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Identification
NameSertraline
Accession NumberDB01104  (APRD00175)
TypeSmall Molecule
GroupsApproved
Description

Sertraline hydrochloride belongs to a class of antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs). Despite distinct structural differences between compounds in this class, SSRIs possess similar pharmacological activity. As with other antidepressant agents, several weeks of therapy may be required before a clinical effect is seen. SSRIs are potent inhibitors of neuronal serotonin reuptake. They have little to no effect on norepinephrine or dopamine reuptake and do not antagonize α- or β-adrenergic, dopamine D2 or histamine H1 receptors. During acute use, SSRIs block serotonin reuptake and increase serotonin stimulation of somatodendritic 5-HT1A and terminal autoreceptors. Chronic use leads to desensitization of somatodendritic 5-HT1A and terminal autoreceptors. The overall clinical effect of increased mood and decreased anxiety is thought to be due to adaptive changes in neuronal function that leads to enhanced serotonergic neurotransmission. Side effects include dry mouth, nausea, dizziness, drowsiness, sexual dysfunction and headache (see Toxicity section below for a more detailed listing of side effects). Compared to other agents in this class, sertraline may cause greater diarrheal and male sexual dysfunction effects. Side effects generally occur within the first two weeks of therapy and are usually less severe and frequent than those observed with tricyclic antidepressants. Sertraline may be used to treat major depressive disorder, obsessive-compulsive disorder (OCD), panic disorder, post-traumatic stress disorder (PTSD), premenstrual dysphoric disorder (PMDD) and social anxiety disorder (social phobia).

Structure
Thumb
Synonyms
(+)-Sertraline
(1S-cis)-1,2,3,4-Tetrahydro-4-(3,4-dichlorophenyl)-N-methyl-1-naphthalenamine
(1S,4S)-Sertraline
cis-(+)-Sertraline
CP 51974
Sertralina
Sertraline
Sertralinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Sertralinecapsule100 mgoralActavis Pharma Company2006-11-08Not applicableCanada
Act Sertralinecapsule50 mgoralActavis Pharma Company2006-11-08Not applicableCanada
Act Sertralinecapsule25 mgoralActavis Pharma Company2006-11-08Not applicableCanada
Auro-sertralinecapsule25 mgoralAuro Pharma Inc2012-10-18Not applicableCanada
Auro-sertralinecapsule100 mgoralAuro Pharma Inc2012-10-18Not applicableCanada
Auro-sertralinecapsule50 mgoralAuro Pharma Inc2012-10-18Not applicableCanada
Bio-sertralinecapsule100 mgoralBiomed PharmaNot applicableNot applicableCanada
Bio-sertralinecapsule50 mgoralBiomed PharmaNot applicableNot applicableCanada
Bio-sertralinecapsule25 mgoralBiomed PharmaNot applicableNot applicableCanada
Dom-sertralinecapsule100 mgoralDominion Pharmacal2002-05-31Not applicableCanada
Dom-sertralinecapsule50 mgoralDominion Pharmacal2002-05-31Not applicableCanada
Dom-sertralinecapsule25 mgoralDominion Pharmacal2002-05-31Not applicableCanada
Gd-sertralinecapsule100 mgoralGenmed A Division Of Pfizer Canada Inc2010-11-11Not applicableCanada
Gd-sertralinecapsule50 mgoralGenmed A Division Of Pfizer Canada Inc2010-11-11Not applicableCanada
Gd-sertralinecapsule25 mgoralGenmed A Division Of Pfizer Canada Inc2010-11-11Not applicableCanada
Ipg-sertralinecapsule100 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Ipg-sertralinecapsule50 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Ipg-sertralinecapsule25 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Jamp-sertralinecapsule25 mgoralJamp Pharma Corporation2011-10-06Not applicableCanada
Jamp-sertralinecapsule50 mgoralJamp Pharma Corporation2011-10-06Not applicableCanada
Jamp-sertralinecapsule100 mgoralJamp Pharma Corporation2011-10-06Not applicableCanada
Mar-sertralinecapsule100 mgoralMarcan Pharmaceuticals Inc2014-01-16Not applicableCanada
Mar-sertralinecapsule50 mgoralMarcan Pharmaceuticals Inc2014-01-06Not applicableCanada
Mar-sertralinecapsule25 mgoralMarcan Pharmaceuticals Inc2014-01-16Not applicableCanada
Mint-sertralinecapsule100 mgoralMint Pharmaceuticals Inc2013-04-29Not applicableCanada
Mint-sertralinecapsule50 mgoralMint Pharmaceuticals Inc2013-04-29Not applicableCanada
Mint-sertralinecapsule25 mgoralMint Pharmaceuticals Inc2013-04-29Not applicableCanada
Mylan-sertralinecapsule100 mgoralMylan Pharmaceuticals Ulc2000-07-24Not applicableCanada
Mylan-sertralinecapsule50 mgoralMylan Pharmaceuticals Ulc2000-07-24Not applicableCanada
Mylan-sertralinecapsule25 mgoralMylan Pharmaceuticals Ulc2000-07-24Not applicableCanada
Nu-sertraline Capsulescapsule100 mgoralNu Pharm Inc2003-06-272012-09-04Canada
Nu-sertraline Capsulescapsule50 mgoralNu Pharm Inc2003-06-272012-09-04Canada
Nu-sertraline Capsulescapsule25 mgoralNu Pharm Inc2003-06-272012-09-04Canada
PHL-sertralinecapsule100 mgoralPharmel Inc2002-05-31Not applicableCanada
PHL-sertralinecapsule50 mgoralPharmel Inc2002-05-31Not applicableCanada
PHL-sertralinecapsule25 mgoralPharmel Inc2002-05-31Not applicableCanada
PMS-sertralinecapsule100 mgoralPharmascience Inc2002-01-30Not applicableCanada
PMS-sertralinecapsule50 mgoralPharmascience Inc2002-01-30Not applicableCanada
PMS-sertralinecapsule25 mgoralPharmascience Inc2002-01-30Not applicableCanada
Priva-sertralinecapsule50 mgoralPharmapar IncNot applicableNot applicableCanada
Priva-sertralinecapsule25 mgoralPharmapar IncNot applicableNot applicableCanada
Priva-sertralinecapsule100 mgoralPharmapar IncNot applicableNot applicableCanada
Q-sertralinecapsule100 mgoralQd Pharmaceuticals Ulc2012-02-032015-08-21Canada
Q-sertralinecapsule50 mgoralQd Pharmaceuticals Ulc2012-02-032015-08-21Canada
Q-sertralinecapsule25 mgoralQd Pharmaceuticals Ulc2012-02-032015-08-21Canada
Ran-sertralinecapsule100 mgoralRanbaxy Pharmaceuticals Canada Inc.2011-11-24Not applicableCanada
Ran-sertralinecapsule50 mgoralRanbaxy Pharmaceuticals Canada Inc.2011-11-24Not applicableCanada
Ran-sertralinecapsule25 mgoralRanbaxy Pharmaceuticals Canada Inc.2011-11-24Not applicableCanada
Ratio-sertralinecapsule100 mgoralRatiopharm Inc Division Of Teva Canada Limited2002-07-052014-09-19Canada
Ratio-sertralinecapsule50 mgoralRatiopharm Inc Division Of Teva Canada Limited2002-07-052014-09-24Canada
Ratio-sertralinecapsule25 mgoralRatiopharm Inc Division Of Teva Canada Limited2002-07-052014-09-19Canada
Riva-sertralinecapsule50 mgoralLaboratoire Riva Inc2005-10-01Not applicableCanada
Riva-sertralinecapsule25 mgoralLaboratoire Riva Inc2005-01-10Not applicableCanada
Riva-sertralinecapsule100 mgoralLaboratoire Riva Inc2005-01-10Not applicableCanada
Sandoz Sertralinecapsule50 mgoralSandoz Canada Incorporated2002-02-13Not applicableCanada
Sandoz Sertralinecapsule100 mgoralSandoz Canada Incorporated2002-02-13Not applicableCanada
Sandoz Sertralinecapsule25 mgoralSandoz Canada Incorporated2002-02-13Not applicableCanada
Sertralinecapsule100 mgoralSanis Health Inc2010-08-03Not applicableCanada
Sertralinecapsule100 mgoralSivem Pharmaceuticals Ulc2012-06-10Not applicableCanada
Sertralinecapsule50 mgoralSanis Health Inc2010-08-03Not applicableCanada
Sertralinecapsule50 mgoralSivem Pharmaceuticals Ulc2012-06-10Not applicableCanada
Sertralinecapsule100 mgoralMeliapharm Inc2010-10-122014-06-25Canada
Sertralinecapsule25 mgoralSanis Health Inc2010-08-03Not applicableCanada
