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Identification
NameAmitriptyline
Accession NumberDB00321  (APRD00227)
TypeSmall Molecule
GroupsApproved
Description

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

Structure
Thumb
Synonyms
10,11-dihydro-5-(gamma-Dimethylaminopropylidene)-5H-dibenzo(a,D)cycloheptene
10,11-dihydro-N,N-Dimethyl-5H-dibenzo(a,D)heptalene-delta(5),gamma-propylamine
3-(10,11-dihydro-5H-Dibenzo(a,D)cyclohepten-5-ylidene)-N,N-dimethyl-1-propanamine
3-(10,11-dihydro-5H-Dibenzo[a,D]cyclohepten-5-ylidene)-N,N-dimethylpropan-1-amine
5-(3-Dimethylaminopropylidene)-10,11-dihydro-5H-dibenzo(a,D)cycloheptatriene
5-(3-Dimethylaminopropylidene)-10,11-dihydro-5H-dibenzo(a,D)cycloheptene
5-(gamma-Dimethylaminopropylidene)-5H-dibenzo[a,D][1,4]cycloheptadiene
Amitriptilina
Amitriptylin
Amitriptyline
Amitriptylinum
External Identifiers
  • MK 230
  • N 750
  • Ro 4-1575
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amitriptylinetablet50 mgoralSivem Pharmaceuticals Ulc2016-02-11Not applicableCanada
Amitriptylinetablet25 mgoralSivem Pharmaceuticals Ulc2016-02-11Not applicableCanada
Amitriptylinetablet10 mgoralSivem Pharmaceuticals Ulc2016-02-11Not applicableCanada
Amitriptyline 10 Tabtablet10 mgoralDuchesnay Inc1981-12-312003-07-18Canada
Amitriptyline 25 Tabtablet25 mgoralDuchesnay Inc1981-12-312003-07-18Canada
Amitriptyline HCl Tab 25mgtablet25 mgoralD.C. Labs Limited1977-12-312003-07-11Canada
Amitriptyline HCl Tab 50mgtablet50 mgoralD.C. Labs Limited1977-12-312003-07-11Canada
Amitriptyline Tablets B.p 25mgtablet25 mgoralClonmel Healthcare Limited1992-12-311996-09-09Canada
Amitriptyline-10tablet10 mgoralPro Doc Limitee1976-12-31Not applicableCanada
Amitriptyline-25tablet25 mgoralPro Doc Limitee1976-12-31Not applicableCanada
Amitriptyline-50tablet50 mgoralPro Doc Limitee1978-12-31Not applicableCanada
Bio-amitriptylinetablet10 mgoralBiomed Pharma2003-04-23Not applicableCanada
Bio-amitriptylinetablet50 mgoralBiomed Pharma2003-04-23Not applicableCanada
Bio-amitriptylinetablet25 mgoralBiomed Pharma2003-04-23Not applicableCanada
Dom-amitriptylinetablet25 mgoralBiomed Pharma2004-02-062013-08-02Canada
Dom-amitriptylinetablet10 mgoralBiomed Pharma2004-02-062013-08-02Canada
Dom-amitriptylinetablet50 mgoralBiomed Pharma2004-02-062013-08-02Canada
Elaviltablet10 mgoralAa Pharma Inc1975-12-31Not applicableCanada
Elaviltablet75 mgoralAa Pharma Inc1987-12-31Not applicableCanada
Elaviltablet50 mgoralAa Pharma Inc1975-12-31Not applicableCanada
Elaviltablet25 mgoralAa Pharma Inc1975-12-31Not applicableCanada
Elavil Pamoate Syr 10mg/5mlsyrup2 mgoralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1968-12-311998-08-14Canada
Elavil Tablet 10mgtablet10 mgoral1560678 Ontario Inc.1961-12-312003-08-02Canada
Elavil Tablet 25mgtablet25 mgoral1560678 Ontario Inc.1961-12-312003-08-02Canada
Elavil Tablet 50mgtablet50 mgoral1560678 Ontario Inc.1964-12-312010-05-05Canada
Elavil Tablet 75mgtablet75 mgoral1560678 Ontario Inc.1976-12-312010-05-05Canada
Ipg-amitriptylinetablet10 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Ipg-amitriptylinetablet75 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Ipg-amitriptylinetablet50 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Ipg-amitriptylinetablet25 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Jamp-amitriptyline Tabletstablet10 mgoralJamp Pharma Corporation2015-01-12Not applicableCanada
Jamp-amitriptyline Tabletstablet75 mgoralJamp Pharma Corporation2015-01-12Not applicableCanada
Jamp-amitriptyline Tabletstablet50 mgoralJamp Pharma Corporation2015-01-12Not applicableCanada
Jamp-amitriptyline Tabletstablet25 mgoralJamp Pharma Corporation2015-01-12Not applicableCanada
Levatetablet75 mgoralBiomed Pharma1979-12-31Not applicableCanada
Levatetablet25 mgoralBiomed Pharma1974-12-31Not applicableCanada
Levatetablet10 mgoralBiomed Pharma1965-12-31Not applicableCanada
Levatetablet50 mgoralBiomed Pharma1969-12-31Not applicableCanada
Mar-amitriptylinetablet25 mgoralMarcan Pharmaceuticals Inc2015-04-24Not applicableCanada
Mar-amitriptylinetablet10 mgoralMarcan Pharmaceuticals Inc2015-04-24Not applicableCanada
Mar-amitriptylinetablet75 mgoralMarcan Pharmaceuticals Inc2015-04-27Not applicableCanada
Mar-amitriptylinetablet50 mgoralMarcan Pharmaceuticals Inc2015-04-24Not applicableCanada
Novo-triptyn Tab 10mgtablet10 mgoralNovopharm Limited1972-12-31Not applicableCanada
Novo-triptyn Tab 25mgtablet25 mgoralNovopharm Limited1972-12-31Not applicableCanada
Novo-triptyn Tab 50mgtablet50 mgoralNovopharm Limited1972-12-31Not applicableCanada
Nu-amitriptyline Tabletstablet75 mgoralNu Pharm IncNot applicableNot applicableCanada
Nu-amitriptyline Tabletstablet50 mgoralNu Pharm IncNot applicableNot applicableCanada
Nu-amitriptyline Tabletstablet25 mgoralNu Pharm IncNot applicableNot applicableCanada
Nu-amitriptyline Tabletstablet10 mgoralNu Pharm IncNot applicableNot applicableCanada
PMS-amitriptylinetablet50 mgoralBiomed Pharma2003-12-112013-08-02Canada
PMS-amitriptylinetablet25 mgoralBiomed Pharma2003-12-112013-08-02Canada
PMS-amitriptylinetablet10 mgoralBiomed Pharma2003-12-112013-08-02Canada
PMS-amitriptyline Tablets 10mgtablet10 mgoralPharmascience Inc1988-12-31Not applicableCanada
PMS-amitriptyline Tablets 25mgtablet25 mgoralPharmascience Inc1988-12-31Not applicableCanada
PMS-amitriptyline Tablets 50mgtablet50 mgoralPharmascience Inc1988-12-31Not applicableCanada
Teva-amitriptylinetablet50 mgoralTeva Canada Limited2014-12-03Not applicableCanada
Teva-amitriptylinetablet25 mgoralTeva Canada Limited2014-12-03Not applicableCanada
Teva-amitriptylinetablet10 mgoralTeva Canada Limited2014-12-03Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralbryant ranch prepack1977-11-29Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralContract Pharmacy Services Pa1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralGLENVIEW PHARMA INC.1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralNorthstar Rx LLC2014-12-01Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralQualitest Pharmaceuticals1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet150 mg/1oralREMEDYREPACK INC.2010-12-13Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralPd Rx Pharmaceuticals, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralA S Medication Solutions Llc1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralH.J. Harkins Company, Inc.1977-11-29Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralPd Rx Pharmaceuticals, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralREMEDYREPACK INC.2015-06-02Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralSTAT Rx USA LLC1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralMylan Pharmaceuticals Inc.1978-04-10Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralSTAT Rx USA LLC2009-11-19Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralAidarex Pharmaceuticals LLC1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralMedsource Pharmaceuticals2014-12-05Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralUnit Dose Services1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralA S Medication Solutions Llc1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralSun Pharmaceutical Industries, Inc.1987-07-14Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralDIRECT RX2014-01-01Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralTYA Pharmaceuticals1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralAphena Pharma Solutions Tennessee, Llc1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralAvera Mc Kennan Hospital2015-03-23Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralNorthstar Rx LLC2014-12-01Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralProficient Rx LP1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralDispensing Solutions, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralPreferred Pharmaceuticals, Inc.2011-06-09Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralSandoz Inc1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralC.O. Truxton, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralAccord Healthcare Inc.2014-12-05Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-10-31Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralMylan Institutional Inc.1994-10-26Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralPhysicians Total Care, Inc.2003-02-04Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralClinical Solutions Wholesale1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralBlenheim Pharmacal, Inc.2010-03-03Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralQualitest Pharmaceuticals1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet100 mg/1oralREMEDYREPACK INC.2010-12-13Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralSTAT Rx USA LLC1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralA S Medication Solutions Llc1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralH.J. Harkins Company, Inc.1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralPd Rx Pharmaceuticals, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralREMEDYREPACK INC.2015-03-25Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralSTAT Rx USA LLC1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralbryant ranch prepack1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralContract Pharmacy Services Pa2010-02-16Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralGLENVIEW PHARMA INC.1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralNorthstar Rx LLC2014-12-01Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralProficient Rx LP1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralDispensing Solutions, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralPreferred Pharmaceuticals, Inc.2011-06-09Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralProficient Rx LP2014-12-05Not applicableUs
