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Pharmacology: Rosuvastatin calcium is a synthetic heptanoic acid-derivative antilipemic agent. The drug is an inhibitor of 3-hydroxymethylglutaryl-CoA (HMG-CoA) reductase (i.e., statin), which catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis. Rosuvastatin reduces total and LDL-cholesterol, apo B, and non-HDL-cholesterol concentrations and increases HDL-cholesterol concentrations in patients with homozygous and heterozygous familial hypercholesterolemia, nonfamilial forms of hypercholesterolemia, and mixed dyslipidemia. Rosuvastatin also reduces triglyceride concentrations in patients with primary hypertriglyceridemia.
Pharmacokinetics: Rosuvastatin is incompletely absorbed from the gastrointestinal tract, with an absolute bioavailability of about 20%. Peak plasma concentrations are achieved about 5 hours after an oral dose.
It is taken up extensively by the liver, its primary site of action, and undergoes limited metabolism, mainly by the cytochrome P450 isoenzyme CYP2C9. It is about 90% bound to plasma proteins.
The plasma elimination half-life of Rosuvastatin is about 19 hours. About 90% of an oral dose of Rosuvastatin appears in the faeces, including absorbed and non-absorbed drug, and the remainder is excreted in the urine; about 5% of a dose is excreted unchanged in urine.
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