Description
Mechanism of Action
Simvastatin, an antilipemic agent is a competitive inhibitor of HMG-CoA reductase, the enzyme that catalyses the early and rate-limiting step in cholesterol biosynthesis reduces total cholesterol, LDL-cholesterol and triglycerides and increases HDL-cholesterol levels.
Absorption: Well absorbed from the GI tract (85%). Bioavailability: <5%. Peak plasma concentration: 1-2 hr.
Distribution: Plasma protein binding: Approx 95%.
Metabolism: Extensively hepatic via CYP3A4 isoenzyme to β-hydroxyacid (major active metabolite).
Excretion: Mainly via faeces (60% as metabolites); urine (10-15%, inactive form). Elimination half-life: 1.9 hr (active metabolite).
MIMS Class
Dyslipidaemic Agents
ATC Classification
C10AA01 – simvastatin; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.;
