedrineAmitriptyline may decrease the antihypertensive activities of Pseudoephedrine.Approved
PyrimethamineThe metabolism of Amitriptyline can be decreased when combined with Pyrimethamine.Approved, Investigational, Vet Approved
QuazepamThe serum concentration of Amitriptyline can be increased when it is combined with Quazepam.Approved, Illicit
QuetiapineAmitriptyline may increase the QTc-prolonging activities of Quetiapine.Approved
QuinaprilThe serum concentration of Amitriptyline can be increased when it is combined with Quinapril.Approved, Investigational
QuinidineAmitriptyline may increase the QTc-prolonging activities of Quinidine.Approved, Investigational
QuinineAmitriptyline may increase the QTc-prolonging activities of Quinine.Approved
QuinisocaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Quinisocaine.Experimental
RabeprazoleThe metabolism of Amitriptyline can be decreased when combined with Rabeprazole.Approved, Investigational
RacecadotrilThe serum concentration of Amitriptyline can be increased when it is combined with Racecadotril.Investigational
RacepinephrineAmitriptyline may decrease the antihypertensive activities of Racepinephrine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ramelteon.Approved, Investigational
RamiprilThe serum concentration of Amitriptyline can be increased when it is combined with Ramipril.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Amitriptyline.Approved, Investigational
RasagilineRasagiline may increase the serotonergic activities of Amitriptyline.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Amitriptyline.Approved
RemikirenThe serum concentration of Amitriptyline can be increased when it is combined with Remikiren.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Remoxipride.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Amitriptyline.Approved, Investigational
RifabutinThe metabolism of Amitriptyline can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe metabolism of Amitriptyline can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Amitriptyline can be increased when combined with Rifapentine.Approved, Investigational
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Amitriptyline.Approved, Investigational
RisperidoneAmitriptyline may decrease the antihypertensive activities of Risperidone.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ritanserin.Investigational
RitobegronAmitriptyline may increase the stimulatory activities of Ritobegron.Investigational
RitodrineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ritodrine.Approved, Investigational
RitonavirThe metabolism of Amitriptyline can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Amitriptyline can be increased when it is combined with Rivaroxaban.Approved
RizatriptanThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Rizatriptan.Approved
RolapitantThe metabolism of Amitriptyline can be decreased when combined with Rolapitant.Approved, Investigational
RomifidineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Romifidine.Vet Approved
RopiniroleAmitriptyline may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ropivacaine.Approved
RosiglitazoneThe metabolism of Amitriptyline can be decreased when combined with Rosiglitazone.Approved, Investigational
RotigotineAmitriptyline may increase the sedative activities of Rotigotine.Approved
RucaparibThe metabolism of Amitriptyline can be decreased when combined with Rucaparib.Approved, Investigational
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Amitriptyline.Approved
S-3304The serum concentration of Amitriptyline can be increased when it is combined with S-3304.Investigational
SafrazineSafrazine may increase the serotonergic activities of Amitriptyline.Withdrawn
SalbutamolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Salbutamol.Approved, Vet Approved
SalmeterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Salmeterol.Approved
SaquinavirThe metabolism of Amitriptyline can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Amitriptyline can be decreased when used in combination with Sarilumab.Approved, Investigational
SaxagliptinThe serum concentration of Amitriptyline can be increased when it is combined with Saxagliptin.Approved
ScopolamineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Scopolamine.Approved, Investigational
SecobarbitalThe metabolism of Amitriptyline can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineSelegiline may increase the serotonergic activities of Amitriptyline.Approved, Investigational, Vet Approved
SepranoloneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Sepranolone.Investigational
SertindoleThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Sertindole.Approved, Investigational, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Amitriptyline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Amitriptyline.Approved, Vet Approved
SildenafilThe metabolism of Amitriptyline can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Amitriptyline.Approved
SiltuximabThe serum concentration of Amitriptyline can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Amitriptyline can be increased when it is combined with Simeprevir.Approved
SitagliptinThe serum concentration of Amitriptyline can be increased when it is combined with Sitagliptin.Approved, Investigational
SivelestatThe serum concentration of Amitriptyline can be increased when it is combined with Sivelestat.Investigational
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.Approved
Sodium phosphateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Sodium phosphate.Approved
SorafenibThe metabolism of Amitriptyline can be decreased when combined with Sorafenib.Approved, Investigational
SotalolAmitriptyline may increase the QTc-prolonging activities of Sotalol.Approved
SpiraprilThe serum concentration of Amitriptyline can be increased when it is combined with Spirapril.Approved
St. John's WortThe metabolism of Amitriptyline can be increased when combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Amitriptyline can be increased when it is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Amitriptyline.Approved, Investigational
SulfadiazineThe metabolism of Amitriptyline can be decreased when combined with Sulfadiazine.Approved, Investigational, Vet Approved
SulfamethoxazoleThe metabolism of Amitriptyline can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Amitriptyline can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Sulpiride.Approved, Investigational
SultoprideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Sultopride.Experimental
SumatriptanThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Sumatriptan.Approved, Investigational
SuvorexantAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved, Investigational
TamoxifenThe metabolism of Amitriptyline can be decreased when combined with Tamoxifen.Approved
TandospironeThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tasimelteon.Approved, Investigational
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Amitriptyline.Approved
TelaprevirThe metabolism of Amitriptyline can be decreased when combined with Telaprevir.Approved, Withdrawn
TelavancinAmitriptyline may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinThe metabolism of Amitriptyline can be decreased when combined with Telithromycin.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Amitriptyline.Approved, Investigational
TemocaprilThe serum concentration of Amitriptyline can be increased when it is combined with Temocapril.Experimental, Investigational
Tenofovir disoproxilThe metabolism of Amitriptyline can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerbinafineThe metabolism of Amitriptyline can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerbutalineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Terbutaline.Approved
