A class of drugs commonly used to lower blood cholesterol. The hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors, or statins, are the most potent, best tolerated and most widely used cholesterol lowering agents and represent some of the most commonly prescribed medications in the United States. HMG-CoA reductase is the rate limiting step in cholesterol synthesis by the liver, and inhibition of its activity causes a significant decrease in total and LDL cholesterol levels. The statins also have minor effects on triglyceride and HDL levels.
List of Statins
Seven statins are available in the United States (year of approval and brand name in parentheses): lovastatin (1987: Mevacor), pravastatin (1991: Pravachol), simvastatin (1991: Zocor), fluvastatin (1993: Lescol), atorvastatin (1996: Lipitor), rosuvastatin (2003: Crestor) and pitavastatin (2009: Livalo).
Liver toxicity of Statins
All 7 statins have been associated with mild-to-moderate serum aminotransferase elevations during therapy that are typically transient, asymptomatic and may resolve even with continuation without dose adjustment. All have also been associated rare instances of clinically apparent acute liver injury and the frequency of reports reflects, in some part, the frequency of their use. Nevertheless, the most reports have been with atorvastatin and simvastatin and the fewest with pravastatin and pitavastatin.
The latency to onset variables considerably and can be more than 6 months or even several years after starting. The majority of cases are hepatocellular but cholestatic hepatitis is also well described for most statins. Cases with autoimmune features have been reported with atorvastatin, simvastatin, rosuvastatin and fluvastatin, as well as with combinations of these agents with ezetimibe.
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