降血脂藥物對LDL-C 低密度膽固醇效果 Rosuvastatin 最強

Effect on LDL cholesterol

Potency — Aside from proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, statins are the most powerful drugs for lowering low-density lipoprotein (LDL) cholesterol, with reductions in the range of 30 to 63 percent (table 3) [6-10]. When switching between statin drugs, equipotent doses with regard to LDL cholesterol reduction can be found in the figure (figure 2).

Rosuvastatin 效果比 Atorvastatin 強

Rosuvastatin 和 Atorvastatin 兩者又比其他四種 statin 強 (simvastatin, lovastatin, pravastatin. fluvastatin) 

當使用至每種藥物各自的最大劑量, 降低 LDL-C 的效果, rosuvastatin 和 atorvastatin 比其他 statin 強

Rosuvastatin is somewhat more potent than atorvastatin [10,11], and both these agents are significantly more potent than simvastatin, lovastatin, pravastatin, and fluvastatin [11,12]. At maximal prescribed doses, LDL cholesterol reduction is greater with rosuvastatin and atorvastatin than with the other available statins (figure 2).

Fluvastatin 40mg QD 效果最弱. 但如果使用到 80mg QD 效果與其他三種(除Rosuvastatin 和 Atorvastatin外)降血脂藥物相近

At doses of up to 40 mg/day, fluvastatin is the least potent statin (figure 2). However, at doses of 80 mg/day, fluvastatin is as effective on lowering LDL cholesterol as most statins other than rosuvastatin and atorvastatin [13]. Fluvastatin, pitavastatin, and pravastatin are less likely to have drug interactions or produce muscle toxicity than some other statins. (See 'Side effects' below.)

Simvastatin 不建議使用至每天 80 mg. 雖然降血脂效果強, 但副作用例如橫紋肌溶解會增加

因此simvastatin 建議每天不要超過 40 mg. 此外, 若病患先前曾經服用 simvastatin 80mg 而無副作用, 仍建議換成其他種類statin, 因為如果之後持續服用 simvastatin 80 mg qd 會增加肌病變機率

高劑量 simvastatin 適合一小部分患者, 包括服用多年仍沒有不良反應, 或無法忍受其他降血脂藥物副作用. 

Although simvastatin 80 mg/day is a high-intensity dose of statin, given high rates of adverse muscle symptoms including rhabdomyolysis [14] and the availability of generic rosuvastatin and atorvastatin, we suggest not treating patients with doses of simvastatin above 40 mg/day. Additionally, clinicians should strongly consider switching even patients who are currently tolerating simvastatin 80 mg/day to one of these other statin options, since future medication therapy or illness could increase the risk for development of myopathy on high-dose simvastatin. High-dose simvastatin may be appropriate for a small number of patients who have tolerated it well for many years or who are intolerant of other high-potency statin options.

Statins類藥物與 bile acid sequestrant 或 cholesterol absorption inhinitor ezetimibe 合併使用有加成作用
There is an additive hypolipidemic effect when any of the statins is used in combination with a bile acid sequestrant (figure 3) [15-17], or the cholesterol absorption inhibitor ezetimibe.