Identification

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Name
Trazodone
Accession Number
DB00656  (APRD00533)
Type
Small Molecule
Groups
Approved, Investigational
Description

Trazodone is triazolopyridine derivative from the serotonin receptor antagonists and reuptake inhibitors (SARIs) class of antidepressants.11 It is used in adults and has been shown to be comparable in efficacy to other drugs such as tricyclic antidepressants (TCAs), selective serotonin reuptake inhibitors (SSRIs), and serotonin-norepinephrine receptor inhibitor (SNRIs) in the treatment of depression.20 A unique feature of this drug is that it does not promote the anxiety symptoms, sexual symptoms, or insomnia, which are commonly associated with SSRI and SNRI therapy.20 Trazodone acts on various receptors, including certain histamine, serotonin, and adrenergic receptors, distinguishing it from other antidepressants that cover a narrow range of neurotransmitters.20 It was initially granted FDA approval in 1981.21

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 IDs
J10.767K
Product Ingredients
IngredientUNIICASInChI Key
Trazodone hydrochloride6E8ZO8LRNM25332-39-2OHHDIOKRWWOXMT-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DesyrelTablet150 mg/1OralPhysicians Total Care, Inc.2007-01-012011-05-31Us
DesyrelTablet300 mg/1OralBristol Myers Squibb2007-01-012008-11-30Us
DesyrelTablet150 mg/1OralBristol Myers Squibb2007-01-012008-06-30Us
Desyrel Dividose Tab 300mgTabletOralBristol Labs Division Of Bristol Myers Squibb1989-12-311999-08-09Canada
Desyrel Dividose Tablet 150 mgTabletOralBristol Myers Squibb1988-12-312010-01-05Canada
Desyrel Tab 100mgTabletOralBristol Myers Squibb1983-12-312010-09-07Canada
Desyrel Tab 50mgTabletOralBristol Myers Squibb1983-12-312010-05-14Canada
OleptroTablet, extended release150 mg/1OralAngelini Pharma Inc.2010-02-022016-02-29Us
OleptroTablet, extended release300 mgOralAngelini Pharma Inc.2011-03-09Not applicableCanada
OleptroTablet, extended release150 mgOralAngelini Pharma Inc.2011-03-09Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-trazodone D Tablets 150mgTabletOralApotex Corporation1995-12-31Not applicableCanada
Apo-trazodone Tablets 100mgTabletOralApotex Corporation1995-12-31Not applicableCanada
Apo-trazodone Tablets 50mgTabletOralApotex Corporation1995-12-31Not applicableCanada
Dom-trazodone Tablets - 50mgTabletOralDominion Pharmacal1996-12-31Not applicableCanada
Dom-trazodone Tablets-100mgTabletOralDominion Pharmacal1996-12-31Not applicableCanada
Mar-trazodoneTabletOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Mar-trazodoneTabletOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Mar-trazodoneTabletOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Mylan-trazodoneTabletOralMylan Pharmaceuticals1997-11-282016-06-28Canada
Mylan-trazodoneTabletOralMylan Pharmaceuticals1997-09-052016-06-28Canada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
TrazamineTrazodone hydrochloride (50 mg/1) + Choline (250 mg/1)KitOralPhysician Therapeutics Llc2011-02-03Not applicableUs
International/Other Brands
Beneficat / Deprax / Desirel / Desyrel Dividose (Bristol-Myers Squibb) / Mesyrel / Molipaxin / Thombran / Trialodine / Trittico
Categories
UNII
YBK48BXK30
CAS number
19794-93-5
Weight
Average: 371.864
Monoisotopic: 371.151288058
Chemical Formula
C19H22ClN5O
InChI Key
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

Pharmacology

Indication

Trazodone is indicated for the treatment of major depressive disorder (MDD).21 It has been used off-label for adjunct therapy in alcohol dependence, and off-label to treat anxiety and insomnia.21 It may also be used off-label to treat symptoms of dementia, Alzheimer’s disease, schizophrenia, eating disorders, and fibromyalgia due to its effects on various neurotransmitter receptors.10