Amitriptyline Hydrochloridetablet, film coated150 mg/1oralMylan Pharmaceuticals Inc.1978-04-10Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralAccord Healthcare Inc.2014-12-05Not applicableUs
Amitriptyline Hydrochloridetablet, film coated150 mg/1oralAidarex Pharmaceuticals LLC1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-05-31Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralMylan Institutional Inc.1994-02-16Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralPhysicians Total Care, Inc.1994-10-04Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralClinical Solutions Wholesale1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralBlenheim Pharmacal, Inc.2010-08-04Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralQualitest Pharmaceuticals1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralRebel Distributors Corp.1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralSTAT Rx USA LLC1977-11-29Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralA S Medication Solutions Llc1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralH.J. Harkins Company, Inc.1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralCardinal Health2011-06-17Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralREMEDYREPACK INC.2015-03-07Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralBlenheim Pharmacal, Inc.2011-10-05Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralbryant ranch prepack1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralContract Pharmacy Services Pa2010-02-16Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralPreferred Pharmaceuticals, Inc.1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated150 mg/1oralSandoz Inc1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralMylan Pharmaceuticals Inc.1978-04-10Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralAccord Healthcare Inc.2014-12-05Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralAidarex Pharmaceuticals LLC1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet10 mg/1oralREMEDYREPACK INC.2012-09-17Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralMylan Institutional Inc.1994-02-15Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralPhysicians Total Care, Inc.1995-11-07Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralSun Pharmaceutical Industries, Inc.1987-07-14Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralMajor Pharmaceuticals2009-06-10Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralProficient Rx LP1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralDispensing Solutions, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralPreferred Pharmaceuticals, Inc.2011-06-09Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralCarilion Materials Management1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralQualitest Pharmaceuticals1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralRebel Distributors Corp.1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralSTAT Rx USA LLC1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralA S Medication Solutions Llc1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated150 mg/1oralREMEDYREPACK INC.2013-10-15Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralCardinal Health2011-06-17Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralREMEDYREPACK INC.2015-03-03Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Amitriptyline Hydrochloridetablet25 mg/1oralbryant ranch prepack2009-10-23Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralContract Pharmacy Services Pa1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralPreferred Pharmaceuticals, Inc.1977-11-29Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralSandoz Inc1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralMylan Pharmaceuticals Inc.1978-04-10Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralAccord Healthcare Inc.2014-12-05Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralAidarex Pharmaceuticals LLC1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet100 mg/1oralREMEDYREPACK INC.2011-12-06Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralUnit Dose Services1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralPhysicians Total Care, Inc.1996-06-18Not applicableUs
Amitriptyline Hydrochloridetablet, film coated150 mg/1oralSun Pharmaceutical Industries, Inc.1987-07-14Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralMajor Pharmaceuticals2009-06-10Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralDIRECT RX2015-01-01Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralDispensing Solutions, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated150 mg/1oralDispensing Solutions, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralPd Rx Pharmaceuticals, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralQualitest Pharmaceuticals1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralRebel Distributors Corp.1977-11-29Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralLake Erie Medical DBA Quality Care Products LLC1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-08-24Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralREMEDYREPACK INC.2013-06-04Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralCardinal Health2011-06-17Not applicableUs
Amitriptyline Hydrochloridetablet50 mg/1oralSt. Mary's Medical Park Pharmacy2009-12-01Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralbryant ranch prepack1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralContract Pharmacy Services Pa2010-02-16Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralPreferred Pharmaceuticals, Inc.1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralSandoz Inc1977-11-29Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralMylan Pharmaceuticals Inc.1978-04-10Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralAccord Healthcare Inc.2014-12-05Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralAidarex Pharmaceuticals LLC1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralREMEDYREPACK INC.2010-12-16Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralUnit Dose Services1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralA S Medication Solutions Llc1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralSun Pharmaceutical Industries, Inc.1987-07-14Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1977-11-29Not applicableUs
Amitriptyline Hydrochloridetablet50 mg/1oralDIRECT RX2014-01-01Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralMed Vantx, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralAphena Pharma Solutions Tennessee, Llc1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated150 mg/1oralNorthstar Rx LLC2014-12-01Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralC.O. Truxton, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralRebel Distributors Corp.1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-03-02Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralMylan Institutional Inc.1994-12-13Not applicableUs
Amitriptyline Hydrochloridetablet, film coated150 mg/1oralPhysicians Total Care, Inc.1995-07-25Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralAmerican Health Packaging2015-03-31Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralProficient Rx LP2014-12-05Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralContract Pharmacy Services Pa1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralPreferred Pharmaceuticals, Inc.1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralSandoz Inc1977-11-29Not applicableUs
