Pharmacokinetics
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 the human body, particularly mCPP, which may contribute to the side effect profile of trazodone. mCPP has been shown to activate numerous serotonin receptors, including 5-HT2C. Approximately 70–75% of 14C-labelled trazodone was found to be excreted in the urine within 72 hours. Trazodone is highly protein-bound.
As a consequence of the production of mCPP as a metabolite, patients administered trazodone may test positive on EMIT II urine tests for the presence of MDMA.
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