Sertralinecapsule25 mgoralSivem Pharmaceuticals Ulc2012-06-10Not applicableCanada
Sertralinecapsule50 mgoralMeliapharm Inc2010-10-122014-06-25Canada
Sertralinecapsule25 mgoralMeliapharm Inc2010-10-122014-06-25Canada
Sertralinecapsule100 mgoralSanis Health Inc2009-10-222010-06-08Canada
Sertralinecapsule100 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Sertralinecapsule50 mgoralSanis Health Inc2009-10-222010-06-08Canada
Sertralinecapsule50 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Sertralinecapsule25 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Sertralinecapsule25 mgoralSanis Health Inc2009-10-222010-06-08Canada
Sertraline Hydrochloridetablet, film coated100 mg/1oralREMEDYREPACK INC.2013-05-13Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralPd Rx Pharmaceuticals, Inc.1992-02-11Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralLife Line Home Care Services1992-02-11Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-12-19Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralPd Rx Pharmaceuticals, Inc.1992-02-11Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-07Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralContract Pharmacy Services Pa2010-03-15Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralCardinal Health1992-02-11Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-07Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralGreenstone LLC1992-02-11Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralCardinal Health1992-02-11Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralKAISER FOUNDATION HOSPITALS2012-01-06Not applicableUs
Sertraline Hydrochloridesolution, concentrate20 mg/mLoralGreenstone LLC1992-02-11Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralPhysicians Total Care, Inc.2006-08-16Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralPd Rx Pharmaceuticals, Inc.1992-02-11Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralGreenstone LLC1992-02-11Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralPhysicians Total Care, Inc.2006-08-24Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralPd Rx Pharmaceuticals, Inc.1992-02-11Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralGreenstone LLC1992-02-11Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralPhysicians Total Care, Inc.2006-09-12Not applicableUs
Sertraline-100capsule100.0 mgoralPro Doc Limitee2001-02-15Not applicableCanada
Sertraline-25capsule25.0 mgoralPro Doc Limitee2001-02-15Not applicableCanada
Sertraline-50capsule50.0 mgoralPro Doc Limitee2001-02-15Not applicableCanada
Teva-sertralinecapsule25 mgoralTeva Canada Limited1999-08-16Not applicableCanada
Teva-sertralinecapsule50 mgoralTeva Canada Limited1999-08-16Not applicableCanada
Teva-sertralinecapsule100 mgoralTeva Canada Limited1999-08-16Not applicableCanada
Van-sertralinecapsule25 mgoralVanc Pharmaceuticals Inc2015-06-10Not applicableCanada
Van-sertralinecapsule100 mgoralVanc Pharmaceuticals Inc2015-06-10Not applicableCanada
Van-sertralinecapsule50 mgoralVanc Pharmaceuticals Inc2015-06-10Not applicableCanada
Zolofttablet, film coated50 mg/1oralRoerig1992-02-11Not applicableUs
Zolofttablet, film coated50 mg/1oralPd Rx Pharmaceuticals, Inc.1992-02-11Not applicableUs
Zolofttablet, film coated50 mg/1oralAphena Pharma Solutions Tennessee, Llc1992-02-11Not applicableUs
Zolofttablet, film coated100 mg/1oralREMEDYREPACK INC.2013-02-25Not applicableUs
Zolofttablet, film coated100 mg/1oralAphena Pharma Solutions Tennessee, Llc1992-02-11Not applicableUs
Zolofttablet, film coated50 mg/1oralCardinal Health1992-02-11Not applicableUs
Zolofttablet, film coated100 mg/1oralSTAT Rx USA LLC1992-02-11Not applicableUs
Zolofttablet, film coated50 mg/1oralSTAT Rx USA LLC1992-02-11Not applicableUs
Zolofttablet, film coated100 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-04-03Not applicableUs
Zolofttablet, film coated50 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-04-03Not applicableUs
Zolofttablet, film coated25 mg/1oralRoerig1992-02-11Not applicableUs
Zoloftsolution, concentrate20 mg/mLoralRoerig1992-02-11Not applicableUs
Zoloftcapsule25 mgoralPfizer Canada Inc1995-12-31Not applicableCanada
Zolofttablet, film coated100 mg/1oralRoerig1992-02-11Not applicableUs
Zoloft Cap 100mgcapsule100 mgoralPfizer Canada Inc1992-12-31Not applicableCanada
Zoloft Cap 50mgcapsule50 mgoralPfizer Canada Inc1992-12-31Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-sertralinecapsule100 mgoralApotex Inc1999-09-01Not applicableCanada
Apo-sertralinecapsule50 mgoralApotex Inc1999-09-01Not applicableCanada
Apo-sertralinecapsule25 mgoralApotex Inc1999-09-01Not applicableCanada
Sertralinetablet, film coated50 mg/1oralReady Meds2012-11-06Not applicableUs
Sertralinetablet, film coated50 mg/1oralExelan Pharmaceuticals, Inc.2012-08-20Not applicableUs
Sertralinetablet, film coated50 mg/1oralClinical Solutions Wholesale2007-02-06Not applicableUs
Sertralinetablet50 mg/1oralInternational Labs, Inc.2012-02-20Not applicableUs
Sertralinetablet, film coated100 mg/1oralClinical Solutions Wholesale2007-02-06Not applicableUs
Sertralinetablet, film coated100 mg/1oralLupin Pharmaceuticals, Inc.2007-02-06Not applicableUs
Sertralinetablet, film coated25 mg/1oralExelan Pharmaceuticals, Inc.2012-08-20Not applicableUs
Sertralinetablet, film coated25 mg/1oralClinical Solutions Wholesale2007-02-06Not applicableUs
Sertralinetablet, film coated25 mg/1oralProficient Rx LP2007-02-06Not applicableUs
Sertralinetablet, film coated100 mg/1oralAidarex Pharmaceuticals LLC2007-02-06Not applicableUs
Sertralinetablet, film coated50 mg/1oralLupin Pharmaceuticals, Inc.2007-02-06Not applicableUs
Sertralinetablet, film coated100 mg/1oralProficient Rx LP2007-02-06Not applicableUs
Sertralinetablet, film coated25 mg/1oralLupin Pharmaceuticals, Inc.2007-02-06Not applicableUs
Sertralinetablet, film coated50 mg/1oralAphena Pharma Solutions Tennessee, Llc2012-08-20Not applicableUs
Sertralinetablet, film coated50 mg/1oralProficient Rx LP2007-02-06Not applicableUs
Sertralinetablet, film coated25 mg/1oralWest ward Pharmaceutical Corp2012-11-06Not applicableUs
Sertralinetablet, film coated25 mg/1oralAphena Pharma Solutions Tennessee, Llc2012-08-20Not applicableUs
Sertralinetablet50 mg/1oralDIRECT RX2014-01-01Not applicableUs
Sertralinetablet, film coated50 mg/1oralWest ward Pharmaceutical Corp2012-11-06Not applicableUs
Sertralinetablet, film coated100 mg/1oralAphena Pharma Solutions Tennessee, Llc2012-08-20Not applicableUs
Sertralinetablet, film coated100 mg/1oralNorthwind Pharmaceuticals2014-05-27Not applicableUs
Sertralinetablet100 mg/1oralDIRECT RX2014-01-01Not applicableUs
Sertralinetablet100 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2007-12-18Not applicableUs
Sertralinetablet, film coated100 mg/1oralWest ward Pharmaceutical Corp2012-11-06Not applicableUs
Sertralinetablet, film coated25 mg/1oralTYA Pharmaceuticals2007-02-06Not applicableUs
Sertralinetablet, film coated100 mg/1oralREMEDYREPACK INC.2015-12-24Not applicableUs
Sertralinetablet50 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2007-12-18Not applicableUs
Sertralinetablet, film coated50 mg/1oralNorthwind Pharmaceuticals, LLC2014-07-11Not applicableUs
Sertralinetablet25 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2007-12-18Not applicableUs
