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Identification
NameProtriptyline
Accession NumberDB00344  (APRD00441)
TypeSmall Molecule
GroupsApproved
Description

Protriptyline hydrochloride 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, protriptyline does not affect mood or arousal, but may cause sedation. In depressed individuals, protriptyline exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. In addition, TCAs 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. Protriptyline may be used for the treatment of depression.

Structure
Thumb
Synonyms
3-(5H-dibenzo[a,d][7]annulen-5-yl)-N-methylpropan-1-amine
3-(5H-Dibenzo[a,D]cyclohepten-5-yl)-N-methyl-1-propanamine
5-(3-Methylaminopropyl)-5H-dibenzo[a,D]cycloheptene
7-(3-Methylaminopropyl)-1,2:5,6-dibenzocycloheptatriene
Amimetilina
N-Methyl-5H-dibenzo[a,D]cycloheptene-5-propanamine
N-Methyl-5H-dibenzo[a,D]cycloheptene-5-propylamine
Protriptilina
Protriptylin
Protriptyline
Protriptylinum
External Identifiers
  • MK 240
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Triptil Tab 10mgtablet10 mgoralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1966-12-312001-01-25Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Protriptyline Hydrochloridetablet5 mg/1oralRoxane Laboratories, Inc2008-09-16Not applicableUs
Protriptyline Hydrochloridetablet, film coated10 mg/1oralRising Pharmaceuticals, Inc2010-06-11Not applicableUs
Protriptyline Hydrochloridetablet, film coated5 mg/1oralRising Pharmaceuticals, Inc2010-06-11Not applicableUs
Protriptyline Hydrochloridetablet, film coated10 mg/1oralHi Tech Pharmacal Co., Inc.2013-10-28Not applicableUs
Protriptyline Hydrochloridetablet, film coated5 mg/1oralHi Tech Pharmacal Co., Inc.2013-10-28Not applicableUs
Protriptyline Hydrochloridetablet, film coated10 mg/1oralEpic Pharma, LLC2013-01-09Not applicableUs
Protriptyline Hydrochloridetablet, film coated5 mg/1oralEpic Pharma, LLC2013-01-09Not applicableUs
Protriptyline Hydrochloridetablet10 mg/1oralRoxane Laboratories, Inc2008-09-16Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
TriptilNot Available
VivactilOdyssey
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Protriptyline hydrochloride
ThumbNot applicableDBSALT001192
Categories
UNII4NDU154T12
CAS number438-60-8
WeightAverage: 263.3767
Monoisotopic: 263.167399677
Chemical FormulaC19H21N
InChI KeyInChIKey=BWPIARFWQZKAIA-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/h2-5,7-10,12-13,19-20H,6,11,14H2,1H3
IUPAC Name
methyl(3-{tricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,9,11,13-heptaen-2-yl}propyl)amine
SMILES
CNCCCC1C2=CC=CC=C2C=CC2=CC=CC=C12
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dibenzocycloheptenes. These are compounds containing a dibenzocycloheptene moiety, which consists of two benzene connected by a cycloheptene ring.
KingdomOrganic compounds
Super ClassBenzenoids
ClassDibenzocycloheptenes
Sub ClassNot Available
Direct ParentDibenzocycloheptenes
Alternative Parents
Substituents
  • Dibenzocycloheptene
  • Aralkylamine
  • Secondary amine
  • Secondary aliphatic amine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic homopolycyclic compound
Molecular FrameworkAromatic homopolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of depression.
PharmacodynamicsProtriptyline is a tricyclic antidepressant. It was thought that tricyclic antidepressants work by inhibiting the reuptake of the neurotransmitters norepinephrine and serotonin by nerve cells. However, this response occurs immediately, yet mood does not lift for approximately two weeks. It is now thought that changes occur in receptor sensitivity in the cerebral cortex and hippocampus. The hippocampus is part of the limbic system, a part of the brain involved in emotions. Presynaptic receptors are affected: α1 and β1 receptors are sensitized, α2 receptors are desensitised (leading to increased noradrenaline production). Tricyclics are also known as effective analgesics for different types of pain, especially neuropathic or neuralgic pain. A precise mechanism for their analgesic action is unknown, but it is thought that they modulate anti-pain opioid systems in the CNS via an indirect serotonergic route. They are also effective in migraine prophylaxis, but not in abortion of acute migraine attack. The mechanism of their anti-migraine action is also thought to be serotonergic.
Mechanism of actionProtriptyline acts by decreasing the reuptake of norepinephrine and serotonin (5-HT).
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationCumulative urinary excretion during 16 days accounted for approximately 50% of the drug. The fecal route of excretion did not seem to be important.