Associated Conditions
Pharmacodynamics

Trazodone treats depressed mood and other depression-related symptoms and shows benefit in the treatment of insomnia due to its sedating effects.20 It is known to prolong the cardiac QT-interval.21 Memory, alertness, and cognition may be decreased by trazodone, especially in elderly patients due to its central nervous system depressant effects.9

A note on priapism

Trazodone has been associated with the occurrence of priapism, a painful and persistent incidence of penile tissue erection that is unrelievable and can cause permanent neurological damage if left untreated. Patients must be advised to seek immediate medical attention if priapism is suspected.15,21

Mechanism of action

The mechanism of action of trazodone is not fully understood, however, it is known to inhibit the reuptake of serotonin and block both histamine and alpha-1-adrenergic receptors.20 Despite the fact that trazodone is frequently considered a selective serotonin reuptake inhibitor, several reports have shown that other mechanisms including antagonism at serotonin 5-HT1a, 5-HT1c, and 5-HT2 receptor subtypes may occur.9,20 The strongest antagonism of trazodone is reported to occur at the serotonin 5-HT21c receptors, preventing serotonin uptake.1 In addition to acting on serotonin receptors, trazodone has been shown to inhibit serotonin transporters.18,19 The antidepressant effects of trazodone result from the inhibition of receptor uptake, which normally decreases circulating neurotransmitters, contributing to depressive symptoms.13,14

TargetActionsOrganism
A5-hydroxytryptamine receptor 2A
antagonist
Humans
A5-hydroxytryptamine receptor 2C
agonist
Humans
ASodium-dependent serotonin transporter
inhibitor
Humans
A5-hydroxytryptamine receptor 1A
antagonist
partial agonist
Humans
UHistamine H1 receptor
antagonist
Humans
NAlpha-1A adrenergic receptor
antagonist
Humans
NAlpha-2A adrenergic receptor
antagonist
Humans
U5-hydroxytryptamine receptor 1C
antagonist
partial agonist
Rat
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

Trazodone is rapidly absorbed in the gastrointestinal tract after oral administration, with a bioavailability ranging from 63-91% 9 and an AUC0−t of 18193.0 ng·h/mL.17 Food may impact absorption in a variable fashion, and may sometimes lead to decreases in the Cmax of trazodone.9,16 In the fed state in 8 healthy volunteers, the Cmax was measured to be 1.47 +/- 0.16 micrograms/mL, and in the fasted state, was measured at 1.88 +/- 0.42 micrograms/mL. The average Tmax after a single dose of 300 mg was 8 hours. Food may increase absorption by up to 20%.25

Volume of distribution

A single-dose pharmacokinetic study of 8 volunteers taking trazodone determined a volume of distribution of 0.84 +/- 0.16 L/kg.16 The FDA medical review of trazodone reports a volume of distribution of 0.47 to 0.84 L/kg.25

Protein binding

The plasma protein binding of trazodone is 89-95% according to in vitro studies.22

Metabolism

Trazodone is heavily metabolized and activated in the liver by CYP3A4 enzyme to the active metabolite, m-chlorophenylpiperazine (mCPP).3,4 The full metabolism of trazodone has not been thoroughly.22 Some other metabolites that have been identified are a dihydrodiol metabolite and carboxylic acid.2

Route of elimination

Less than 1% of an oral dose is excreted unchanged in the urine.22 In a pharmacokinetic study, about 60-70% of radiolabeled was excreted urine within 48 hours. Approximately 9-29% was found to be excreted in feces over a range of 60 to 100 hours.22 According to the FDA medical review, the kidneys are responsible for 70 to 75% of trazodone excretion. About 21% of trazodone is reported to be excreted by the fecal route and 0.13% of the parent drug is eliminated in the urine as unchanged drug.25

Half life

The plasma elimination half-life was markedly prolonged (13.6 versus 6 hours) elderly volunteers in the fasted state when compared with younger volunteers.9 Another study of 8 healthy individuals taking a single dose of trazodone indicated a terminal elimination half-life of 7.3 +/- 0.8 hr.16