Amitriptyline Hydrochloridetablet, film coated150 mg/1oralQualitest Pharmaceuticals1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet25 mg/1oralREMEDYREPACK INC.2010-12-13Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralPd Rx Pharmaceuticals, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralUnit Dose Services1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralA S Medication Solutions Llc1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralSun Pharmaceutical Industries, Inc.1987-07-14Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralREMEDYREPACK INC.2015-06-05Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralSTAT Rx USA LLC1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated150 mg/1oralbryant ranch prepack1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralContract Pharmacy Services Pa1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralGLENVIEW PHARMA INC.1977-11-29Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralNorthstar Rx LLC2014-12-01Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralMylan Pharmaceuticals Inc.1978-04-10Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralSTAT Rx USA LLC1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralAidarex Pharmaceuticals LLC1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralREMEDYREPACK INC.2011-04-18Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralUnit Dose Services1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralA S Medication Solutions Llc1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralSun Pharmaceutical Industries, Inc.1987-07-14Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1977-11-21Not applicableUs
Amitriptyline Hydrochloridetablet25 mg/1oralDIRECT RX2014-01-01Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralTYA Pharmaceuticals1977-11-29Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralAphena Pharma Solutions Tennessee, Llc1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralNorthstar Rx LLC2014-12-01Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralC.O. Truxton, Inc.1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated150 mg/1oralAccord Healthcare Inc.2014-12-05Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC1977-11-29Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-09-01Not applicableUs
Amitriptyline Hydrochloridetablet, film coated75 mg/1oralMylan Institutional Inc.1994-02-16Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralPhysicians Total Care, Inc.1999-09-13Not applicableUs
Amitriptyline Hydrochloridetablet, film coated50 mg/1oralClinical Solutions Wholesale1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated10 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralProficient Rx LP1997-09-11Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralContract Pharmacy Services Pa2010-02-16Not applicableUs
Amitriptyline Hydrochloridetablet, film coated100 mg/1oralPreferred Pharmaceuticals, Inc.2011-06-09Not applicableUs
Amitriptyline Hydrochloridetablet, film coated25 mg/1oralSandoz Inc1977-11-21Not applicableUs
Apo-amitriptylinetablet75 mgoralApotex Inc2013-06-12Not applicableCanada
Apo-amitriptylinetablet50 mgoralApotex Inc2013-06-12Not applicableCanada
Apo-amitriptylinetablet25 mgoralApotex Inc2013-06-12Not applicableCanada
Apo-amitriptylinetablet10 mgoralApotex Inc2013-06-12Not applicableCanada
Elavil 25 mgtablet25 mg/1oralThompson Medical Solutions Llc1997-09-11Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Equipto - Amitriptyline External Cream Compounding KitkittopicalAlvix Laboratories, LLC2015-01-20Not applicableUs
International Brands
NameCompany
AdeprilTeofarma
AmitrypRaza
ConmitripCondrugs
EndepAlphapharm
FiordaDriburg
KamitrinSaga
LaroxylDeva
LatilinLa Pharmaceuticals
MaxitripInvision
RedomexLundbeck
SarotenLundbeck
SarotexLundbeck
Sarotex RetardLundbeck
SyneudonKrewel Meuselbach
TryptanolMerck Sharp & Dohme
TryptanolSquare
TryptizolAlgorithm
Uxen RetardSanofi-Aventis
Brand mixtures
NameLabellerIngredients
Apo Peram Tab 2-25Apotex Inc
Apo Peram Tab 3-15Apotex Inc
Chlordiazepoxide and Amitriptyline HClPar Pharmaceutical Inc
Chlordiazepoxide and Amitriptyline HydrochlorideMylan Pharmaceuticals Inc.
Elavil Plus TabTriton Pharma Inc
Etrafon 2 10Schering Plough Canada Inc
Etrafon A TabSchering Plough Canada Inc
Etrafon D TabSchering Plough Canada Inc
Etrafon F TabSchering Plough Canada Inc
Perphenazine and Amitriptyline HydrochlorideMylan Pharmaceuticals Inc.
PMS-levazine 2/25 TabPharmascience Inc
PMS-levazine 3/15 TabPharmascience Inc
PMS-levazine 4/25 TabPharmascience Inc
Proavil TabPro Doc Limitee
Sentravil PM-25Physician Therapeutics Llc
Triavil TabMerck Frosst Canada & Cie, Merck Frosst Canada & Co.
Salts
Name/CASStructureProperties
Amitriptyline Hydrochloride
Thumb
  • InChI Key: KFYRPLNVJVHZGT-UHFFFAOYSA-N
  • Monoisotopic Mass: 313.15972748
  • Average Mass: 313.864
DBSALT000009
Amitriptyline Pamoate
ThumbNot applicableDBSALT001193
Categories
UNII1806D8D52K
CAS number50-48-6
WeightAverage: 277.4033
Monoisotopic: 277.183049741
Chemical FormulaC20H23N
InChI KeyInChIKey=KRMDCWKBEZIMAB-UHFFFAOYSA-N
InChI
InChI=1S/C20H23N/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20/h3-6,8-12H,7,13-15H2,1-2H3
IUPAC Name
dimethyl(3-{tricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,11,13-hexaen-2-ylidene}propyl)amine
SMILES
CN(C)CCC=C1C2=CC=CC=C2CCC2=CC=CC=C12
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
  • Tertiary aliphatic amine
  • Tertiary amine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic homopolycyclic compound
Molecular FrameworkAromatic homopolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of depression, chronic pain, irritable bowel syndrome, sleep disorders, diabetic neuropathy, agitation and insomnia, and migraine prophylaxis.
PharmacodynamicsAmitriptyline, a tertiary amine tricyclic antidepressant, is structurally related to both the skeletal muscle relaxant cyclobenzaprine and the thioxanthene antipsychotics such as thiothixene. It is extremely sedating, and thus improvement of sleep patterns can be the first benefit of treatment. Amitriptyline exhibits strong anticholinergic activity, cardiovascular effects including orthostatic hypotension, changes in heart rhythm and conduction, and a lowering of the seizure threshold. As with other antidepressants, several weeks of therapy may be required in order to realize the full clinical benefit of amitriptyline. Although not a labelled indication, amitriptyline is widely used in the management of chronic nonmalignant pain (e.g., post-herpetic neuralgia, fibromyalgia).
Mechanism of actionAmitriptyline is metabolized to nortriptyline which inhibits the reuptake of norepinephrine and serotonin almost equally. Amitriptyline inhibits the membrane pump mechanism responsible for uptake of norepinephrine and serotonin in adrenergic and serotonergic neurons. Pharmacologically this action may potentiate or prolong neuronal activity since reuptake of these biogenic amines is important physiologically in terminating transmitting activity. This interference with the reuptake of norepinephrine and/or serotonin is believed by some to underlie the antidepressant activity of amitriptyline.
Related Articles
AbsorptionRapidly and well absorbed following oral administration (bioavailability is 30-60% due to first pass metabolism). Peak plasma concentrations occur 2-12 hours following oral or intramuscular administration.
Volume of distributionNot Available
Protein bindingVery highly protein bound (90% or more) in plasma and tissues
Metabolism

Exclusively hepatic, with first pass effect. Amitriptyline is demethylated in the liver to its primary active metabolite, nortriptyline.

SubstrateEnzymesProduct
Amitriptyline
NortriptylineDetails
Amitriptyline
E-10-HydroxyamitriptylineDetails
E-10-Hydroxyamitriptyline
E-10-HydroxynortriptylineDetails
E-10-Hydroxynortriptyline
Not Available
E-10-HydroxydesmethylnortriptylineDetails
Nortriptyline
E-10-HydroxynortriptylineDetails
Nortriptyline
Not Available
DesmethylnortriptylineDetails
Desmethylnortriptyline
E-10-HydroxydesmethylnortriptylineDetails
Route of eliminationVirtually the entire dose is excreted as glucuronide or sulfate conjugate of metabolites, with little unchanged drug appearing in the urine. 25-50% of a single orally administered dose is excreted in urine as inactive metabolites within 24 hours. Small amounts are excreted in feces via biliary elimination.
