Identification

Name
Nortriptyline
Accession Number
DB00540  (APRD00602)
Type
Small Molecule
Groups
Approved
Description

Nortriptyline hydrochloride, the N-demethylated active metabolite of amitriptyline, is a dibenzocycloheptene-derivative tricyclic antidepressant (TCA). 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, nortriptyline does not affect mood or arousal, but may cause sedation. In depressed individuals, nortriptyline exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Secondary amine TCAs, such as nortriptyline, are more potent inhibitors of norepinephrine reuptake than tertiary amine TCAs, such as amitriptyline. 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. See toxicity section below for a complete listing of side effects. Nortriptyline exerts less anticholinergic and sedative side effects compared to the tertiary amine TCAs, amitriptyline and clomipramine. Nortriptyline 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-N-Methyl-5H-dibenzo[a,D]cycloheptene-delta(5,gamma)-propylamine
  • 3-(10,11-dihydro-5H-Dibenzo[a,D]cyclohepten-5-ylidene)-N-methyl-1-propanamine
  • Ateben
  • Avantyl
  • Demethylamitriptyline
  • Desmethylamitriptyline
  • Noritren
  • Nortriptyline
  • Psychostyl
  • Sensaval
External IDs
NCI-169453
Product Ingredients
IngredientUNIICASInChI Key
Nortriptyline Hydrochloride00FN6IH15D894-71-3SHAYBENGXDALFF-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AventylCapsule10 mgOralAa Pharma Inc1965-12-31Not applicableCanada
AventylCapsule25 mgOralAa Pharma Inc1965-12-31Not applicableCanada
NortriptylineCapsule25 mgOralPharmel Inc1998-06-042014-09-08Canada
NortriptylineCapsule10 mgOralPharmel Inc1998-06-042014-09-08Canada
Nortriptyline-10Capsule10 mgOralPro Doc Limitee2008-03-072016-07-18Canada
Nortriptyline-25Capsule25 mgOralPro Doc Limitee2008-03-072016-07-18Canada
NorventylCapsule10 mgOralValeant Canada Lp Valeant Canada S.E.C.1997-02-042014-07-30Canada
NorventylCapsule25 mgOralValeant Canada Lp Valeant Canada S.E.C.1997-02-042014-07-30Canada
PamelorCapsule10 mg/1OralMallinckrodt2010-08-03Not applicableUs
PamelorCapsule50 mg/1OralMallinckrodt2010-08-03Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-nortriptyline - Cap 10mgCapsule10 mgOralApotex Corporation1996-09-26Not applicableCanada
Apo-nortriptyline - Cap 25mgCapsule25 mgOralApotex Corporation1996-09-26Not applicableCanada
Ava-nortriptylineCapsule25 mgOralAvanstra Inc2011-11-282014-08-21Canada
Ava-nortriptylineCapsule10 mgOralAvanstra Inc2011-11-282014-08-21Canada
Dom-nortriptyline 10mg CapsulesCapsule10 mgOralDominion Pharmacal1995-10-012014-09-08Canada
Dom-nortriptyline 25mg CapsulesCapsule25 mgOralDominion Pharmacal1995-10-012014-09-08Canada
Gen-nortriptyline Capsules 10mgCapsule10 mgOralGenpharm Ulc1997-09-052009-08-05Canada
Gen-nortriptyline Capsules 25mgCapsule25 mgOralGenpharm Ulc1997-09-052009-08-05Canada
Nortriptyline HydrochlorideCapsule75 mg/1OralMayne Pharma2016-07-18Not applicableUs
Nortriptyline HydrochlorideCapsule10 mg/1OralRemedy Repack2010-11-162017-03-09Us
International/Other Brands
Allegron / Aventyl / Noritren / Norpress / Nortrilen / Sensoval
Categories
UNII
BL03SY4LXB
CAS number
72-69-5
Weight
Average: 263.3767
Monoisotopic: 263.167399677
Chemical Formula
C19H21N
InChI Key
PHVGLTMQBUFIQQ-UHFFFAOYSA-N
InChI
InChI=1S/C19H21N/c1-20-14-6-11-19-17-9-4-2-7-15(17)12-13-16-8-3-5-10-18(16)19/h2-5,7-11,20H,6,12-14H2,1H3
IUPAC Name
methyl(3-{tricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,11,13-hexaen-2-ylidene}propyl)amine
SMILES
CNCCC=C1C2=CC=CC=C2CCC2=CC=CC=C12

Pharmacology

Indication

For the treatment of depression, chronic pain, irritable bowel syndrome, sleep disorders, diabetic neuropathy, agitation and insomnia, and migraine prophylaxis.

Structured Indications
Pharmacodynamics

Similar to protriptyline, nortriptyline is a tricyclic antidepressant of the dibenzocycloheptene type and is the active metabolite of amitriptyline.

Mechanism of action

It is believed that nortriptyline either inhibits the reuptake of the neurotransmitter serotonin at the neuronal membrane or acts at beta-adrenergic receptors. Tricyclic antidepressants do not inhibit monoamine oxidase nor do they affect dopamine reuptake.

TargetActionsOrganism
ASodium-dependent noradrenaline transporter
inhibitor
Human
ASodium-dependent serotonin transporter
inhibitor
Human
A5-hydroxytryptamine receptor 2A
antagonist
Human
U5-hydroxytryptamine receptor 1A
antagonist
Human
NHistamine H1 receptor
antagonist
Human
NAlpha-1A adrenergic receptor
antagonist
Human
NAlpha-1D adrenergic 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
U5-hydroxytryptamine receptor 2C
antagonist
Human
U5-hydroxytryptamine receptor 6
binder
Human
UAlpha-1B adrenergic receptor
antagonist
Human
UAlpha-2 adrenergic receptors
antagonist
Human
UBeta adrenergic receptor
antagonist
Human
UD(2) dopamine receptor
antagonist
Human
USigma receptor
binder
Human
U5-hydroxytryptamine receptor 1C
antagonist
Rat
Absorption

Well absorbed from the GI tract. Peak plasma concentrations occur 7-8.5 hours following oral administration.

Volume of distribution
Not Available
Protein binding

Highly protein-bound in plasma and tissues.

Metabolism

Undergoes hepatic metabolism via the same pathway as other TCAs.

Route of elimination

Approximately one-third of a single orally administered dose is excreted in urine within 24 hours. Small amounts are excreted in feces via biliary elimination.