Sertralinetablet, film coated100 mg/1oralExelan Pharmaceuticals, Inc.2012-08-20Not applicableUs
Sertralinetablet, film coated100 mg/1oralREMEDYREPACK INC.2015-04-14Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralNorth Star Rx Llc2007-02-06Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralCobalt Laboratories Inc.2007-02-06Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralMajor Pharmaceuticals2013-05-15Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralMajor Pharmaceuticals2013-05-15Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralMylan Pharmaceuticals Inc.2013-05-18Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralWest ward Pharmaceutical Corp2009-08-10Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralMed Vantx, Inc.2007-02-06Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2007-12-18Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralPreferred Pharmaceuticals, Inc.2012-02-27Not applicableUs
Sertraline Hydrochloridetablet, coated50 mg/1oralRanbaxy Pharmaceuticals Inc.2007-02-06Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralREMEDYREPACK INC.2013-02-15Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralKeltman Pharmaceuticals Inc.2011-09-09Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralAccord Healthcare, Inc.2015-10-01Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralMed Vantx, Inc.2007-02-06Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralMed Health Pharma, LLC2011-07-04Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralPreferred Pharmaceuticals, Inc.2012-02-27Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralREMEDYREPACK INC.2012-03-07Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralState of Florida DOH Central Pharmacy2014-11-01Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralLake Erie Medical DBA Quality Care Products LLC2007-01-02Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralH.J. Harkins Company Inc.2007-12-18Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralMed Health Pharma, LLC2011-07-04Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralCardinal Health2013-07-05Not applicableUs
Sertraline Hydrochloridetablet, coated25 mg/1oralRanbaxy Pharmaceuticals Inc.2007-02-06Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralSt Marys Medical Park Pharmacy2014-02-05Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralNorth Star Rx Llc2007-02-06Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralCobalt Laboratories Inc.2007-02-06Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralMajor Pharmaceuticals2013-05-15Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralMylan Pharmaceuticals Inc.2013-05-29Not applicableUs
Sertraline Hydrochloridesolution, concentrate20 mg/mLoralAurobindo Pharma Limited2008-10-31Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2010-12-01Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2007-12-18Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralPreferred Pharmaceuticals, Inc.2013-03-25Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralREMEDYREPACK INC.2013-03-28Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralMylan Institutional Inc.2012-08-06Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralREMEDYREPACK INC.2011-03-28Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralREMEDYREPACK INC.2014-03-17Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralCardinal Health2013-07-05Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralSt Marys Medical Park Pharmacy2014-02-05Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralMylan Pharmaceuticals Inc.2013-05-29Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralAurobindo Pharma Limited2007-02-06Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralbryant ranch prepack2007-09-05Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralLegacy Pharmaceutical Packaging, Llc2007-10-18Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralREMEDYREPACK INC.2013-02-28Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralREMEDYREPACK INC.2014-02-10Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralMc Kesson Contract Packaging2011-09-27Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralMylan Institutional Inc.2012-08-06Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralMedsource Pharmaceuticals2007-10-18Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralREMEDYREPACK INC.2014-02-26Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralClinical Solutions Wholesale2007-10-18Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralCardinal Health2007-12-182016-03-11Us
Sertraline Hydrochloridetablet, film coated100 mg/1oralApotex Corp2007-02-06Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralNorth Star Rx Llc2007-02-06Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralTorrent Pharmaceuticals Limited2007-09-05Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralAurobindo Pharma Limited2007-02-06Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralbryant ranch prepack2007-12-18Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralAidarex Pharmaceuticals LLC2007-10-18Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralLegacy Pharmaceutical Packaging, Llc2007-10-18Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralRebel Distributors Corp2009-07-01Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralCardinal Health2010-12-15Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralMc Kesson Contract Packaging2011-09-27Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralMylan Institutional Inc.2012-08-06Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralREMEDYREPACK INC.2013-05-06Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralClinical Solutions Wholesale2007-10-18Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralCardinal Health2007-12-182016-03-11Us
Sertraline Hydrochloridetablet, film coated50 mg/1oralApotex Corp2007-02-06Not applicableUs
Sertraline Hydrochloridesolution20 mg/mLoralNorth Star Rx Llc2008-10-31Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralTorrent Pharmaceuticals Limited2007-09-05Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralAidarex Pharmaceuticals LLC2007-10-18Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralLegacy Pharmaceutical Packaging, Llc2007-10-18Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralRebel Distributors Corp2009-07-01Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralAmerican Health Packaging2010-12-15Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralMc Kesson Contract Packaging2011-09-27Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralUnit Dose Services2007-12-18Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralREMEDYREPACK INC.2013-03-27Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralClinical Solutions Wholesale, Llc2007-10-18Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralCardinal Health2007-12-182016-03-11Us