A two-phase pattern of trazodone elimination has been reported. Initially, the half-life is reported to range from 3 to 6 hours and the second phase of elimination to range from 5 to 9 hours.25

Clearance

A decrease in total apparent clearance (5.1 versus 10.8 L/h) was seen elderly volunteers in the fasted state when compared with younger volunteers.9 Another pharmacokinetic study determined the total body clearance of trazodone to be 5.3 +/- 0.9 L/hr in 8 healthy patients taking a single dose of trazodone.16

Toxicity

The oral LD50 of trazodone is 690 mg/kg in rats.22

An overdose of trazodone may result in central nervous system, cardiac, respiratory effects. Signs and symptoms may include dyspnea, bradycardia, hypotension, mental status changes, lack of coordination, and coma, among others.23 In addition, an overdose may result in priapism, a persistent unrelievable penile tissue erection that may cause permanent damage if not treated promptly.15 No specific antidote exists for a trazodone overdose. If an overdose occurs, consider the possibility that trazodone may have been combined with other drugs. Contact a poison control center in case of overdose for the most current management guidelines.21 Dialysis does not accelerate trazodone clearance.9

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
(R)-warfarinTrazodone may decrease the anticoagulant activities of (R)-warfarin.
(S)-WarfarinTrazodone may decrease the anticoagulant activities of (S)-Warfarin.
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidineThe metabolism of Trazodone can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic AcidThe risk or severity of hypertension can be increased when Trazodone is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
1-benzylimidazoleThe risk or severity of hypertension can be increased when Trazodone is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when Trazodone is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of serotonin syndrome can be increased when Trazodone is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,5-diiodothyropropionic acidThe therapeutic efficacy of 3,5-diiodothyropropionic acid can be decreased when used in combination with Trazodone.
3,5-DiiodotyrosineThe therapeutic efficacy of 3,5-Diiodotyrosine can be decreased when used in combination with Trazodone.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of serotonin syndrome can be increased when Trazodone is combined with 4-Bromo-2,5-dimethoxyamphetamine.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Avoid alcohol.
  • Food decreases the rate and extent of absorption.

