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Safety of HMG-CoA Reductase Inhibitors: Focus on Atorvastatin

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Abstract

Statins effectively lower LDL-cholesterol and some members of this class have been shown to reduce the risk of major cardiovascular events and total mortality in patients with or at risk for coronary heart disease. Statins are in general well tolerated. Withdrawal rates related to adverse events are low (≤3%). The most common adverse events are mild gastrointestinal symptoms. Elevated serum transaminase levels occur infrequently (≤1.5%). These are generally asymptomatic, reversible and rarely require drug withdrawal. Statins do not cause adverse endocrine effects, do not alter glycemic control in diabetic patients, and do not increase cancer risk. Dose-related myopathy and/or rhabdomyolysis also occurs very rarely, although the risk is increased by concomitant administration of cyclosporine, niacin, fibrates, or by CYP3A4 isoenzyme inhibitors (e.g. erythromycin, systemic azole antifungal agents etc.) with statins metabolized by this isoenzyme. The pharmacokinetics of the individual statin should be considered in patients receiving polypharmacological treatments, to minimize the risk of unfavorable drug interactions. Atorvastatin is well tolerated in long-term treatment of dyslipidemia and is characterized by a safety profile similar to the other available statins.

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Bernini, F., Poli, A. & Paoletti, R. Safety of HMG-CoA Reductase Inhibitors: Focus on Atorvastatin. Cardiovasc Drugs Ther 15, 211–218 (2001). https://doi.org/10.1023/A:1011908004965

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