Trazodone


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 associa...

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Pharmacology

Indication

For the treatment of depression.

Pharmacodynamic

Trazodone is an antidepressant and hypnotic chemically unrelated to tricyclic, tetracyclic, or other... Read more

Mechanismofaction

Trazodone binds at 5-HT2 receptor, it acts as a serotonin agonist at high doses and a serotonin anta... Read more

Absorption

Rapidly and almost completely absorbed following oral administration. Food may decrease the rate and... Read more

Proteinbinding

89-95% bound to plasma proteins in vitro

Volumeofdistribution

Information currently not available.

Clearance

Information currently not available.

Halflife

Undergoes biphasic elimination with an initial phase t1/2 α of 3-6 hours and a term... Read more

Routeofelimination

Information currently not available.

Toxicity

LD50=96mg/kg (i.v. in mice)


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Drowsiness US
  • Kind: experimental
    • Percent: 41%
  • Kind: placebo
    • Percent: 20%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 34%
  • Kind: placebo
    • Percent: 20%
  • Clinical Trial
    Dizziness/lightheadedness US
  • Kind: experimental
    • Percent: 28%
  • Kind: placebo
    • Percent: 15%
  • Clinical Trial
    Drowsiness US
  • Kind: experimental
    • Percent: 24%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Hypertension US
  • Kind: experimental
    • Percent: 20%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dizziness/lightheadedness US
  • Kind: experimental
    • Percent: 20%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 20%
  • Kind: placebo
    • Percent: 16%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: 15%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 15%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: 15%
  • Kind: placebo
    • Percent: 11%
  • Clinical Trial
    Suicidal thoughts or behaviours US
  • Kind: experimental
    • Percent: 14
  • Clinical Trial
    Nausea and vomiting US
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 10%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Nausea and vomiting US
  • Kind: experimental
    • Percent: 10%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Edema US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Hypotension US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Aches/pains US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Abdominal/gastric disorder US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Weight Loss US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Nasal/sinus congestion US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Malaise US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Suicidal thoughts or behaviours US
    • adult
  • Kind: experimental
    • Percent: 5
  • Clinical Trial
    Syncope US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Aches/pains US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Tremors US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Incoordination US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Weight Gain US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Edema US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Syncope US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Decreased concentration US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Malaise US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Head full-heavy US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Eye irritation (redness, tired, itchy) US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Tremors US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Nasal/sinus congestion US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Malaise US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Paresthesia US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Retrograde ejaculation US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Tachycardia US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Shortness of Breath US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Palpitations US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Sinus Bradycardia US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Disorientation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial

    Contraindications

    Information currently not available.

    Food Interactions

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

    Interactions

    Type in a drug name to check for interaction with Trazodone

    Trazodone may decrease the anticoagulant activities of (R)-warfarin.
    Trazodone may decrease the anticoagulant activities of (S)-Warfarin.
    The risk or severity of hypertension can be increased when Trazodone is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
    The risk or severity of hypertension can be increased when Trazodone is combined with 1-benzylimidazole.
    The risk or severity of hypoglycemia can be increased when Trazodone is combined with 2,4-thiazolidinedione.
    The therapeutic efficacy of Trazodone can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
    The therapeutic efficacy of Trazodone can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The therapeutic efficacy of 3,5-diiodothyropropionic acid can be decreased when used in combination with Trazodone.
    The therapeutic efficacy of 3,5-Diiodotyrosine can be decreased when used in combination with Trazodone.
    The therapeutic efficacy of Trazodone can be decreased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine.
    The risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyphenethylamine is combined with Trazodone.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Trazodone.
    The risk or severity of adverse effects can be increased when Trazodone is combined with 4-Methoxyamphetamine.
    The metabolism of 5-androstenedione can be decreased when combined with Trazodone.
    The risk or severity of adverse effects can be increased when 5-methoxy-N,N-dimethyltryptamine is combined with Trazodone.
    The metabolism of Trazodone can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Trazodone.
    The metabolism of Trazodone can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The risk or severity of adverse effects can be increased when Trazodone is combined with 7-Nitroindazole.
    7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the serotonergic activities of Trazodone.

    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]

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