References

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]
  8. Davis JL, Schirmer J, Medlin E: Pharmacokinetics, pharmacodynamics and clinical use of trazodone and its active metabolite m-chlorophenylpiperazine in the horse. J Vet Pharmacol Ther. 2018 Jun;41(3):393-401. doi: 10.1111/jvp.12477. Epub 2018 Jan 14. [PubMed:29333613]
  9. Haria M, Fitton A, McTavish D: Trazodone. A review of its pharmacology, therapeutic use in depression and therapeutic potential in other disorders. Drugs Aging. 1994 Apr;4(4):331-55. doi: 10.2165/00002512-199404040-00006. [PubMed:8019056]
  10. Fagiolini A, Comandini A, Catena Dell'Osso M, Kasper S: Rediscovering trazodone for the treatment of major depressive disorder. CNS Drugs. 2012 Dec;26(12):1033-49. doi: 10.1007/s40263-012-0010-5. [PubMed:23192413]
  11. Mandrioli R, Protti M, Mercolini L: New-Generation, Non-SSRI Antidepressants: Therapeutic Drug Monitoring and Pharmacological Interactions. Part 1: SNRIs, SMSs, SARIs. Curr Med Chem. 2018;25(7):772-792. doi: 10.2174/0929867324666170712165042. [PubMed:28707591]
  12. Jaffer KY, Chang T, Vanle B, Dang J, Steiner AJ, Loera N, Abdelmesseh M, Danovitch I, Ishak WW: Trazodone for Insomnia: A Systematic Review. Innov Clin Neurosci. 2017 Aug 1;14(7-8):24-34. eCollection 2017 Jul-Aug. [PubMed:29552421]
  13. Blier P: Neurotransmitter targeting in the treatment of depression. J Clin Psychiatry. 2013;74 Suppl 2:19-24. doi: 10.4088/JCP.12084su1c.04. [PubMed:24191974]
  14. Nutt DJ: Relationship of neurotransmitters to the symptoms of major depressive disorder. J Clin Psychiatry. 2008;69 Suppl E1:4-7. [PubMed:18494537]
  15. Hoffmann P, Neu ET, Neu D: Penile amputation after trazodone-induced priapism: a case report. Prim Care Companion J Clin Psychiatry. 2010;12(2). doi: 10.4088/PCC.09l00816gry. [PubMed:20694124]
  16. Nilsen OG, Dale O: Single dose pharmacokinetics of trazodone in healthy subjects. Pharmacol Toxicol. 1992 Aug;71(2):150-3. [PubMed:1438031]
  17. Kale P, Agrawal YK: Pharmacokinetics of single oral dose trazodone: a randomized, two-period, cross-over trial in healthy, adult, human volunteers under fed condition. Front Pharmacol. 2015 Oct 2;6:224. doi: 10.3389/fphar.2015.00224. eCollection 2015. [PubMed:26483693]
  18. 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]
  19. Stahl SM: Mechanism of action of trazodone: a multifunctional drug. CNS Spectr. 2009 Oct;14(10):536-46. [PubMed:20095366]
  20. Justin J. Shin; Abdolreza Saadabadi. (2019). Trazodone, StatPearls. Stat Pearls.
  21. Trazodone [Link]
  22. Monograph, Trazodone [Link]
  23. Trazodone overdose, NIH Medline [Link]
  24. Rapid structure determination of microgram-level drug metabolites using HPLC-MS, fraction collection and NMR spectroscopy [Link]
  25. FDA application review, Trazodone [Link]
External Links
Human Metabolome Database
HMDB0014794
KEGG Drug
D08626
KEGG Compound
C07156
PubChem Compound
5533