TeriflunomideThe serum concentration of Amitriptyline can be decreased when it is combined with Teriflunomide.Approved
TetrabenazineAmitriptyline may increase the QTc-prolonging activities of Tetrabenazine.Approved, Investigational
TetracaineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tetracaine.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tetrahydropalmatine.Investigational
TetrodotoxinThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tetrodotoxin.Investigational
ThalidomideAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
TheophyllineThe metabolism of Amitriptyline can be decreased when combined with Theophylline.Approved
ThiamylalThe metabolism of Amitriptyline can be increased when combined with Thiamylal.Approved, Vet Approved
ThiopentalThe metabolism of Amitriptyline can be increased when combined with Thiopental.Approved, Vet Approved
ThiopropazateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Thiopropazate.Experimental
ThioproperazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Thioproperazine.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Amitriptyline.Approved, Withdrawn
ThiorphanThe serum concentration of Amitriptyline can be increased when it is combined with Thiorphan.Experimental
ThiotepaThe metabolism of Amitriptyline can be decreased when combined with Thiotepa.Approved, Investigational
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Amitriptyline.Approved
Thyroid, porcineThyroid, porcine may increase the arrhythmogenic activities of Amitriptyline.Approved
TiagabineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tiagabine.Approved, Investigational
TiaprideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tiapride.Approved, Investigational
TicagrelorThe metabolism of Amitriptyline can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Amitriptyline can be decreased when combined with Ticlopidine.Approved
TiletamineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tiletamine.Vet Approved
TilidineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tilidine.Experimental
TioclomarolAmitriptyline may increase the anticoagulant activities of Tioclomarol.Experimental
TipranavirThe metabolism of Amitriptyline can be decreased when combined with Tipranavir.Approved, Investigational
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Amitriptyline.Approved, Investigational
TocilizumabThe serum concentration of Amitriptyline can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Amitriptyline can be decreased when combined with Tolbutamide.Approved, Investigational
TolcaponeThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tolcapone.Approved, Withdrawn
ToloxatoneToloxatone may increase the serotonergic activities of Amitriptyline.Approved
TopiramateTopiramate may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.Approved
TopiroxostatThe metabolism of Amitriptyline can be decreased when combined with Topiroxostat.Approved, Investigational
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Amitriptyline.Approved, Investigational
ToremifeneAmitriptyline may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TramadolAmitriptyline may increase the neuroexcitatory activities of Tramadol.Approved, Investigational
TrandolaprilThe serum concentration of Amitriptyline can be increased when it is combined with Trandolapril.Approved
TranylcypromineTranylcypromine may increase the serotonergic activities of Amitriptyline.Approved, Investigational
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Amitriptyline.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Amitriptyline.Approved, Investigational
Tricaine methanesulfonateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tricaine methanesulfonate.Vet Approved
TrichloroethyleneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Trichloroethylene.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Amitriptyline.Approved, Investigational
TrifluperidolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Trifluperidol.Experimental
TriflupromazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe metabolism of Amitriptyline can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Trimipramine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Triprolidine.Approved
TropisetronTropisetron may increase the serotonergic activities of Amitriptyline.Approved, Investigational
UbenimexThe serum concentration of Amitriptyline can be increased when it is combined with Ubenimex.Experimental, Investigational
UlinastatinThe serum concentration of Amitriptyline can be increased when it is combined with Ulinastatin.Investigational
Valproic AcidThe serum concentration of Amitriptyline can be increased when it is combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Amitriptyline can be decreased when combined with Valsartan.Approved, Investigational
VandetanibAmitriptyline may increase the QTc-prolonging activities of Vandetanib.Approved
VemurafenibThe risk or severity of QTc prolongation can be increased when Vemurafenib is combined with Amitriptyline.Approved
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Amitriptyline.Approved
VeraliprideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Veralipride.Experimental
VerapamilThe metabolism of Amitriptyline can be decreased when combined with Verapamil.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Vigabatrin.Approved
VilanterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Vilanterol.Approved
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Amitriptyline.Approved
VildagliptinThe serum concentration of Amitriptyline can be increased when it is combined with Vildagliptin.Approved, Investigational
VincristineThe excretion of Vincristine can be decreased when combined with Amitriptyline.Approved, Investigational
Vinyl etherThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Vinyl ether.Experimental
VoriconazoleThe metabolism of Amitriptyline can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Amitriptyline.Approved, Investigational
WarfarinAmitriptyline may increase the anticoagulant activities of Warfarin.Approved
XenonThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Xenon.Experimental
XimelagatranThe serum concentration of Amitriptyline can be increased when it is combined with Ximelagatran.Approved, Investigational, Withdrawn
XylazineAmitriptyline may decrease the antihypertensive activities of Xylazine.Vet Approved
XylometazolineAmitriptyline may decrease the antihypertensive activities of Xylometazoline.Approved, Investigational
YohimbineThe serum concentration of Yohimbine can be increased when it is combined with Amitriptyline.Approved, Investigational, Vet Approved
Z-Val-Ala-Asp fluoromethyl ketoneThe serum concentration of Amitriptyline can be increased when it is combined with Z-Val-Ala-Asp fluoromethyl ketone.Experimental
ZafirlukastThe metabolism of Amitriptyline can be decreased when combined with Zafirlukast.Approved, Investigational
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Amitriptyline.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ziconotide.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Zimelidine.Withdrawn
ZiprasidoneAmitriptyline may increase the QTc-prolonging activities of Ziprasidone.Approved
ZofenoprilThe serum concentration of Amitriptyline can be increased when it is combined with Zofenopril.Experimental
ZolazepamThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Zolazepam.Vet Approved
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Amitriptyline.Approved, Investigational
ZolpidemAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Amitriptyline.Approved
ZotepineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Zotepine.Approved, Investigational, Withdrawn
ZucapsaicinThe metabolism of Amitriptyline can be decreased when combined with Zucapsaicin.Approved, Investigational
ZuclopenthixolAmitriptyline may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (caffeine).