Half life

16 to 90+ hours

Clearance
Not Available
Toxicity

Symptoms of overdose include cardiac dysrhythmias, severe hypotension, shock, congestive heart failure, pulmonary edema, convulsions, and CNS depression, including coma. Changes in the electrocardiogram, particularly in QRS axis or width, are clinically significant indicators of tricyclic antidepressant toxicity. 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 nortriptyline.Details
Cytochrome P450 2D6CYP2D6*3Not Available2549delAEffect Directly StudiedThe presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of nortriptyline.Details
Cytochrome P450 2D6CYP2D6*4Not AvailableA alleleEffect Directly StudiedThe presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of nortriptyline.Details
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole-gene deletionEffect Directly StudiedThe presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of nortriptyline.Details
Cytochrome P450 2D6CYP2D6*6Not Available1707delTEffect Directly StudiedThe presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of nortriptyline.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 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 2D6CYP2D6*3Not AvailableG alleleEffect Directly StudiedThe presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of nortriptyline.Details
Cytochrome P450 2D6CYP2D6*4Not Available3877G>AEffect Directly StudiedThe presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of nortriptyline.Details

Interactions

Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe serum concentration of Nortriptyline can be increased when it is combined with 1,10-Phenanthroline.Experimental
2,5-Dimethoxy-4-ethylamphetamineNortriptyline may increase the stimulatory activities of 2,5-Dimethoxy-4-ethylamphetamine.Experimental, Illicit
2,5-Dimethoxy-4-ethylthioamphetamineNortriptyline may increase the stimulatory activities of 2,5-Dimethoxy-4-ethylthioamphetamine.Experimental
3,4-DichloroisocoumarinThe serum concentration of Nortriptyline can be increased when it is combined with 3,4-Dichloroisocoumarin.Experimental
3,4-MethylenedioxyamphetamineNortriptyline may increase the stimulatory activities of 3,4-Methylenedioxyamphetamine.Experimental, Illicit
4-(2-Aminoethyl)Benzenesulfonyl FluorideThe serum concentration of Nortriptyline can be increased when it is combined with 4-(2-Aminoethyl)Benzenesulfonyl Fluoride.Experimental
4-Bromo-2,5-dimethoxyamphetamineNortriptyline may increase the stimulatory activities of 4-Bromo-2,5-dimethoxyamphetamine.Experimental, Illicit
4-MethoxyamphetamineNortriptyline may decrease the antihypertensive activities of 4-Methoxyamphetamine.Experimental, Illicit
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the serotonergic activities of Nortriptyline.Experimental
AbirateroneThe serum concentration of Nortriptyline can be increased when it is combined with Abiraterone.Approved
AcenocoumarolNortriptyline may increase the anticoagulant activities of Acenocoumarol.Approved
AgmatineNortriptyline may decrease the antihypertensive activities of Agmatine.Experimental, Investigational
AlogliptinThe serum concentration of Nortriptyline can be increased when it is combined with Alogliptin.Approved
Alpha-1-proteinase inhibitorThe serum concentration of Nortriptyline can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
AltretamineAltretamine may increase the orthostatic hypotensive activities of Nortriptyline.Approved
AmiodaroneThe metabolism of Nortriptyline can be decreased when combined with Amiodarone.Approved, Investigational
AmobarbitalThe metabolism of Nortriptyline can be increased when combined with Amobarbital.Approved, Illicit
AmphetamineNortriptyline may increase the stimulatory activities of Amphetamine.Approved, Illicit
AmprenavirThe serum concentration of Nortriptyline can be increased when it is combined with Amprenavir.Approved
Antithrombin III humanThe serum concentration of Nortriptyline can be increased when it is combined with Antithrombin III human.Approved
ApixabanThe serum concentration of Nortriptyline can be increased when it is combined with Apixaban.Approved
ApomorphineNortriptyline may decrease the antihypertensive activities of Apomorphine.Approved, Investigational
ApraclonidineNortriptyline may decrease the antihypertensive activities of Apraclonidine.Approved
AprepitantThe serum concentration of Nortriptyline can be increased when it is combined with Aprepitant.Approved, Investigational
AprotininThe serum concentration of Nortriptyline can be increased when it is combined with Aprotinin.Approved, Withdrawn
ArbutamineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Arbutamine.Approved
ArformoterolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Arformoterol.Approved, Investigational
ArgatrobanThe serum concentration of Nortriptyline can be increased when it is combined with Argatroban.Approved, Investigational
ArmodafinilThe metabolism of Nortriptyline can be decreased when combined with Armodafinil.Approved, Investigational
ArtemetherThe metabolism of Nortriptyline can be decreased when combined with Artemether.Approved
AsunaprevirThe serum concentration of Nortriptyline can be increased when it is combined with Asunaprevir.Approved, Investigational
AtazanavirThe metabolism of Nortriptyline can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Nortriptyline can be decreased when combined with Atomoxetine.Approved
AzithromycinThe metabolism of Nortriptyline can be decreased when combined with Azithromycin.Approved
BambuterolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Bambuterol.Approved, Investigational
BarbexacloneThe metabolism of Nortriptyline can be increased when combined with Barbexaclone.Experimental
BarbitalThe metabolism of Nortriptyline can be increased when combined with Barbital.Illicit
BatimastatThe serum concentration of Nortriptyline can be increased when it is combined with Batimastat.Experimental
BenazeprilThe serum concentration of Nortriptyline can be increased when it is combined with Benazepril.Approved, Investigational
BenzamidineThe serum concentration of Nortriptyline can be increased when it is combined with Benzamidine.Experimental
BenzphetamineNortriptyline may decrease the antihypertensive activities of Benzphetamine.Approved, Illicit
BetaxololThe metabolism of Nortriptyline can be decreased when combined with Betaxolol.Approved
BethanidineNortriptyline may decrease the antihypertensive activities of Bethanidine.Approved
BivalirudinThe serum concentration of Nortriptyline can be increased when it is combined with Bivalirudin.Approved, Investigational
BoceprevirThe metabolism of Nortriptyline can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Nortriptyline can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Nortriptyline can be decreased when it is combined with Bosentan.Approved, Investigational
BrofaromineBrofaromine may increase the serotonergic activities of Nortriptyline.Experimental
BromocriptineNortriptyline may decrease the antihypertensive activities of Bromocriptine.Approved, Investigational
BupropionThe metabolism of Nortriptyline can be decreased when combined with Bupropion.Approved
CaffeineThe metabolism of Nortriptyline can be decreased when combined with Caffeine.Approved
CamostatThe serum concentration of Nortriptyline can be increased when it is combined with Camostat.Experimental
CandoxatrilThe serum concentration of Nortriptyline can be increased when it is combined with Candoxatril.Experimental
CandoxatrilatThe serum concentration of Nortriptyline can be increased when it is combined with Candoxatrilat.Experimental
CapecitabineThe metabolism of Nortriptyline can be decreased when combined with Capecitabine.Approved, Investigational
CaptoprilThe serum concentration of Nortriptyline can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Nortriptyline can be increased when combined with Carbamazepine.Approved, Investigational