Half life10 to 50 hours, with an average of 15 hours
ClearanceNot Available
ToxicityLD50=350 mg/kg (in mice). Symptoms of overdose include abnormally low blood pressure, confusion, convulsions, dilated pupils and other eye problems, disturbed concentration, drowsiness, hallucinations, impaired heart function, rapid or irregular heartbeat, reduced body temperature, stupor, and unresponsiveness or coma. Side effects include: sedation, hypotension, blurred vision, dry mouth, constipation, urinary retention, postural hypotension, tachycardia, hypertension, ECG changes, heart failure, impaired memory and delirium, and precipitation of hypomanic or manic episodes in bipolar depression. Withdrawal symptoms include gastrointestinal disturbances, anxiety, and insomnia.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Cytochrome P450 2D6
Gene symbol: CYP2D6
UniProt: P10635
rs3892097 CYP2D6*4A AllelePoor drug metabolizer, lower dose requirements, higher risk for adverse side effects18070221
Multidrug resistance protein 1
Gene symbol: ABCB1
UniProt: P08183
rs2032583 Not AvailableC AlleleImproved response to antidepressant medication17913323
Multidrug resistance protein 1
Gene symbol: ABCB1
UniProt: P08183
rs2032583 Not AvailableA > GIncrease risk of adverse effects22641028
SNP Mediated Adverse Drug Reactions
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeAdverse ReactionReference(s)
Multidrug resistance protein 1
Gene symbol: ABCB1
UniProt: P08183
rs1045642 Not AvailableT Allele, homozygousPostural hypotension12082591
Cytochrome P450 2C19
Gene symbol: CYP2C19
UniProt: P33261
rs4244285 CYP2C19*2G > AThose with the AA or AG genotype are poor metabolizers of amitriptyline20531370
Cytochrome P450 2D6
Gene symbol: CYP2D6
UniProt: P10635
rs3892097 CYP2D6*4C > TIncrease risk of side effects and decrease drug metabolism18070221
Cytochrome P450 2D6
Gene symbol: CYP2D6
UniProt: P10635
rs3892097 CYP2D6*4C > TIncrease risk of side effects and decrease drug metabolism9918137
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9941
Blood Brain Barrier+0.9512
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.7567
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IIInhibitor0.6447
Renal organic cation transporterInhibitor0.7955
CYP450 2C9 substrateNon-substrate0.7826
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.7501
CYP450 1A2 substrateInhibitor0.7324
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8933
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9158
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6955
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.8127
BiodegradationNot ready biodegradable0.8727
Rat acute toxicity2.9697 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7531
hERG inhibition (predictor II)Inhibitor0.6767
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Hoffmann la roche inc
  • Watson laboratories inc
  • Astrazeneca pharmaceuticals lp
  • Bristol myers squibb co
  • Warner chilcott div warner lambert co
  • American therapeutics inc
  • Caraco pharmaceutical laboratories ltd
  • Copley pharmaceutical inc
  • Halsey drug co inc
  • Lederle laboratories div american cyanamid co
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • Pliva inc
  • Purepac pharmaceutical co
  • Roxane laboratories inc
  • Sandoz inc
  • Superpharm corp
  • Teva pharmaceuticals usa inc
  • Ucb inc
  • Usl pharma inc
  • Vangard laboratories inc div midway medical co
  • Vintage pharmaceuticals inc
  • West ward pharmaceutical corp
Packagers
Dosage forms
FormRouteStrength
Tabletoral10 mg/1
Tabletoral100 mg/1
Tabletoral150 mg/1
Tabletoral25 mg/1
Tabletoral50 mg/1
Tablet, film coatedoral10 mg/1
Tablet, film coatedoral100 mg/1
Tablet, film coatedoral150 mg/1
Tablet, film coatedoral25 mg/1
Tablet, film coatedoral50 mg/1
Tablet, film coatedoral75 mg/1
Syruporal2 mg
Kittopical
Tabletoral75 mg
Tabletoral10 mg
Tabletoral25 mg
Tabletoral50 mg
Tabletoral
Tablet, film coatedoral
Kit
Prices
Unit descriptionCostUnit
Amitriptyline hcl powder7.34USD g
Amitriptyline hcl 150 mg tablet1.18USD tablet
Amitriptyline hcl 100 mg tablet0.66USD tablet
Amitriptyline hcl 75 mg tablet0.54USD tablet
Apo-Amitriptyline 75 mg Tablet0.38USD tablet
Amitriptyline hcl 50 mg tablet0.37USD tablet
Amitriptyline hcl 10 mg tablet0.3USD tablet
Apo-Amitriptyline 50 mg Tablet0.25USD tablet
Amitriptyline hcl 25 mg tablet0.21USD tablet
Apo-Amitriptyline 25 mg Tablet0.13USD tablet
Apo-Amitriptyline 10 mg Tablet0.07USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point187-189.5Tristram, E.W. and Tull, R.J.; US. Patent 3,205,264: September 7,1965; assigned to Merck & Co., Inc.
water solubility9.71 mg/L (at 24 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP4.92HANSCH,C ET AL. (1995)
logS-4.46ADME Research, USCD
pKa9.4SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.0045 mg/mLALOGPS
logP5.1ALOGPS
logP4.81ChemAxon
logS-4.8ALOGPS
pKa (Strongest Basic)9.76ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area3.24 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity101.51 m3·mol-1ChemAxon
Polarizability33.74 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (7.48 KB)
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-0a4i-9210000000-989cd234a8cdf04c5f69View in MoNA
References
Synthesis Reference

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

US4567202
General References
  1. Otaka M, Jin M, Odashima M, Matsuhashi T, Wada I, Horikawa Y, Komatsu K, Ohba R, Oyake J, Hatakeyama N, Watanabe S: New strategy of therapy for functional dyspepsia using famotidine, mosapride and amitriptyline. Aliment Pharmacol Ther. 2005 Jun;21 Suppl 2:42-6. [PubMed:15943846 ]
External Links
ATC CodesN06AA09N06CA01
AHFS Codes
  • 28:16.04.28
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.6 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Amitriptyline can be increased when it is combined with Abiraterone.
AcenocoumarolAmitriptyline may increase the anticoagulant activities of Acenocoumarol.
AcepromazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Acepromazine.
AcetaminophenThe metabolism of Amitriptyline can be increased when combined with Acetaminophen.
AcetophenazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Acetophenazine.
Acetylsalicylic acidAmitriptyline may increase the antiplatelet activities of Acetylsalicylic acid.
AclidiniumAclidinium may increase the anticholinergic activities of Amitriptyline.
AltretamineAltretamine may increase the orthostatic hypotensive activities of Amitriptyline.
AmisulprideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Amisulpride.
AmobarbitalThe metabolism of Amitriptyline can be increased when combined with Amobarbital.
AmphetamineAmitriptyline may increase the stimulatory activities of Amphetamine.
ApraclonidineThe therapeutic efficacy of Apraclonidine can be decreased when used in combination with Amitriptyline.
ArformoterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Arformoterol.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Amitriptyline.
ArticaineAmitriptyline may increase the activities of Articaine.
AtazanavirThe serum concentration of Amitriptyline can be increased when it is combined with Atazanavir.
AzelastineAmitriptyline 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 Amitriptyline.
BatimastatThe serum concentration of Amitriptyline can be increased when it is combined with Batimastat.
BenzphetamineAmitriptyline may increase the stimulatory activities of Benzphetamine.
BenzquinamideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Benzquinamide.
Botulinum Toxin Type AAmitriptyline may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BAmitriptyline may increase the anticholinergic activities of Botulinum Toxin Type B.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
BuprenorphineAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BupropionThe metabolism of Amitriptyline can be decreased when combined with Bupropion.
ButabarbitalThe metabolism of Amitriptyline can be increased when combined with Butabarbital.
ButalbitalThe metabolism of Amitriptyline can be increased when combined with Butalbital.
ButethalThe metabolism of Amitriptyline can be increased when combined with Butethal.
CaffeineThe metabolism of Amitriptyline can be increased when combined with Caffeine.
CarbamazepineThe metabolism of Amitriptyline can be increased when combined with Carbamazepine.
CarphenazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Carphenazine.
CathinoneAmitriptyline may increase the stimulatory activities of Cathinone.
CelecoxibAmitriptyline may increase the antiplatelet activities of Celecoxib.
ChlormezanoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Chlorpromazine.
ChlorpropamideAmitriptyline may increase the hypoglycemic activities of Chlorpropamide.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Chlorprothixene.
CimetidineThe metabolism of Amitriptyline can be decreased when combined with Cimetidine.