  • Avoid St.John's Wort.
  • Take with food to reduce irritation.

References

Synthesis Reference

Manfred Durr, Benedikt Gajdos, Klaus-Dieter Gneuss, Ekkehard Harhausen, Jurgen Seidel, "Pharmaceutical amitriptylin oxide preparation and process for its manufacture." U.S. Patent US4567202, issued January 28, 1986.

US4567202
General References
  1. Otaka M, Jin M, Odashima M, Matsuhashi T, Wada I, Horikawa Y, Komatsu K, Ohba R, Oyake J, Hatakeyama N, Watanabe S: New strategy of therapy for functional dyspepsia using famotidine, mosapride and amitriptyline. Aliment Pharmacol Ther. 2005 Jun;21 Suppl 2:42-6. [PubMed:15943846]
  2. Hisaoka K, Tsuchioka M, Yano R, Maeda N, Kajitani N, Morioka N, Nakata Y, Takebayashi M: Tricyclic antidepressant amitriptyline activates fibroblast growth factor receptor signaling in glial cells: involvement in glial cell line-derived neurotrophic factor production. J Biol Chem. 2011 Jun 17;286(24):21118-28. doi: 10.1074/jbc.M111.224683. Epub 2011 Apr 22. [PubMed:21515689]
  3. Yan L, Wang Q, Fu Q, Ye Q, Xiao H, Wan Q: Amitriptyline inhibits currents and decreases the mRNA expression of voltage-gated sodium channels in cultured rat cortical neurons. Brain Res. 2010 Jun 8;1336:1-9. doi: 10.1016/j.brainres.2010.04.016. Epub 2010 Apr 14. [PubMed:20398637]
External Links
Human Metabolome Database
HMDB0014466
KEGG Compound
C06824
PubChem Compound
2160
PubChem Substance
46508798
ChemSpider
2075
BindingDB
50020712
ChEBI
2666
ChEMBL
CHEMBL629
Therapeutic Targets Database
DNC001466
PharmGKB
PA448385
IUPHAR
200
Guide to Pharmacology
GtP Drug Page
HET
TP0
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Amitriptyline
ATC Codes
N06AA09 — AmitriptylineN06CA01 — Amitriptyline and psycholeptics
AHFS Codes
  • 28:16.04.28 — Tricyclics and Other Norepinephrine-reuptake Inhibitors
PDB Entries
3apv / 5ha9
FDA label
Download (1 MB)
MSDS
Download (73.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHealthy Volunteers2
1Not Yet RecruitingNot AvailableDepression1
1, 2CompletedTreatmentFibromyalgia1
2CompletedTreatmentAdhesive Capsulitis1
2CompletedTreatmentBrain Injury / Post-Traumatic Headaches1
2CompletedTreatmentCarpal Tunnel Syndrome (CTS) / Cumulative Trauma Disorders / Pain / Repetitive Strain Injury1
2CompletedTreatmentChronic Oral Food Refusal1
2CompletedTreatmentCystic Fibrosis (CF) / Infection NOS / Pseudomonas Aeruginosa1
2CompletedTreatmentFibromyalgia / Growth Hormone Deficiency (GHD)1
2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Peripheral Nervous System Diseases1
2CompletedTreatmentMajor Depressive Disorder (MDD)1
2Not Yet RecruitingBasic ScienceHeadaches / Migraine Disorders / Migraines / Migrainous Headache1
2TerminatedTreatmentPruritus1
2Unknown StatusTreatmentCystic Fibrosis (CF) / Pneumonia1
2Unknown StatusTreatmentGallbladder Dyskinesia1
2Unknown StatusTreatmentIntervertebral Disc Displacement / Intervertebral Disc Herniation1
2, 3CompletedTreatmentDiabetes Mellitus (DM) / Peripheral Neuropathy1
2, 3CompletedTreatmentDyspepsia and Other Specified Disorders of Function of Stomach1
2, 3CompletedTreatmentFemale Genital Diseases1
2, 3SuspendedTreatmentChronic Laryngeal Neuropathy / Laryngeal Diseases1
2, 3TerminatedTreatmentChronic Laryngeal Neuropathy / Laryngeal Diseases1
2, 3Unknown StatusTreatmentFibromyalgia1
3Active Not RecruitingTreatmentPain1
3CompletedSupportive CareChronic Myeloproliferative Disorders / Leukemias / Lymphoproliferative Disorders / Malignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm / Myelodysplastic Syndromes / Myelodysplastic/Myeloproliferative Neoplasms / Neurotoxicity / Pain / Unspecified Adult Solid Tumor, Protocol Specific1
3CompletedTreatmentBladder Diseases / Interstitial Cystitis1
3CompletedTreatmentMajor Depressive Disorder (MDD)1
3CompletedTreatmentMigraines1
3CompletedTreatmentUnipolar Depression1
3RecruitingTreatmentAmitriptyline / Hansen's Disease / Leprosy Neuropathy / Pain, Neuropathic1
3RecruitingTreatmentVulvodynia1
3TerminatedPreventionHeadaches / Migraine Disorders / Migraines1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3TerminatedTreatmentSleeplessness1
3Unknown StatusTreatmentCancers / Neurocostal neuralgia1
3Unknown StatusTreatmentHeadaches1
4CompletedTreatmentAnxiety Disorders / Moods Disorders / Schizophrenic Disorders1
4CompletedTreatmentCervical Pain1
4CompletedTreatmentFibromyalgia2
4CompletedTreatmentFunctional Gastrointestinal Disorders1
4CompletedTreatmentNeuropathic Pain Caused by Lumbar Radicular Pain1
4CompletedTreatmentPain / Postoperative pain / Traumatic Amputations1
