Pharmacology: Serotonin is 5-hydroxytryptamine (5-HT), the mechanism of which is presumed to be linked to its inhibition of CNS neuronal uptake of serotonin (5-HT). Sertraline hydrochloride blocks the uptake of serotonin into human platelets.
Pharmacokinetics: In man, following oral once-daily dosing over the range of 50-200 mg for 14 days, mean peak plasma concentrations (Cmax) of sertraline hydrochloride occurred between 4.5-8.4 hrs post-dosing. The average terminal elimination half-life of plasma sertraline is about 26 hrs. Based on this pharmacokinetic parameter, steady-state sertraline plasma levels should be achieved after approximately 1 week of once-daily dosing. The effects of food on the bioavailability of sertraline hydrochloride on subjects administered with a single dose showed AUC slightly increased. The Cmax was 25% greater, while the time to reach peak plasma concentration decreased from 8 hrs post-dosing to 5.5 hrs.