PubChem Substance
46506648
ChemSpider
5332
BindingDB
50073444
ChEBI
9654
ChEMBL
CHEMBL621
Therapeutic Targets Database
DAP000104
PharmGKB
PA451744
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Trazodone
ATC Codes
N06AX05 — Trazodone
AHFS Codes
  • 28:16.04.24 — Serotonin Modulators
MSDS
Download (73.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0WithdrawnBasic ScienceSleep Apnea, Obstructive; Post-Traumatic Stress Disorders1
1CompletedOtherHealthy Volunteers1
1CompletedTreatmentBioavailability / Healthy Volunteers / Pharmacokinetics1
1CompletedTreatmentDepression2
1CompletedTreatmentHealthy Volunteers3
1RecruitingTreatmentOSAS (Obstructive Sleep Apneas Syndrome)1
1Unknown StatusTreatmentHealthy Volunteers1
1, 2CompletedTreatmentHypoactive Sexual Desire Disorder (DSM-IV-TR Defined) / Sexual Interest/Arousal Disorder (DSM-5 Defined)1
2Active Not RecruitingBasic ScienceSleep Disordered Breathing (SDB) / Spinal Cord Injuries (SCI)1
2CompletedTreatmentAlcohol Dependence1
2CompletedTreatmentPainful Diabetic Neuropathy (PDN)1
2Not Yet RecruitingTreatmentMajor Depressive Disorder (MDD)1
2RecruitingTreatmentPainful Diabetic Neuropathy (PDN)1
2, 3CompletedTreatmentDepression1
3CompletedTreatmentAlzheimer's Disease (AD)1
3CompletedTreatmentAlzheimer's Disease (AD) / Insomnia / Sleep / Sleep disorders and disturbances1
3CompletedTreatmentMajor Depressive Disorder (MDD)2
3CompletedTreatmentOpiate Addiction / Poor Quality Sleep1
3CompletedTreatmentSleep Disorder1
3Not Yet RecruitingTreatmentInsomnia1
3RecruitingTreatmentEnd Stage Renal Disease (ESRD) / Insomnia1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3WithdrawnTreatmentDepressive Disorder, Treatment-Resistant1
4CompletedTreatmentFibromyalgia1
4CompletedTreatmentSchizophrenic Disorders1
4RecruitingOtherSleep Apnea / Spinal Cord Injuries (SCI)1
4RecruitingTreatmentCerebral Infarctions / Sleep Apnea Syndromes1
4RecruitingTreatmentPain, Chronic / Sleep Bruxism / Sleep Disorder / TMD / TMJ Pain1
4TerminatedTreatmentInsomnia / Mental Health Disorder / Substance Use Disorder (SUD)1
4Unknown StatusTreatmentMajor Depressive Disorder (MDD)1
4WithdrawnTreatmentAgitation / Delirium1
Not AvailableCompletedBasic ScienceOSAS (Obstructive Sleep Apneas Syndrome)1
Not AvailableCompletedTreatmentInsomnia1
Not AvailableCompletedTreatmentInsomnia Comorbid to Psychiatric Disorder / Primary Insomnia1
Not AvailableCompletedTreatmentSexual Dysfunctions1
Not AvailableCompletedTreatmentSpinal Stenosis of Lumbar Region1
Not AvailableRecruitingTreatmentAlcohol-Related Disorders / Brain Injury / Depression / Disease, Chronic / Mild Cognitive Impairment (MCI) / Pain / Posttraumatic Stress Disorders / Quality of Life / Substance-Related Disorders / Suicidal Thoughts / Wounds and Injuries1
Not AvailableRecruitingTreatmentAntidepressant Drug Adverse Reaction / Depression1
Not AvailableUnknown StatusTreatmentTreatment Resistant Depression (TRD)1