CelecoxibThe metabolism of Nortriptyline can be decreased when combined with Celecoxib.Approved, Investigational
CeliprololThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Celiprolol.Approved, Investigational
CeritinibThe serum concentration of Nortriptyline can be increased when it is combined with Ceritinib.Approved
ChloramphenicolThe metabolism of Nortriptyline can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChloroquineThe metabolism of Nortriptyline can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorphentermineNortriptyline may increase the stimulatory activities of Chlorphentermine.Illicit, Withdrawn
ChlorpromazineThe metabolism of Nortriptyline can be decreased when combined with Chlorpromazine.Approved, Vet Approved
CholecalciferolThe metabolism of Nortriptyline can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholesterolThe serum concentration of Nortriptyline can be increased when it is combined with Cholesterol.Experimental, Investigational
ChymostatinThe serum concentration of Nortriptyline can be increased when it is combined with Chymostatin.Experimental
CilastatinThe serum concentration of Nortriptyline can be increased when it is combined with Cilastatin.Approved
CilazaprilThe serum concentration of Nortriptyline can be increased when it is combined with Cilazapril.Approved
CimetidineThe metabolism of Nortriptyline can be decreased when combined with Cimetidine.Approved
CinacalcetThe serum concentration of Nortriptyline can be increased when it is combined with Cinacalcet.Approved
CirazolineNortriptyline may increase the vasopressor activities of Cirazoline.Experimental
CitalopramThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Citalopram.Approved
ClarithromycinThe metabolism of Nortriptyline can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Nortriptyline can be decreased when combined with Clemastine.Approved
ClenbuterolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Clenbuterol.Approved, Investigational, Vet Approved
ClobazamThe metabolism of Nortriptyline can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Nortriptyline can be decreased when combined with Clomipramine.Approved, Vet Approved
ClonidineNortriptyline may decrease the antihypertensive activities of Clonidine.Approved
ClorindioneNortriptyline may increase the anticoagulant activities of Clorindione.Experimental
ClotrimazoleThe metabolism of Nortriptyline can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Nortriptyline can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Nortriptyline can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Nortriptyline can be decreased when combined with Cocaine.Approved, Illicit
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Nortriptyline.Approved, Investigational
CrisaboroleThe metabolism of Nortriptyline can be decreased when combined with Crisaborole.Approved, Investigational
CrizotinibThe metabolism of Nortriptyline can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Nortriptyline can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Nortriptyline can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
Dabigatran etexilateThe serum concentration of Nortriptyline can be increased when it is combined with Dabigatran etexilate.Approved
DabrafenibThe serum concentration of Nortriptyline can be decreased when it is combined with Dabrafenib.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Nortriptyline.Investigational
DarexabanThe serum concentration of Nortriptyline can be increased when it is combined with Darexaban.Investigational
DarifenacinThe metabolism of Nortriptyline can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Nortriptyline can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Nortriptyline can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Nortriptyline can be decreased when it is combined with Deferasirox.Approved, Investigational
DelanzomibThe serum concentration of Nortriptyline can be increased when it is combined with Delanzomib.Investigational
DelaprilThe serum concentration of Nortriptyline can be increased when it is combined with Delapril.Experimental
DelavirdineThe metabolism of Nortriptyline can be decreased when combined with Delavirdine.Approved
DesipramineThe metabolism of Nortriptyline can be decreased when combined with Desipramine.Approved
DesmopressinThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Desmopressin.Approved
DexmedetomidineNortriptyline 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 Nortriptyline.Approved
DextroamphetamineNortriptyline may increase the stimulatory activities of Dextroamphetamine.Approved, Illicit
DicoumarolNortriptyline may increase the anticoagulant activities of Dicoumarol.Approved
DiethylpropionNortriptyline may increase the stimulatory activities of Diethylpropion.Approved, Illicit
DihydroergotamineNortriptyline may decrease the antihypertensive activities of Dihydroergotamine.Approved
DiltiazemThe metabolism of Nortriptyline can be decreased when combined with Diltiazem.Approved
DiphenadioneNortriptyline may increase the anticoagulant activities of Diphenadione.Experimental
DiphenhydramineThe metabolism of Nortriptyline can be decreased when combined with Diphenhydramine.Approved
DipivefrinNortriptyline may decrease the antihypertensive activities of Dipivefrin.Approved
DobutamineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Dobutamine.Approved
DosulepinThe metabolism of Nortriptyline can be decreased when combined with Dosulepin.Approved
DoxycyclineThe metabolism of Nortriptyline can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Nortriptyline can be decreased when combined with Dronedarone.Approved
DroxidopaNortriptyline may decrease the antihypertensive activities of Droxidopa.Approved, Investigational
DuloxetineDuloxetine may increase the serotonergic activities of Nortriptyline.Approved
EcabetThe serum concentration of Nortriptyline can be increased when it is combined with Ecabet.Approved, Investigational
EdoxabanThe serum concentration of Nortriptyline can be increased when it is combined with Edoxaban.Approved
EfavirenzThe metabolism of Nortriptyline can be decreased when combined with Efavirenz.Approved, Investigational
ElafinThe serum concentration of Nortriptyline can be increased when it is combined with Elafin.Investigational
EliglustatThe metabolism of Nortriptyline can be decreased when combined with Eliglustat.Approved
EnalaprilThe serum concentration of Nortriptyline can be increased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe serum concentration of Nortriptyline can be increased when it is combined with Enalaprilat.Approved
EnalkirenThe serum concentration of Nortriptyline can be increased when it is combined with Enalkiren.Experimental
EnzalutamideThe serum concentration of Nortriptyline can be decreased when it is combined with Enzalutamide.Approved
EphedraNortriptyline may decrease the antihypertensive activities of Ephedra.Approved, Nutraceutical, Withdrawn
Epigallocatechin GallateThe serum concentration of Nortriptyline can be increased when it is combined with Epigallocatechin Gallate.Investigational
EpinephrineNortriptyline may decrease the antihypertensive activities of Epinephrine.Approved, Vet Approved
ErgotamineNortriptyline may decrease the antihypertensive activities of Ergotamine.Approved
ErythromycinThe metabolism of Nortriptyline can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe metabolism of Nortriptyline can be decreased when combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Nortriptyline can be decreased when combined with Esomeprazole.Approved, Investigational
Ethyl biscoumacetateNortriptyline may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtomidateNortriptyline may decrease the antihypertensive activities of Etomidate.Approved