4CompletedTreatmentPain / Spinal Cord Injuries (SCI)1
4Enrolling by InvitationPreventionChronic Daily Headache / Transformed Migraine1
4RecruitingTreatmentMyofacial Pain1
4RecruitingTreatmentPain, Chronic2
4TerminatedTreatmentChronic Neuropathic Pain1
4TerminatedTreatmentHeadaches1
4Unknown StatusNot AvailableMajor Depressive Disorder (MDD)1
4WithdrawnTreatmentDiarrhea- Predominant Irritable Bowel Syndrome / Quality of Life1
Not AvailableCompletedNot AvailableHealthy Participants1
Not AvailableCompletedNot AvailableHealthy Volunteers1
Not AvailableCompletedOtherMigraines / Preventive Treatment1
Not AvailableCompletedTreatmentFibromyalgia / Sleep Initiation and Maintenance Disorders1
Not AvailableCompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Peripheral Nervous System Diseases1
Not AvailableCompletedTreatmentMigraines1
Not AvailableNot Yet RecruitingNot AvailableIrritable Bowel Syndrome (IBS)1
Not AvailableRecruitingBasic ScienceHeadache, Tension-Type1
Not AvailableUnknown StatusTreatmentFunctional Dyspepsia1
Not AvailableUnknown StatusTreatmentTreatment Resistant Depression (TRD)1

Pharmacoeconomics

Manufacturers
  • Hoffmann la roche inc
  • Watson laboratories inc
  • Astrazeneca pharmaceuticals lp
  • Bristol myers squibb co
  • Warner chilcott div warner lambert co
  • American therapeutics inc
  • Caraco pharmaceutical laboratories ltd
  • Copley pharmaceutical inc
  • Halsey drug co inc
  • Lederle laboratories div american cyanamid co
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • Pliva inc
  • Purepac pharmaceutical co
  • Roxane laboratories inc
  • Sandoz inc
  • Superpharm corp
  • Teva pharmaceuticals usa inc
  • Ucb inc
  • Usl pharma inc
  • Vangard laboratories inc div midway medical co
  • Vintage pharmaceuticals inc
  • West ward pharmaceutical corp
Packagers
  • 4uOrtho LLC
  • Advanced Pharmaceutical Services Inc.
  • Amerisource Health Services Corp.
  • Apotheca Inc.
  • A-S Medication Solutions LLC
  • Blenheim Pharmacal
  • Bryant Ranch Prepack
  • Caraco Pharmaceutical Labs
  • Cardinal Health
  • Caremark LLC
  • Comprehensive Consultant Services Inc.
  • Corepharma LLC
  • Coupler Enterprises Inc.
  • DHHS Program Support Center Supply Service Center
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Group Health Cooperative
  • H.J. Harkins Co. Inc.
  • Heartland Repack Services LLC
  • Innoviant Pharmacy Inc.
  • Kaiser Foundation Hospital
  • Keltman Pharmaceuticals Inc.
  • Lake Erie Medical and Surgical Supply
  • Legacy Pharmaceuticals Packaging LLC
  • Liberty Pharmaceuticals
  • Major Pharmaceuticals
  • Medisca Inc.
  • Medvantx Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mutual Pharmaceutical Co.
  • Mylan
  • Nanjing Famu Chemicals Co. Ltd.
  • Neuman Distributors Inc.
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pharmedix
  • Pharmpak Inc.
  • Physicians Total Care Inc.
  • Pliva Inc.
  • Preferred Pharmaceuticals Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Prescript Pharmaceuticals
  • Prescription Dispensing Service Inc.
  • Qualitest
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Remedy Repack
  • Sandhills Packaging Inc.
  • Sandoz
  • Southwood Pharmaceuticals
  • St Mary's Medical Park Pharmacy
  • Stat Rx Usa
  • UDL Laboratories
  • United Research Laboratories Inc.
  • Va Cmop Dallas
  • Valeant Ltd.
  • Vangard Labs Inc.
  • Vintage Pharmaceuticals Inc.
Dosage forms
FormRouteStrength
TabletOral10 mg/1
TabletOral100 mg/1
TabletOral150 mg/1
TabletOral25 mg/1
TabletOral50 mg/1
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral150 mg/1
Tablet, film coatedOral25 mg/1
Tablet, film coatedOral50 mg/1
Tablet, film coatedOral75 mg/1
TabletOral10 mg
TabletOral25 mg
TabletOral50 mg
TabletOral75 mg
SyrupOral2 mg
KitTopical
TabletOral
Tablet, film coatedOral
TabletOral100 mg
Kit
Prices
Unit descriptionCostUnit
Amitriptyline hcl powder7.34USD g
Amitriptyline hcl 150 mg tablet1.18USD tablet
Amitriptyline hcl 100 mg tablet0.66USD tablet
Amitriptyline hcl 75 mg tablet0.54USD tablet
Apo-Amitriptyline 75 mg Tablet0.38USD tablet
Amitriptyline hcl 50 mg tablet0.37USD tablet
Amitriptyline hcl 10 mg tablet0.3USD tablet
Apo-Amitriptyline 50 mg Tablet0.25USD tablet
Amitriptyline hcl 25 mg tablet0.21USD tablet
Apo-Amitriptyline 25 mg Tablet0.13USD tablet
Apo-Amitriptyline 10 mg Tablet0.07USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)187-189.5Tristram, E.W. and Tull, R.J.; US. Patent 3,205,264: September 7,1965; assigned to Merck & Co., Inc.
