Serenata Mechanism of Action

Pharmacology: Pharmacodynamics: Sertraline potently and selectively inhibits serotonin reuptake, thereby increasing the serotonin concentrations in synaptic cleft and prolongs its activity at postsynaptic receptor sites, which is reported to be responsible for its antidepressant action. It has only very weak effects on norepinephrine and dopamine neuronal reuptake. At clinical doses, sertraline blocks the uptake of serotonin into human platelets.
Like most clinically effective antidepressants, sertraline down regulates brain norepinephrine and serotonin receptors in animals. In receptor binding studies, sertraline has no significant affinity for adrenergic (alpha(1), alpha(2) and beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5-HT1A, 5-HT1B, 5-HT2) or benzodiazepine binding sites.
Pharmacokinetics: Sertraline is slowly absorbed from the gastro-intestinal tract with peak plasma concentrations occurring about 4.5 to 8.5 hours after ingestion. It undergoes extensive first-pass metabolism in the liver. The main pathway is demethylation to N-desmethylsertraline; further metabolism and glucuronide conjugation occurs. Sertraline is widely distributed throughout the body tissues and is highly (about 98%) bound to plasma proteins. The plasma elimination half-life of sertraline is reported to be 24 to 26 hours.
Sertraline is excreted in approximately equal amounts in the urine and faeces, mainly as metabolites. Sertraline is distributed into breast milk.