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Pharmacology: Pharmacodynamics: Rosuvastatin is a lipid regulating drug; it is a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate determining enzyme for cholesterol synthesis. Inhibition of HMG-CoA reductase leads to reduced cholesterol synthesis in the liver and lower intracellular cholesterol concentrations; this stimulates an increase in low-density-lipoprotein (LDL)-cholesterol receptors on hepatocyte membranes, thereby increasing the clearance of LDL from the circulation. HMG-CoA reductase inhibitors (also called statins) reduce total cholesterol, LDL-cholesterol, and very-low-density lipoprotein (VLDL)-cholesterol concentrations in plasma.
They also tend to reduce triglycerides and to increase high-density lipoprotein (HDL)-cholesterol concentrations.
Pharmacokinetics: Onset of action: Within 1 week; maximal at 4 weeks.
Distribution: Vd: 134 L.
Protein binding: 88%.
Metabolism: Hepatic (10%), via CYP2C9 (1 active metabolite identified: N-desmethyl rosuvastatin, one-sixth to one-half the HMG-CoA reductase activity of the parent compound).
Bioavailability: 20% (high first-pass extraction by liver).
Asian patients have been noted to have increased bioavailability.
Half-life elimination: 19 hours.
Time to peak, plasma: 3-5 hours.
Excretion: Feces (90%), primarily as unchanged drug.
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