Half lifeNot Available
ClearanceNot Available
ToxicitySide effects include anxiety, blood disorders, confusion, decreased libido, dizziness, flushing, headache, impotence, insomnia, low blood pressure, nightmares, rapid or irregular heartbeat, rash, seizures, sensitivity to sunlight, stomach and intestinal discomfort, 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9862
Caco-2 permeable+0.7821
P-glycoprotein substrateSubstrate0.7406
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IIInhibitor0.5597
Renal organic cation transporterInhibitor0.6622
CYP450 2C9 substrateNon-substrate0.7206
CYP450 2D6 substrateSubstrate0.9034
CYP450 3A4 substrateSubstrate0.5285
CYP450 1A2 substrateNon-inhibitor0.7595
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8933
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorInhibitor0.641
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7512
Ames testNon AMES toxic0.6
CarcinogenicityNon-carcinogens0.9322
BiodegradationNot ready biodegradable0.7732
Rat acute toxicity3.0087 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.736
hERG inhibition (predictor II)Inhibitor0.8132
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Sanofi aventis us llc
  • Pfizer laboratories div pfizer inc
  • Roxane laboratories inc
  • Sigmapharm laboratories llc
  • Odyssey pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral10 mg/1
Tabletoral5 mg/1
Tablet, film coatedoral10 mg/1
Tablet, film coatedoral5 mg/1
Tabletoral10 mg
Prices
Unit descriptionCostUnit
Tofranil-PM 30 125 mg capsule Bottle588.33USD bottle
Tofranil-PM 30 150 mg capsule Bottle588.33USD bottle
Tofranil-PM 30 75 mg capsule Bottle588.33USD bottle
Tofranil 30 50 mg tablet Bottle185.09USD bottle
Tofranil-pm 100 mg capsule19.23USD capsule
Tofranil-pm 150 mg capsule18.86USD capsule
Tofranil-pm 75 mg capsule18.86USD capsule
Tofranil-pm 125 mg capsule18.68USD capsule
Anafranil 25 mg capsule13.51USD capsule
Anafranil 50 mg capsule13.51USD capsule
Anafranil 75 mg capsule13.24USD capsule
Tofranil 50 mg tablet6.64USD tablet
Norpramin 150 mg tablet6.23USD tablet
Surmontil 100 mg capsule5.92USD capsule
Tofranil 25 mg tablet4.97USD tablet
Tofranil 10 mg tablet4.73USD tablet
Norpramin 100 mg tablet4.27USD tablet
Surmontil 50 mg capsule4.15USD capsule
Vivactil 10 mg tablet4.05USD tablet
Norpramin 75 mg tablet3.27USD tablet
Protriptyline hcl 10 mg tablet3.07USD tablet
Vivactil 5 mg tablet2.86USD tablet
Norpramin 50 mg tablet2.59USD tablet
Surmontil 25 mg capsule2.49USD capsule
Protriptyline hcl 5 mg tablet2.12USD tablet
Norpramin 25 mg tablet1.4USD tablet
Norpramin 10 mg tablet1.16USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point169-171 °C (Protriptyline HCl)Not Available
water solubility1.04 mg/LNot Available
logP4.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000231 mg/mLALOGPS
logP4.65ALOGPS
logP4.5ChemAxon
logS-6.1ALOGPS
pKa (Strongest Basic)10.54ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area12.03 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity87.3 m3·mol-1ChemAxon
Polarizability31.6 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-006x-8910000000-ec599ee02d998905757eView in MoNA
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesN06AA11
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Protriptyline can be increased when it is combined with Abiraterone.
AcepromazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Acetophenazine.
AclidiniumAclidinium may increase the anticholinergic activities of Protriptyline.
AltretamineAltretamine may increase the orthostatic hypotensive activities of Protriptyline.
AmisulprideThe risk or severity of adverse effects can be increased when Protriptyline is combined with Amisulpride.
AmphetamineProtriptyline may increase the stimulatory activities of Amphetamine.
AripiprazoleThe risk or severity of adverse effects can be increased when Protriptyline is combined with Aripiprazole.
AzelastineProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Protriptyline.
BatimastatThe serum concentration of Protriptyline can be increased when it is combined with Batimastat.
BenzquinamideThe risk or severity of adverse effects can be increased when Protriptyline is combined with Benzquinamide.
Botulinum Toxin Type AProtriptyline may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BProtriptyline may increase the anticholinergic activities of Botulinum Toxin Type B.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
BuprenorphineProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ButabarbitalThe metabolism of Protriptyline can be increased when combined with Butabarbital.
ButethalThe metabolism of Protriptyline can be increased when combined with Butethal.
CarbamazepineThe metabolism of Protriptyline can be increased when combined with Carbamazepine.
CarphenazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Carphenazine.
