Description

Simple

A medication used to treat depression.

Clinical

A serotonin uptake inhibitor used to treat major depressive disorder.

Overview

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.[Read more

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.[ Read more

Pharmacodynamic

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 kno... Read more

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.[ Read more

Absorption

Trazodone is rapidly absorbed in the gastrointestinal tract after oral administration, with a bioavailability ranging from 63-91% [ Read more

Protein binding

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

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.[ Read more

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.[ Read more

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.[ Read more

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 ov... Read more

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, men... Read more

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
    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
    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
    Hallucinations US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Delusions US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial

    Contraindications

    • Recommended Actions:
      • Do not coadminister within 14 days of discontinuing MAO inhibitors.
    • Regions: US
    • With Categories:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996

    Food Interactions

    Avoid alcohol.

    Avoid St. John's Wort. The risk of serotonin syndrome may be increased.

    Take after a meal. Should be taken shortly after a light meal or snack.