Hayasaki M, Hanabayashi T, Ri J, Takada Y, Ito K, Noda K, Iida M, Chan C, Yamada Y, Osugi S
Jpn J Antibiot. 1986 Sep;39(9):2497-518.
Patients, who had undergone cesarean sections, and those who had experienced premature rupture of membranes, received cefotiam (CTM) and the clinical efficacy and the safety for mothers and fetuses were investigated. At the same time, pharmacokinetic analysis was done to study the maternal fetal transfer. Following results were observed. In cases of premature rupture of membranes, the maternal-fetal transfer ratio after intravenous administrations of CTM was 50.3% at a dosage of 1 g. Maternal and fetal serum concentrations of CTM were maintained higher levels than the MIC80 (0.78 micrograms/ml) against major pathogens excluding anaerobic of gynecologic-obstetric infections and were maintained up to 5.87 hours and 6.15 hours in mothers and fetuses, respectively. The CTM was administered once every 12 hours at a dosage of 1 g to 38 cases up to the 3rd or 4th day of puerperium after the rupture of membranes. Also, the CTM was administered up to times of delivery to another 20 cases, in one of which the fetus developed pneumonia. The maternal-fetal prophylactic effect was recognized in 98.3% (57/58) of cases. Forty-three cesarean section cases received CTM at a dosage level of 1 g by one-hour intravenous drip infusion in the following manner: after surgery to the 4th day, twice a day; from the 5th to the 7th day, once a day. Postoperative prophylactic effect against infection was achieved in all the cases. In 1 case, a slight transient elevation in the maternal GOT was observed. Neonatal jaundice with total bilirubin levels higher than 15.0 mg/dl was observed in 19 neonates (32.8%) in the group in which premature rupture of the membranes had occurred. However, the cause/effect relationship between CTM and the total bilirubin levels is unclear. The maternal-fetal transition of CTM was excellent, and the safety toward the fetus and neonate was high. When an antimicrobial activity and pharmacokinetics are considered, CTM will be a useful drug in the treatment of perinatal infections.
对接受剖宫产的患者以及胎膜早破的患者使用头孢替安（CTM），并研究其临床疗效以及对母婴的安全性。同时，进行药代动力学分析以研究母胎转运情况。观察到以下结果。在胎膜早破的病例中，静脉注射1g剂量的CTM后母胎转运率为50.3%。CTM在母体和胎儿血清中的浓度维持在高于针对除妇产科感染厌氧菌外的主要病原体的MIC80（0.78微克/毫升）的较高水平，在母体和胎儿中分别维持长达5.87小时和6.15小时。对38例胎膜早破后至产褥期第3天或第4天的患者，以1g的剂量每12小时给予CTM一次。另外，对另外20例患者直至分娩时给予CTM，其中1例胎儿发生肺炎。在98.3%（57/58）的病例中确认了母胎预防效果。43例剖宫产病例以1g的剂量通过1小时静脉滴注的方式接受CTM，具体方式如下：术后至第4天，每日2次；第5天至第7天，每日1次。所有病例均实现了术后抗感染预防效果。1例患者母体谷草转氨酶出现轻微短暂升高。在发生胎膜早破的组中，19例新生儿（32.8%）出现总胆红素水平高于15.0mg/dl的新生儿黄疸。然而，CTM与总胆红素水平之间的因果关系尚不清楚。CTM的母胎转运良好，对胎儿和新生儿的安全性高。考虑到抗菌活性和药代动力学，CTM将是治疗围产期感染的一种有用药物。