Sertraline Hydrochloridetablet, film coated25 mg/1oralApotex Corp2007-02-06Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralSTAT Rx USA LLC2007-12-18Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralTorrent Pharmaceuticals Limited2007-09-05Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralAurobindo Pharma Limited2007-02-06Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralbryant ranch prepack2007-12-18Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralUnit Dose Services2007-12-18Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralCardinal Health2007-02-01Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralInternational Labs, Inc.2009-05-07Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralHikma Pharmaceutical2009-08-10Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralSTAT Rx USA LLC2007-12-18Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralAurolife Pharma LLC2011-03-15Not applicableUs
Sertraline Hydrochloridetablet, coated200 mg/1oralRanbaxy Pharmaceuticals Inc.2007-02-06Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralCamber Pharmaceuticals Inc.2007-10-18Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralLegacy Pharmaceutical Packaging, Llc2007-10-18Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralRebel Distributors Corp2009-07-01Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralAmerican Health Packaging2011-04-06Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralCipla Limited2007-02-06Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralCardinal Health2007-02-01Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralInternational Labs, Inc.2009-05-10Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralHikma Pharmaceutical2009-08-10Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralSTAT Rx USA LLC2007-12-18Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralAurolife Pharma LLC2011-03-15Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralWest ward Pharmaceutical Corp2009-08-10Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralTYA Pharmaceuticals2007-10-18Not applicableUs
Sertraline Hydrochloridetablet, coated150 mg/1oralRanbaxy Pharmaceuticals Inc.2007-02-06Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralCamber Pharmaceuticals Inc.2007-10-18Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralLegacy Pharmaceutical Packaging, Llc2007-10-18Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralAccord Healthcare, Inc.2015-10-01Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralAmerican Health Packaging2010-12-16Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralCipla Limited2007-02-06Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralUnit Dose Services2007-12-18Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralAphena Pharma Solutions Tennessee, Inc.2012-02-03Not applicableUs
Sertraline Hydrochloridetablet100 mg/1oralH.J. Harkins Company Inc.2007-12-18Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralCobalt Laboratories Inc.2007-02-06Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralAurolife Pharma LLC2011-03-15Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralWest ward Pharmaceutical Corp2009-08-10Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralTYA Pharmaceuticals2007-10-18Not applicableUs
Sertraline Hydrochloridetablet, coated100 mg/1oralRanbaxy Pharmaceuticals Inc.2007-02-06Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralCamber Pharmaceuticals Inc.2007-10-18Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralLegacy Pharmaceutical Packaging, Llc2007-10-18Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralAccord Healthcare, Inc.2015-10-01Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralMed Vantx, Inc.2007-02-06Not applicableUs
Sertraline Hydrochloridetablet25 mg/1oralCipla Limited2007-02-06Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralREMEDYREPACK INC.2012-03-14Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralPd Rx Pharmaceuticals, Inc.2009-08-10Not applicableUs
Sertraline Hydrochloridetablet50 mg/1oralH.J. Harkins Company Inc.2007-12-18Not applicableUs
Sertraline Hydrochloridetablet, film coated100 mg/1oralMed Health Pharma, LLC2011-07-04Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralCardinal Health2007-02-01Not applicableUs
Sertraline Hydrochloridetablet, film coated50 mg/1oralInternational Labs, Inc.2009-05-12Not applicableUs
Sertraline Hydrochloridetablet, film coated25 mg/1oralHikma Pharmaceutical2009-08-10Not applicableUs
Sertraline Hydrochloride Tabletstablet, film coated100 mg/1oralMajor Pharmaceuticals2009-11-10Not applicableUs
Sertraline Hydrochloride Tabletstablet, film coated50 mg/1oralMajor Pharmaceuticals2009-11-10Not applicableUs
Sertraline Hydrochloride Tabletstablet, film coated25 mg/1oralMajor Pharmaceuticals2009-11-10Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
LustralNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Sertraline Hydrochloride
Thumb
  • InChI Key: BLFQGGGGFNSJKA-XHXSRVRCSA-N
  • Monoisotopic Mass: 341.050482702
  • Average Mass: 342.691
DBSALT000808
Categories
UNIIQUC7NX6WMB
CAS number79617-96-2
WeightAverage: 306.23
Monoisotopic: 305.073804963
Chemical FormulaC17H17Cl2N
InChI KeyInChIKey=VGKDLMBJGBXTGI-SJCJKPOMSA-N
InChI
InChI=1S/C17H17Cl2N/c1-20-17-9-7-12(13-4-2-3-5-14(13)17)11-6-8-15(18)16(19)10-11/h2-6,8,10,12,17,20H,7,9H2,1H3/t12-,17-/m0/s1
IUPAC Name
(1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalen-1-amine
SMILES
CN[[email protected]]1CC[C@@H](C2=CC(Cl)=C(Cl)C=C2)C2=CC=CC=C12
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as tametralines. These are compounds containing a tametraline moiety, which consists of a tetrahydronaphthalene linked to a phenyl group to form N-methyl-4-phenyl-1,2,3,4-tetrahydronaphthalen-1-amine skeleton.
KingdomOrganic compounds
Super ClassBenzenoids
ClassTetralins
Sub ClassTametralines
Direct ParentTametralines
Alternative Parents
Substituents
  • Tametraline
  • 1,2-dichlorobenzene
  • Aralkylamine
  • Halobenzene
  • Chlorobenzene
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Secondary amine
  • Secondary aliphatic amine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic homopolycyclic compound
Molecular FrameworkAromatic homopolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the management of major depressive disorder, posttraumatic stress disorder, obsessive-compulsive disorder, panic disorder with or without agoraphobia, premenstrual dysphoric disorder, social phobia, premature ejaculation, and vascular headaches.
PharmacodynamicsSertraline, an antidepressant drug similar to citalopram, fluoxetine, and paroxetine, is of the selective serotonin reuptake inhibitor (SSRI) type. Sertraline has one active metabolite and, like the other SSRIs, have less sedative, anticholinergic, and cardiovascular effects than the tricyclic antidepressant drugs because it does not have clinically important anticholinergic, antihistamine, or adrenergic blocking activity.
Mechanism of actionThe exact mechanism of action sertraline is not fully known, but the drug appears to selectively inhibit the reuptake of serotonin at the presynaptic membrane. This results in an increased synaptic concentration of serotonin in the CNS, which leads to numerous functional changes associated with enhanced serotonergic neurotransmission. It is suggested that these modifications are responsible for the antidepressant action observed during long term administration of antidepressants. It has also been hypothesized that obsessive-compulsive disorder is caused by the dysregulation of serotonin, as it is treated by sertraline, and the drug corrects this imbalance.
