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氟伐他汀是第一个人工合成的甲基羟戊二酰辅酶A还原酶抑制剂,氟伐他汀口服后约98%被胃肠道吸收,绝对生物利用度为20%~30%,广泛与血浆蛋白结合(≥99%),半衰期为1.2h。原发性高胆固醇血症病人用氟伐他汀20~40mg/d治疗后,可减少血清LDL-C19%~31%,减少总胆醇15%~21%。减少甘油三酯1%~12%;而HDL-C则升高2%~10%。氟伐他汀20mg/d至少与洛伐他汀20mg/d、吉非贝齐1200mg/d有相同疗效。氟伐他汀40mg/d至少与普伐他汀20mg/d、辛伐他汀10mg/d、苯扎贝特400mg/d有相同疗效。它与消胆胺、苯扎贝特、烟酸等药物合用可使疗效加强。前物经济学显示,氟伐他汀费用一疗效比值明显优于洛伐他汀、辛伐他汀、普伐他汀。
Fluvastatin is the first synthetic methylhydroxyglutaryl coenzyme A reductase inhibitor, fluvastatin about 98% after oral absorption by the gastrointestinal tract, the absolute bioavailability of 20% to 30%, with a wide range of Plasma protein binding (≥99%), half-life of 1.2h. Primary hypercholesterolemia patients treated with fluvastatin 20 ~ 40mg / d, can reduce serum LDL-C19% ~ 31%, reduce the total cholesterol by 15% to 21%. Reduce triglycerides 1% ~ 12%; while HDL-C increased by 2% to 10%. Fluvastatin 20mg / d at least with lovastatin 20mg / d, gemfibrozil 1200mg / d have the same effect. Fluvastatin 40mg / d at least with pravastatin 20mg / d, simvastatin 10mg / d, bezafibrate 400mg / d have the same effect. It is combined with cholestyramine, bezafibrate, niacin and other drugs can enhance the efficacy. The former economics shows that fluvastatin cost-effective ratio was significantly better than lovastatin, simvastatin, pravastatin.