water solubility9.71 mg/L (at 24 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP4.92HANSCH,C ET AL. (1995)
logS-4.46ADME Research, USCD
pKa9.4SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.0045 mg/mLALOGPS
logP5.1ALOGPS
logP4.81ChemAxon
logS-4.8ALOGPS
pKa (Strongest Basic)9.76ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area3.24 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity101.51 m3·mol-1ChemAxon
Polarizability33.74 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9941
Blood Brain Barrier+0.9512
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.7567
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IIInhibitor0.6447
Renal organic cation transporterInhibitor0.7955
CYP450 2C9 substrateNon-substrate0.7826
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.7501
CYP450 1A2 substrateInhibitor0.7324
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8933
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9158
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6955
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.8127
BiodegradationNot ready biodegradable0.8727
Rat acute toxicity2.9697 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7531
hERG inhibition (predictor II)Inhibitor0.6767
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (7.48 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - EI-BGC-MSsplash10-0a4i-9010000000-2afae55587735e5a8ce1
Mass Spectrum (Electron Ionization)MSsplash10-0a4i-9210000000-989cd234a8cdf04c5f69
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-05po-5890000000-4cce07a2d07337e4ce90
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-001i-1590000000-35080e23f36a6ed30005
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-004i-0090000000-66d4e2dc0e65719c8949
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-004i-0190000000-18fad36e219aa0091dcf
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-05o3-3980000000-bd3bb65e31837e45268f
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0aou-2940000000-c3c71a4ddeb15eb427b4
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-05mo-2930000000-f6bc4a5899aed7b3047e
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0fr6-2930000000-c348567e54820b6ddff3
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-004i-0090000000-fae7f4e9cc1f20e9a2dd
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-004i-0190000000-42ecf4fcfbd4bd102322
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-05o3-3980000000-69e1e5d2fdd46de25ba4
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0aou-2940000000-853a0f18213b600d48ae
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-05mo-2930000000-9493535ee63a9a708527
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0fr6-2930000000-fba97ca65c4bf1940385
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-001i-1690000000-99ea606fc86c8400c4ce
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-004i-0090000000-8155764b5e04e44b4ca2
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-004i-0190000000-7e3a5d063f540759d63f
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0apl-0960000000-e35715828f4c02816f19
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0lfu-0940000000-a6befd2c2f6b01d0c348
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0v03-0940000000-cab5377d28cf5d892f47
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004i-2590000000-85fb81c2565771c07a12

Taxonomy

Description
This compound belongs to the class of organic compounds known as dibenzocycloheptenes. These are compounds containing a dibenzocycloheptene moiety, which consists of two benzene rings connected by a cycloheptene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Dibenzocycloheptenes
Sub Class
Not Available
Direct Parent
Dibenzocycloheptenes
Alternative Parents
Trialkylamines / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Dibenzocycloheptene / Tertiary aliphatic amine / Tertiary amine / Organic nitrogen compound / Organopnictogen compound / Hydrocarbon derivative / Organonitrogen compound / Amine / Aromatic homopolycyclic compound
Molecular Framework
Aromatic homopolycyclic compounds
External Descriptors
tertiary amine, organic tricyclic compound (CHEBI:2666)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Norepinephrine:sodium symporter activity
Specific Function
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name
SLC6A2
Uniprot ID
P23975
Uniprot Name
Sodium-dependent noradrenaline transporter
Molecular Weight
69331.42 Da
References
  1. Vaishnavi SN, Nemeroff CB, Plott SJ, Rao SG, Kranzler J, Owens MJ: Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity. Biol Psychiatry. 2004 Feb 1;55(3):320-2. [PubMed:14744476]
  2. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Serotonin:sodium symporter activity
Specific Function
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into t...
Gene Name
SLC6A4
Uniprot ID
P31645
Uniprot Name
Sodium-dependent serotonin transporter
Molecular Weight
70324.165 Da
References
  1. Gould GG, Altamirano AV, Javors MA, Frazer A: A comparison of the chronic treatment effects of venlafaxine and other antidepressants on serotonin and norepinephrine transporters. Biol Psychiatry. 2006 Mar 1;59(5):408-14. Epub 2005 Sep 2. [PubMed:16140280]
  2. Troelsen KB, Nielsen EO, Mirza NR: Chronic treatment with duloxetine is necessary for an anxiolytic-like response in the mouse zero maze: the role of the serotonin transporter. Psychopharmacology (Berl). 2005 Oct;181(4):741-50. Epub 2005 Sep 29. [PubMed:16032412]
  3. Vaishnavi SN, Nemeroff CB, Plott SJ, Rao SG, Kranzler J, Owens MJ: Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity. Biol Psychiatry. 2004 Feb 1;55(3):320-2. [PubMed:14744476]
  4. Ushijima K, Sakaguchi H, Sato Y, To H, Koyanagi S, Higuchi S, Ohdo S: Chronopharmacological study of antidepressants in forced swimming test of mice. J Pharmacol Exp Ther. 2005 Nov;315(2):764-70. Epub 2005 Aug 3. [PubMed:16079297]
  5. Kalia M: Neurobiological basis of depression: an update. Metabolism. 2005 May;54(5 Suppl 1):24-7. [PubMed:15877309]
  6. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821]
  7. Werling LL, Keller A, Frank JG, Nuwayhid SJ: A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder. Exp Neurol. 2007 Oct;207(2):248-57. Epub 2007 Jun 30. [PubMed:17689532]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Opioid receptor activity
Specific Function
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
Gene Name
OPRD1
Uniprot ID
P41143
Uniprot Name
Delta-type opioid receptor
Molecular Weight
40368.235 Da
References
  1. Onali P, Dedoni S, Olianas MC: Direct agonist activity of tricyclic antidepressants at distinct opioid receptor subtypes. J Pharmacol Exp Ther. 2010 Jan;332(1):255-65. doi: 10.1124/jpet.109.159939. Epub 2009 Oct 14. [PubMed:19828880]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Opioid receptor activity
Specific Function
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
Gene Name
OPRK1
Uniprot ID
P41145
Uniprot Name
Kappa-type opioid receptor
Molecular Weight
42644.665 Da
References
  1. Onali P, Dedoni S, Olianas MC: Direct agonist activity of tricyclic antidepressants at distinct opioid receptor subtypes. J Pharmacol Exp Ther. 2010 Jan;332(1):255-65. doi: 10.1124/jpet.109.159939. Epub 2009 Oct 14. [PubMed:19828880]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Transmembrane receptor protein tyrosine kinase activity
Specific Function
Receptor tyrosine kinase involved in the development and the maturation of the central and peripheral nervous systems through regulation of proliferation, differentiation and survival of sympatheti...