Related Articles
AbsorptionThe effects of food on the bioavailability of the sertraline tablet and oral concentrate were studied in subjects administered a single dose with and without food. For the tablet, AUC was slightly increased when drug was administered with food but the Cmax was 25% greater, while the time to reach peak plasma concentration (Tmax) decreased from 8 hours post-dosing to 5.5 hours. For the oral concentrate, Tmax was slightly prolonged from 5.9 hours to 7.0 hours with food.
Volume of distributionNot Available
Protein binding98% bound to serum proteins, principally to albumin and α1-acid glycoprotein
Metabolism

Extensively metabolized in the liver. Sertraline metabolism involves N-demethylation, N-hydroxylation, oxidative deamination, and glucuronidation of sertraline carbamic acid. Sertraline undergoes N-demethylation primarily catalyzed by cytochrome P450 (CYP) 2B6, with CYP2C19, CYP3A4 and CYP2D6 contributing to a lesser extent. Deamination occurs via CYP3A4 and CYP2C19. In vitro studies have shown that monoamine oxidase A and B may also catalyze sertraline deamination. Sertraline N-carbamoyl glucuronidation has also been observed in human liver microsomes.

SubstrateEnzymesProduct
Sertraline
norsertralineDetails
Route of eliminationSertraline is extensively metabolized and excretion of unchanged drug in urine is a minor route of elimination.
Half lifeThe elimination half-life of sertraline is approximately 25-26 hours. The elimination half-life of desmethylsertraline is approximately 62-104 hours.
ClearanceNot Available
ToxicitySymptoms of toxicity include alopecia, decreased libido, diarrhea, ejaculation disorder, fatigue, insomnia, somnolence and serotonin syndrome. The most frequently observed side effects include: GI effects such as nausea, diarrhea or loose stools, dyspepsia, and dry mouth; nervous system effects such as somnolence, dizziness, insomnia, and tremor; sexual dysfunction in males (principally ejaculatory delay); and sweating.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9713
Caco-2 permeable+0.6995
P-glycoprotein substrateNon-substrate0.5858
P-glycoprotein inhibitor IInhibitor0.7333
P-glycoprotein inhibitor IINon-inhibitor0.8319
Renal organic cation transporterNon-inhibitor0.6726
CYP450 2C9 substrateNon-substrate0.71
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.6304
CYP450 1A2 substrateInhibitor0.7909
CYP450 2C9 inhibitorNon-inhibitor0.9307
CYP450 2D6 inhibitorNon-inhibitor0.6469
CYP450 2C19 inhibitorInhibitor0.6839
CYP450 3A4 inhibitorNon-inhibitor0.5442
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6633
Ames testAMES toxic0.5353
CarcinogenicityNon-carcinogens0.8499
BiodegradationNot ready biodegradable0.9522
Rat acute toxicity2.5020 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9151
hERG inhibition (predictor II)Inhibitor0.7185
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral100 mg/1
Tabletoral25 mg/1
Tabletoral50 mg/1
Solutionoral20 mg/mL
Tablet, coatedoral100 mg/1
Tablet, coatedoral150 mg/1
Tablet, coatedoral200 mg/1
Tablet, coatedoral25 mg/1
Tablet, coatedoral50 mg/1
Capsuleoral100.0 mg
Capsuleoral25.0 mg
Capsuleoral50.0 mg
Capsuleoral25 mg
Solution, concentrateoral20 mg/mL
Tablet, film coatedoral100 mg/1
Tablet, film coatedoral25 mg/1
Tablet, film coatedoral50 mg/1
Capsuleoral100 mg
Capsuleoral50 mg
Prices
Unit descriptionCostUnit
Sertraline hcl powder480.0USD g
Zoloft 20 mg/ml Concentrate 60ml Bottle94.75USD bottle
Sertraline HCl 20 mg/ml Concentrate 60ml Bottle66.85USD bottle
Zoloft 50 mg tablet4.02USD tablet
Zoloft 100 mg tablet3.94USD tablet
Zoloft 25 mg tablet3.94USD tablet
Sertraline hcl 100 mg tablet2.77USD tablet
Sertraline hcl 25 mg tablet2.77USD tablet
Sertraline hcl 50 mg tablet2.77USD tablet
Zoloft 100 mg Capsule1.9USD capsule
Zoloft 50 mg Capsule1.81USD capsule
Apo-Sertraline 100 mg Capsule1.06USD capsule
Co Sertraline 100 mg Capsule1.06USD capsule
Mylan-Sertraline 100 mg Capsule1.06USD capsule
Novo-Sertraline 100 mg Capsule1.06USD capsule
Phl-Sertraline 100 mg Capsule1.06USD capsule
Pms-Sertraline 100 mg Capsule1.06USD capsule
Ratio-Sertraline 100 mg Capsule1.06USD capsule
Sandoz Sertraline 100 mg Capsule1.06USD capsule
Sertraline 100 mg Capsule1.06USD capsule
Apo-Sertraline 50 mg Capsule1.01USD capsule
Co Sertraline 50 mg Capsule1.01USD capsule
Mylan-Sertraline 50 mg Capsule1.01USD capsule
Novo-Sertraline 50 mg Capsule1.01USD capsule
Phl-Sertraline 50 mg Capsule1.01USD capsule
Pms-Sertraline 50 mg Capsule1.01USD capsule
Ratio-Sertraline 50 mg Capsule1.01USD capsule
Sandoz Sertraline 50 mg Capsule1.01USD capsule
Sertraline 50 mg Capsule1.01USD capsule
Zoloft 25 mg Capsule0.91USD capsule
Apo-Sertraline 25 mg Capsule0.51USD capsule
Co Sertraline 25 mg Capsule0.51USD capsule
Mylan-Sertraline 25 mg Capsule0.51USD capsule
Novo-Sertraline 25 mg Capsule0.51USD capsule
Phl-Sertraline 25 mg Capsule0.51USD capsule
Pms-Sertraline 25 mg Capsule0.51USD capsule
Ratio-Sertraline 25 mg Capsule0.51USD capsule
Sandoz Sertraline 25 mg Capsule0.51USD capsule
Sertraline 25 mg Capsule0.51USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2029065 No1994-11-082010-10-31Canada
US4962128 No1992-11-022009-11-02Us
US6727283 Yes2000-04-112020-04-11Us
US7067555 Yes2000-04-112020-04-11Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point243-245 °CNot Available
water solubility3.5mg/LNot Available
logP5.1Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000145 mg/mLALOGPS
logP5.06ALOGPS
logP5.15ChemAxon
logS-6.3ALOGPS
pKa (Strongest Basic)9.85ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area12.03 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity85.74 m3·mol-1ChemAxon
Polarizability32.44 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-00b9-2890000000-d53a90b04ec8457ad2f1View in MoNA
References
Synthesis Reference

George J. Quallich, Michael T. Williams, “Process for preparing sertraline intermediates.” U.S. Patent US4839104, issued February, 1977.

