Heim K L, Halstenson C E, Comty C M, Affrime M B, Matzke G R
Antimicrob Agents Chemother. 1986 Jul;30(1):15-9. doi: 10.1128/AAC.30.1.15.
The disposition of cefotaxime (CTX) and desacetyl cefotaxime (DAC) was studied in eight noninfected patients on continuous ambulatory peritoneal dialysis. Each patient received a single intravenous (i.v.) infusion and an intraperitoneal (i.p.) instillation of 2 g of CTX. Multiple blood and dialysate samples were collected during the 72-h period after drug administration. The half-life, steady-state volume of distribution, and total body clearance of CTX following i.v. administration were 2.2 +/- 1.0 h (mean +/- standard deviation), 0.17 +/- 0.03 liters/kg, and 81.0 +/- 31.0 ml/min, respectively. No significant differences were observed in these parameters after i.p. administration. The continuous ambulatory peritoneal dialysis clearances of CTX and DAC were 1.82 +/- 0.43 and 2.84 +/- 0.70 ml/min, respectively, after i.v. administration. The bioavailability of CTX after i.p. instillation was 74.6 +/- 21.3%. Peak peritoneal dialysate CTX and DAC concentrations of 264.3 and 25.8 mg/liter, respectively, were observed after i.p. dosing. Administration (i.v.) of 2 g every 12 h or i.p. instillation of 2 g every 24 h may be used for the treatment of i.p. infections with highly susceptible organisms (MIC less than 1.0 microgram/ml).
在8例持续非卧床腹膜透析的非感染患者中研究了头孢噻肟(CTX)和去乙酰头孢噻肟(DAC)的处置情况。每位患者接受单次静脉注射和2g CTX的腹腔内滴注。给药后72小时内采集多份血液和透析液样本。静脉给药后,CTX的半衰期、稳态分布容积和全身清除率分别为2.2±1.0小时(平均值±标准差)、0.17±0.03升/千克和81.0±31.0毫升/分钟。腹腔给药后这些参数未观察到显著差异。静脉给药后,CTX和DAC的持续非卧床腹膜透析清除率分别为1.82±0.43和2.84±0.70毫升/分钟。腹腔内滴注后CTX的生物利用度为74.6±21.3%。腹腔给药后观察到腹膜透析液中CTX和DAC的峰值浓度分别为264.3和25.8毫克/升。每12小时静脉注射2g或每24小时腹腔内滴注2g可用于治疗对高度敏感菌(MIC小于1.0微克/毫升)的腹腔感染。