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Identification
NameTrazodone
Accession NumberDB00656  (APRD00533)
TypeSmall Molecule
GroupsApproved, Investigational
Description

A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309)

Structure
Thumb
Synonyms
2-(3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl)[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one
Trazodona
Trazodone
Trazodonum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Desyrel Dividose Tab 300mgtablet300 mgoralBristol Labs Division Of Bristol Myers Squibb1989-12-311999-08-09Canada
Desyrel Dividose Tablet 150 mgtablet150 mgoralBristol Myers Squibb Canada1988-12-312010-01-05Canada
Desyrel Tab 100mgtablet100 mgoralBristol Myers Squibb Canada1983-12-312010-09-07Canada
Desyrel Tab 50mgtablet50 mgoralBristol Myers Squibb Canada1983-12-312010-05-14Canada
Dom-trazodone Tablets - 50mgtablet50 mgoralDominion Pharmacal1996-12-31Not applicableCanada
Dom-trazodone Tablets-100mgtablet100 mgoralDominion Pharmacal1996-12-31Not applicableCanada
Mar-trazodonetablet50 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Mar-trazodonetablet100 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Mar-trazodonetablet150 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Mylan-trazodonetablet150 mgoralMylan Pharmaceuticals Ulc1997-11-28Not applicableCanada
Mylan-trazodonetablet100 mgoralMylan Pharmaceuticals Ulc1997-09-05Not applicableCanada
Mylan-trazodonetablet50 mgoralMylan Pharmaceuticals Ulc1997-09-05Not applicableCanada
Ntp-trazodonetablet150 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-trazodonetablet100 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-trazodonetablet50 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Nu-trazodone - Tab 100mgtablet100 mgoralNu Pharm Inc1995-12-312012-09-04Canada
Nu-trazodone - Tab 50mgtablet50 mgoralNu Pharm Inc1995-12-312012-09-04Canada
Nu-trazodone-D - Tab 150mgtablet150 mgoralNu Pharm Inc1995-12-312012-09-04Canada
Oleptrotablet, extended release150 mg/1oralAngelini Pharma Inc.2010-02-022016-03-29Us
Oleptrotablet (extended-release)300 mgoralAngelini Pharma Inc2011-03-09Not applicableCanada
Oleptrotablet (extended-release)150 mgoralAngelini Pharma Inc2011-03-09Not applicableCanada
Oleptrotablet, extended release300 mg/1oralAngelini Pharma Inc.2010-02-022016-03-29Us
Penta-trazodone Tabletstablet150 mgoralPentapharm Ltd.Not applicableNot applicableCanada
Penta-trazodone Tabletstablet100 mgoralPentapharm Ltd.Not applicableNot applicableCanada
Penta-trazodone Tabletstablet50 mgoralPentapharm Ltd.Not applicableNot applicableCanada
PHL-trazodonetablet100 mgoralPharmel Inc1998-02-17Not applicableCanada
PHL-trazodonetablet50 mgoralPharmel Inc1998-02-17Not applicableCanada
PMS Trazodone HCl Tab 100mgtablet100 mgoralPharmascience Inc1993-12-31Not applicableCanada
PMS Trazodone HCl Tab 50mgtablet50 mgoralPharmascience Inc1993-12-31Not applicableCanada
PMS-trazodonetablet68.25 mgoralPharmascience Inc1998-02-17Not applicableCanada
Ratio-trazodonetablet150 mgoralTeva Canada Limited2006-03-10Not applicableCanada
Ratio-trazodonetablet100 mgoralTeva Canada Limited2006-03-10Not applicableCanada
Ratio-trazodonetablet50 mgoralTeva Canada Limited2006-03-10Not applicableCanada
Ratio-trazodone Tab 150mgtablet150 mgoralRatiopharm Inc Division Of Teva Canada Limited1994-12-312009-01-22Canada
Ratio-trazodone Tablets 100mgtablet100 mgoralRatiopharm Inc Division Of Teva Canada Limited1994-12-312009-01-22Canada
Ratio-trazodone Tablets 50mgtablet50 mgoralRatiopharm Inc Division Of Teva Canada Limited1994-12-312009-01-22Canada
Scheinpharm Trazodonetablet50 mgoralSchein Pharmaceutical Canada Inc.2000-09-132004-07-26Canada
Scheinpharm Trazodonetablet100 mgoralSchein Pharmaceutical Canada Inc.2000-09-132004-07-26Canada
Teva-trazodonetablet50 mgoralTeva Canada Limited1995-12-31Not applicableCanada
Teva-trazodonetablet100 mgoralTeva Canada Limited1995-12-31Not applicableCanada
Teva-trazodonetablet150 mgoralTeva Canada Limited1995-12-31Not applicableCanada
Trazodonetablet150 mgoralSanis Health Inc2010-04-30Not applicableCanada
Trazodonetablet100 mgoralSanis Health Inc2010-04-30Not applicableCanada
Trazodonetablet50 mgoralSanis Health Inc2010-04-30Not applicableCanada
Trazodone - 100 - Tab 100mgtablet100 mgoralPro Doc Limitee1996-12-31Not applicableCanada
Trazodone-150 D - Tab 150mgtablet150 mgoralPro Doc Limitee1996-12-31Not applicableCanada
Trazodone-50 - Tab 50mgtablet50 mgoralPro Doc Limitee1996-12-31Not applicableCanada
Trazoreltablet150 mgoralValeant Canada Lp Valeant Canada S.E.C.1997-02-042014-07-30Canada
Trazoreltablet100 mgoralValeant Canada Lp Valeant Canada S.E.C.1997-03-072014-07-30Canada
Trazoreltablet50 mgoralValeant Canada Lp Valeant Canada S.E.C.1997-02-042014-07-30Canada
Zym-trazodonetablet100 mgoralZymcan Pharmaceuticals Inc2009-06-232014-06-16Canada
Zym-trazodonetablet50 mgoralZymcan Pharmaceuticals Inc2009-06-232014-06-16Canada