EtravirineThe metabolism of Nortriptyline can be decreased when combined with Etravirine.Approved
FaldaprevirThe serum concentration of Nortriptyline can be increased when it is combined with Faldaprevir.Investigational
FenoterolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Fenoterol.Approved, Investigational
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nortriptyline.Approved
FloxuridineThe metabolism of Nortriptyline can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Nortriptyline can be decreased when combined with Fluconazole.Approved
FluindioneNortriptyline may increase the anticoagulant activities of Fluindione.Investigational
FluorouracilThe metabolism of Nortriptyline can be decreased when combined with Fluorouracil.Approved
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Nortriptyline.Approved, Vet Approved
FluvastatinThe metabolism of Nortriptyline can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Nortriptyline.Approved, Investigational
FormoterolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Formoterol.Approved, Investigational
FosamprenavirThe serum concentration of Nortriptyline can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Nortriptyline can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe serum concentration of Nortriptyline can be increased when it is combined with Fosinopril.Approved
FosphenytoinThe metabolism of Nortriptyline can be increased when combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the serotonergic activities of Nortriptyline.Approved, Investigational, Vet Approved
Fusidic AcidThe serum concentration of Nortriptyline can be increased when it is combined with Fusidic Acid.Approved
GabexateThe serum concentration of Nortriptyline can be increased when it is combined with Gabexate.Investigational
GeldanamycinThe serum concentration of Nortriptyline can be increased when it is combined with Geldanamycin.Experimental, Investigational
GemfibrozilThe metabolism of Nortriptyline can be decreased when combined with Gemfibrozil.Approved
GepefrineNortriptyline may increase the stimulatory activities of Gepefrine.Experimental
GM6001The serum concentration of Nortriptyline can be increased when it is combined with GM6001.Experimental
GuanabenzNortriptyline may decrease the antihypertensive activities of Guanabenz.Approved, Investigational
GuanfacineNortriptyline may decrease the antihypertensive activities of Guanfacine.Approved, Investigational
HaloperidolThe metabolism of Nortriptyline can be decreased when combined with Haloperidol.Approved
HarmalineHarmaline may increase the serotonergic activities of Nortriptyline.Experimental
HexobarbitalThe metabolism of Nortriptyline can be increased when combined with Hexobarbital.Approved
HydroxyamphetamineNortriptyline may increase the stimulatory activities of Hydroxyamphetamine.Approved
IdelalisibThe metabolism of Nortriptyline can be decreased when combined with Idelalisib.Approved
IdraparinuxThe serum concentration of Nortriptyline can be increased when it is combined with Idraparinux.Investigational
ImatinibThe metabolism of Nortriptyline can be decreased when combined with Imatinib.Approved
ImidaprilThe serum concentration of Nortriptyline can be increased when it is combined with Imidapril.Investigational
ImipramineThe metabolism of Nortriptyline can be decreased when combined with Imipramine.Approved
IndacaterolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Indacaterol.Approved
IndinavirThe metabolism of Nortriptyline can be decreased when combined with Indinavir.Approved
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Nortriptyline.Approved, Investigational
Iofetamine I-123Nortriptyline may increase the stimulatory activities of Iofetamine I-123.Approved
IproniazidIproniazid may increase the serotonergic activities of Nortriptyline.Withdrawn
IrbesartanThe metabolism of Nortriptyline can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Nortriptyline can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoetarineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Isoetarine.Approved
IsoflurophateThe serum concentration of Nortriptyline can be increased when it is combined with Isoflurophate.Approved, Investigational, Withdrawn
IsoniazidThe metabolism of Nortriptyline can be decreased when combined with Isoniazid.Approved
IsoprenalineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Isoprenaline.Approved
IsradipineThe metabolism of Nortriptyline can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Nortriptyline can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Nortriptyline can be increased when it is combined with Ivacaftor.Approved
IxazomibThe serum concentration of Nortriptyline can be increased when it is combined with Ixazomib.Approved
KetoconazoleThe metabolism of Nortriptyline can be decreased when combined with Ketoconazole.Approved, Investigational
L-TryptophanL-Tryptophan may increase the serotonergic activities of Nortriptyline.Approved, Nutraceutical, Withdrawn
LeflunomideThe metabolism of Nortriptyline can be decreased when combined with Leflunomide.Approved, Investigational
LepirudinThe serum concentration of Nortriptyline can be increased when it is combined with Lepirudin.Approved
LetaxabanThe serum concentration of Nortriptyline can be increased when it is combined with Letaxaban.Investigational
LevonordefrinNortriptyline may decrease the antihypertensive activities of Levonordefrin.Approved
LevosalbutamolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Levosalbutamol.Approved
LidocaineThe metabolism of Nortriptyline can be decreased when combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Nortriptyline can be increased when it is combined with Linagliptin.Approved
LinezolidLinezolid may increase the serotonergic activities of Nortriptyline.Approved, Investigational
LisdexamfetamineNortriptyline may increase the stimulatory activities of Lisdexamfetamine.Approved, Investigational
LisinoprilThe serum concentration of Nortriptyline can be increased when it is combined with Lisinopril.Approved, Investigational
LithiumLithium may increase the neurotoxic activities of Nortriptyline.Approved
LobeglitazoneThe metabolism of Nortriptyline can be decreased when combined with Lobeglitazone.Approved, Investigational
LofexidineNortriptyline may decrease the antihypertensive activities of Lofexidine.Approved, Investigational
LopinavirThe metabolism of Nortriptyline can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Nortriptyline can be decreased when combined with Lorcaserin.Approved
LorpiprazoleThe serum concentration of Nortriptyline can be increased when it is combined with Lorpiprazole.Approved
LosartanThe metabolism of Nortriptyline can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Nortriptyline can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Nortriptyline can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Nortriptyline can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Nortriptyline can be decreased when combined with Lumefantrine.Approved
ManidipineThe metabolism of Nortriptyline can be decreased when combined with Manidipine.Approved, Investigational
MelagatranThe serum concentration of Nortriptyline can be increased when it is combined with Melagatran.Experimental
MephedroneNortriptyline may increase the stimulatory activities of Mephedrone.Investigational
MephentermineNortriptyline may increase the vasopressor activities of Mephentermine.Approved
MetaraminolNortriptyline may increase the vasopressor activities of Metaraminol.Approved, Investigational
MethadoneThe metabolism of Nortriptyline can be decreased when combined with Methadone.Approved
MethamphetamineNortriptyline may decrease the antihypertensive activities of Methamphetamine.Approved, Illicit
MethohexitalThe metabolism of Nortriptyline can be increased when combined with Methohexital.Approved