CathinoneProtriptyline may increase the stimulatory activities of Cathinone.
ChlormezanoneThe risk or severity of adverse effects can be increased when Protriptyline is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Chlorpromazine.
ChlorpropamideProtriptyline may increase the hypoglycemic activities of Chlorpropamide.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Protriptyline is combined with Chlorprothixene.
CimetidineThe metabolism of Protriptyline can be decreased when combined with Cimetidine.
Cimetropium BromideProtriptyline may increase the anticholinergic activities of Cimetropium Bromide.
CinacalcetThe serum concentration of Protriptyline can be increased when it is combined with Cinacalcet.
CisaprideProtriptyline may increase the arrhythmogenic activities of Cisapride.
CitalopramThe risk or severity of adverse effects can be increased when Protriptyline is combined with Citalopram.
ClozapineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Clozapine.
CobicistatThe serum concentration of Protriptyline can be increased when it is combined with Cobicistat.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Protriptyline.
DarunavirThe serum concentration of Protriptyline can be increased when it is combined with Darunavir.
DesmopressinThe risk or severity of adverse effects can be increased when Protriptyline is combined with Desmopressin.
DexmethylphenidateThe risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with Protriptyline.
DicoumarolProtriptyline may increase the anticoagulant activities of Dicoumarol.
DipivefrinThe therapeutic efficacy of Dipivefrin can be decreased when used in combination with Protriptyline.
DofetilideProtriptyline may increase the QTc-prolonging activities of Dofetilide.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
DuloxetineDuloxetine may increase the serotonergic activities of Protriptyline.
EluxadolineProtriptyline may increase the activities of Eluxadoline.
EscitalopramThe risk or severity of adverse effects can be increased when Protriptyline is combined with Escitalopram.
EthanolProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FencamfamineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Fencamfamine.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Protriptyline.
FlupentixolThe risk or severity of adverse effects can be increased when Protriptyline is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Protriptyline is combined with Fluspirilene.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Protriptyline.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Protriptyline is combined with Glucagon recombinant.
GoserelinProtriptyline may increase the QTc-prolonging activities of Goserelin.
GranisetronGranisetron may increase the serotonergic activities of Protriptyline.
HaloperidolThe risk or severity of adverse effects can be increased when Protriptyline is combined with Haloperidol.
HeptabarbitalThe metabolism of Protriptyline can be increased when combined with Heptabarbital.
HexobarbitalThe metabolism of Protriptyline can be increased when combined with Hexobarbital.
HydrocodoneProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Protriptyline.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Protriptyline.
IsoflurophateThe serum concentration of Protriptyline can be increased when it is combined with Isoflurophate.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Protriptyline.
LeuprolideProtriptyline may increase the QTc-prolonging activities of Leuprolide.
LinezolidLinezolid may increase the serotonergic activities of Protriptyline.
LiothyronineLiothyronine may increase the arrhythmogenic activities of Protriptyline.
LithiumLithium may increase the neurotoxic activities of Protriptyline.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Protriptyline.
LoxapineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Loxapine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
MesoridazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Mesoridazine.
MethohexitalThe metabolism of Protriptyline can be increased when combined with Methohexital.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Methotrimeprazine.
Methylene blueProtriptyline may increase the serotonergic activities of Methylene blue.
MethylphenidateThe risk or severity of adverse effects can be increased when Methylphenidate is combined with Protriptyline.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Protriptyline.
MetyrosineProtriptyline may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the anticholinergic activities of Protriptyline.
MidodrineProtriptyline may increase the activities of Midodrine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Protriptyline.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
MirabegronThe risk or severity of adverse effects can be increased when Protriptyline is combined with Mirabegron.
MolindoneThe risk or severity of adverse effects can be increased when Protriptyline is combined with Molindone.
MorphineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Morphine.
MoxonidineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Protriptyline.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
NicorandilProtriptyline may increase the hypotensive activities of Nicorandil.
OlanzapineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Protriptyline is combined with Ondansetron.
OrciprenalineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Orciprenaline.
OrphenadrineProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PaliperidoneThe risk or severity of adverse effects can be increased when Protriptyline is combined with Paliperidone.
PanobinostatThe serum concentration of Protriptyline can be increased when it is combined with Panobinostat.
ParaldehydeProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Protriptyline.
Peginterferon alfa-2bThe serum concentration of Protriptyline can be decreased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe metabolism of Protriptyline can be increased when combined with Pentobarbital.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
PerphenazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Perphenazine.
PhenelzinePhenelzine may increase the serotonergic activities of Protriptyline.
PimozideThe risk or severity of adverse effects can be increased when Protriptyline is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Piperacetazine.
Potassium ChlorideProtriptyline may increase the ulcerogenic activities of Potassium Chloride.
