Trazodone (Desyrel®, Trittico®, Thombran®, Trialodine®) is a psychoactive compound with sedative, anxiolytic, and antidepressant properties. The manufacturer claims that the antidepressant activity becomes evident in the first week of therapy. Trazodone has less prominent anticholinergic (dry mouth, constipation, tachycardia) and adrenolytic (hypotension, male sexual problems) side effects than most tricyclic antidepressants. The incidence of nausea and vomiting observed with Trazodone is relatively low compared to SSRIs.

Mechanism of action

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Trazodone is a serotonin reuptake inhibitor and is also a 5-HT₂ receptor antagonist. However, in contrast to the selective serotonin reuptake inhibitors such as fluoxetine (Prozac®), trazodone's antidepressant effects may be due to its antagonistic effect at the 5-HT₂ receptor site (PMID 1365657).

Pharmacokinetics

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Trazodone is well absorbed after oral administration with mean peak blood levels obtained at approximately 1 hour after ingestion. Absorption is somewhat delayed and enhanced by food. The mean blood elimination half-life is biphasic: the first phase's half-life is 3-6 hours, and the following phase's half-life is 5-9 hours. The drug is extensively metabolized with 3 or 4 major metabolites having been identified in man. Approximately 70-75% of C¹⁴-labelled trazodone was found to be excreted in the urine within 72 hours (PMID 1037253). Trazodone is highly protein-bound.

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