MethotrimeprazineThe metabolism of Nortriptyline can be decreased when combined with Methotrimeprazine.Approved
MethoxamineNortriptyline may increase the vasopressor activities of Methoxamine.Approved, Investigational
MethoxyphenamineNortriptyline may increase the stimulatory activities of Methoxyphenamine.Experimental
Methylene blueNortriptyline 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 Nortriptyline.Approved, Investigational
MethylphenobarbitalThe metabolism of Nortriptyline can be increased when combined with Methylphenobarbital.Approved
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Nortriptyline.Approved, Investigational
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Nortriptyline.Approved, Investigational
MetyrosineThe risk or severity of adverse effects can be increased when Metyrosine is combined with Nortriptyline.Approved
MexiletineThe metabolism of Nortriptyline can be decreased when combined with Mexiletine.Approved
MidodrineNortriptyline may increase the vasopressor activities of Midodrine.Approved
MidomafetamineNortriptyline may increase the stimulatory activities of Midomafetamine.Experimental, Illicit, Investigational
MidostaurinThe metabolism of Nortriptyline can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Nortriptyline can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineMinaprine may increase the serotonergic activities of Nortriptyline.Approved
MirabegronThe metabolism of Nortriptyline can be decreased when combined with Mirabegron.Approved
MitotaneThe serum concentration of Nortriptyline can be decreased when it is combined with Mitotane.Approved
MMDANortriptyline may increase the stimulatory activities of MMDA.Experimental, Illicit
MoclobemideThe metabolism of Nortriptyline can be decreased when combined with Moclobemide.Approved
ModafinilThe metabolism of Nortriptyline can be decreased when combined with Modafinil.Approved, Investigational
MoexiprilThe serum concentration of Nortriptyline can be increased when it is combined with Moexipril.Approved
MoxonidineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Nortriptyline.Approved, Investigational
N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-ProlineThe serum concentration of Nortriptyline can be increased when it is combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline.Experimental
NafamostatThe serum concentration of Nortriptyline can be increased when it is combined with Nafamostat.Approved, Investigational
NaphazolineNortriptyline may decrease the antihypertensive activities of Naphazoline.Approved
NefazodoneThe metabolism of Nortriptyline can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Nortriptyline can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Nortriptyline can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Nortriptyline can be increased when combined with Nevirapine.Approved
NialamideNialamide may increase the serotonergic activities of Nortriptyline.Withdrawn
NicardipineThe metabolism of Nortriptyline can be decreased when combined with Nicardipine.Approved
NicorandilNortriptyline may increase the hypotensive activities of Nicorandil.Approved, Investigational
NilotinibThe metabolism of Nortriptyline can be decreased when combined with Nilotinib.Approved, Investigational
NitroaspirinThe serum concentration of Nortriptyline can be increased when it is combined with Nitroaspirin.Investigational
NorepinephrineNortriptyline may decrease the antihypertensive activities of Norepinephrine.Approved
OlaparibThe metabolism of Nortriptyline can be decreased when combined with Olaparib.Approved
OlodaterolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Olodaterol.Approved
OmapatrilatThe serum concentration of Nortriptyline can be increased when it is combined with Omapatrilat.Investigational
OmeprazoleThe metabolism of Nortriptyline can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OrciprenalineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Orciprenaline.Approved
OsimertinibThe serum concentration of Nortriptyline can be increased when it is combined with Osimertinib.Approved
OtamixabanThe serum concentration of Nortriptyline can be increased when it is combined with Otamixaban.Investigational
OxymetazolineNortriptyline may decrease the antihypertensive activities of Oxymetazoline.Approved
PalbociclibThe serum concentration of Nortriptyline can be increased when it is combined with Palbociclib.Approved
PaliperidoneNortriptyline may decrease the antihypertensive activities of Paliperidone.Approved
PanobinostatThe serum concentration of Nortriptyline can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Nortriptyline can be decreased when combined with Pantoprazole.Approved
PargylinePargyline may increase the serotonergic activities of Nortriptyline.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Nortriptyline.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Nortriptyline can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe metabolism of Nortriptyline can be increased when combined with Pentobarbital.Approved, Vet Approved
PergolideNortriptyline may decrease the antihypertensive activities of Pergolide.Approved, Investigational, Vet Approved, Withdrawn
PerindoprilThe serum concentration of Nortriptyline can be increased when it is combined with Perindopril.Approved
PhenindioneNortriptyline may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenobarbitalThe metabolism of Nortriptyline can be increased when combined with Phenobarbital.Approved
PhenprocoumonNortriptyline may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhentermineNortriptyline may increase the stimulatory activities of Phentermine.Approved, Illicit
PhenylephrineNortriptyline may increase the vasopressor activities of Phenylephrine.Approved
PhenylpropanolamineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Phenylpropanolamine.Approved, Vet Approved, Withdrawn
PhenytoinThe metabolism of Nortriptyline can be increased when combined with Phenytoin.Approved, Vet Approved
PhosphoramidonThe serum concentration of Nortriptyline can be increased when it is combined with Phosphoramidon.Experimental
PirbuterolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Pirbuterol.Approved
PirlindolePirlindole may increase the serotonergic activities of Nortriptyline.Approved
PosaconazoleThe metabolism of Nortriptyline can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Nortriptyline can be increased when combined with Primidone.Approved, Vet Approved
PrinomastatThe serum concentration of Nortriptyline can be increased when it is combined with Prinomastat.Investigational
ProcaterolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Procaterol.Approved, Investigational
PromazineThe metabolism of Nortriptyline can be decreased when combined with Promazine.Approved, Vet Approved
PseudoephedrineNortriptyline may decrease the antihypertensive activities of Pseudoephedrine.Approved
PyrimethamineThe metabolism of Nortriptyline can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuinaprilThe serum concentration of Nortriptyline can be increased when it is combined with Quinapril.Approved, Investigational
QuinidineNortriptyline may increase the QTc-prolonging activities of Quinidine.Approved
QuinineThe metabolism of Nortriptyline can be decreased when combined with Quinine.Approved
RacecadotrilThe serum concentration of Nortriptyline can be increased when it is combined with Racecadotril.Investigational
RamiprilThe serum concentration of Nortriptyline can be increased when it is combined with Ramipril.Approved
RanolazineThe metabolism of Nortriptyline can be decreased when combined with Ranolazine.Approved, Investigational
RemikirenThe serum concentration of Nortriptyline can be increased when it is combined with Remikiren.Approved