PramipexoleProtriptyline may increase the sedative activities of Pramipexole.
PramlintidePramlintide may increase the anticholinergic activities of Protriptyline.
PrimidoneThe metabolism of Protriptyline can be increased when combined with Primidone.
ProchlorperazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Prochlorperazine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Protriptyline.
PromazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Promazine.
QuetiapineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Quetiapine.
QuinidineProtriptyline may increase the QTc-prolonging activities of Quinidine.
RamosetronProtriptyline may increase the activities of Ramosetron.
RemoxiprideThe risk or severity of adverse effects can be increased when Protriptyline is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Protriptyline is combined with Risperidone.
RitonavirThe metabolism of Protriptyline can be decreased when combined with Ritonavir.
RopiniroleProtriptyline may increase the sedative activities of Ropinirole.
RotigotineProtriptyline may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Protriptyline.
SecobarbitalThe metabolism of Protriptyline can be increased when combined with Secobarbital.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Protriptyline.
SertindoleThe risk or severity of adverse effects can be increased when Protriptyline is combined with Sertindole.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Protriptyline.
SimeprevirThe serum concentration of Protriptyline can be increased when it is combined with Simeprevir.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
St. John's WortThe metabolism of Protriptyline can be increased when combined with St. John's Wort.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Protriptyline.
SuvorexantProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Protriptyline can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Protriptyline.
TerbinafineThe metabolism of Protriptyline can be decreased when combined with Terbinafine.
ThalidomideProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Protriptyline is combined with Thiothixene.
TiclopidineThe metabolism of Protriptyline can be decreased when combined with Ticlopidine.
TiotropiumProtriptyline may increase the anticholinergic activities of Tiotropium.
TopiramateThe risk or severity of adverse effects can be increased when Protriptyline is combined with Topiramate.
TramadolProtriptyline may increase the neuroexcitatory activities of Tramadol.
TranylcypromineTranylcypromine may increase the serotonergic activities of Protriptyline.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Protriptyline.
TrifluoperazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Triflupromazine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Protriptyline.
Valproic AcidThe serum concentration of Protriptyline can be increased when it is combined with Valproic Acid.
YohimbineThe serum concentration of Yohimbine can be increased when it is combined with Protriptyline.
ZiprasidoneThe risk or severity of adverse effects can be increased when Protriptyline is combined with Ziprasidone.
ZolpidemProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Protriptyline is combined with Zuclopenthixol.
Food InteractionsNot Available

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
Molecular Weight:
69331.42 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. 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 ]
  4. Cheetham SC, Viggers JA, Butler SA, Prow MR, Heal DJ: [3H]nisoxetine--a radioligand for noradrenaline reuptake sites: correlation with inhibition of [3H]noradrenaline uptake and effect of DSP-4 lesioning and antidepressant treatments. Neuropharmacology. 1996 Jan;35(1):63-70. [PubMed:8684598 ]
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 the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin an...
Gene Name:
SLC6A4
Uniprot ID:
P31645
Molecular Weight:
70324.165 Da
References
  1. McDougle CJ, Epperson CN, Price LH, Gelernter J: Evidence for linkage disequilibrium between serotonin transporter protein gene (SLC6A4) and obsessive compulsive disorder. Mol Psychiatry. 1998 May;3(3):270-3. [PubMed:9672904 ]
  2. Rouillon F, Blachier C, Dreyfus JP, Bouhassira M, Allicar MP: [Pharmaco-epidemiologic study of the use of antidepressant drugs in the general population]. Encephale. 1996 May;22 Spec No 1:39-48. [PubMed:8767026 ]
  3. Frazer A, Daws LC: Serotonin transporter function in vivo: assessment by chronoamperometry. Ann N Y Acad Sci. 1998 Dec 15;861:217-29. [PubMed:9928259 ]
  4. Daws LC, Toney GM, Gerhardt GA, Frazer A: In vivo chronoamperometric measures of extracellular serotonin clearance in rat dorsal hippocampus: contribution of serotonin and norepinephrine transporters. J Pharmacol Exp Ther. 1998 Aug;286(2):967-76. [PubMed:9694957 ]
  5. 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 ]
  6. Kovachich GB, Aronson CE, Brunswick DJ: Effect of repeated administration of antidepressants on serotonin uptake sites in limbic and neocortical structures of rat brain determined by quantitative autoradiography. Neuropsychopharmacology. 1992 Dec;7(4):317-24. [PubMed:1476595 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 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 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Ibrahim S, Peggins J, Knapton A, Licht T, Aszalos A: Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation. J Pharmacol Exp Ther. 2000 Dec;295(3):1276-83. [PubMed:11082465 ]
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:09