Stalenhoef A F, Stuyt P M, de Graaf J
Department of Medicine, University Hospital Nijmegen, The Netherlands.
Neth J Med. 1997 Jul;51(1):10-5. doi: 10.1016/s0300-2977(97)00010-7.
Ketoconazole is an imidazole derivative that is active as a broad-spectrum antifungal agent. It is also an inhibitor of cholesterol production both in vivo and in vitro.
We compared the effect of low-dose ketoconazole (200 mg/day) or simvastatin (20-40 mg/day) on lipids, lipoproteins and lipoprotein(a) [Lp(a)] in 10 patients with familial hypercholesterolaemia.
Ketoconazole reduced serum total cholesterol and low-density lipoprotein (LDL)-cholesterol by 7.6 and 9.7%, respectively. Simvastatin was more effective, the respective changes being -34.4 and -40.6%. Serum triglycerides and high-density lipoprotein (HDL) were unchanged by ketoconazole therapy, whereas simvastatin decreased triglyceride levels by 33.8% and increased HDL-cholesterol levels by 8.7%. Median Lp(a) levels tended to increase during simvastatin and to decrease during ketoconazole therapy. However, due to the wide range of baseline concentrations of Lp(a), these changes were not significant.
Ketoconazole has some hypocholesterolaemic potential, but the effect of simvastatin is much more pronounced. The increase in Lp(a) during simvastatin therapy has been reported earlier, whereas ketoconazole does not exhibit an effect on the level of Lp(a).
酮康唑是一种咪唑衍生物，作为一种广谱抗真菌剂具有活性。它在体内和体外也是胆固醇生成的抑制剂。
我们比较了低剂量酮康唑（200毫克/天）或辛伐他汀（20 - 40毫克/天）对10例家族性高胆固醇血症患者的血脂、脂蛋白和脂蛋白(a)[Lp(a)]的影响。
酮康唑使血清总胆固醇和低密度脂蛋白（LDL）胆固醇分别降低了7.6%和9.7%。辛伐他汀更有效，各自的变化分别为-34.4%和-40.6%。酮康唑治疗对血清甘油三酯和高密度脂蛋白（HDL）无影响，而辛伐他汀使甘油三酯水平降低了33.8%，使HDL胆固醇水平升高了8.7%。在辛伐他汀治疗期间，Lp(a)水平中位数趋于升高，而在酮康唑治疗期间趋于降低。然而，由于Lp(a)的基线浓度范围较宽，这些变化并不显著。
酮康唑有一定的降胆固醇潜力，但辛伐他汀的效果更显著。辛伐他汀治疗期间Lp(a)升高此前已有报道，而酮康唑对Lp(a)水平无影响。
