Sign Out
Pharmacology: Pharmacodynamics: Atorvastatin inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis (reduces the production of mevalonic acid from HMG-CoA); this then results in a compensatory increase in the expression of LDL receptors on hepatocyte membranes and a stimulate LDL catabolism.
Pharmacokinetics: Onset of action: Initial change 3-5 days, maximal reduction in plasma cholesterol and triglyceride 2-4 weeks.
Absorption: Rapidly absorbed; extensive first-pass metabolism in GI mucosa and liver.
Distribution: Vd~381 L.
Protein binding: ≥98%.
Metabolism: Hepatic via CYP34; forms active Ortho- and parahydroxylated derivatives and inactive beta-oxidation product.
Bioavailability: ~14% (parent drug) and ~30% (parent drug and equipotent metabolites).
Half-life elimination: Parent drug ~14 hours and metabolites 20-30 hours.
Time to peak, serum: 1-2 hours.
Excretion: Bile, urine (<2% as unchanged drug).
Continue with Google