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Statin Drugs
- Lovastatin (Mevacor)
- Simvastatin (Zocor); Simvastatin/Ezetimibe Combo (Vytorin)
- Pravastatin (Pravachol)
- Fluvastatin (Lescol)
- Atorvastatin (Lipitor)
- Rosuvastatin (Crestor)
"Lo, Sim, Pra, Flu, Ator, Rosu"
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Statin Drug Indications
- Lowering LDL levels
- Mild increase in HDLs
- Decrease of Triglycerides
- Decrease Cardiovascular events
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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
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Absorption, Distribution, Metabolism, and Elimination
- Intestinal
- 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.
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Side Effects (SEs)
- Myopathy
- 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.
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Clinical Use
- Repeat lipid levels and hepatic transaminases should be checked at about six weeks after instituting
- therapy.
- 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.
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