Zym-trazodonetablet68.25 mgoralZymcan Pharmaceuticals Inc2004-04-062014-06-16Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-trazodone D Tablets 150mgtablet150 mgoralApotex Inc1995-12-31Not applicableCanada
Apo-trazodone Tablets 100mgtablet100 mgoralApotex Inc1995-12-31Not applicableCanada
Apo-trazodone Tablets 50mgtablet50 mgoralApotex Inc1995-12-31Not applicableCanada
Trazodonetablet100 mg/1oralPd Rx Pharmaceuticals, Inc.2010-01-01Not applicableUs
Trazodonetablet50 mg/1oralNorthwind Pharmaceuticals, LLC2014-12-01Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralSTAT RX LLC USA1987-12-11Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralPhysicians Total Care, Inc.1996-04-09Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralUnit Dose Services2011-01-20Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralClinical Solutions Wholesale1990-09-30Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralREMEDYREPACK INC.2010-09-28Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralCardinal Health1990-09-30Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralbryant ranch prepack1990-09-30Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralPhysicians Total Care, Inc.1997-05-08Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralApotex Corp2014-12-31Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralClinical Solutions Wholesale1990-09-30Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralPreferred Pharmaceuticals, Inc2012-02-28Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralContract Pharmacy Services Pa2010-08-11Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralSTAT RX LLC USA1987-12-11Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralbryant ranch prepack2011-01-20Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralCarilion Materials Management1990-09-30Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralBlenheim Pharmacal, Inc.2012-01-18Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralPreferred Pharmaceuticals, Inc2012-02-28Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralKAISER FOUNDATION HOSPITALS1987-12-22Not applicableUs
Trazodone Hydrochloridetablet, film coated100 mg/1oralAphena Pharma Solutions Tennessee, Llc2010-05-30Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralAidarex Pharmaceuticals LLC1990-09-30Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralCardinal Health1990-09-30Not applicableUs
Trazodone Hydrochloridetablet, film coated50 mg/1oralbryant ranch prepack2010-05-30Not applicableUs
Trazodone Hydrochloridetablet300 mg/1oralApotex Corp2009-01-05Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralLegacy Pharmaceutical Packaging2008-11-17Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralContract Pharmacy Services Pa2010-03-09Not applicableUs
Trazodone Hydrochloridetablet300 mg/1oralTorrent Pharmaceuticals Limited2013-11-27Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralMajor Pharmaceuticals2004-02-03Not applicableUs
Trazodone Hydrochloridetablet, film coated50 mg/1oralAphena Pharma Solutions Tennessee, Llc2010-05-30Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralAidarex Pharmaceuticals LLC1990-09-30Not applicableUs
Trazodone Hydrochloridetablet, film coated100 mg/1oralA S Medication Solutions Llc2010-05-30Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralPliva Inc.1990-09-30Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralClinical Solutions Wholesale1990-09-30Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralLegacy Pharmaceutical Packaging2008-11-17Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralContract Pharmacy Services Pa2010-03-09Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralTorrent Pharmaceuticals Limited2013-11-27Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralMajor Pharmaceuticals2004-02-03Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralSTAT Rx USA LLC2008-11-17Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralREMEDYREPACK INC.2013-03-27Not applicableUs
Trazodone Hydrochloridetablet, film coated50 mg/1oralA S Medication Solutions Llc2010-05-30Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralPliva Inc.1990-09-30Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralCardinal Health2011-01-202016-03-11Us
Trazodone Hydrochloridetablet100 mg/1oralProficient Rx LP1990-09-30Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralApotex Corp2008-11-17Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralKeltman Pharmaceuticals Inc.2010-11-17Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralContract Pharmacy Services Pa2010-08-11Not applicableUs
Trazodone Hydrochloridetablet, film coated50 mg/1oralProficient Rx LP2010-05-30Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralTorrent Pharmaceuticals Limited2013-11-27Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2011-01-20Not applicableUs