Cimetropium BromideAmitriptyline may increase the anticholinergic activities of Cimetropium Bromide.
CinacalcetThe serum concentration of Amitriptyline can be increased when it is combined with Cinacalcet.
CisaprideAmitriptyline may increase the arrhythmogenic activities of Cisapride.
CitalopramThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Citalopram.
ClonidineAmitriptyline may decrease the antihypertensive activities of Clonidine.
ClozapineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Clozapine.
CobicistatThe serum concentration of Amitriptyline can be increased when it is combined with Cobicistat.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Amitriptyline.
DarunavirThe serum concentration of Amitriptyline can be increased when it is combined with Darunavir.
DesmopressinThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Desmopressin.
DexmedetomidineAmitriptyline may decrease the antihypertensive activities of Dexmedetomidine.
DexmethylphenidateThe risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with Amitriptyline.
DextroamphetamineAmitriptyline may increase the stimulatory activities of Dextroamphetamine.
DiclofenacAmitriptyline may increase the antiplatelet activities of Diclofenac.
DicoumarolAmitriptyline may increase the anticoagulant activities of Dicoumarol.
DiflunisalAmitriptyline may increase the antiplatelet activities of Diflunisal.
DihydrocodeineAmitriptyline may increase the antiplatelet activities of Dihydrocodeine.
DipivefrinThe therapeutic efficacy of Dipivefrin can be decreased when used in combination with Amitriptyline.
DofetilideAmitriptyline may increase the QTc-prolonging activities of Dofetilide.
DopamineAmitriptyline may increase the activities of Dopamine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
DuloxetineDuloxetine may increase the serotonergic activities of Amitriptyline.
EluxadolineAmitriptyline may increase the activities of Eluxadoline.
EpinephrineAmitriptyline may increase the activities of Epinephrine.
EscitalopramThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Escitalopram.
EthanolAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EtodolacAmitriptyline may increase the antiplatelet activities of Etodolac.
FencamfamineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fencamfamine.
FenoprofenAmitriptyline may increase the antiplatelet activities of Fenoprofen.
FloctafenineAmitriptyline may increase the antiplatelet activities of Floctafenine.
FluconazoleAmitriptyline may increase the QTc-prolonging activities of Fluconazole.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Amitriptyline.
FlupentixolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fluphenazine.
FlurbiprofenAmitriptyline may increase the antiplatelet activities of Flurbiprofen.
FluspirileneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fluspirilene.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Fluticasone Propionate.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Amitriptyline.
FormoterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Formoterol.
FosamprenavirThe serum concentration of Amitriptyline can be increased when it is combined with Fosamprenavir.
GliclazideAmitriptyline may increase the hypoglycemic activities of Gliclazide.
GlimepirideAmitriptyline may increase the hypoglycemic activities of Glimepiride.
GlipizideAmitriptyline may increase the hypoglycemic activities of Glipizide.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Glucagon recombinant.
GlyburideAmitriptyline may increase the hypoglycemic activities of Glyburide.
GoserelinAmitriptyline may increase the QTc-prolonging activities of Goserelin.
GranisetronGranisetron may increase the serotonergic activities of Amitriptyline.
GuanfacineAmitriptyline may decrease the antihypertensive activities of Guanfacine.
HaloperidolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Haloperidol.
HeptabarbitalThe metabolism of Amitriptyline can be increased when combined with Heptabarbital.
HexobarbitalThe metabolism of Amitriptyline can be increased when combined with Hexobarbital.
HydrocodoneAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
IbuprofenAmitriptyline may increase the antiplatelet activities of Ibuprofen.
IcosapentAmitriptyline may increase the antiplatelet activities of Icosapent.
IndacaterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Indacaterol.
IndinavirThe serum concentration of Amitriptyline can be increased when it is combined with Indinavir.
IndomethacinAmitriptyline may increase the antiplatelet activities of Indomethacin.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Amitriptyline.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Amitriptyline.
IsocarboxazidIsocarboxazid may increase the serotonergic activities of Amitriptyline.
IsoflurophateThe serum concentration of Amitriptyline can be increased when it is combined with Isoflurophate.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Amitriptyline.
KetoprofenAmitriptyline may increase the antiplatelet activities of Ketoprofen.
KetorolacAmitriptyline may increase the antiplatelet activities of Ketorolac.
LeuprolideAmitriptyline may increase the QTc-prolonging activities of Leuprolide.
LevonordefrinAmitriptyline may increase the activities of Levonordefrin.
LevothyroxineLevothyroxine may increase the arrhythmogenic activities of Amitriptyline.
LinezolidLinezolid may increase the serotonergic activities of Amitriptyline.
LiothyronineLiothyronine may increase the arrhythmogenic activities of Amitriptyline.
LiotrixLiotrix may increase the arrhythmogenic activities of Amitriptyline.
LisdexamfetamineAmitriptyline may increase the stimulatory activities of Lisdexamfetamine.
LithiumLithium may increase the neurotoxic activities of Amitriptyline.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Amitriptyline.
LoxapineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Loxapine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
Mefenamic acidAmitriptyline may increase the antiplatelet activities of Mefenamic acid.
MeloxicamAmitriptyline may increase the antiplatelet activities of Meloxicam.
MepivacaineAmitriptyline may increase the activities of Mepivacaine.
MesoridazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Mesoridazine.
MethamphetamineAmitriptyline may increase the stimulatory activities of Methamphetamine.
MethohexitalThe metabolism of Amitriptyline can be increased when combined with Methohexital.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Methotrimeprazine.
MethyldopaAmitriptyline may decrease the antihypertensive activities of Methyldopa.
Methylene blueAmitriptyline may increase the serotonergic activities of Methylene blue.
MethylphenidateThe risk or severity of adverse effects can be increased when Methylphenidate is combined with Amitriptyline.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Amitriptyline.
MetyrosineAmitriptyline may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the anticholinergic activities of Amitriptyline.
MidodrineAmitriptyline may increase the activities of Midodrine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Amitriptyline.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
MirabegronThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Mirabegron.
MoclobemideMoclobemide may increase the serotonergic activities of Amitriptyline.
MolindoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Molindone.
MorphineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Morphine.
MoxonidineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Amitriptyline.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
NabumetoneAmitriptyline may increase the antiplatelet activities of Nabumetone.
NaphazolineAmitriptyline may increase the activities of Naphazoline.
NaproxenAmitriptyline may increase the antiplatelet activities of Naproxen.
NelfinavirThe serum concentration of Amitriptyline can be increased when it is combined with Nelfinavir.
NicorandilAmitriptyline may increase the hypotensive activities of Nicorandil.
NorepinephrineAmitriptyline may increase the activities of Norepinephrine.
OlanzapineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Olanzapine.
OlodaterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Olodaterol.
OndansetronThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ondansetron.
OrciprenalineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Orciprenaline.
OrphenadrineAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxaprozinAmitriptyline may increase the antiplatelet activities of Oxaprozin.
OxymetazolineAmitriptyline may increase the activities of Oxymetazoline.
PaliperidoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Paliperidone.
PanobinostatThe serum concentration of Amitriptyline can be increased when it is combined with Panobinostat.
ParaldehydeAmitriptyline 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 Amitriptyline.
Peginterferon alfa-2bThe serum concentration of Amitriptyline can be decreased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe metabolism of Amitriptyline can be increased when combined with Pentobarbital.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
PerphenazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Perphenazine.
PhendimetrazineAmitriptyline may increase the stimulatory activities of Phendimetrazine.
PhenelzinePhenelzine may increase the serotonergic activities of Amitriptyline.
PheniramineAmitriptyline may increase the activities of Pheniramine.
PhenobarbitalThe metabolism of Amitriptyline can be increased when combined with Phenobarbital.
PhentermineAmitriptyline may increase the stimulatory activities of Phentermine.