RifabutinThe metabolism of Nortriptyline can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Nortriptyline can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Nortriptyline can be increased when combined with Rifapentine.Approved
RisperidoneNortriptyline may decrease the antihypertensive activities of Risperidone.Approved, Investigational
RitobegronNortriptyline may increase the stimulatory activities of Ritobegron.Investigational
RitodrineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Ritodrine.Approved, Investigational
RitonavirThe metabolism of Nortriptyline can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Nortriptyline can be increased when it is combined with Rivaroxaban.Approved
RolapitantThe metabolism of Nortriptyline can be decreased when combined with Rolapitant.Approved
RopiniroleThe therapeutic efficacy of Ropinirole can be decreased when used in combination with Nortriptyline.Approved, Investigational
RucaparibThe metabolism of Nortriptyline can be decreased when combined with Rucaparib.Approved, Investigational
S-3304The serum concentration of Nortriptyline can be increased when it is combined with S-3304.Investigational
SalbutamolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Salbutamol.Approved, Vet Approved
SalmeterolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Salmeterol.Approved
SaquinavirThe metabolism of Nortriptyline can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Nortriptyline can be decreased when used in combination with Sarilumab.Approved
SaxagliptinThe serum concentration of Nortriptyline can be increased when it is combined with Saxagliptin.Approved
SecobarbitalThe metabolism of Nortriptyline can be increased when combined with Secobarbital.Approved, Vet Approved
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Nortriptyline.Approved
SildenafilThe metabolism of Nortriptyline can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Nortriptyline can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Nortriptyline can be increased when it is combined with Simeprevir.Approved
SitagliptinThe serum concentration of Nortriptyline can be increased when it is combined with Sitagliptin.Approved, Investigational
SivelestatThe serum concentration of Nortriptyline can be increased when it is combined with Sivelestat.Investigational
Sodium phosphateThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Sodium phosphate.Approved
SorafenibThe metabolism of Nortriptyline can be decreased when combined with Sorafenib.Approved, Investigational
SpiraprilThe serum concentration of Nortriptyline can be increased when it is combined with Spirapril.Approved
St. John's WortThe metabolism of Nortriptyline can be increased when combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Nortriptyline can be increased when it is combined with Stiripentol.Approved
SulfadiazineThe metabolism of Nortriptyline can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Nortriptyline can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Nortriptyline can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TelaprevirThe metabolism of Nortriptyline can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Nortriptyline can be decreased when combined with Telithromycin.Approved
TemocaprilThe serum concentration of Nortriptyline can be increased when it is combined with Temocapril.Experimental, Investigational
Tenofovir disoproxilThe metabolism of Nortriptyline can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerbinafineThe metabolism of Nortriptyline can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerbutalineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Terbutaline.Approved
TeriflunomideThe serum concentration of Nortriptyline can be decreased when it is combined with Teriflunomide.Approved
ThalidomideNortriptyline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
TheophyllineThe metabolism of Nortriptyline can be decreased when combined with Theophylline.Approved
ThiamylalThe metabolism of Nortriptyline can be increased when combined with Thiamylal.Approved, Vet Approved
ThiopentalThe metabolism of Nortriptyline can be increased when combined with Thiopental.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Nortriptyline.Approved, Withdrawn
ThiorphanThe serum concentration of Nortriptyline can be increased when it is combined with Thiorphan.Experimental
TicagrelorThe metabolism of Nortriptyline can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Nortriptyline can be decreased when combined with Ticlopidine.Approved
TioclomarolNortriptyline may increase the anticoagulant activities of Tioclomarol.Experimental
TipranavirThe metabolism of Nortriptyline can be decreased when combined with Tipranavir.Approved, Investigational
TizanidineNortriptyline may decrease the antihypertensive activities of Tizanidine.Approved
TocilizumabThe serum concentration of Nortriptyline can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Nortriptyline can be decreased when combined with Tolbutamide.Approved
ToloxatoneToloxatone may increase the serotonergic activities of Nortriptyline.Approved
TopiramateThe metabolism of Nortriptyline can be decreased when combined with Topiramate.Approved
TopiroxostatThe metabolism of Nortriptyline can be decreased when combined with Topiroxostat.Approved, Investigational
TramadolNortriptyline may increase the neuroexcitatory activities of Tramadol.Approved, Investigational
TrandolaprilThe serum concentration of Nortriptyline can be increased when it is combined with Trandolapril.Approved
TranylcypromineThe metabolism of Nortriptyline can be decreased when combined with Tranylcypromine.Approved
TrimethoprimThe metabolism of Nortriptyline can be decreased when combined with Trimethoprim.Approved, Vet Approved
UbenimexThe serum concentration of Nortriptyline can be increased when it is combined with Ubenimex.Experimental, Investigational
UlinastatinThe serum concentration of Nortriptyline can be increased when it is combined with Ulinastatin.Investigational
Valproic AcidThe serum concentration of Nortriptyline can be increased when it is combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Nortriptyline can be decreased when combined with Valsartan.Approved, Investigational
VemurafenibThe serum concentration of Nortriptyline can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Nortriptyline can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Nortriptyline can be decreased when combined with Verapamil.Approved
VilanterolThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Vilanterol.Approved
VildagliptinThe serum concentration of Nortriptyline can be increased when it is combined with Vildagliptin.Approved, Investigational
VoriconazoleThe metabolism of Nortriptyline can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinNortriptyline may increase the anticoagulant activities of Warfarin.Approved
XimelagatranThe serum concentration of Nortriptyline can be increased when it is combined with Ximelagatran.Approved, Investigational, Withdrawn
XylometazolineNortriptyline may decrease the antihypertensive activities of Xylometazoline.Approved
YohimbineThe serum concentration of Yohimbine can be increased when it is combined with Nortriptyline.Approved, Vet Approved
Z-Val-Ala-Asp fluoromethyl ketoneThe serum concentration of Nortriptyline can be increased when it is combined with Z-Val-Ala-Asp fluoromethyl ketone.Experimental
ZafirlukastThe metabolism of Nortriptyline can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe metabolism of Nortriptyline can be decreased when combined with Ziprasidone.Approved
ZofenoprilThe serum concentration of Nortriptyline can be increased when it is combined with Zofenopril.Experimental
ZucapsaicinThe metabolism of Nortriptyline can be decreased when combined with Zucapsaicin.Approved
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (caffeine).
  • Take with food to reduce irritation.