Gene Name
NTRK1
Uniprot ID
P04629
Uniprot Name
High affinity nerve growth factor receptor
Molecular Weight
87496.465 Da
References
  1. Jang SW, Liu X, Chan CB, Weinshenker D, Hall RA, Xiao G, Ye K: Amitriptyline is a TrkA and TrkB receptor agonist that promotes TrkA/TrkB heterodimerization and has potent neurotrophic activity. Chem Biol. 2009 Jun 26;16(6):644-56. doi: 10.1016/j.chembiol.2009.05.010. [PubMed:19549602]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Protein homodimerization activity
Specific Function
Receptor tyrosine kinase involved in the development and the maturation of the central and the peripheral nervous systems through regulation of neuron survival, proliferation, migration, differenti...
Gene Name
NTRK2
Uniprot ID
Q16620
Uniprot Name
BDNF/NT-3 growth factors receptor
Molecular Weight
91998.175 Da
References
  1. Jang SW, Liu X, Chan CB, Weinshenker D, Hall RA, Xiao G, Ye K: Amitriptyline is a TrkA and TrkB receptor agonist that promotes TrkA/TrkB heterodimerization and has potent neurotrophic activity. Chem Biol. 2009 Jun 26;16(6):644-56. doi: 10.1016/j.chembiol.2009.05.010. [PubMed:19549602]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217]
  2. Nojimoto FD, Mueller A, Hebeler-Barbosa F, Akinaga J, Lima V, Kiguti LR, Pupo AS: The tricyclic antidepressants amitriptyline, nortriptyline and imipramine are weak antagonists of human and rat alpha1B-adrenoceptors. Neuropharmacology. 2010 Jul-Aug;59(1-2):49-57. doi: 10.1016/j.neuropharm.2010.03.015. Epub 2010 Apr 2. [PubMed:20363235]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Alpha1-adrenergic receptor activity
Specific Function
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name
ADRA1D
Uniprot ID
P25100
Uniprot Name
Alpha-1D adrenergic receptor
Molecular Weight
60462.205 Da
References
  1. Nojimoto FD, Mueller A, Hebeler-Barbosa F, Akinaga J, Lima V, Kiguti LR, Pupo AS: The tricyclic antidepressants amitriptyline, nortriptyline and imipramine are weak antagonists of human and rat alpha1B-adrenoceptors. Neuropharmacology. 2010 Jul-Aug;59(1-2):49-57. doi: 10.1016/j.neuropharm.2010.03.015. Epub 2010 Apr 2. [PubMed:20363235]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217]
  2. Ozdogan UK, Lahdesmaki J, Mansikka H, Scheinin M: Loss of amitriptyline analgesia in alpha 2A-adrenoceptor deficient mice. Eur J Pharmacol. 2004 Feb 6;485(1-3):193-6. [PubMed:14757140]
Details
12. Histamine H1 receptor
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
Molecular Weight
66127.445 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Guanyl-nucleotide exchange factor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Voltage-gated potassium channel activity
Specific Function
Probably important in the regulation of neuronal excitability. Associates with KCNQ3 to form a potassium channel with essentially identical properties to the channel underlying the native M-current...
Gene Name
KCNQ2
Uniprot ID
O43526
Uniprot Name
Potassium voltage-gated channel subfamily KQT member 2
Molecular Weight
95846.575 Da
References
  1. Punke MA, Friederich P: Amitriptyline is a potent blocker of human Kv1.1 and Kv7.2/7.3 channels. Anesth Analg. 2007 May;104(5):1256-64, tables of contents. [PubMed:17456683]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Voltage-gated potassium channel activity
Specific Function
Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain and the central nervous system, but also in the kidney (PubMed:1990381...
Gene Name
KCNA1
Uniprot ID
Q09470
Uniprot Name
Potassium voltage-gated channel subfamily A member 1
Molecular Weight
56465.01 Da
References
  1. Punke MA, Friederich P: Amitriptyline is a potent blocker of human Kv1.1 and Kv7.2/7.3 channels. Anesth Analg. 2007 May;104(5):1256-64, tables of contents. [PubMed:17456683]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Voltage-gated potassium channel activity
Specific Function
Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain. Mediates the major part of the dendritic A-type current I(SA) in brai...