Trazodone Hydrochloridetablet300 mg/1oralAv Kare, Inc.2014-02-06Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralREMEDYREPACK INC.2013-03-27Not applicableUs
Trazodone Hydrochloridetablet, film coated150 mg/1oralMutual Pharmaceutical Company, Inc.1993-03-24Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralPliva Inc.1990-09-30Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralPd Rx Pharmaceuticals, Inc.1990-09-30Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralCardinal Health2011-01-202016-03-11Us
Trazodone Hydrochloridetablet50 mg/1oralProficient Rx LP1990-09-30Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralApotex Corp2008-11-17Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralAv Kare, Inc.2014-02-06Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralRebel Distributors Corp.1988-03-09Not applicableUs
Trazodone Hydrochloridetablet, film coated100 mg/1oralMutual Pharmaceutical Company, Inc.1993-03-24Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralLake Erie Medical DBA Quality Care Products LLC1990-09-30Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralPd Rx Pharmaceuticals, Inc.1990-09-30Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralCardinal Health2004-02-03Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralDIRECT RX2014-01-01Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralApotex Corp2008-11-17Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralKeltman Pharmaceuticals Inc.2010-11-17Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralDispensing Solutions, Inc.2011-01-20Not applicableUs
Trazodone Hydrochloridetablet, film coated150 mg/1oralA S Medication Solutions1993-03-24Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralTorrent Pharmaceuticals Limited2013-11-27Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralAvera Mc Kennan Hospital2015-04-17Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2011-01-20Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralAv Kare, Inc.2014-02-06Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralRebel Distributors Corp.1987-12-11Not applicableUs
Trazodone Hydrochloridetablet, film coated50 mg/1oralMutual Pharmaceutical Company, Inc.1993-03-24Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-12-14Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralCardinal Health2008-11-17Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralCardinal Health2004-02-03Not applicableUs
Trazodone Hydrochloridetablet100 1/1oralDIRECT RX2014-01-01Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralGolden State Medical Supply, Inc.2008-11-17Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralAmerican Health Packaging2012-09-03Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralMed Vantx, Inc.2011-01-20Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralMajor Pharmaceuticals2008-11-17Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralBlenheim Pharmacal, Inc.2014-05-22Not applicableUs
Trazodone Hydrochloridetablet, film coated100 mg/1oralREMEDYREPACK INC.2016-01-07Not applicableUs
Trazodone Hydrochloridetablet, film coated100 mg/1oralQualitest Pharmaceuticals2010-05-30Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralAv Kare, Inc.2014-02-06Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralRebel Distributors Corp.1987-12-11Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-12-14Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralCardinal Health1990-09-30Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralDispensing Solutions, Inc.2011-01-20Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralDIRECT RX2014-01-01Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralGolden State Medical Supply, Inc.2008-11-17Not applicableUs
Trazodone Hydrochloridetablet, film coated100 mg/1oralAmerican Health Packaging2013-12-16Not applicableUs
Trazodone Hydrochloridetablet, film coated50 mg/1oralMed Vantx, Inc.1993-03-24Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralMajor Pharmaceuticals2008-11-17Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralBlenheim Pharmacal, Inc.2011-04-01Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralMc Kesson Contract Packaging2012-01-25Not applicableUs
Trazodone Hydrochloridetablet, film coated50 mg/1oralQualitest Pharmaceuticals2010-05-30Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralAidarex Pharmaceuticals LLC1990-09-30Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralSTAT RX LLC USA1988-03-09Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralUnit Dose Services2011-01-20Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralREMEDYREPACK INC.2010-10-26Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralCardinal Health1990-09-30Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralPhysicians Total Care, Inc.1992-02-20Not applicableUs