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
  • Advanced Pharmaceutical Services Inc.
  • Amerisource Health Services Corp.
  • Apotex Inc.
  • Apothecon
  • AQ Pharmaceuticals Inc.
  • A-S Medication Solutions LLC
  • Barr Pharmaceuticals
  • Bristol-Myers Squibb Co.
  • Bryant Ranch Prepack
  • Cardinal Health
  • Caremark LLC
  • Corepharma LLC
  • Coupler Enterprises Inc.
  • DHHS Program Support Center Supply Service Center
  • Direct Dispensing Inc.
  • DispenseXpress Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Golden State Medical Supply Inc.
  • Goldline Laboratories Inc.
  • H.J. Harkins Co. Inc.
  • Heartland Repack Services LLC
  • Innoviant Pharmacy Inc.
  • Kaiser Foundation Hospital
  • Keltman Pharmaceuticals Inc.
  • Labopharm Inc.
  • Lake Erie Medical and Surgical Supply
  • Letco Medical Inc.
  • Liberty Pharmaceuticals
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Medisca Inc.
  • Medvantx Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mutual Pharmaceutical Co.
  • Mylan
  • Neighborcare Repackaging Inc.
  • Novopharm Ltd.
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pharma Pac LLC
  • Pharmaceutical Utilization Management Program VA Inc.
  • Pharmacy Service Center
  • Physicians Total Care Inc.
  • Pliva Inc.
  • Preferred Pharmaceuticals Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Prescription Dispensing Service Inc.
  • Qualitest
  • Rebel Distributors Corp.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Sandhills Packaging Inc.
  • Shanghai World Prospect Industrial Co. Ltd.
  • Southwood Pharmaceuticals
  • St Mary's Medical Park Pharmacy
  • Stat Rx Usa
  • Teva Pharmaceutical Industries Ltd.
  • United Research Laboratories Inc.
  • Va Cmop Dallas
  • Vangard Labs Inc.
Dosage forms
FormRouteStrength
TabletOral300 mg/1
Tablet, extended releaseOral150 mg/1
Tablet, extended releaseOral150 mg
Tablet, extended releaseOral300 mg
Tablet, extended releaseOral300 mg/1
TabletOral
KitOral
TabletOral100 mg
TabletOral150 mg
TabletOral50 mg
PowderNot applicable1 kg/1kg
TabletOral100 mg/1
TabletOral100 mg/301
TabletOral150 mg/1
TabletOral50 mg/301
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
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8133893No2012-03-132029-03-13Us
US6607748No2003-08-192020-06-29Us
US7829120No2010-11-092027-03-27Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)231-234https://pdf.hres.ca/dpd_pm/00007839.PDF
boiling point (°C)528.5https://www.lookchem.com/Trazodone/
logP2.68http://www.t3db.ca/toxins/T3D2852
logS-3.1http://www.t3db.ca/toxins/T3D2852
pKa6.74https://patents.google.com/patent/EP1931346B1
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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0a4i-7980000000-5d2bde624fdd9a946993
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00di-0609000000-cee74b5bf3182c2aa324

