McKenney James M
School of Pharmacy, Medical College of Virginia, Virginia Commonwealth University, Richmond, USA.
Am J Health Syst Pharm. 2005 May 15;62(10):1033-47. doi: 10.1093/ajhp/62.10.1033.
The chemistry, pharmacology, pharmacokinetics, drug interactions, clinical efficacy, adverse effects, dosage and administration, and place in therapy of rosuvastatin are reviewed.
Rosuvastatin, the latest statin to receive approved labeling by the Food and Drug Administration, has shown superior efficacy in lowering low-density-lipoprotein (LDL) cholesterol. At daily doses of 5-40 mg, rosuvastatin produces mean reductions in plasma LDL cholesterol of 45-63%, statistically greater than those achieved with equivalent doses of atorvastatin, simvastatin, and pravastatin. Rosuvastatin also improves triglyceride, non-high-density lipoprotein (HDL)-cholesterol, and HDL cholesterol levels to produce a more favorable lipid profile. Rosuvastatin's safety was studied in more than 10,000 patients, exceeding the number of patients evaluated before the launch of any other statin. Many of these patients took the drug for up to 96 weeks. With regard to muscle, renal, and hepatic toxicity and the withdrawal rate due to adverse events, rosuvastatin demonstrates a safety profile similar to that of the other marketed statins. Rosuvastatin undergoes only minor metabolism (10% of the administered dose) by the cytochrome P-450 2C9 isoenzyme. Significant drug interactions were reported with cyclosporine, gemfibrozil, warfarin, and antacids. Evidence suggests that rosuvastatin will be a valuable addition to the choices for treatment of patients with dyslipidemia.
Rosuvastatin has greater efficacy in lowering LDL cholesterol and non-HDL-cholesterol concentrations than the other statins. It has been shown to enable more patients to reach their LDL cholesterol goals than other statins and to do so with an acceptable safety profile.
对瑞舒伐他汀的化学性质、药理学、药代动力学、药物相互作用、临床疗效、不良反应、剂量与用法以及在治疗中的地位进行综述。
瑞舒伐他汀是最新一种获得美国食品药品监督管理局批准标签的他汀类药物，在降低低密度脂蛋白（LDL）胆固醇方面显示出卓越疗效。每日剂量为5 - 40毫克时，瑞舒伐他汀可使血浆LDL胆固醇平均降低45% - 63%，在统计学上显著高于同等剂量的阿托伐他汀、辛伐他汀和普伐他汀所达到的降幅。瑞舒伐他汀还能改善甘油三酯、非高密度脂蛋白（HDL）胆固醇以及HDL胆固醇水平，从而产生更有利的血脂谱。在超过10000名患者中对瑞舒伐他汀的安全性进行了研究，这一患者数量超过了其他任何他汀类药物上市前评估的患者数量。这些患者中有许多人服用该药物长达96周。在肌肉、肾脏和肝脏毒性以及因不良事件导致的撤药率方面，瑞舒伐他汀显示出与其他已上市他汀类药物相似的安全性。瑞舒伐他汀仅通过细胞色素P - 450 2C9同工酶进行少量代谢（占给药剂量的10%）。已报道与环孢素、吉非贝齐、华法林和抗酸剂存在显著的药物相互作用。有证据表明，瑞舒伐他汀将成为血脂异常患者治疗选择中的一个有价值的补充。
瑞舒伐他汀在降低LDL胆固醇和非HDL胆固醇浓度方面比其他他汀类药物更有效。已证明与其他他汀类药物相比，它能使更多患者达到LDL胆固醇目标，并且安全性可接受。
