Atorvastatin
is rapidly captivated afterwards articulate administering with best claret
concentrations accomplished in 1 to 2 hours. The complete bioavailability of
atorvastatin (parent drug) is about 14% and the systemic availability of
HMG-CoA reductase inhibitory action is about 30%. The low systemic
bioavailability is due to presystemic approval by gastrointestinal film and
first-pass metabolism in the liver.
Atorvastatin
is abundantly metabolized to ortho- and parahydroxylated derivatives and
assorted beta-oxidation products. In vitro inhibition of HMG-CoA reductase by
ortho- and parahydroxylated metabolites is agnate to that of atorvastatin.
About 70% of circulating inhibitory action for HMG-CoA reductase is attributed
to alive metabolites. CYP3A4 is aswell complex in the metabolism of atorvastatin.
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