Trazodone Hydrochloridetablet, film coated50 mg/1oralREMEDYREPACK INC.2015-11-12Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralGolden State Medical Supply, Inc.2008-11-17Not applicableUs
Trazodone Hydrochloridetablet, film coated50 mg/1oralAmerican Health Packaging2013-12-16Not applicableUs
Trazodone Hydrochloridetablet100 mg/1oralTYA Pharmaceuticals1990-09-30Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralCarilion Materials Management1990-09-30Not applicableUs
Trazodone Hydrochloridetablet150 mg/1oralBlenheim Pharmacal, Inc.2010-03-03Not applicableUs
Trazodone Hydrochloridetablet50 mg/1oralMc Kesson Contract Packaging2011-10-11Not applicableUs
Trazodone Hydrochloridetablet300 mg/1oralBarr Laboratories Inc.1999-05-03Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
BeneficatNot Available
DepraxNot Available
DesirelNot Available
DesyrelBristol-Myers Squibb
Desyrel DividoseBristol-Myers Squibb
MesyrelNot Available
MolipaxinNot Available
ThombranNot Available
TrialodineNot Available
TritticoNot Available
Brand mixtures
NameLabellerIngredients
TrazaminePhysician Therapeutics Llc
Salts
Name/CASStructureProperties
Trazodone Hydrochloride
25332-39-2
Thumb
  • InChI Key: OHHDIOKRWWOXMT-UHFFFAOYSA-N
  • Monoisotopic Mass: 407.127965797
  • Average Mass: 408.325
DBSALT000344
Categories
UNIIYBK48BXK30
CAS number19794-93-5
WeightAverage: 371.864
Monoisotopic: 371.151288058
Chemical FormulaC19H22ClN5O
InChI KeyInChIKey=PHLBKPHSAVXXEF-UHFFFAOYSA-N
InChI
InChI=1S/C19H22ClN5O/c20-16-5-3-6-17(15-16)23-13-11-22(12-14-23)8-4-10-25-19(26)24-9-2-1-7-18(24)21-25/h1-3,5-7,9,15H,4,8,10-14H2
IUPAC Name
2-{3-[4-(3-chlorophenyl)piperazin-1-yl]propyl}-2H,3H-[1,2,4]triazolo[4,3-a]pyridin-3-one
SMILES
ClC1=CC=CC(=C1)N1CCN(CCCN2N=C3C=CC=CN3C2=O)CC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazinanes
Sub ClassPiperazines
Direct ParentPhenylpiperazines
Alternative Parents
Substituents
  • N-arylpiperazine
  • Phenylpiperazine
  • Triazolopyridine
  • Substituted aniline
  • Dialkylarylamine
  • N-alkylpiperazine
  • Pyridinone
  • Halobenzene
  • Chlorobenzene
  • Aniline
  • Benzenoid
  • Pyridine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • 1,2,4-triazole
  • Triazole
  • Azole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of depression.
PharmacodynamicsTrazodone is an antidepressant and hypnotic chemically unrelated to tricyclic, tetracyclic, or other known antidepressant agents. The mechanism of trazodone's antidepressant action in man is not fully understood. In animals, trazodone selectively inhibits serotonin uptake by brain synaptosomes and potentiates the behavioral changes induced by the serotonin precursor, 5-hydroxytryptophan. Cardiac conduction effects of trazodone in the anesthetized dog are qualitatively dissimilar and quantitatively less pronounced than those seen with tricyclic antidepressants. Trazodone is not a monoamine oxidase inhibitor and, unlike amphetamine-type drugs, does not stimulate the central nervous system. In man, trazodone is well absorbed after oral administration without selective localization in any tissue. Since the clearance of trazodone from the body is sufficiently variable, in some patients trazodone may accumulate in the plasma.
Mechanism of actionTrazodone binds at 5-HT2 receptor, it acts as a serotonin agonist at high doses and a serotonin antagonist at low doses. Like fluoxetine, trazodone's antidepressant activity likely results from blockage of serotonin reuptake by inhibiting serotonin reuptake pump at the presynaptic neuronal membrane. If used for long time periods, postsynaptic neuronal receptor binding sites may also be affected. The sedative effect of trazodone is likely the result of alpha-adrenergic blocking action and modest histamine blockade at H1 receptor. It weakly blocks presynaptic alpha2-adrenergic receptors and strongly inhibits postsynaptic alpha1 receptors. Trazodone does not affect the reuptake of norepinephrine or dopamine within the CNS.
Related Articles
AbsorptionRapidly and almost completely absorbed following oral administration. Food may decrease the rate and extent of absorption.
Volume of distributionNot Available
Protein binding89-95% bound to plasma proteins in vitro
Metabolism

Undergoes extensive hepatic metabolism via hydroxylation, N-dealkylation, N-oxidation and splitting of the pyridine ring. Cytochrome P450 (CYP) 3A4 catalyzes the formation of the major active metabolite, m-chlorophenylpiperazine (m-CPP). Metabolites may be further conjugated to glucuonic acid or glutathione. CYP2D6 is responsible for 4'-hydroxylation of m-CPP and the formation of at least one glutathione conjugates of m-CPP, a quinone imine-sulhydryl adduct. Oxotriazolopyridinpropionic acid, an inactive metabolite, and its conjugates account for about 20% of the total excreted oral dose. Less than 1% of the oral dose is excreted unchanged. Approximately 70-75% of the dose is eliminated in urine with the remainder being excreted in feces via biliary elimination.

