Raedsch R, Plachky J, Wolf N, Simonis G
Department of Medicine, University of Heidelberg, Püttlingen, Germany.
Eur J Drug Metab Pharmacokinet. 1995 Apr-Jun;20(2):113-8. doi: 10.1007/BF03226364.
Hypolipidemic drugs like etofibrate and bezafibrate may induce lithogenic bile and increase the risk of gallstone formation. In this study, biliary lipids, lithogenic index and biliary drug concentrations were investigated in 6 hyperlipidemic patients after cholecystectomy. Patients were treated once daily for 5 days with either 500 mg/day etofibrate or 400 mg/day bezafibrate. Hepatic bile was collected for 6 days via T-drainage in 4 hourly aliquots. In the patients treated with etofibrate, the range of the lithogenic index remained stable with 0.89-1.69 before and 0.78-1.51 after 5 day drug therapy. In the bezafibrate group, the range of the lithogenic index rose from 0.81-1.40 to 1.26-1.66 mainly as a result of an increase of biliary cholesterol concentrations. Biliary drug concentrations were substantially higher under bezafibrate treatment than under etofibrate treatment. In conclusion, the fibrate drugs, etofibrate and bezafibrate, are different with regard to lithogenicity of bile and extent of biliary excretion. The safety profile of etofibrate may be preferably compared to other fibrate drugs.
降脂药物如益多酯和苯扎贝特可能会导致胆汁致石性增加,并增加胆结石形成的风险。在本研究中,对6例胆囊切除术后的高脂血症患者的胆汁脂质、致石指数和胆汁药物浓度进行了研究。患者每天接受一次治疗,连续5天,分别给予500mg/天的益多酯或400mg/天的苯扎贝特。通过T形引流管每4小时采集一次肝胆汁,共采集6天。在接受益多酯治疗的患者中,致石指数范围在药物治疗5天前为0.89 - 1.69,治疗后为0.78 - 1.51,保持稳定。在苯扎贝特组中,致石指数范围从0.81 - 1.40上升至1.26 - 1.66,主要是由于胆汁胆固醇浓度增加所致。苯扎贝特治疗组的胆汁药物浓度显著高于益多酯治疗组。总之,贝特类药物益多酯和苯扎贝特在胆汁致石性和胆汁排泄程度方面存在差异。与其他贝特类药物相比,益多酯的安全性可能更佳。