PhenylephrineAmitriptyline may increase the activities of Phenylephrine.
PimozideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Piperacetazine.
PirbuterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Pirbuterol.
PiroxicamAmitriptyline may increase the antiplatelet activities of Piroxicam.
Potassium ChlorideAmitriptyline may increase the ulcerogenic activities of Potassium Chloride.
PramipexoleAmitriptyline may increase the sedative activities of Pramipexole.
PramlintidePramlintide may increase the anticholinergic activities of Amitriptyline.
PrimidoneThe metabolism of Amitriptyline can be increased when combined with Primidone.
ProcarbazineProcarbazine may increase the serotonergic activities of Amitriptyline.
ProchlorperazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Prochlorperazine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Amitriptyline.
PromazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Promazine.
PropylhexedrineAmitriptyline may increase the activities of Propylhexedrine.
QuetiapineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Quetiapine.
QuinidineAmitriptyline may increase the QTc-prolonging activities of Quinidine.
RacepinephrineAmitriptyline may increase the activities of Racepinephrine.
RamosetronAmitriptyline may increase the activities of Ramosetron.
RasagilineRasagiline may increase the serotonergic activities of Amitriptyline.
RemoxiprideThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Risperidone.
RitonavirThe metabolism of Amitriptyline can be decreased when combined with Ritonavir.
RopiniroleAmitriptyline may increase the sedative activities of Ropinirole.
RotigotineAmitriptyline may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Amitriptyline.
SalbutamolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Salbutamol.
SalmeterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Salmeterol.
SaquinavirThe serum concentration of Amitriptyline can be increased when it is combined with Saquinavir.
SecobarbitalThe metabolism of Amitriptyline can be increased when combined with Secobarbital.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Amitriptyline.
SelegilineSelegiline may increase the serotonergic activities of Amitriptyline.
SertindoleThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Sertindole.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Amitriptyline.
SimeprevirThe serum concentration of Amitriptyline can be increased when it is combined with Simeprevir.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
St. John's WortThe metabolism of Amitriptyline can be increased when combined with St. John's Wort.
SulindacAmitriptyline may increase the antiplatelet activities of Sulindac.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Amitriptyline.
SuvorexantAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Amitriptyline can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Amitriptyline.
TerbinafineThe metabolism of Amitriptyline can be decreased when combined with Terbinafine.
TerbutalineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Terbutaline.
ThalidomideAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Thiothixene.
Thyroid, porcineThyroid extract may increase the arrhythmogenic activities of Amitriptyline.
Tiaprofenic acidAmitriptyline may increase the antiplatelet activities of Tiaprofenic acid.
TiclopidineThe metabolism of Amitriptyline can be decreased when combined with Ticlopidine.
TiotropiumAmitriptyline may increase the anticholinergic activities of Tiotropium.
TipranavirThe serum concentration of Amitriptyline can be increased when it is combined with Tipranavir.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Amitriptyline.
TolazamideAmitriptyline may increase the hypoglycemic activities of Tolazamide.
TolbutamideAmitriptyline may increase the hypoglycemic activities of Tolbutamide.
TolmetinAmitriptyline may increase the antiplatelet activities of Tolmetin.
TopiramateTopiramate may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
TramadolAmitriptyline may increase the neuroexcitatory activities of Tramadol.
TranylcypromineTranylcypromine may increase the serotonergic activities of Amitriptyline.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Amitriptyline.
TrifluoperazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Triflupromazine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Amitriptyline.
Valproic AcidThe serum concentration of Amitriptyline can be increased when it is combined with Valproic Acid.
VilanterolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Vilanterol.
WarfarinAmitriptyline may increase the anticoagulant activities of Warfarin.
YohimbineThe serum concentration of Yohimbine can be increased when it is combined with Amitriptyline.
ZiprasidoneThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Ziprasidone.
ZolpidemAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Zuclopenthixol.
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (caffeine).
  • Avoid St.John's Wort.
  • Take with food to reduce irritation.

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. Vaishnavi SN, Nemeroff CB, Plott SJ, Rao SG, Kranzler J, Owens MJ: Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity. Biol Psychiatry. 2004 Feb 1;55(3):320-2. [PubMed:14744476 ]
  2. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Serotonin:sodium symporter activity
Specific Function:
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into 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. Gould GG, Altamirano AV, Javors MA, Frazer A: A comparison of the chronic treatment effects of venlafaxine and other antidepressants on serotonin and norepinephrine transporters. Biol Psychiatry. 2006 Mar 1;59(5):408-14. Epub 2005 Sep 2. [PubMed:16140280 ]
  2. Troelsen KB, Nielsen EO, Mirza NR: Chronic treatment with duloxetine is necessary for an anxiolytic-like response in the mouse zero maze: the role of the serotonin transporter. Psychopharmacology (Berl). 2005 Oct;181(4):741-50. Epub 2005 Sep 29. [PubMed:16032412 ]
  3. Vaishnavi SN, Nemeroff CB, Plott SJ, Rao SG, Kranzler J, Owens MJ: Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity. Biol Psychiatry. 2004 Feb 1;55(3):320-2. [PubMed:14744476 ]
  4. Ushijima K, Sakaguchi H, Sato Y, To H, Koyanagi S, Higuchi S, Ohdo S: Chronopharmacological study of antidepressants in forced swimming test of mice. J Pharmacol Exp Ther. 2005 Nov;315(2):764-70. Epub 2005 Aug 3. [PubMed:16079297 ]
  5. Kalia M: Neurobiological basis of depression: an update. Metabolism. 2005 May;54(5 Suppl 1):24-7. [PubMed:15877309 ]
  6. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821 ]
  7. Werling LL, Keller A, Frank JG, Nuwayhid SJ: A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder. Exp Neurol. 2007 Oct;207(2):248-57. Epub 2007 Jun 30. [PubMed:17689532 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Virus receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Opioid receptor activity
Specific Function:
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurot...
Gene Name:
OPRD1
Uniprot ID:
P41143
Molecular Weight:
40368.235 Da
References
  1. Onali P, Dedoni S, Olianas MC: Direct agonist activity of tricyclic antidepressants at distinct opioid receptor subtypes. J Pharmacol Exp Ther. 2010 Jan;332(1):255-65. doi: 10.1124/jpet.109.159939. Epub 2009 Oct 14. [PubMed:19828880 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Opioid receptor activity
Specific Function:
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates th...
Gene Name:
OPRK1
Uniprot ID:
P41145
Molecular Weight:
42644.665 Da
References
  1. Onali P, Dedoni S, Olianas MC: Direct agonist activity of tricyclic antidepressants at distinct opioid receptor subtypes. J Pharmacol Exp Ther. 2010 Jan;332(1):255-65. doi: 10.1124/jpet.109.159939. Epub 2009 Oct 14. [PubMed:19828880 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Receptor tyrosine kinase involved in the development and the maturation of the central and peripheral nervous systems through regulation of proliferation, differentiation and survival of sympathetic and nervous neurons. High affinity receptor for NGF which is its primary ligand, it can also bind and be activated by NTF3/neurotrophin-3. However, NTF3 only supports axonal extension through NTRK1 ...
Gene Name:
NTRK1
Uniprot ID:
P04629
Molecular Weight:
87496.465 Da
References
  1. Jang SW, Liu X, Chan CB, Weinshenker D, Hall RA, Xiao G, Ye K: Amitriptyline is a TrkA and TrkB receptor agonist that promotes TrkA/TrkB heterodimerization and has potent neurotrophic activity. Chem Biol. 2009 Jun 26;16(6):644-56. doi: 10.1016/j.chembiol.2009.05.010. [PubMed:19549602 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Protein homodimerization activity
Specific Function:
Receptor tyrosine kinase involved in the development and the maturation of the central and the peripheral nervous systems through regulation of neuron survival, proliferation, migration, differentiation, and synapse formation and plasticity. Receptor for BDNF/brain-derived neurotrophic factor and NTF4/neurotrophin-4. Alternatively can also bind NTF3/neurotrophin-3 which is less efficient in act...