SubstrateEnzymesProduct
Trazodone
4'-hydroxytrazodone glutathione Details
Trazodone
m-chlorophenylpiperazine (m-CPP) Details
Trazodone
triazolopropionic acidDetails
Trazodone
triazolopyridinone epoxideDetails
Trazodone
4'-hydroxytrazodone Details
Trazodone
Not Available
GlutathioneDetails
Trazodone
Not Available
Glucuonic acidDetails
Trazodone
Not Available
Oxotriazolopyridinpropionic acidDetails
Route of eliminationNot Available
Half lifeUndergoes biphasic elimination with an initial phase t1/2 α of 3-6 hours and a terminal phase t1/2 β of 5-9 hours.
ClearanceNot Available
ToxicityLD50=96mg/kg (i.v. in mice)
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+0.9829
Caco-2 permeable-0.6166
P-glycoprotein substrateSubstrate0.547
P-glycoprotein inhibitor IInhibitor0.8634
P-glycoprotein inhibitor IIInhibitor0.8889
Renal organic cation transporterInhibitor0.6479
CYP450 2C9 substrateNon-substrate0.7897
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateSubstrate0.7408
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.6613
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.83
Ames testNon AMES toxic0.5133
CarcinogenicityNon-carcinogens0.8545
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7007 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.8994
hERG inhibition (predictor II)Inhibitor0.7503
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Labopharm inc
  • Apothecon inc div bristol myers squibb
  • Alvogen inc
  • American therapeutics inc
  • Apotex inc
  • Matrix laboratories ltd
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Pliva inc
  • Quantum pharmics ltd
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Usl pharma inc
  • Vintage pharmaceuticals llc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral150 mg
Tabletoral50 mg
Tabletoral300 mg
Tablet (extended-release)oral150 mg
Tablet (extended-release)oral300 mg
Tablet, extended releaseoral150 mg/1
Tablet, extended releaseoral300 mg/1
Tabletoral100 mg
Tabletoral68.25 mg
Kit
Tabletoral100 1/1
Tabletoral100 mg/1
Tabletoral150 mg/1
Tabletoral300 mg/1
Tabletoral50 mg/1
Tablet, film coatedoral100 mg/1
Tablet, film coatedoral150 mg/1
Tablet, film coatedoral50 mg/1
Prices
Unit descriptionCostUnit
Trazodone hcl powder8.26USD g
Desyrel 300 mg tablet6.03USD tablet
TraZODone HCl 300 mg tablet5.65USD tablet
Trazodone 300 mg tablet5.44USD tablet
Desyrel 100 mg tablet4.6USD tablet
Desyrel 150 mg tablet3.39USD tablet
TraZODone HCl 150 mg tablet1.53USD tablet
Trazodone 150 mg tablet1.47USD tablet
Desyrel 50 mg tablet1.33USD tablet
TraZODone HCl 100 mg tablet0.76USD tablet
Trazodone 100 mg tablet0.73USD tablet
Apo-Trazodone D 150 mg Tablet0.61USD tablet
Desyrel Dividose 150 mg Tablet0.61USD tablet
Novo-Trazodone 150 mg Tablet0.61USD tablet
Nu-Trazodone-D 150 mg Tablet0.61USD tablet
Ratio-Trazodone 150 mg Tablet0.61USD tablet
TraZODone HCl 50 mg tablet0.59USD tablet
Trazodone 50 mg tablet0.57USD tablet
Nu-Trazodone 100 mg Tablet0.41USD tablet
Pms-Trazodone 100 mg Tablet0.41USD tablet
Ratio-Trazodone 100 mg Tablet0.41USD tablet
Apo-Trazodone 100 mg Tablet0.41USD tablet
Desyrel 100 mg Tablet0.41USD tablet
Mylan-Trazodone 100 mg Tablet0.41USD tablet
Novo-Trazodone 100 mg Tablet0.41USD tablet
Pms-Trazodone 75 mg Tablet0.34USD tablet
Apo-Trazodone 50 mg Tablet0.23USD tablet
Mylan-Trazodone 50 mg Tablet0.23USD tablet
Novo-Trazodone 50 mg Tablet0.23USD tablet
Nu-Trazodone 50 mg Tablet0.23USD tablet
Pms-Trazodone 50 mg Tablet0.23USD tablet
Ratio-Trazodone 50 mg Tablet0.23USD tablet
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Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6607748 No2000-06-292020-06-29Us
US7829120 No2007-03-272027-03-27Us
US8133893 No2009-03-132029-03-13Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point87 °CPhysProp
water solubilitySparigly solubleNot Available
logP2.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.29 mg/mLALOGPS
logP2.68ALOGPS
logP3.13ChemAxon
logS-3.1ALOGPS
pKa (Strongest Basic)7.09ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area42.39 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity105.88 m3·mol-1ChemAxon