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazinanes
Sub Class
Piperazines
Direct Parent
Phenylpiperazines
Alternative Parents
N-arylpiperazines / Aryl 1,2,4-triazolones / Triazolopyridines / Aniline and substituted anilines / Dialkylarylamines / Pyridinones / Chlorobenzenes / N-alkylpiperazines / Aryl chlorides / Heteroaromatic compounds
show 7 more
Substituents
Phenylpiperazine / N-arylpiperazine / Aryl 1,2,4-triazol-3-one / Triazolopyridine / Tertiary aliphatic/aromatic amine / Aniline or substituted anilines / Dialkylarylamine / Pyridinone / Chlorobenzene / N-alkylpiperazine
show 24 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
N-arylpiperazine, monochlorobenzenes, N-alkylpiperazine, triazolopyridine (CHEBI:9654)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. 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. doi: 10.1016/s0014-2999(99)00644-5. [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. 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]
  4. 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]
  5. Balsara JJ, Jadhav SA, Gaonkar RK, Gaikwad RV, Jadhav JH: Effects of the antidepressant trazodone, a 5-HT 2A/2C receptor antagonist, on dopamine-dependent behaviors in rats. Psychopharmacology (Berl). 2005 May;179(3):597-605. doi: 10.1007/s00213-004-2095-0. Epub 2004 Dec 22. [PubMed:15614572]
  6. Stryjer R, Strous RD, Bar F, Poyurovsky M, Weizman A, Kotler M: Treatment of neuroleptic-induced akathisia with the 5-HT2A antagonist trazodone. Clin Neuropharmacol. 2003 May-Jun;26(3):137-41. [PubMed:12782915]
  7. Trazodone [Link]
Kind
Protein
Organism
Humans
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-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
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]
  3. 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. doi: 10.1016/s0014-2999(99)00644-5. [PubMed:10594316]
  4. 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]
  5. Balsara JJ, Jadhav SA, Gaonkar RK, Gaikwad RV, Jadhav JH: Effects of the antidepressant trazodone, a 5-HT 2A/2C receptor antagonist, on dopamine-dependent behaviors in rats. Psychopharmacology (Berl). 2005 May;179(3):597-605. doi: 10.1007/s00213-004-2095-0. Epub 2004 Dec 22. [PubMed:15614572]
  6. Trazodone [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Serotonin:sodium symporter activity
Specific Function
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into t...
Gene Name
SLC6A4
Uniprot ID
P31645
Uniprot Name
Sodium-dependent serotonin transporter
Molecular Weight
70324.165 Da
References
  1. 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. Stahl SM: Mechanism of action of trazodone: a multifunctional drug. CNS Spectr. 2009 Oct;14(10):536-46. [PubMed:20095366]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
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...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
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]
  4. Sultan MA, Courtney DB: Adjunctive Trazodone and Depression Outcome in Adolescents Treated with Serotonin Re-uptake Inhibitors. J Can Acad Child Adolesc Psychiatry. 2017 Fall;26(3):233-240. Epub 2017 Oct 1. [PubMed:29056986]
Details
5. Histamine H1 receptor
Kind
Protein
Organism
Humans
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 catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. 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]
  2. 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]
  3. Justin J. Shin; Abdolreza Saadabadi. (2019). Trazodone, StatPearls. Stat Pearls.
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217]
  2. Ashford JW: Treatment of Alzheimer's Disease: Trazodone, Sleep, Serotonin, Norepinephrine, and Future Directions. J Alzheimers Dis. 2019;67(3):923-930. doi: 10.3233/JAD-181106. [PubMed:30776014]
  3. Justin J. Shin; Abdolreza Saadabadi. (2019). Trazodone, StatPearls. Stat Pearls.
Kind
Protein
Organism
Humans
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 oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
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. Price LH, Charney DS, Heninger GR: Effects of trazodone treatment on alpha-2 adrenoceptor function in depressed patients. Psychopharmacology (Berl). 1986;89(1):38-44. [PubMed:3016788]
  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]
Kind
Protein
Organism
Rat
Pharmacological action
Unknown
Actions
Antagonist
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, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
Htr2c
Uniprot ID
P08909
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51916.005 Da
References
  1. Haria M, Fitton A, McTavish D: Trazodone. A review of its pharmacology, therapeutic use in depression and therapeutic potential in other disorders. Drugs Aging. 1994 Apr;4(4):331-55. doi: 10.2165/00002512-199404040-00006. [PubMed:8019056]
  2. Li AA, Marek GJ, Hand TH, Seiden LS: Antidepressant-like effects of trazodone on a behavioral screen are mediated by trazodone, not the metabolite m-chlorophenylpiperazine. Eur J Pharmacol. 1990 Feb 27;177(3):137-44. doi: 10.1016/0014-2999(90)90263-6. [PubMed:2311675]
  3. Jenck F, Moreau JL, Mutel V, Martin JR: Brain 5-HT1C receptors and antidepressants. Prog Neuropsychopharmacol Biol Psychiatry. 1994 May;18(3):563-74. [PubMed:8078990]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. 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. Flockhart Table of Drug Interactions [Link]
  4. Trazodone [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Wen B, Ma L, 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. Najibi A, Heidari R, Zarifi J, Jamshidzadeh A, Firoozabadi N, Niknahad H: Evaluating the Role of Drug Metabolism and Reactive Intermediates in Trazodone-Induced Cytotoxicity toward Freshly-Isolated Rat Hepatocytes. Drug Res (Stuttg). 2016 Nov;66(11):592-596. doi: 10.1055/s-0042-109536. Epub 2016 Sep 19. [PubMed:27643409]
  3. Mrazek DA: Psychiatric pharmacogenomic testing in clinical practice. Dialogues Clin Neurosci. 2010;12(1):69-76. [PubMed:20373668]
  4. Wu AH, Lorizio W, Tchu S, Lynch K, Gerona R, Ji W, Ruan W, Ruddy KJ, Desantis SD, Burstein HJ, Ziv E: Estimation of tamoxifen metabolite concentrations in the blood of breast cancer patients through CYP2D6 genotype activity score. Breast Cancer Res Treat. 2012 Jun;133(2):677-83. doi: 10.1007/s10549-012-1963-2. [PubMed:22294487]
  5. Chubak J, Bowles EJ, Yu O, Buist DS, Fujii M, Boudreau DM: Breast cancer recurrence in relation to antidepressant use. Cancer Causes Control. 2016 Jan;27(1):125-36. doi: 10.1007/s10552-015-0689-y. Epub 2015 Oct 30. [PubMed:26518198]

Transporters

Kind
Protein
Organism
Humans
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
Uniprot Name
Multidrug resistance protein 1
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]
  2. Smolders EJ, de Kanter CT, de Knegt RJ, van der Valk M, Drenth JP, Burger DM: Drug-Drug Interactions Between Direct-Acting Antivirals and Psychoactive Medications. Clin Pharmacokinet. 2016 Dec;55(12):1471-1494. doi: 10.1007/s40262-016-0407-2. [PubMed:27317413]

Drug created on June 13, 2005 07:24 / Updated on December 08, 2019 20:10