Statin類藥物藉由抑制肝臟的膽固醇生合成及增加肝臟細胞LDL接受器的數量與活性,有效降低血中膽固醇與LDL數值,被視為是高膽固醇脂血症的第一線用藥;同時,也能降低那些有冠狀動脈疾病(CHD)危險因子病人的罹病率和死亡率。雖然接近95%的病患服用後都有良好的耐受性,但仍有發生不良反應的可能,以橫紋肌溶解症為例,大約是每年10萬人中才有3-4個案例;但當statins併服其他如gemfibrozil等CYP3A4抑制劑的藥品時,橫紋肌溶解症的發生率就會上升十倍。故選擇statins為治療藥物之前,必須考量多重因素,包括病人年齡、本身的疾病狀態、血脂濃度、肝腎功能、藥物交互作用等,醫師必須謹慎的衡量利弊來選擇藥物,並監測其不良反應的發生。
Statins (3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors) are the most powerful drugs for lowering of serum low-density lipoprotein cholesterol (LDL-C) concentration. The best-described mechanism of action of statins is upregulation of LDL receptor activity and reduction in the entry of LDL-C into the circulation. Several major lipid-lowering trials have shown that statin therapy is beneficial in patients with dyslipidemias for both primary and secondary prevention of coronary heart disease. Although most patients tolerate statins quite well, myopathy, myalgia, myositis are associated with the class of drugs. Myositis with rhabdomyolysis is rare, and the incidence of fatal rhabdomyolysis is 0.15deaths per 1million statin prescriptions. The risk is substantially increased for most statins extensively metabolized by cytochrome P-450 3A4 with concurrent therapy with drugs that interfere with CYP3A4. The choice of statin depends on a number of factors, including the degree of hyperlipidemia, age, the presence of renal and kidney function, drug interactions. Be vigilant when patients report any unexplained muscle pain or weakness. As was recently pointed out,” All statins are not created equal.”