US4839104
General References
  1. Couzin J: The brains behind blockbusters. Science. 2005 Jul 29;309(5735):728. [PubMed:16051786 ]
  2. Fabre LF, Abuzzahab FS, Amin M, Claghorn JL, Mendels J, Petrie WM, Dube S, Small JG: Sertraline safety and efficacy in major depression: a double-blind fixed-dose comparison with placebo. Biol Psychiatry. 1995 Nov 1;38(9):592-602. [PubMed:8573661 ]
  3. Kronig MH, Apter J, Asnis G, Bystritsky A, Curtis G, Ferguson J, Landbloom R, Munjack D, Riesenberg R, Robinson D, Roy-Byrne P, Phillips K, Du Pont IJ: Placebo-controlled, multicenter study of sertraline treatment for obsessive-compulsive disorder. J Clin Psychopharmacol. 1999 Apr;19(2):172-6. [PubMed:10211919 ]
  4. Brady K, Pearlstein T, Asnis GM, Baker D, Rothbaum B, Sikes CR, Farfel GM: Efficacy and safety of sertraline treatment of posttraumatic stress disorder: a randomized controlled trial. JAMA. 2000 Apr 12;283(14):1837-44. [PubMed:10770145 ]
  5. Yonkers KA, Halbreich U, Freeman E, Brown C, Endicott J, Frank E, Parry B, Pearlstein T, Severino S, Stout A, Stone A, Harrison W: Symptomatic improvement of premenstrual dysphoric disorder with sertraline treatment. A randomized controlled trial. Sertraline Premenstrual Dysphoric Collaborative Study Group. JAMA. 1997 Sep 24;278(12):983-8. [PubMed:9307345 ]
  6. Shelton RC: The role of sertraline in the management of depression. Clin Ther. 1994 Sep-Oct;16(5):768-82; discussion 767. [PubMed:7859236 ]
  7. Murdoch D, McTavish D: Sertraline. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in depression and obsessive-compulsive disorder. Drugs. 1992 Oct;44(4):604-24. [PubMed:1281075 ]
External Links
ATC CodesN06AB06
AHFS Codes
  • 28:16.04.20
PDB EntriesNot Available
FDA labelDownload (98.7 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabSertraline may increase the anticoagulant activities of Abciximab.
AcenocoumarolSertraline may increase the anticoagulant activities of Acenocoumarol.
AcepromazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Acetophenazine.
Acetylsalicylic acidSertraline may increase the antiplatelet activities of Acetylsalicylic acid.
AlteplaseSertraline may increase the anticoagulant activities of Alteplase.
AmisulprideThe risk or severity of adverse effects can be increased when Sertraline is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Sertraline is combined with Amitriptyline.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Sertraline.
AmoxapineThe risk or severity of adverse effects can be increased when Sertraline is combined with Amoxapine.
AnistreplaseSertraline may increase the anticoagulant activities of Anistreplase.
ApixabanThe risk or severity of adverse effects can be increased when Sertraline is combined with Apixaban.
AripiprazoleThe risk or severity of adverse effects can be increased when Sertraline is combined with Aripiprazole.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Sertraline.
BenzquinamideThe risk or severity of adverse effects can be increased when Sertraline is combined with Benzquinamide.
BortezomibThe metabolism of Bortezomib can be decreased when combined with Sertraline.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Sertraline.
BuspironeBuspirone may increase the serotonergic activities of Sertraline.
CarbamazepineThe metabolism of Carbamazepine can be decreased when combined with Sertraline.
CarphenazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Carphenazine.
ChlormezanoneThe risk or severity of adverse effects can be increased when Sertraline is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Sertraline is combined with Chlorprothixene.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Sertraline.
CimetidineThe metabolism of Sertraline can be decreased when combined with Cimetidine.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Sertraline.
Citric AcidSertraline may increase the anticoagulant activities of Citric Acid.
ClarithromycinThe metabolism of Sertraline can be decreased when combined with Clarithromycin.
ClomipramineThe risk or severity of adverse effects can be increased when Sertraline is combined with Clomipramine.
ClopidogrelThe serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Sertraline resulting in a loss in efficacy.
ClozapineThe risk or severity of adverse effects can be increased when Sertraline is combined with Clozapine.
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Sertraline.
CollagenaseThe risk or severity of adverse effects can be increased when Sertraline is combined with Collagenase.
CyproheptadineThe therapeutic efficacy of Sertraline can be decreased when used in combination with Cyproheptadine.
Dabigatran etexilateSertraline may increase the anticoagulant activities of Dabigatran etexilate.
DalteparinSertraline may increase the anticoagulant activities of Dalteparin.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Sertraline.
DarunavirThe serum concentration of Sertraline can be decreased when it is combined with Darunavir.
DasatinibDasatinib may increase the anticoagulant activities of Sertraline.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Sertraline is combined with Deoxycholic Acid.
DesipramineThe risk or severity of adverse effects can be increased when Sertraline is combined with Desipramine.
DesmopressinThe risk or severity of adverse effects can be increased when Sertraline is combined with Desmopressin.
DextromethorphanSertraline may increase the serotonergic activities of Dextromethorphan.
DicoumarolSertraline may increase the anticoagulant activities of Dicoumarol.
DisulfiramThe risk or severity of adverse effects can be increased when Disulfiram is combined with Sertraline.
DofetilideSertraline may increase the QTc-prolonging activities of Dofetilide.
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Sertraline.
DoxepinThe risk or severity of adverse effects can be increased when Sertraline is combined with Doxepin.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Sertraline.
DroperidolThe risk or severity of adverse effects can be increased when Sertraline is combined with Droperidol.
Edetic AcidSertraline may increase the anticoagulant activities of Edetic Acid.
EfavirenzThe serum concentration of Sertraline can be decreased when it is combined with Efavirenz.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Sertraline.
EnoxaparinSertraline may increase the anticoagulant activities of Enoxaparin.
EthanolThe risk or severity of adverse effects can be increased when Ethanol is combined with Sertraline.
Ethyl biscoumacetateSertraline may increase the anticoagulant activities of Ethyl biscoumacetate.
FencamfamineThe risk or severity of adverse effects can be increased when Sertraline is combined with Fencamfamine.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Sertraline.
FlupentixolThe risk or severity of adverse effects can be increased when Sertraline is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Sertraline is combined with Fluspirilene.
FluvoxamineThe metabolism of Fluvoxamine can be decreased when combined with Sertraline.
Fondaparinux sodiumSertraline may increase the anticoagulant activities of Fondaparinux sodium.
FosphenytoinThe serum concentration of Sertraline can be decreased when it is combined with Fosphenytoin.
GalantamineThe metabolism of Galantamine can be decreased when combined with Sertraline.
GlucosamineGlucosamine may increase the antiplatelet activities of Sertraline.
GoserelinSertraline may increase the QTc-prolonging activities of Goserelin.
GranisetronGranisetron may increase the serotonergic activities of Sertraline.