Gene Name
KCND2
Uniprot ID
Q9NZV8
Uniprot Name
Potassium voltage-gated channel subfamily D member 2
Molecular Weight
70535.825 Da
References
  1. Casis O, Sanchez-Chapula JA: Disopyramide, imipramine, and amitriptyline bind to a common site on the transient outward K+ channel. J Cardiovasc Pharmacol. 1998 Oct;32(4):521-6. [PubMed:9781919]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Pore-forming (alpha) subunit of voltage-gated rapidly inactivating A-type potassium channels. May contribute to I(To) current in heart and I(Sa) current in neurons. Channel properties are modulated...
Gene Name
KCND3
Uniprot ID
Q9UK17
Uniprot Name
Potassium voltage-gated channel subfamily D member 3
Molecular Weight
73450.53 Da
References
  1. Casis O, Sanchez-Chapula JA: Disopyramide, imipramine, and amitriptyline bind to a common site on the transient outward K+ channel. J Cardiovasc Pharmacol. 1998 Oct;32(4):521-6. [PubMed:9781919]
Details
22. Histamine H2 receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Blocker
General Function
Histamine receptor activity
Specific Function
The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and diff...
Gene Name
HRH2
Uniprot ID
P25021
Uniprot Name
Histamine H2 receptor
Molecular Weight
40097.65 Da
References
  1. Angus JA, Black JW: Pharmacological assay of cardiac H2-receptor blockade by amitriptyline and lysergic acid diethylamide. Circ Res. 1980 Jun;46(6 Pt 2):I64-9. [PubMed:6103762]
Details
23. Histamine H4 receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Histamine receptor activity
Specific Function
The H4 subclass of histamine receptors could mediate the histamine signals in peripheral tissues. Displays a significant level of constitutive activity (spontaneous activity in the absence of agoni...
Gene Name
HRH4
Uniprot ID
Q9H3N8
Uniprot Name
Histamine H4 receptor
Molecular Weight
44495.375 Da
References
  1. Nguyen T, Shapiro DA, George SR, Setola V, Lee DK, Cheng R, Rauser L, Lee SP, Lynch KR, Roth BL, O'Dowd BF: Discovery of a novel member of the histamine receptor family. Mol Pharmacol. 2001 Mar;59(3):427-33. [PubMed:11179435]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Opioid receptor activity
Specific Function
Functions in lipid transport from the endoplasmic reticulum and is involved in a wide array of cellular functions probably through regulation of the biogenesis of lipid microdomains at the plasma m...
Gene Name
SIGMAR1
Uniprot ID
Q99720
Uniprot Name
Sigma non-opioid intracellular receptor 1
Molecular Weight
25127.52 Da
References
  1. Villard V, Meunier J, Chevallier N, Maurice T: Pharmacological interaction with the sigma1 (sigma1)-receptor in the acute behavioral effects of antidepressants. J Pharmacol Sci. 2011;115(3):279-92. [PubMed:21427517]
  2. Werling LL, Keller A, Frank JG, Nuwayhid SJ: A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder. Exp Neurol. 2007 Oct;207(2):248-57. Epub 2007 Jun 30. [PubMed:17689532]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Di Matteo V, De Blasi A, Di Giulio C, Esposito E: Role of 5-HT(2C) receptors in the control of central dopamine function. Trends Pharmacol Sci. 2001 May;22(5):229-32. [PubMed:11339973]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
Molecular Weight
56835.375 Da
References
  1. Nojimoto FD, Mueller A, Hebeler-Barbosa F, Akinaga J, Lima V, Kiguti LR, Pupo AS: The tricyclic antidepressants amitriptyline, nortriptyline and imipramine are weak antagonists of human and rat alpha1B-adrenoceptors. Neuropharmacology. 2010 Jul-Aug;59(1-2):49-57. doi: 10.1016/j.neuropharm.2010.03.015. Epub 2010 Apr 2. [PubMed:20363235]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
Molecular Weight
53554.43 Da
References
  1. Lucchelli A, Santagostino-Barbone MG, D'Agostino G, Masoero E, Tonini M: The interaction of antidepressant drugs with enteric 5-HT7 receptors. Naunyn Schmiedebergs Arch Pharmacol. 2000 Sep;362(3):284-9. [PubMed:10997731]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. Werling LL, Keller A, Frank JG, Nuwayhid SJ: A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder. Exp Neurol. 2007 Oct;207(2):248-57. Epub 2007 Jun 30. [PubMed:17689532]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Voltage-gated calcium channel activity
Specific Function
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
Gene Name
OPRM1
Uniprot ID
P35372
Uniprot Name
Mu-type opioid receptor
Molecular Weight
44778.855 Da
References
  1. Wahlstrom A, Lenhammar L, Ask B, Rane A: Tricyclic antidepressants inhibit opioid receptor binding in human brain and hepatic morphine glucuronidation. Pharmacol Toxicol. 1994 Jul;75(1):23-7. [PubMed:7971731]
  2. Hamon M, Gozlan H, Bourgoin S, Benoliel JJ, Mauborgne A, Taquet H, Cesselin F, Mico JA: Opioid receptors and neuropeptides in the CNS in rats treated chronically with amoxapine or amitriptyline. Neuropharmacology. 1987 Jun;26(6):531-9. [PubMed:3037421]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 Da
References
  1. Werling LL, Keller A, Frank JG, Nuwayhid SJ: A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder. Exp Neurol. 2007 Oct;207(2):248-57. Epub 2007 Jun 30. [PubMed:17689532]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR6
Uniprot ID
P50406
Uniprot Name
5-hydroxytryptamine receptor 6
Molecular Weight
46953.625 Da
References
  1. Kohen R, Metcalf MA, Khan N, Druck T, Huebner K, Lachowicz JE, Meltzer HY, Sibley DR, Roth BL, Hamblin MW: Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. J Neurochem. 1996 Jan;66(1):47-56. [PubMed:8522988]
  2. Sebben M, Ansanay H, Bockaert J, Dumuis A: 5-HT6 receptors positively coupled to adenylyl cyclase in striatal neurones in culture. Neuroreport. 1994 Dec 20;5(18):2553-7. [PubMed:7696602]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Voltage-gated potassium channel activity
Specific Function
Probably important in the regulation of neuronal excitability. Associates with KCNQ2 or KCNQ5 to form a potassium channel with essentially identical properties to the channel underlying the native ...