Gene Name:
NTRK2
Uniprot ID:
Q16620
Molecular Weight:
91998.175 Da
References
  1. Jang SW, Liu X, Chan CB, Weinshenker D, Hall RA, Xiao G, Ye K: Amitriptyline is a TrkA and TrkB receptor agonist that promotes TrkA/TrkB heterodimerization and has potent neurotrophic activity. Chem Biol. 2009 Jun 26;16(6):644-56. doi: 10.1016/j.chembiol.2009.05.010. [PubMed:19549602 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
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
Molecular Weight:
60462.205 Da
References
  1. Nojimoto FD, Mueller A, Hebeler-Barbosa F, Akinaga J, Lima V, Kiguti LR, Pupo AS: The tricyclic antidepressants amitriptyline, nortriptyline and imipramine are weak antagonists of human and rat alpha1B-adrenoceptors. Neuropharmacology. 2010 Jul-Aug;59(1-2):49-57. doi: 10.1016/j.neuropharm.2010.03.015. Epub 2010 Apr 2. [PubMed:20363235 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217 ]
  2. Ozdogan UK, Lahdesmaki J, Mansikka H, Scheinin M: Loss of amitriptyline analgesia in alpha 2A-adrenoceptor deficient mice. Eur J Pharmacol. 2004 Feb 6;485(1-3):193-6. [PubMed:14757140 ]
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 catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
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 action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
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 action of G proteins. Primary transducing effect is inhibition of adenylate cyclase.
Gene Name:
CHRM4
Uniprot ID:
P08173
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM5
Uniprot ID:
P08912
Molecular Weight:
60073.205 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inhibitor
General Function:
Voltage-gated potassium channel activity
Specific Function:
Probably important in the regulation of neuronal excitability. Associates with KCNQ3 to form a potassium channel with essentially identical properties to the channel underlying the native M-current, a slowly activating and deactivating potassium conductance which plays a critical role in determining the subthreshold electrical excitability of neurons as well as the responsiveness to synaptic in...
Gene Name:
KCNQ2
Uniprot ID:
O43526
Molecular Weight:
95846.575 Da
References
  1. Punke MA, Friederich P: Amitriptyline is a potent blocker of human Kv1.1 and Kv7.2/7.3 channels. Anesth Analg. 2007 May;104(5):1256-64, tables of contents. [PubMed:17456683 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inhibitor
General Function:
Voltage-gated potassium channel activity
Specific Function:
Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain and the central nervous system, but also in the kidney (PubMed:19903818). Contributes to the regulation of the membrane potential and nerve signaling, and prevents neuronal hyperexcitability (PubMed:17156368). Forms tetrameric potassium-selective channels through which ...
Gene Name:
KCNA1
Uniprot ID:
Q09470
Molecular Weight:
56465.01 Da
References
  1. Punke MA, Friederich P: Amitriptyline is a potent blocker of human Kv1.1 and Kv7.2/7.3 channels. Anesth Analg. 2007 May;104(5):1256-64, tables of contents. [PubMed:17456683 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inhibitor
General Function:
Voltage-gated potassium channel activity
Specific Function:
Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain. Mediates the major part of the dendritic A-type current I(SA) in brain neurons (By similarity). This current is activated at membrane potentials that are below the threshold for action potentials. It regulates neuronal excitability, prolongs the latency before the firs...
Gene Name:
KCND2
Uniprot ID:
Q9NZV8
Molecular Weight:
70535.825 Da
References
  1. Casis O, Sanchez-Chapula JA: Disopyramide, imipramine, and amitriptyline bind to a common site on the transient outward K+ channel. J Cardiovasc Pharmacol. 1998 Oct;32(4):521-6. [PubMed:9781919 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Pore-forming (alpha) subunit of voltage-gated rapidly inactivating A-type potassium channels. May contribute to I(To) current in heart and I(Sa) current in neurons. Channel properties are modulated by interactions with other alpha subunits and with regulatory subunits.
Gene Name:
KCND3
Uniprot ID:
Q9UK17
Molecular Weight:
73450.53 Da
References
  1. Casis O, Sanchez-Chapula JA: Disopyramide, imipramine, and amitriptyline bind to a common site on the transient outward K+ channel. J Cardiovasc Pharmacol. 1998 Oct;32(4):521-6. [PubMed:9781919 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
blocker
General Function:
Histamine receptor activity
Specific Function:
The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and differentiation. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and, through a separate G protein-dependent mechanism, the phosphoinositide/protein kinase (PKC) si...
Gene Name:
HRH2
Uniprot ID:
P25021
Molecular Weight:
40097.65 Da
References
  1. Angus JA, Black JW: Pharmacological assay of cardiac H2-receptor blockade by amitriptyline and lysergic acid diethylamide. Circ Res. 1980 Jun;46(6 Pt 2):I64-9. [PubMed:6103762 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Histamine receptor activity
Specific Function:
The H4 subclass of histamine receptors could mediate the histamine signals in peripheral tissues. Displays a significant level of constitutive activity (spontaneous activity in the absence of agonist).
Gene Name:
HRH4
Uniprot ID:
Q9H3N8
Molecular Weight:
44495.375 Da
References
  1. Nguyen T, Shapiro DA, George SR, Setola V, Lee DK, Cheng R, Rauser L, Lee SP, Lynch KR, Roth BL, O'Dowd BF: Discovery of a novel member of the histamine receptor family. Mol Pharmacol. 2001 Mar;59(3):427-33. [PubMed:11179435 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Opioid receptor activity
Specific Function:
Functions in lipid transport from the endoplasmic reticulum and is involved in a wide array of cellular functions probably through regulation of the biogenesis of lipid microdomains at the plasma membrane. Involved in the regulation of different receptors it plays a role in BDNF signaling and EGF signaling. Also regulates ion channels like the potassium channel and could modulate neurotransmitt...
Gene Name:
SIGMAR1
Uniprot ID:
Q99720
Molecular Weight:
25127.52 Da
References
  1. Villard V, Meunier J, Chevallier N, Maurice T: Pharmacological interaction with the sigma1 (sigma1)-receptor in the acute behavioral effects of antidepressants. J Pharmacol Sci. 2011;115(3):279-92. [PubMed:21427517 ]
  2. Werling LL, Keller A, Frank JG, Nuwayhid SJ: A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder. Exp Neurol. 2007 Oct;207(2):248-57. Epub 2007 Jun 30. [PubMed:17689532 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
Molecular Weight:
51820.705 Da
References
  1. Di Matteo V, De Blasi A, Di Giulio C, Esposito E: Role of 5-HT(2C) receptors in the control of central dopamine function. Trends Pharmacol Sci. 2001 May;22(5):229-32. [PubMed:11339973 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. Nojimoto FD, Mueller A, Hebeler-Barbosa F, Akinaga J, Lima V, Kiguti LR, Pupo AS: The tricyclic antidepressants amitriptyline, nortriptyline and imipramine are weak antagonists of human and rat alpha1B-adrenoceptors. Neuropharmacology. 2010 Jul-Aug;59(1-2):49-57. doi: 10.1016/j.neuropharm.2010.03.015. Epub 2010 Apr 2. [PubMed:20363235 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53554.43 Da
References
  1. Lucchelli A, Santagostino-Barbone MG, D'Agostino G, Masoero E, Tonini M: The interaction of antidepressant drugs with enteric 5-HT7 receptors. Naunyn Schmiedebergs Arch Pharmacol. 2000 Sep;362(3):284-9. [PubMed:10997731 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate c...
