Since 1980s, statins have proved to be essential drugs in current medical practice as they provide significant reduction in cardiovascular morbidity and mortality. The results of clinical trials favoring the least low-density lipoprotein (LDL) cholesterol levels and the corresponding declines recommended in treatment guidelines for target LDL-cholesterol levels have increased the importance of statins. Among them, rosuvastatin has become an important alternative in the treatment of hypercholesterolemia, with its high efficacy in reducing LDL- and non-high-density lipoprotein (non-HDL) cholesterol levels. The approved dose range of rosuvastatin is 10-40 mg/day. The classical initial dose of 10 mg reduces LDL-cholesterol, triglyceride, and total cholesterol levels by 50%, 19%, and 35%, respectively, with an increase of 8% in HDL-cholesterol. It is the statin whose initial dose provides the highest reduction in LDL-cholesterol. Peak plasma concentrations are reached in 3-5 hours and its plasma half-life is the longest among all statins with 19 hours; thus, it is recommended as a single daily dose. No decrease in its efficacy has been reported in cases of diabetes and metabolic syndrome which are associated with dyslipidemia characterized with low HDL and high triglyceride levels. Since rosuvastatin is eliminated by both hepatic and renal mechanisms, its initial dose should be as low as 5 mg in hepatic or renal insufficiencies. Since it may interact with cyclosporin, warfarin, fibric acid derivatives, and antacids, the use of rosuvastatin with these drugs requires caution, preferably with a 5-mg initial dose.
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