Polarizability40.12 Å3ChemAxon
Number of Rings4ChemAxon
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)splash10-0a4i-7980000000-5d2bde624fdd9a946993View in MoNA
References
Synthesis ReferenceNot Available
General References
  1. Marek GJ, McDougle CJ, Price LH, Seiden LS: A comparison of trazodone and fluoxetine: implications for a serotonergic mechanism of antidepressant action. Psychopharmacology (Berl). 1992;109(1-2):2-11. [PubMed:1365657 ]
  2. Jauch R, Kopitar Z, Prox A, Zimmer A: [Pharmacokinetics and metabolism of trazodone in man (author's transl)]. Arzneimittelforschung. 1976;26(11):2084-9. [PubMed:1037253 ]
  3. Rotzinger S, Fang J, Baker GB: Trazodone is metabolized to m-chlorophenylpiperazine by CYP3A4 from human sources. Drug Metab Dispos. 1998 Jun;26(6):572-5. [PubMed:9616194 ]
  4. Kalgutkar AS, Henne KR, Lame ME, Vaz AD, Collin C, Soglia JR, Zhao SX, Hop CE: Metabolic activation of the nontricyclic antidepressant trazodone to electrophilic quinone-imine and epoxide intermediates in human liver microsomes and recombinant P4503A4. Chem Biol Interact. 2005 Jun 30;155(1-2):10-20. Epub 2005 Apr 18. [PubMed:15978881 ]
  5. Otani K, Yasui N, Kaneko S, Ishida M, Ohkubo T, Osanai T, Sugawara K, Fukushima Y: Trazodone treatment increases plasma prolactin concentrations in depressed patients. Int Clin Psychopharmacol. 1995 Jun;10(2):115-7. [PubMed:7673654 ]
  6. Saletu-Zyhlarz GM, Abu-Bakr MH, Anderer P, Gruber G, Mandl M, Strobl R, Gollner D, Prause W, Saletu B: Insomnia in depression: differences in objective and subjective sleep and awakening quality to normal controls and acute effects of trazodone. Prog Neuropsychopharmacol Biol Psychiatry. 2002 Feb;26(2):249-60. [PubMed:11817501 ]
  7. Fink HA, MacDonald R, Rutks IR, Wilt TJ: Trazodone for erectile dysfunction: a systematic review and meta-analysis. BJU Int. 2003 Sep;92(4):441-6. [PubMed:12930437 ]
External Links
ATC CodesN06AX05
AHFS Codes
  • 28:16.04.24
PDB EntriesNot Available
FDA labelDownload (151 KB)
MSDSDownload (73.7 KB)
Interactions
Drug Interactions
Drug
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Trazodone.
AcetophenazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Acetophenazine.
AmisulprideThe risk or severity of adverse effects can be increased when Trazodone is combined with Amisulpride.
AprepitantThe serum concentration of Trazodone can be increased when it is combined with Aprepitant.
AripiprazoleThe risk or severity of adverse effects can be increased when Trazodone is combined with Aripiprazole.
AtazanavirThe serum concentration of Trazodone can be increased when it is combined with Atazanavir.
BenzquinamideThe risk or severity of adverse effects can be increased when Trazodone is combined with Benzquinamide.
BexaroteneThe serum concentration of Trazodone can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Trazodone can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Trazodone can be decreased when it is combined with Bosentan.
BuspironeBuspirone may increase the serotonergic activities of Trazodone.
CarphenazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Carphenazine.
ChlormezanoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Trazodone is combined with Chlorprothixene.
CitalopramCitalopram may increase the serotonergic activities of Trazodone.
ClozapineThe risk or severity of adverse effects can be increased when Trazodone is combined with Clozapine.
ConivaptanThe serum concentration of Trazodone can be increased when it is combined with Conivaptan.
DabrafenibThe serum concentration of Trazodone can be decreased when it is combined with Dabrafenib.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Trazodone.
DarunavirThe serum concentration of Trazodone can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Trazodone can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Trazodone can be decreased when it is combined with Deferasirox.
DofetilideTrazodone may increase the QTc-prolonging activities of Dofetilide.
DroperidolThe risk or severity of adverse effects can be increased when Trazodone is combined with Droperidol.