Gene Name
KCNQ3
Uniprot ID
O43525
Uniprot Name
Potassium voltage-gated channel subfamily KQT member 3
Molecular Weight
96741.515 Da
References
  1. Punke MA, Friederich P: Amitriptyline is a potent blocker of human Kv1.1 and Kv7.2/7.3 channels. Anesth Analg. 2007 May;104(5):1256-64, tables of contents. [PubMed:17456683]
Kind
Protein group
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Receptor signaling protein activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately e...

Components:
References
  1. Werling LL, Keller A, Frank JG, Nuwayhid SJ: A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder. Exp Neurol. 2007 Oct;207(2):248-57. Epub 2007 Jun 30. [PubMed:17689532]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Baumann P: Pharmacokinetic-pharmacodynamic relationship of the selective serotonin reuptake inhibitors. Clin Pharmacokinet. 1996 Dec;31(6):444-69. [PubMed:8968657]
  2. Wen B, Ma L, Zhu M: Bioactivation of the tricyclic antidepressant amitriptyline and its metabolite nortriptyline to arene oxide intermediates in human liver microsomes and recombinant P450s. Chem Biol Interact. 2008 May 9;173(1):59-67. doi: 10.1016/j.cbi.2008.02.001. Epub 2008 Feb 14. [PubMed:18359012]
  3. Ghahramani P, Ellis SW, Lennard MS, Ramsay LE, Tucker GT: Cytochromes P450 mediating the N-demethylation of amitriptyline. Br J Clin Pharmacol. 1997 Feb;43(2):137-44. [PubMed:9131945]
  4. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  5. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  6. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560]
  7. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Wen B, Ma L, Zhu M: Bioactivation of the tricyclic antidepressant amitriptyline and its metabolite nortriptyline to arene oxide intermediates in human liver microsomes and recombinant P450s. Chem Biol Interact. 2008 May 9;173(1):59-67. doi: 10.1016/j.cbi.2008.02.001. Epub 2008 Feb 14. [PubMed:18359012]
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  4. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
  6. Website [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Shin JG, Park JY, Kim MJ, Shon JH, Yoon YR, Cha IJ, Lee SS, Oh SW, Kim SW, Flockhart DA: Inhibitory effects of tricyclic antidepressants (TCAs) on human cytochrome P450 enzymes in vitro: mechanism of drug interaction between TCAs and phenytoin. Drug Metab Dispos. 2002 Oct;30(10):1102-7. [PubMed:12228186]
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  4. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Ghahramani P, Ellis SW, Lennard MS, Ramsay LE, Tucker GT: Cytochromes P450 mediating the N-demethylation of amitriptyline. Br J Clin Pharmacol. 1997 Feb;43(2):137-44. [PubMed:9131945]
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  4. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Wen B, Ma L, Zhu M: Bioactivation of the tricyclic antidepressant amitriptyline and its metabolite nortriptyline to arene oxide intermediates in human liver microsomes and recombinant P450s. Chem Biol Interact. 2008 May 9;173(1):59-67. doi: 10.1016/j.cbi.2008.02.001. Epub 2008 Feb 14. [PubMed:18359012]
  2. Ghahramani P, Ellis SW, Lennard MS, Ramsay LE, Tucker GT: Cytochromes P450 mediating the N-demethylation of amitriptyline. Br J Clin Pharmacol. 1997 Feb;43(2):137-44. [PubMed:9131945]
  3. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  4. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  5. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Wen B, Ma L, Zhu M: Bioactivation of the tricyclic antidepressant amitriptyline and its metabolite nortriptyline to arene oxide intermediates in human liver microsomes and recombinant P450s. Chem Biol Interact. 2008 May 9;173(1):59-67. doi: 10.1016/j.cbi.2008.02.001. Epub 2008 Feb 14. [PubMed:18359012]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
No
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Brinkschulte M, Breyer-Pfaff U: The contribution of alpha 1-acid glycoprotein, lipoproteins, and albumin to the plasma binding of perazine, amitriptyline, and nortriptyline in healthy man. Naunyn Schmiedebergs Arch Pharmacol. 1980 Oct;314(1):61-6. [PubMed:6108517]
  2. Banerjee T, Singh SK, Kishore N: Binding of naproxen and amitriptyline to bovine serum albumin: biophysical aspects. J Phys Chem B. 2006 Nov 30;110(47):24147-56. [PubMed:17125386]
Kind
Protein
Organism
Human
Pharmacological action
No
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
Molecular Weight
23511.38 Da
References
  1. Brinkschulte M, Breyer-Pfaff U: The contribution of alpha 1-acid glycoprotein, lipoproteins, and albumin to the plasma binding of perazine, amitriptyline, and nortriptyline in healthy man. Naunyn Schmiedebergs Arch Pharmacol. 1980 Oct;314(1):61-6. [PubMed:6108517]
  2. Ferry DG, Caplan NB, Cubeddu LX: Interaction between antidepressants and alpha 1-adrenergic receptor antagonists on the binding to alpha 1-acid glycoprotein. J Pharm Sci. 1986 Feb;75(2):146-9. [PubMed:2870173]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [PubMed:12438524]
  2. Faassen F, Vogel G, Spanings H, Vromans H: Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22. [PubMed:12954186]

Drug created on June 13, 2005 07:24 / Updated on April 23, 2018 22:58