Gonik B, Cotton D B, Feldman S, Cleary T G, Pickering L K
Am J Perinatol. 1985 Apr;2(2):114-7. doi: 10.1055/s-2007-999926.
A scarcity of pharmacokinetic data are available on cefotaxime in the obstetric patient. Fifteen patients received either 1 or 2 gm of cefotaxime after cesarean section. After intravenous administration of the designated dose, serial blood samples were analyzed for cefotaxime and its active metabolite, desacetyl cefotaxime (DCTX), by high-pressure liquid chromatography. The mean (+/- SD) peak concentrations of cefotaxime were 14.1 +/- 7.9 micrograms/ml and 40.0 +/- 32.5 micrograms/ml for the 1- and 2-gm dosage regimens, respectively. Detectable trough concentrations were 0.87 +/- 0.24 and 1.0 +/- 0.26, respectively, with many values falling below the sensitivity limits of the assay (0.5 micrograms/ml). The mean peak concentrations of DCTX for the two doses were 5.5 +/- 1.9 micrograms/ml and 10.9 +/- 6.2 micrograms/ml, respectively. Measurable trough levels for DCTX were more frequently identified, than for cefotaxime, at the end of the dosing interval due to an extended half-life as compared to its parent compound. Pharmacokinetic parameters of cefotaxime demonstrated large volumes of distribution and high clearance rates. Our data suggest altered pharmacokinetics of this agent in the obstetric patient when compared to previous studies in nonpregnant patients. This may be important in the seriously ill gravida where dosage adjustments in cefotaxime administration may be needed.
关于产科患者中头孢噻肟的药代动力学数据匮乏。15名患者在剖宫产术后接受了1克或2克的头孢噻肟。静脉注射指定剂量后,通过高压液相色谱法对系列血样进行头孢噻肟及其活性代谢产物去乙酰头孢噻肟(DCTX)分析。对于1克和2克的给药方案,头孢噻肟的平均(±标准差)峰值浓度分别为14.1±7.9微克/毫升和40.0±32.5微克/毫升。可检测到的谷浓度分别为0.87±0.24和1.0±0.26,许多值低于检测方法的灵敏度极限(0.5微克/毫升)。两剂DCTX的平均峰值浓度分别为5.5±1.9微克/毫升和10.9±6.2微克/毫升。由于与母体化合物相比半衰期延长,在给药间隔结束时,DCTX可测量的谷浓度比头孢噻肟更常被检测到。头孢噻肟的药代动力学参数显示分布容积大且清除率高。我们的数据表明,与先前在非妊娠患者中的研究相比,该药物在产科患者中的药代动力学发生了改变。这对于可能需要调整头孢噻肟给药剂量的重症孕妇可能很重要。