EscitalopramEscitalopram may increase the serotonergic activities of Trazodone.
EthanolThe risk or severity of adverse effects can be increased when Ethanol is combined with Trazodone.
FencamfamineThe risk or severity of adverse effects can be increased when Trazodone is combined with Fencamfamine.
FluconazoleThe metabolism of Trazodone can be decreased when combined with Fluconazole.
FluoxetineFluoxetine may increase the serotonergic activities of Trazodone.
FlupentixolThe risk or severity of adverse effects can be increased when Trazodone is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Trazodone is combined with Fluspirilene.
FluvoxamineFluvoxamine may increase the serotonergic activities of Trazodone.
FosamprenavirThe serum concentration of Trazodone can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Trazodone can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Trazodone can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Trazodone can be increased when it is combined with Fusidic Acid.
GoserelinTrazodone may increase the QTc-prolonging activities of Goserelin.
GranisetronGranisetron may increase the serotonergic activities of Trazodone.
HaloperidolThe risk or severity of adverse effects can be increased when Trazodone is combined with Haloperidol.
IdelalisibThe serum concentration of Trazodone can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Trazodone can be increased when it is combined with Indinavir.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Trazodone.
IvacaftorThe serum concentration of Trazodone can be increased when it is combined with Ivacaftor.
LeuprolideTrazodone may increase the QTc-prolonging activities of Leuprolide.
LinezolidLinezolid may increase the serotonergic activities of Trazodone.
LopinavirLopinavir may increase the QTc-prolonging activities of Trazodone.
LoxapineThe risk or severity of adverse effects can be increased when Trazodone is combined with Loxapine.
LuliconazoleThe serum concentration of Trazodone can be increased when it is combined with Luliconazole.
MesoridazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Mesoridazine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Methotrimeprazine.
Methylene blueTrazodone may increase the serotonergic activities of Methylene blue.
MetoclopramideThe risk or severity of adverse effects can be increased when Trazodone is combined with Metoclopramide.
MifepristoneThe serum concentration of Trazodone can be increased when it is combined with Mifepristone.
MitotaneThe serum concentration of Trazodone can be decreased when it is combined with Mitotane.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Trazodone.
MolindoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Molindone.
NelfinavirThe serum concentration of Trazodone can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Trazodone can be increased when it is combined with Netupitant.
OlanzapineThe risk or severity of adverse effects can be increased when Trazodone is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Trazodone is combined with Ondansetron.
PalbociclibThe serum concentration of Trazodone can be increased when it is combined with Palbociclib.
PaliperidoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Paliperidone.
ParoxetineParoxetine may increase the serotonergic activities of Trazodone.
PerphenazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Perphenazine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Trazodone.
PhenytoinThe serum concentration of Trazodone can be decreased when it is combined with Phenytoin.
PimozideThe risk or severity of adverse effects can be increased when Trazodone is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Piperacetazine.
PipotiazineThe risk or severity of adverse effects can be increased when Pipotiazine is combined with Trazodone.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Trazodone.
ProchlorperazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Promazine.
QuetiapineThe risk or severity of adverse effects can be increased when Trazodone is combined with Quetiapine.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Trazodone.
RemoxiprideThe risk or severity of adverse effects can be increased when Trazodone is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Trazodone is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Risperidone.
RitonavirThe serum concentration of Trazodone can be increased when it is combined with Ritonavir.
SaquinavirSaquinavir may increase the QTc-prolonging activities of Trazodone.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Trazodone.
SertindoleThe risk or severity of adverse effects can be increased when Trazodone is combined with Sertindole.
SertralineSertraline may increase the serotonergic activities of Trazodone.
SiltuximabThe serum concentration of Trazodone can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Trazodone can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Trazodone can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Trazodone can be increased when it is combined with Stiripentol.
SulpirideThe risk or severity of adverse effects can be increased when Trazodone is combined with Sulpiride.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Trazodone.
TelaprevirThe serum concentration of Trazodone can be increased when it is combined with Telaprevir.
ThioridazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Trazodone is combined with Thiothixene.
TipranavirThe serum concentration of Trazodone can be increased when it is combined with Tipranavir.
TocilizumabThe serum concentration of Trazodone can be decreased when it is combined with Tocilizumab.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Trazodone.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Trazodone.
TrifluoperazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Trazodone is combined with Triflupromazine.
VenlafaxineVenlafaxine may increase the serotonergic activities of Trazodone.
VilazodoneVilazodone may increase the serotonergic activities of Trazodone.
VortioxetineVortioxetine may increase the serotonergic activities of Trazodone.
WarfarinTrazodone may decrease the anticoagulant activities of Warfarin.
ZiprasidoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Ziprasidone.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Trazodone is combined with Zuclopenthixol.
