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Pharmacology: Pharmacokinetics: Peak plasma concentrations of rosuvastatin were reached 5 hours following oral dosing. The absolute bioavailability of rosuvastatin is approximately 20%. Rosuvastatin is 90% bound to plasma proteins, mostly albumin. This binding is reversible and independent of plasma concentrations. Mean volume of distribution at steady-state of rosuvastatin is approximately 134 liters.
Rosuvastatin is not extensively metabolized; approximately 10% of radiolabeled dose is recovered as metabolite. The major metabolite is N-desmethyl rosuvastatin, which is formed principally by cytochrome P450 isoenzyme CYP2C9. Overall, greater than 90% of active plasma HMG-CoA reductase inhibitory activity is accounted for rosuvastatin in the parent compound. Following oral administration, rosuvastatin and its metabolites are primarily excreted in feces (90%). The elimination half-life of rosuvastatin is approximately 19 hours.
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