Gene Name:
HTR1D
Uniprot ID:
P28221
Molecular Weight:
41906.38 Da
References
  1. Werling LL, Keller A, Frank JG, Nuwayhid SJ: A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder. Exp Neurol. 2007 Oct;207(2):248-57. Epub 2007 Jun 30. [PubMed:17689532 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Voltage-gated calcium channel activity
Specific Function:
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociati...
Gene Name:
OPRM1
Uniprot ID:
P35372
Molecular Weight:
44778.855 Da
References
  1. Wahlstrom A, Lenhammar L, Ask B, Rane A: Tricyclic antidepressants inhibit opioid receptor binding in human brain and hepatic morphine glucuronidation. Pharmacol Toxicol. 1994 Jul;75(1):23-7. [PubMed:7971731 ]
  2. Hamon M, Gozlan H, Bourgoin S, Benoliel JJ, Mauborgne A, Taquet H, Cesselin F, Mico JA: Opioid receptors and neuropeptides in the CNS in rats treated chronically with amoxapine or amitriptyline. Neuropharmacology. 1987 Jun;26(6):531-9. [PubMed:3037421 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
Molecular Weight:
43567.535 Da
References
  1. Werling LL, Keller A, Frank JG, Nuwayhid SJ: A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder. Exp Neurol. 2007 Oct;207(2):248-57. Epub 2007 Jun 30. [PubMed:17689532 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs (By similarity). Controls pyramidal neurons migration during corticogenesis, through...
Gene Name:
HTR6
Uniprot ID:
P50406
Molecular Weight:
46953.625 Da
References
  1. Kohen R, Metcalf MA, Khan N, Druck T, Huebner K, Lachowicz JE, Meltzer HY, Sibley DR, Roth BL, Hamblin MW: Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. J Neurochem. 1996 Jan;66(1):47-56. [PubMed:8522988 ]
  2. Sebben M, Ansanay H, Bockaert J, Dumuis A: 5-HT6 receptors positively coupled to adenylyl cyclase in striatal neurones in culture. Neuroreport. 1994 Dec 20;5(18):2553-7. [PubMed:7696602 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Voltage-gated potassium channel activity
Specific Function:
Probably important in the regulation of neuronal excitability. Associates with KCNQ2 or KCNQ5 to form a potassium channel with essentially identical properties to the channel underlying the native M-current, a slowly activating and deactivating potassium conductance which plays a critical role in determining the subthreshold electrical excitability of neurons as well as the responsiveness to sy...
Gene Name:
KCNQ3
Uniprot ID:
O43525
Molecular Weight:
96741.515 Da
References
  1. Punke MA, Friederich P: Amitriptyline is a potent blocker of human Kv1.1 and Kv7.2/7.3 channels. Anesth Analg. 2007 May;104(5):1256-64, tables of contents. [PubMed:17456683 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Receptor signaling protein activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
Components:
NameUniProt IDDetails
Beta-1 adrenergic receptorP08588 Details
Beta-2 adrenergic receptorP07550 Details
Beta-3 adrenergic receptorP13945 Details
References
  1. Werling LL, Keller A, Frank JG, Nuwayhid SJ: A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder. Exp Neurol. 2007 Oct;207(2):248-57. Epub 2007 Jun 30. [PubMed:17689532 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Baumann P: Pharmacokinetic-pharmacodynamic relationship of the selective serotonin reuptake inhibitors. Clin Pharmacokinet. 1996 Dec;31(6):444-69. [PubMed:8968657 ]
  2. Wen B, Ma L, Zhu M: Bioactivation of the tricyclic antidepressant amitriptyline and its metabolite nortriptyline to arene oxide intermediates in human liver microsomes and recombinant P450s. Chem Biol Interact. 2008 May 9;173(1):59-67. doi: 10.1016/j.cbi.2008.02.001. Epub 2008 Feb 14. [PubMed:18359012 ]
  3. Ghahramani P, Ellis SW, Lennard MS, Ramsay LE, Tucker GT: Cytochromes P450 mediating the N-demethylation of amitriptyline. Br J Clin Pharmacol. 1997 Feb;43(2):137-44. [PubMed:9131945 ]
  4. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  5. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  6. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560 ]
  7. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Wen B, Ma L, Zhu M: Bioactivation of the tricyclic antidepressant amitriptyline and its metabolite nortriptyline to arene oxide intermediates in human liver microsomes and recombinant P450s. Chem Biol Interact. 2008 May 9;173(1):59-67. doi: 10.1016/j.cbi.2008.02.001. Epub 2008 Feb 14. [PubMed:18359012 ]
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  4. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560 ]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
  6. Website [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Shin JG, Park JY, Kim MJ, Shon JH, Yoon YR, Cha IJ, Lee SS, Oh SW, Kim SW, Flockhart DA: Inhibitory effects of tricyclic antidepressants (TCAs) on human cytochrome P450 enzymes in vitro: mechanism of drug interaction between TCAs and phenytoin. Drug Metab Dispos. 2002 Oct;30(10):1102-7. [PubMed:12228186 ]
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  4. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560 ]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Ghahramani P, Ellis SW, Lennard MS, Ramsay LE, Tucker GT: Cytochromes P450 mediating the N-demethylation of amitriptyline. Br J Clin Pharmacol. 1997 Feb;43(2):137-44. [PubMed:9131945 ]
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  4. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560 ]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Wen B, Ma L, Zhu M: Bioactivation of the tricyclic antidepressant amitriptyline and its metabolite nortriptyline to arene oxide intermediates in human liver microsomes and recombinant P450s. Chem Biol Interact. 2008 May 9;173(1):59-67. doi: 10.1016/j.cbi.2008.02.001. Epub 2008 Feb 14. [PubMed:18359012 ]
  2. Ghahramani P, Ellis SW, Lennard MS, Ramsay LE, Tucker GT: Cytochromes P450 mediating the N-demethylation of amitriptyline. Br J Clin Pharmacol. 1997 Feb;43(2):137-44. [PubMed:9131945 ]
  3. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  4. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  5. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Wen B, Ma L, Zhu M: Bioactivation of the tricyclic antidepressant amitriptyline and its metabolite nortriptyline to arene oxide intermediates in human liver microsomes and recombinant P450s. Chem Biol Interact. 2008 May 9;173(1):59-67. doi: 10.1016/j.cbi.2008.02.001. Epub 2008 Feb 14. [PubMed:18359012 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. [PubMed:11259560 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
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 colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Brinkschulte M, Breyer-Pfaff U: The contribution of alpha 1-acid glycoprotein, lipoproteins, and albumin to the plasma binding of perazine, amitriptyline, and nortriptyline in healthy man. Naunyn Schmiedebergs Arch Pharmacol. 1980 Oct;314(1):61-6. [PubMed:6108517 ]
  2. Banerjee T, Singh SK, Kishore N: Binding of naproxen and amitriptyline to bovine serum albumin: biophysical aspects. J Phys Chem B. 2006 Nov 30;110(47):24147-56. [PubMed:17125386 ]
Kind
Protein
Organism
Human
Pharmacological action
no
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da
References
  1. Brinkschulte M, Breyer-Pfaff U: The contribution of alpha 1-acid glycoprotein, lipoproteins, and albumin to the plasma binding of perazine, amitriptyline, and nortriptyline in healthy man. Naunyn Schmiedebergs Arch Pharmacol. 1980 Oct;314(1):61-6. [PubMed:6108517 ]
  2. Ferry DG, Caplan NB, Cubeddu LX: Interaction between antidepressants and alpha 1-adrenergic receptor antagonists on the binding to alpha 1-acid glycoprotein. J Pharm Sci. 1986 Feb;75(2):146-9. [PubMed:2870173 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [PubMed:12438524 ]
  2. Faassen F, Vogel G, Spanings H, Vromans H: Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22. [PubMed:12954186 ]
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:09