Food Interactions
  • Avoid alcohol.
  • Food decreases the rate and extent of absorption.

Targets

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. Pazzagli M, Giovannini MG, Pepeu G: Trazodone increases extracellular serotonin levels in the frontal cortex of rats. Eur J Pharmacol. 1999 Nov 3;383(3):249-57. [PubMed:10594316 ]
  2. Marcoli M, Rosu C, Bonfanti A, Raiteri M, Maura G: Inhibitory presynaptic 5-hydroxytryptamine(2A) receptors regulate evoked glutamate release from rat cerebellar mossy fibers. J Pharmacol Exp Ther. 2001 Dec;299(3):1106-11. [PubMed:11714900 ]
  3. Marek GJ, McDougle CJ, Price LH, Seiden LS: A comparison of trazodone and fluoxetine: implications for a serotonergic mechanism of antidepressant action. Psychopharmacology (Berl). 1992;109(1-2):2-11. [PubMed:1365657 ]
  4. Luparini MR, Garrone B, Pazzagli M, Pinza M, Pepeu G: A cortical GABA-5HT interaction in the mechanism of action of the antidepressant trazodone. Prog Neuropsychopharmacol Biol Psychiatry. 2004 Nov;28(7):1117-27. [PubMed:15610924 ]
  5. Conn PJ, Sanders-Bush E: Relative efficacies of piperazines at the phosphoinositide hydrolysis-linked serotonergic (5-HT-2 and 5-HT-1c) receptors. J Pharmacol Exp Ther. 1987 Aug;242(2):552-7. [PubMed:3039120 ]
  6. 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
yes
Actions
agonist
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. Fiorella D, Rabin RA, Winter JC: The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of m-chlorophenylpiperazine. Psychopharmacology (Berl). 1995 May;119(2):222-30. [PubMed:7659770 ]
  2. Conn PJ, Sanders-Bush E: Relative efficacies of piperazines at the phosphoinositide hydrolysis-linked serotonergic (5-HT-2 and 5-HT-1c) receptors. J Pharmacol Exp Ther. 1987 Aug;242(2):552-7. [PubMed:3039120 ]
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. 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
partial agonist
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. Odagaki Y, Toyoshima R, Yamauchi T: Trazodone and its active metabolite m-chlorophenylpiperazine as partial agonists at 5-HT1A receptors assessed by [35S]GTPgammaS binding. J Psychopharmacol. 2005 May;19(3):235-41. [PubMed:15888508 ]
  2. 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 ]
  3. Subhash MN, Srinivas BN, Vinod KY: Alterations in 5-HT(1A) receptors and adenylyl cyclase response by trazodone in regions of rat brain. Life Sci. 2002 Aug 16;71(13):1559-67. [PubMed:12127910 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Richelson E, Nelson A: Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro. J Pharmacol Exp Ther. 1984 Jul;230(1):94-102. [PubMed:6086881 ]
  3. Noguchi S, Inukai T, Kuno T, Tanaka C: The suppression of olfactory bulbectomy-induced muricide by antidepressants and antihistamines via histamine H1 receptor blocking. Physiol Behav. 1992 Jun;51(6):1123-7. [PubMed:1353628 ]
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 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  3. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]

Enzymes

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. Rotzinger S, Fang J, Baker GB: Trazodone is metabolized to m-chlorophenylpiperazine by CYP3A4 from human sources. Drug Metab Dispos. 1998 Jun;26(6):572-5. [PubMed:9616194 ]
  2. Kalgutkar AS, Henne KR, Lame ME, Vaz AD, Collin C, Soglia JR, Zhao SX, Hop CE: Metabolic activation of the nontricyclic antidepressant trazodone to electrophilic quinone-imine and epoxide intermediates in human liver microsomes and recombinant P4503A4. Chem Biol Interact. 2005 Jun 30;155(1-2):10-20. Epub 2005 Apr 18. [PubMed:15978881 ]
  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
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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Wen B, Ma L, Rodrigues AD, Zhu M: Detection of novel reactive metabolites of trazodone: evidence for CYP2D6-mediated bioactivation of m-chlorophenylpiperazine. Drug Metab Dispos. 2008 May;36(5):841-50. doi: 10.1124/dmd.107.019471. Epub 2008 Jan 31. [PubMed:18238857 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Carriers

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. 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
inducer
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. Stormer E, von Moltke LL, Perloff MD, Greenblatt DJ: P-glycoprotein interactions of nefazodone and trazodone in cell culture. J Clin Pharmacol. 2001 Jul;41(7):708-14. [PubMed:11452702 ]
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Drug created on June 13, 2005 07:24 / Updated on May 28, 2016 02:12