Description
Mechanism of Action
Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis. It increases the number of hepatic LDL receptors on the cell surface, enhancing uptake and catabolism of LDL. It also decreases apolipoprotein B, triglycerides and increases HDL.
Absorption: Incompletely absorbed from the GI tract. Time to peak plasma concentration: Approx 5 hr. Absolute bioavailability: Approx 20%.
Distribution: Volume of distribution: 134 L. Plasma protein binding: Approx 90%.
Metabolism: Limited metabolism via CYP2C9 isoenzyme.
Excretion: Via faeces (approx 90%); urine (approx 5% as unchanged drug). Elimination half-life: Approx 19 hr.
MIMS Class
Dyslipidaemic Agents
ATC Classification
C10AA07 – rosuvastatin; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia
