1. Mech. of Act. Statins?
2. Additional effects?
3. Route of Administration (ROA)
1. Competitively inhib. HMG-CoA reductase: a hepatic enzyme used for cholesterol biosynthesis
2. Improve vascular endothelium function and anti-inflammatory properties
3. All given via oral administration
Absorption, Distribution, Metabolism, and Elimination
First-pass hepatic uptake allows bioavailability between 5% and 30% of administered doses.
Dose [plasma] peak in 1-4 hours.
The half-lives of these compounds are 1- 4 hours except atorvastatin and rosuvastatin which have half-lives of about 20 hours.
More than 70% of statin metabolites are excreted by the liver with subsequent elimination in the feces.
Side Effects (SEs)
Hepatotoxicity, manifested as elevations in hepatic transaminases.
Myositis with rhabdomyolysis is quite rare (0.01%).
Concomitant use of drugs that diminish statin catabolism is associated with higher rates of myopathy. These drugs include fibrates, especially gemfibrozil, cyclosporine, digoxin, warfarin, macrolide antibiotics, mibefradil, and azole antifungals.
Repeat lipid levels and hepatic transaminases should be checked at about six weeks after instituting
Blood tests to check for myositis or rhabdomyolysis are only indicated for symptomatic patients.
Statins with short halflives (all but atorvastatin and rosuvastatin) should be taken in the evening.