HaloperidolThe risk or severity of adverse effects can be increased when Sertraline is combined with Haloperidol.
HeparinSertraline may increase the anticoagulant activities of Heparin.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Sertraline is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Sertraline.
IcosapentSertraline may increase the antiplatelet activities of Icosapent.
ImipramineThe risk or severity of adverse effects can be increased when Sertraline is combined with Imipramine.
Insulin HumanSertraline may increase the hypoglycemic activities of Insulin Regular.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Sertraline.
Ioflupane I 123Sertraline may decrease effectiveness of Ioflupane I 123 as a diagnostic agent.
L-TryptophanL-Tryptophan may increase the serotonergic activities of Sertraline.
LeuprolideSertraline may increase the QTc-prolonging activities of Leuprolide.
LimaprostLimaprost may increase the antiplatelet activities of Sertraline.
LinezolidLinezolid may increase the serotonergic activities of Sertraline.
LiothyronineThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Sertraline.
LithiumLithium may increase the serotonergic activities of Sertraline.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Sertraline.
LoxapineThe risk or severity of adverse effects can be increased when Sertraline is combined with Loxapine.
MesoridazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Mesoridazine.
MethadoneThe metabolism of Methadone can be decreased when combined with Sertraline.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Methotrimeprazine.
Methylene blueSertraline may increase the serotonergic activities of Methylene blue.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Sertraline.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Sertraline.
MetyrosineThe risk or severity of adverse effects can be increased when Metyrosine is combined with Sertraline.
MifepristoneMifepristone may increase the QTc-prolonging activities of Sertraline.
MolindoneThe risk or severity of adverse effects can be increased when Sertraline is combined with Molindone.
MorphineMorphine may increase the serotonergic activities of Sertraline.
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Sertraline.
NortriptylineThe risk or severity of adverse effects can be increased when Sertraline is combined with Nortriptyline.
ObinutuzumabThe risk or severity of adverse effects can be increased when Sertraline is combined with Obinutuzumab.
OlanzapineThe risk or severity of adverse effects can be increased when Sertraline is combined with Olanzapine.
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Sertraline.
OndansetronThe risk or severity of adverse effects can be increased when Sertraline is combined with Ondansetron.
PaliperidoneThe risk or severity of adverse effects can be increased when Sertraline is combined with Paliperidone.
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Sertraline.
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Sertraline.
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Sertraline.
PerphenazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Perphenazine.
PhenelzinePhenelzine may increase the serotonergic activities of Sertraline.
PhenindioneSertraline may increase the anticoagulant activities of Phenindione.
PhenprocoumonSertraline may increase the anticoagulant activities of Phenprocoumon.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Sertraline.
PimozideThe risk or severity of adverse effects can be increased when Sertraline is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Piperacetazine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Promazine.
PropafenoneSertraline may increase the QTc-prolonging activities of Propafenone.
ProtriptylineThe risk or severity of adverse effects can be increased when Sertraline is combined with Protriptyline.
QuetiapineThe risk or severity of adverse effects can be increased when Sertraline is combined with Quetiapine.
RemoxiprideThe risk or severity of adverse effects can be increased when Sertraline is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Sertraline is combined with Reserpine.
ReteplaseSertraline may increase the anticoagulant activities of Reteplase.
RidogrelSertraline may increase the anticoagulant activities of Ridogrel.
RisperidoneThe metabolism of Risperidone can be decreased when combined with Sertraline.
RivaroxabanSertraline may increase the anticoagulant activities of Rivaroxaban.
SertindoleThe risk or severity of adverse effects can be increased when Sertraline is combined with Sertindole.
StreptokinaseSertraline may increase the anticoagulant activities of Streptokinase.
SulodexideSertraline may increase the anticoagulant activities of Sulodexide.
SulpirideThe risk or severity of adverse effects can be increased when Sertraline is combined with Sulpiride.
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Sertraline resulting in a loss in efficacy.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Sertraline.
TenecteplaseSertraline may increase the anticoagulant activities of Tenecteplase.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Sertraline.
ThiothixeneThe risk or severity of adverse effects can be increased when Sertraline is combined with Thiothixene.
TipranavirTipranavir may increase the antiplatelet activities of Sertraline.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Sertraline.
TositumomabThe risk or severity of adverse effects can be increased when Sertraline is combined with Tositumomab.
TramadolSertraline may increase the neuroexcitatory activities of Tramadol.
TranylcypromineTranylcypromine may increase the serotonergic activities of Sertraline.
TrazodoneSertraline may increase the serotonergic activities of Trazodone.
TreprostinilSertraline may increase the anticoagulant activities of Treprostinil.
TrichlormethiazideSertraline may increase the activities of Trichlormethiazide.
TrifluoperazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Sertraline is combined with Triflupromazine.
TrimipramineThe risk or severity of adverse effects can be increased when Sertraline is combined with Trimipramine.
UrokinaseSertraline may increase the anticoagulant activities of Urokinase.
Vitamin EVitamin E may increase the antiplatelet activities of Sertraline.
WarfarinSertraline may increase the anticoagulant activities of Warfarin.
ZiprasidoneThe risk or severity of adverse effects can be increased when Sertraline is combined with Ziprasidone.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Sertraline is combined with Zuclopenthixol.
Food Interactions
  • Avoid alcohol.
  • Avoid St.John's Wort.
  • Avoid taking with grapefruit juice.
  • Take with food.