References

Synthesis Reference

Abraham Nudelman, "ACID ADDITION SALT OF A NORTRIPTYLINE-GABA CONJUGATE AND A PROCESS OF PREPARING SAME." U.S. Patent US20130184347, issued July 18, 2013.

US20130184347
General References
  1. Prochazka AV, Weaver MJ, Keller RT, Fryer GE, Licari PA, Lofaso D: A randomized trial of nortriptyline for smoking cessation. Arch Intern Med. 1998 Oct 12;158(18):2035-9. [PubMed:9778204]
External Links
Human Metabolome Database
HMDB0014680
KEGG Compound
C07274
PubChem Compound
4543
PubChem Substance
46507783
ChemSpider
4384
BindingDB
112777
ChEBI
7640
ChEMBL
CHEMBL445
Therapeutic Targets Database
DAP001152
PharmGKB
PA450657
IUPHAR
2404
Guide to Pharmacology
GtP Drug Page
HET
21B
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Nortriptyline
ATC Codes
N06AA10 — Nortriptyline
AHFS Codes
  • 28:16.04.28 — Tricyclics and Other Norepinephrine-reuptake Inhibitors
PDB Entries
4m48
FDA label
Download (420 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentCarcinoma, Small Cell1
1CompletedTreatmentAtopic Dermatitis (AD)1
1CompletedTreatmentHealthy Volunteers1
2Active Not RecruitingTreatmentMajor Depressive Disorder (MDD)1
2CompletedTreatmentDepression / Parkinson's Disease (PD)1
2CompletedTreatmentIrritable Bowel Syndrome (IBS)1
2CompletedTreatmentPlaque Psoriasis2
2CompletedTreatmentRadicular syndrome / Sciatica1
2CompletedTreatmentSmoking1
2CompletedTreatmentTemporomandibular Joint Disorders1
2, 3CompletedTreatmentGastroesophageal Reflux Disease1
3CompletedTreatmentGastroesophageal Reflux Disease1
3CompletedTreatmentHerpes Zoster / Pain1
3CompletedTreatmentIdiopathic Gastroparesis1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
4CompletedTreatmentBipolar Disorder (BD)1
4CompletedTreatmentBipolar Disorder (BD) / Depression / Depressive Disorders1
4CompletedTreatmentCryptogenic Sensory Polyneuropathy1
4CompletedTreatmentDepression2
4CompletedTreatmentDepression / Melancholic Depression1
4Not Yet RecruitingTreatmentMajor Depressive Disorder (MDD) / Treatment Resistant Depression (TRD)1
4TerminatedTreatmentMajor Depressive Disorder (MDD)1
4Unknown StatusNot AvailableMajor Depressive Disorder (MDD)1
Not AvailableActive Not RecruitingTreatmentDepression2
Not AvailableCompletedTreatmentDepression1
Not AvailableCompletedTreatmentSpinal Stenosis of Lumbar Region1
Not AvailableRecruitingTreatmentAdverse Reaction to Drug / Depression1
Not AvailableRecruitingTreatmentAntidepressant Drug Adverse Reaction / Depression1
Not AvailableRecruitingTreatmentDepression / Depressive Symptoms1
Not AvailableRecruitingTreatmentMigraine Disorders / Vestibular Migraine1
Not AvailableTerminatedTreatmentNon Ulcer Dyspepsia1
Not AvailableUnknown StatusTreatmentTreatment Resistant Depression (TRD)1

Pharmacoeconomics

Manufacturers
  • Eli lilly and co
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Taro pharmaceuticals inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Tyco healthcare group lp
  • Ranbaxy pharmaceuticals inc
  • Pharmaceutical assoc inc
  • Taro pharmaceutical industries ltd
Packagers
Dosage forms
FormRouteStrength
CapsuleOral10 mg
CapsuleOral25 mg
CapsuleOral10 mg/1
CapsuleOral25 mg/1
CapsuleOral50 mg/1
CapsuleOral75 mg/1
SolutionOral10 mg/5mL
Prices
Unit descriptionCostUnit
Pamelor 30 10 mg capsule Bottle750.05USD bottle
Pamelor 30 25 mg capsule Bottle750.05USD bottle
Pamelor 30 50 mg capsule Bottle750.05USD bottle
Pamelor 10 mg/5ml Solution 480ml Bottle325.97USD bottle
Pamelor 10 mg capsule24.04USD capsule
Pamelor 25 mg capsule24.04USD capsule
Pamelor 50 mg capsule24.04USD capsule
Pamelor 75 mg capsule19.34USD capsule
Nortriptyline hcl powder11.09USD g
Nortriptyline hcl 75 mg capsule1.33USD capsule
Nortriptyline hcl 50 mg capsule0.94USD capsule
Nortriptyline hcl 25 mg capsule0.6USD capsule
Aventyl 25 mg Capsule0.48USD capsule
Nortriptyline HCl 10 mg/5ml Solution0.4USD ml
Nortriptyline hcl 10 mg capsule0.28USD capsule
Apo-Nortriptyline 25 mg Capsule0.27USD capsule
Novo-Nortriptyline 25 mg Capsule0.27USD capsule
Nu-Nortriptyline 25 mg Capsule0.27USD capsule
Pms-Nortriptyline 25 mg Capsule0.27USD capsule
Aventyl 10 mg Capsule0.24USD capsule
Apo-Nortriptyline 10 mg Capsule0.13USD capsule
Novo-Nortriptyline 10 mg Capsule0.13USD capsule
Nu-Nortriptyline 10 mg Capsule0.13USD capsule
Pms-Nortriptyline 10 mg Capsule0.13USD capsule
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)213-215 °CNot Available
logP4.51BRODIN,A (1974)
pKa10.1SANGSTER (2004)
Predicted Properties
PropertyValueSource
Water Solubility0.000874 mg/mLALOGPS
logP4.65ALOGPS
logP4.43ChemAxon
logS-5.5ALOGPS
pKa (Strongest Basic)10.47ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area12.03 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity96.21 m3·mol-1ChemAxon
Polarizability31.87 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9478
Caco-2 permeable+0.774
P-glycoprotein substrateSubstrate0.7863
P-glycoprotein inhibitor IInhibitor0.8876
P-glycoprotein inhibitor IIInhibitor0.5376
Renal organic cation transporterInhibitor0.6903
CYP450 2C9 substrateNon-substrate0.7508
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateSubstrate0.5593
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.7665
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5194
Ames testNon AMES toxic0.5315
CarcinogenicityNon-carcinogens0.9182
BiodegradationReady biodegradable0.5
Rat acute toxicity2.7513 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5809
hERG inhibition (predictor II)Inhibitor0.7763
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (7.76 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - EI-BGC-MSsplash10-0006-9000000000-bb9eae4818c0402317ee
Mass Spectrum (Electron Ionization)MSsplash10-0006-9230000000-15f73e5232a0e230f41b
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/MSsplash10-05nf-5970000000-f92c7d23474b57a4ba50
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03di-0090000000-4c40cb3ec4df8809981e
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-06sl-2590000000-be2abd28b2b0f75dd8bb
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-05mo-3940000000-6a454924ec75665c6175
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-05mo-3930000000-eb8141866b19782dd1e5
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00kf-4930000000-81614e655fc32d5839ce
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00kf-4930000000-f918306a99d07f887503
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0gdl-5930000000-d876ab376d0e9885d06d
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0gb9-5930000000-e51a246750bf8ce7e4ec
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0gbi-5930000000-c2811578219a3a7e1ccf
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03yi-0490000000-094e7bdb831aed030f5f

