ISSUE 1351
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The FDA has approved the marketing of an extended-release formulation of trazodone (Oleptro – Angelini Labopharm) for treatment of major depressive disorder in adults. Immediate-release trazodone has been available for treatment of depression for many years, but is used mostly in low doses for its sedating effects.1
MECHANISM OF ACTION — Trazodone is both an antagonist at serotonin 5HT2A and 5HT2C receptors and a selective serotonin reuptake inhibitor. Its hypnotic activity at low doses is thought to be due mostly to 5HT2A antagonism.2
PHARMACOKINETICS — Taken on an empty stomach, peak serum concentrations (Cmax) of extended-release trazodone are lower than those with 100 mg three times daily of immediate-release trazodone. Taking the extended-release formulation with a high-fat meal can increase Cmax by 86%. The median time to Cmax (Tmax)
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