Boelaert J, Schurgers M, Daneels R, Van Landuyt H W, Weatherley B C
J Antimicrob Chemother. 1987 Jul;20(1):69-76. doi: 10.1093/jac/20.1.69.
Once daily 60 min iv infusions of acyclovir at 2.5 mg/kg were administered to six uraemic patients (three male, three female of mean age 52 years and body weight 60 kg) treated by continuous ambulatory peritoneal dialysis (CAPD). Blood and dialysate samples were taken for analysis of acyclovir by radio-immunoassay. A three-compartment pharmacokinetic model was found necessary to explain the profiles obtained. Steady-state was reached by the third day, with little change in mean peak or trough plasma levels between day one (25 and 3 microM) and day five (29 and 4 microM). Mean total plasma clearance was 46 ml/h/kg, of which 12% was due to peritoneal dialysis. The model parameters predicted efficient transfer of acyclovir from the peritoneum to plasma, such that hypothetical peritoneal dosing might give 91% bioavailability. In patients treated by CAPD, iv acyclovir should be administered at 2.5 mg/kg/day.
对6名接受持续性非卧床腹膜透析(CAPD)治疗的尿毒症患者(3名男性,3名女性,平均年龄52岁,体重60kg)每日进行一次静脉输注阿昔洛韦,剂量为2.5mg/kg,持续60分钟。采集血液和透析液样本,采用放射免疫分析法分析阿昔洛韦。发现有必要采用三室药代动力学模型来解释所获得的曲线。到第三天达到稳态,第一天(25和3微摩尔)和第五天(29和4微摩尔)之间平均峰值或谷值血浆水平变化不大。平均总血浆清除率为46ml/h/kg,其中12%是由于腹膜透析。模型参数预测阿昔洛韦能有效地从腹膜转移到血浆,因此假设腹膜给药可能会有91%的生物利用度。在接受CAPD治疗的患者中,静脉注射阿昔洛韦的剂量应为2.5mg/kg/天。