Targets

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. Benmansour S, Cecchi M, Morilak DA, Gerhardt GA, Javors MA, Gould GG, Frazer A: Effects of chronic antidepressant treatments on serotonin transporter function, density, and mRNA level. J Neurosci. 1999 Dec 1;19(23):10494-501. [PubMed:10575045 ]
  2. Benmansour S, Owens WA, Cecchi M, Morilak DA, Frazer A: Serotonin clearance in vivo is altered to a greater extent by antidepressant-induced downregulation of the serotonin transporter than by acute blockade of this transporter. J Neurosci. 2002 Aug 1;22(15):6766-72. [PubMed:12151556 ]
  3. Borkowska A, Pilaczynska E, Araszkiewicz A, Rybakowski J: [The effect of sertraline on cognitive functions in patients with obsessive-compulsive disorder]. Psychiatr Pol. 2002 Nov-Dec;36(6 Suppl):289-95. [PubMed:12647451 ]
  4. Durham LK, Webb SM, Milos PM, Clary CM, Seymour AB: The serotonin transporter polymorphism, 5HTTLPR, is associated with a faster response time to sertraline in an elderly population with major depressive disorder. Psychopharmacology (Berl). 2004 Aug;174(4):525-9. Epub 2003 Sep 4. [PubMed:12955294 ]
  5. Chen F, Larsen MB, Neubauer HA, Sanchez C, Plenge P, Wiborg O: Characterization of an allosteric citalopram-binding site at the serotonin transporter. J Neurochem. 2005 Jan;92(1):21-8. [PubMed:15606893 ]
  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. David DJ, Bourin M, Hascoet M, Colombel MC, Baker GB, Jolliet P: Comparison of antidepressant activity in 4- and 40-week-old male mice in the forced swimming test: involvement of 5-HT1A and 5-HT1B receptors in old mice. Psychopharmacology (Berl). 2001 Feb;153(4):443-9. [PubMed:11243491 ]
  8. Rogoz Z, Skuza G: Mechanism of synergistic action following co-treatment with pramipexole and fluoxetine or sertraline in the forced swimming test in rats. Pharmacol Rep. 2006 Jul-Aug;58(4):493-500. [PubMed:16963794 ]
  9. Muneoka K, Shirayama Y, Takigawa M, Shioda S: Brain region-specific effects of short-term treatment with duloxetine, venlafaxine, milnacipran and sertraline on monoamine metabolism in rats. Neurochem Res. 2009 Mar;34(3):542-55. doi: 10.1007/s11064-008-9818-2. Epub 2008 Aug 27. [PubMed:18751896 ]
  10. Iehle C, Delos S, Filhol O, Martin PM: Baculovirus-directed expression of human prostatic steroid 5 alpha-reductase 1 in an active form. J Steroid Biochem Mol Biol. 1993 Aug;46(2):177-82. [PubMed:8664165 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Monoamine transmembrane transporter activity
Specific Function:
Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A3
Uniprot ID:
Q01959
Molecular Weight:
68494.255 Da
References
  1. 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 ]
  2. Ghanizadeh A: Sertraline-associated hair loss. J Drugs Dermatol. 2008 Jul;7(7):693-4. [PubMed:18664165 ]
  3. Lemke MR: [Antidepressant effects of dopamine agonists. Experimental and clinical findings]. Nervenarzt. 2007 Jan;78(1):31-8. [PubMed:17187269 ]
  4. Nemeroff CB, Owens MJ: Pharmacologic differences among the SSRIs: focus on monoamine transporters and the HPA axis. CNS Spectr. 2004 Jun;9(6 Suppl 4):23-31. [PubMed:15181382 ]
  5. Goodnick PJ, Goldstein BJ: Selective serotonin reuptake inhibitors in affective disorders--I. Basic pharmacology. J Psychopharmacol. 1998;12(3 Suppl B):S5-20. [PubMed:9808077 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Micallef J, Fakra E, Blin O: [Use of antidepressant drugs in schizophrenic patients with depression]. Encephale. 2006 Mar-Apr;32(2 Pt 1):263-9. [PubMed:16910628 ]
  2. Rojdmark S, von Bahr C: [Metabolic interaction between psychopharmaceuticals. Probable cause of exacerbation of hypothyroidism according to a case report]. Lakartidningen. 2002 Jun 20;99(25):2854-6. [PubMed:12143142 ]
  3. DeVane CL, Donovan JL, Liston HL, Markowitz JS, Cheng KT, Risch SC, Willard L: Comparative CYP3A4 inhibitory effects of venlafaxine, fluoxetine, sertraline, and nefazodone in healthy volunteers. J Clin Psychopharmacol. 2004 Feb;24(1):4-10. [PubMed:14709940 ]
  4. Obach RS, Cox LM, Tremaine LM: Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study. Drug Metab Dispos. 2005 Feb;33(2):262-70. Epub 2004 Nov 16. [PubMed:15547048 ]
  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 ]
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. Micallef J, Fakra E, Blin O: [Use of antidepressant drugs in schizophrenic patients with depression]. Encephale. 2006 Mar-Apr;32(2 Pt 1):263-9. [PubMed:16910628 ]
  3. Rojdmark S, von Bahr C: [Metabolic interaction between psychopharmaceuticals. Probable cause of exacerbation of hypothyroidism according to a case report]. Lakartidningen. 2002 Jun 20;99(25):2854-6. [PubMed:12143142 ]
  4. Obach RS, Cox LM, Tremaine LM: Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study. Drug Metab Dispos. 2005 Feb;33(2):262-70. Epub 2004 Nov 16. [PubMed:15547048 ]
  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. Drug Interactions: Cytochrome P450 Drug Interaction Table [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. Micallef J, Fakra E, Blin O: [Use of antidepressant drugs in schizophrenic patients with depression]. Encephale. 2006 Mar-Apr;32(2 Pt 1):263-9. [PubMed:16910628 ]
  2. Rojdmark S, von Bahr C: [Metabolic interaction between psychopharmaceuticals. Probable cause of exacerbation of hypothyroidism according to a case report]. Lakartidningen. 2002 Jun 20;99(25):2854-6. [PubMed:12143142 ]
  3. Obach RS, Cox LM, Tremaine LM: Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study. Drug Metab Dispos. 2005 Feb;33(2):262-70. Epub 2004 Nov 16. [PubMed:15547048 ]
  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 ]
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. 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. Obach RS, Cox LM, Tremaine LM: Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study. Drug Metab Dispos. 2005 Feb;33(2):262-70. Epub 2004 Nov 16. [PubMed:15547048 ]
  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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Obach RS, Cox LM, Tremaine LM: Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study. Drug Metab Dispos. 2005 Feb;33(2):262-70. Epub 2004 Nov 16. [PubMed:15547048 ]
  2. Walsky RL, Astuccio AV, Obach RS: Evaluation of 227 drugs for in vitro inhibition of cytochrome P450 2B6. J Clin Pharmacol. 2006 Dec;46(12):1426-38. [PubMed:17101742 ]
  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 ]
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. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Primary amine oxidase activity
Specific Function:
Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. MAOB preferentially degrades benzylamine and phenylethylamine.
Gene Name:
MAOB
Uniprot ID:
P27338
Molecular Weight:
58762.475 Da
References
  1. Obach RS, Cox LM, Tremaine LM: Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study. Drug Metab Dispos. 2005 Feb;33(2):262-70. Epub 2004 Nov 16. [PubMed:15547048 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Serotonin binding
Specific Function:
Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. MAOA preferentially oxidizes biogenic amines such as 5-hydroxytryptamine (5-HT), norepinephrine and epinephrine.
Gene Name:
MAOA
Uniprot ID:
P21397
Molecular Weight:
59681.27 Da
References
  1. Obach RS, Cox LM, Tremaine LM: Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study. Drug Metab Dispos. 2005 Feb;33(2):262-70. Epub 2004 Nov 16. [PubMed:15547048 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Not Available
Gene Name:
CYP2B
Uniprot ID:
Q14097
Molecular Weight:
43147.81 Da
References
  1. Haduch A, Wojcikowski J, Daniel WA: Effect of selected antidepressant drugs on cytochrome P450 2B (CYP2B) in rat liver. An in vitro and in vivo study. Pharmacol Rep. 2008 Nov-Dec;60(6):957-65. [PubMed:19211989 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Weiss J, Dormann SM, Martin-Facklam M, Kerpen CJ, Ketabi-Kiyanvash N, Haefeli WE: Inhibition of P-glycoprotein by newer antidepressants. J Pharmacol Exp Ther. 2003 Apr;305(1):197-204. [PubMed:12649369 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on June 25, 2016 03:05