Kosmidis J, Doundoulaki P, Stathakis C, Zerefos N, Bounia A, Daikos G K
Arzneimittelforschung. 1979;29(12a):1960-2.
The kinetics of 6-[(R)-2-[3-methylsulfonyl-2-oxo-imidazolidine-1-carboxamido]-2-phenyl-acetamido]-penicillanic acid sodium salt (mezlocillin, Baypen) in renal failure were studied in 23 patients, given 5 g as i.v. infusion. Serum half-lives (t1/2) were around 60 min in normal renal function, 90 to 120 min in patients with a creatinine clearance (Clcr) of 30-60 ml/min, 160 to 190 min at a ClCr of 15 to 30 ml/min and 6 to 14 h in patients with a ClCr below 10 ml/min. There was a linear correlation between serum creatinine and t1/2. Peritoneal dialysis reduced t1/2 to 3 to 4 h and during haemodialysis t1/2 was 1.4 to 2 h with a mean extraction ratio of 0.25. Levels in urine were very high, even in advanced renal failure and the recovery rate was around 60% of dose in normal renal function, but less in renal failure, being only 10-20% at a ClCr of less than 10 ml/min. Levels in peritoneal dialysate fluctuated between 20 and 30 microgram/ml for 4 to 6 h after the infusion, falling slowly but still averaging 10 to 15 microgram/ml after 18 h. Dosage regimens are proposed for various situations in impaired renal function.
对23例肾衰竭患者静脉输注5g 6-[(R)-2-[3-甲基磺酰基-2-氧代-咪唑烷-1-甲酰胺基]-2-苯基-乙酰胺基]-青霉烷酸钠盐（美洛西林，拜朋）后的药代动力学进行了研究。正常肾功能患者的血清半衰期（t1/2）约为60分钟，肌酐清除率（Clcr）为30 - 60ml/min的患者为90至120分钟，ClCr为15至30ml/min时为160至190分钟，ClCr低于10ml/min的患者为6至14小时。血清肌酐与t1/2之间存在线性相关性。腹膜透析可将t1/2缩短至3至4小时，血液透析期间t1/2为1.4至2小时，平均清除率为0.25。即使在晚期肾衰竭患者中，尿液中的药物浓度也非常高，正常肾功能时药物回收率约为剂量的60%，但在肾衰竭时回收率较低，ClCr低于10ml/min时仅为10 - 20%。输注后4至6小时，腹膜透析液中的药物浓度在20至30μg/ml之间波动，18小时后缓慢下降，但仍平均为10至15μg/ml。针对肾功能受损的各种情况提出了给药方案。
