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[妊娠晚期头孢噻肟经胎盘转运的研究]

[Studies on the transplacental passage of cefotaxime in late pregnancy].

作者信息

Fujimoto S, Kanagawa Y

出版信息

Jpn J Antibiot. 1982 Jul;35(7):1849-54.

PMID:6294365
Abstract

The transplacental passage of a single intravenous dose of cefotaxime (CTX), 1,000 mg, was examined in 11 pregnant women undergoing delivery at term by cesarean section. The results were as follows. 1. Measurements by HPLC: After a single 1,000 mg intravenous dose, the maternal blood level of CTX took the following course: 40.1 +/- 3.4 mcg/ml (mean +/- S.E.) at 15 minutes, 22.5 +/- 1.9 mcg/ml at 30 minutes, 10.8 +/- 0.9 mcg/ml at 60 minutes and 3.2 +/- 0.4 mcg/ml at 120 minutes. Slightly high maternal blood levels of 0.7 and 1.1 mcg/ml were obtained at child deliveries made at 200 minutes, but only a trace amount was found at a child delivery at 356 minutes. The CTX level in the umbilical cord blood was comparatively high until the measurement at 222 minutes, and then declined. IN the amniotic fluid, peak levels were observed at 222 to 252 minutes, thereafter decreasing slowly. Desacetyl-CTX, a metabolite of CTX, showed maternal blood levels of 5.8 +/- 0.5 mcg/ml at 15 minutes, 6.3 +/- 0.6 mcg/ml at 30 minutes, 6.8 +/- 0.7 mcg/ml at 60 minutes and 4.9 +/- 0.7 mcg/ml at 120 minutes. Thus, the maternal blood level of desacetyl-CTX showed an increasing tendency until 60 minutes after intravenous administration, and decreased rapidly from 120 minutes onwards. No consistent tendency was noted in desacetyl-CTX levels in the umbilical cord blood and the amniotic fluid. 2. Measurements by bioassay: Maternal blood levels of CTX determined by bioassay were 45.2 +/- 3.3 mcg/ml at 15 minutes, 25.8 +/- 2.2 mcg/ml at 30 minutes, 12.4 +/- 1.0 mcg/ml at 50 minutes adn 4.0 +/- 0.5 mcg/ml at 120 minutes. At the time of child delivery, maternal blood levels of CTX were 1.1 and 2.6 mcg/ml at 200 minutes, and then decreased slowly. Trace levels were noted at 336 minutes and CTX was undetectable at 356 minutes. 3. The HPLC study demonstrated that the level of CTx remained comparatively high in the umbilical cord blood and the amniotic fluid even 6 hours after administration (0.3--0.4 mcg/ml and 4.0 mcg/ml, respectively). This result suggests, in consideration of CTX's MIC values for causative organisms, that CTX will produce a sufficient clinical effect in perinatal infections. No side effects were observed in the mothers or their babies.

摘要

对11例足月行剖宫产的孕妇静脉注射1000mg头孢噻肟(CTX)后的经胎盘转运情况进行了研究。结果如下:1. 高效液相色谱法(HPLC)测定:单次静脉注射1000mg后,产妇血中CTX浓度变化如下:15分钟时为40.1±3.4μg/ml(均值±标准误),30分钟时为22.5±1.9μg/ml,60分钟时为10.8±0.9μg/ml,120分钟时为3.2±0.4μg/ml。在200分钟分娩时产妇血中CTX浓度略高,分别为0.7和1.1μg/ml,但在356分钟分娩时仅发现微量。脐血中CTX浓度在222分钟测定前相对较高,之后下降。羊水中,在222至252分钟出现峰值,此后缓慢下降。CTX的代谢产物去乙酰头孢噻肟(Desacetyl-CTX),产妇血中浓度在15分钟时为5.8±0.5μg/ml,30分钟时为6.3±0.6μg/ml,60分钟时为6.8±0.7μg/ml,120分钟时为4.9±0.7μg/ml。因此,静脉给药后60分钟内产妇血中去乙酰头孢噻肟浓度呈上升趋势,120分钟后迅速下降。脐血和羊水中去乙酰头孢噻肟浓度无一致变化趋势。2. 生物测定法测定:生物测定法测得的产妇血中CTX浓度在15分钟时为45.2±3.3μg/ml,30分钟时为25.8±2.2μg/ml,50分钟时为12.4±1.0μg/ml,120分钟时为4.0±0.5μg/ml。分娩时,200分钟时产妇血中CTX浓度为1.1和2.6μg/ml,之后缓慢下降。336分钟时为微量,356分钟时未检测到CTX。3. HPLC研究表明,给药6小时后脐血和羊水中CTX浓度仍相对较高(分别为0.3 - 0.4μg/ml和4.0μg/ml)。考虑到CTX对病原菌的最低抑菌浓度(MIC)值,该结果提示CTX对围产期感染将产生足够的临床疗效。未观察到母亲或其婴儿出现副作用。

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