For what conditions are statins used?
Statins are used for treating hyperlipidemia and heterozygous familial hypercholesterolemia for the primary and secondary prevention of coronary heart disease, (angina, heart attack), stroke, peripheral arterial disease (intermittent claudication). Statins have unapproved uses including rheumatoid arthritis and multiple sclerosis.
Are there differences among statins?
There are a variety of ways that statins differ. One of the differences involves potency in the ability to reduce cholesterol plasma levels. Rosuvastatin (Crestor) and atorvastain (Lipitor) are the most potent statins with respect to lowering LDL, followed by simvastatin (Zocor) and pravastatin (Pravachol).
Statins also differ in how strongly they interact with other drugs; this is due to drug metabolism. Of the statins, neither pravastatin (Pravachol) nor rosuvastatin (Crestor) undergo extensive CYP450 metabolism, and are likely to produce muscle toxicity such as myalgia, myopathies, and inflammation of the muscles due to increased plasma levels and subsequently interactions with other drugs.
In patients who have renal disease, dosages of pravastatin (Pravachol), lovastatin (Mevacor, Altocor), rosuvastatin (Crestor), and simvastatin (Zocor) should be adjusted to prevent increased plasma concentration. No adjustment is necessary for atorvastatin (Lipitor) or fluvastatin (Lescol).
The statins differ in their ability to cause side effects. Skeletal muscle toxicity such as rhabdomyolysis may occur when certain drugs are given with statins which causes an increase in the concentration of statins. Cerivastatin (Baycol) was withdrawn from pharmacies worldwide because it caused rhabdomyolysis 10 to 100 times more often than other statins.
What are side effects of statins?
Common side effects include
What are the drug interactions with statins?
Statins [atorvastatin (Lipitor), lovastatin (Mevacor, Altocor), fluvastatin (Lescol), and simvastatin (Zocor)] when taken together with itraconazole (Sporanox), erythromycin (for example, Benzamycin, Emgel, Ilotycin, Staticin), protease inhibitors, nefazodone (Serzone), cyclosporine (Sandimmune, Neoral, Restasis), diltiazem (Cardizem LA, Cardizem Injection, Tiazac), verapamil (Covera-HS, Verelan PM, Calan), and grapefruit juice could cause an interaction that blocks the enzymes in the liver that eliminate statins from the body. This causes an increased level of statins that could result in an increased risk of myopathies and rhabdomyolysis.
Bile acid sequestrants [colestipol (Colestid) and cholestyramine (Questran, Questran Light)] prevent the absorption of statins into the body by binding to them in the intestine. It is recommended that statins be ingested one hour before or four hours after cholestyramine (Questran, Questran Light) or colestipol (Colestid) .
Statins [fluvastatin (Lescol), lovastatin (mevacor, Altocor), rosuvastatin (Crestor), and simvastatin (Zocor)] when taken with warfarin (Coumadin) may cause an increased risk in bleeding. Atorvastatin (Lipitor) and pravastatin (Pravachol) do not have clinically significant effect when given with warfarin (Coumadin).
An increased risk of rhabdomyolysis or liver failure can occur when statins are taken with niacin [nicotinic acid (Niaspan, Niacor)], or fibric acids [gemfibrozil (Lopid), clofibrate (Atromid-S), and fenofibrate (Tricor)].
St John’s Wort decreases the levels of lovastatin (Mevacor, Altocor) and simvastatin (Zocor) and could possibly reducing efficacy of the specified statins.
What are some examples of statins approved by the FDA in the U.S.?
Statins that are approved for use in the U.S. include:
- atorvastatin (Lipitor),
- fluvastatin (Lescol),
- lovastatin (Mevacor, Altocor)
- pravastatin (Pravachol),
- rosuvastatin (Crestor),
- simvastatin (Zocor ), and
- pitavastatin (Livalo).
Robert J. Bryg, MD
Board Certified Internal Medicine with subspecialty in Cardiovascular Disease