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
Dialkylamines / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Dibenzocycloheptene / Secondary amine / Secondary aliphatic amine / Organic nitrogen compound / Organopnictogen compound / Hydrocarbon derivative / Organonitrogen compound / Amine / Aromatic homopolycyclic compound
Molecular Framework
Aromatic homopolycyclic compounds
External Descriptors
organic tricyclic compound (CHEBI:7640)

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. Roubert C, Cox PJ, Bruss M, Hamon M, Bonisch H, Giros B: Determination of residues in the norepinephrine transporter that are critical for tricyclic antidepressant affinity. J Biol Chem. 2001 Mar 16;276(11):8254-60. Epub 2000 Nov 22. [PubMed:11092898]
  2. Roubert C, Sagne C, Kapsimali M, Vernier P, Bourrat F, Giros B: A Na(+)/Cl(-)-dependent transporter for catecholamines, identified as a norepinephrine transporter, is expressed in the brain of the teleost fish medaka (Oryzias latipes). Mol Pharmacol. 2001 Sep;60(3):462-73. [PubMed:11502876]
  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. Kim H, Lim SW, Kim S, Kim JW, Chang YH, Carroll BJ, Kim DK: Monoamine transporter gene polymorphisms and antidepressant response in koreans with late-life depression. JAMA. 2006 Oct 4;296(13):1609-18. [PubMed:17018806]
  5. Barker EL, Blakely RD: Identification of a single amino acid, phenylalanine 586, that is responsible for high affinity interactions of tricyclic antidepressants with the human serotonin transporter. Mol Pharmacol. 1996 Oct;50(4):957-65. [PubMed:8863842]
  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]
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. Joyce PR, Mulder RT, Luty SE, McKenzie JM, Miller AL, Rogers GR, Kennedy MA: Age-dependent antidepressant pharmacogenomics: polymorphisms of the serotonin transporter and G protein beta3 subunit as predictors of response to fluoxetine and nortriptyline. Int J Neuropsychopharmacol. 2003 Dec;6(4):339-46. [PubMed:14604448]
  2. Wisner KL, Hanusa BH, Perel JM, Peindl KS, Piontek CM, Sit DK, Findling RL, Moses-Kolko EL: Postpartum depression: a randomized trial of sertraline versus nortriptyline. J Clin Psychopharmacol. 2006 Aug;26(4):353-60. [PubMed:16855451]
  3. Pollock BG, Ferrell RE, Mulsant BH, Mazumdar S, Miller M, Sweet RA, Davis S, Kirshner MA, Houck PR, Stack JA, Reynolds CF, Kupfer DJ: Allelic variation in the serotonin transporter promoter affects onset of paroxetine treatment response in late-life depression. Neuropsychopharmacology. 2000 Nov;23(5):587-90. [PubMed:11027924]
  4. 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]
  5. Rausch JL, Moeller FG, Johnson ME: Initial platelet serotonin (5-HT) transport kinetics predict nortriptyline treatment outcome. J Clin Psychopharmacol. 2003 Apr;23(2):138-44. [PubMed:12640215]
  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]
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
Antagonist
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]
Details
5. 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]
  2. Sadava D, Wilmington K: Tricyclic antidepressant drugs affect histamine receptors in human leukocytes. Life Sci. 1984 Dec 17;35(25):2545-8. [PubMed:6096660]
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
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
Unknown
Actions
Antagonist
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. Palvimaki EP, Roth BL, Majasuo H, Laakso A, Kuoppamaki M, Syvalahti E, Hietala J: Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor. Psychopharmacology (Berl). 1996 Aug;126(3):234-40. [PubMed:8876023]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
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. Monsma FJ Jr, Shen Y, Ward RP, Hamblin MW, Sibley DR: Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol Pharmacol. 1993 Mar;43(3):320-7. [PubMed:7680751]
  2. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8]
  3. PDSP Ki Database [Link]
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 group
Organism
Human
Pharmacological action
Unknown
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...

Components:
References
  1. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8]
  2. PDSP Ki Database [Link]
Kind
Protein group
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
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. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Peroutka SJ, Snyder SH: Antiemetics: neurotransmitter receptor binding predicts therapeutic actions. Lancet. 1982 Mar 20;1(8273):658-9. [PubMed:6121969]
  2. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8]
  3. PDSP Ki Database [Link]
Kind
Protein group
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Steroid binding
Specific Function
Receptor for progesterone.

Components:
References
  1. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Rat
Pharmacological action
Unknown
Actions
Antagonist
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
P08909
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51916.005 Da
References
  1. Jenck F, Moreau JL, Mutel V, Martin JR, Haefely WE: Evidence for a role of 5-HT1C receptors in the antiserotonergic properties of some antidepressant drugs. Eur J Pharmacol. 1993 Feb 9;231(2):223-9. [PubMed:8453978]

Enzymes

Details
1. Cytochrome P450 2D6
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. 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: Nortriptyline E-10-hydroxylation in vitro is mediated by human CYP2D6 (high affinity) and CYP3A4 (low affinity): implications for interactions with enzyme-inducing drugs. J Clin Pharmacol. 1999 Jun;39(6):567-77. [PubMed:10354960]
  5. Olesen OV, Linnet K: Hydroxylation and demethylation of the tricyclic antidepressant nortriptyline by cDNA-expressed human cytochrome P-450 isozymes. Drug Metab Dispos. 1997 Jun;25(6):740-4. [PubMed:9193876]
  6. 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. 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: Nortriptyline E-10-hydroxylation in vitro is mediated by human CYP2D6 (high affinity) and CYP3A4 (low affinity): implications for interactions with enzyme-inducing drugs. J Clin Pharmacol. 1999 Jun;39(6):567-77. [PubMed:10354960]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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. Olesen OV, Linnet K: Hydroxylation and demethylation of the tricyclic antidepressant nortriptyline by cDNA-expressed human cytochrome P-450 isozymes. Drug Metab Dispos. 1997 Jun;25(6):740-4. [PubMed:9193876]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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. 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]
  2. 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]
  3. Olesen OV, Linnet K: Hydroxylation and demethylation of the tricyclic antidepressant nortriptyline by cDNA-expressed human cytochrome P-450 isozymes. Drug Metab Dispos. 1997 Jun;25(6):740-4. [PubMed:9193876]
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. 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]
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
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gas...
Gene Name
PTGS1
Uniprot ID
P23219
Uniprot Name
Prostaglandin G/H synthase 1
Molecular Weight
68685.82 Da
References
  1. 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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
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]
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]

Drug created on June 13, 2005 07:24 / Updated on January 23, 2018 12:10