Bernard B, Thielen P, Garcia-Cázares J, Ballard C A
Antimicrob Agents Chemother. 1977 Aug;12(2):231-6. doi: 10.1128/AAC.12.2.231.
To evaluate maternal-fetal pharmacology of cefatrizine (BL-S 640), a new oral cephalosporin, a single oral 1,000-mg dose was administered to 33 gravidas (8 to 20 weeks' gestation) at varying intervals within 46 h of an elective therapeutic abortion by hysterectomy or intra-amniotic prostaglandin F(2a) induction. Mean maternal serum concentrations at 1, 2, 4, and 8 h were 3.7, 7.9, 6.5, and 1.6 mug/ml; beyond a 3-h peak, a half-life of 2.4 h was determined. Cefatrizine placental half-life was 4.4 h. None of the 11 fetuses from a prostaglandin F(2a) abortion revealed cefatrizine activity; in contrast, 17 of 22 fetuses from a surgical abortion demonstrated cefatrizine concentrations in two or more samples. Fetal cefatrizine levels were less than 3 mug/g or mug/ml in kidney and urine, less than 2 mug/ml in serum and bile, and less than 2.5 mug/g in lung. After a single maternal dose, cefatrizine has a wide distribution in the fetus in the first half of gestation.
为评估新型口服头孢菌素头孢曲嗪(BL-S 640)的母婴药理学,在通过子宫切除术或羊膜腔内注射前列腺素F(2a)引产进行选择性治疗性流产的46小时内,以不同间隔对33名孕妇(妊娠8至20周)单次口服1000毫克剂量的头孢曲嗪。给药后1、2、4和8小时的母体血清平均浓度分别为3.7、7.9、6.5和1.6微克/毫升;在3小时达到峰值后,确定其半衰期为2.4小时。头孢曲嗪在胎盘的半衰期为4.4小时。在前列腺素F(2a)引产的11例胎儿中,无一例显示有头孢曲嗪活性;相比之下,在手术流产的22例胎儿中,有17例在两个或更多样本中显示有头孢曲嗪浓度。胎儿肾脏和尿液中的头孢曲嗪水平低于3微克/克或微克/毫升,血清和胆汁中低于2微克/毫升,肺中低于2.5微克/克。单次母体给药后,头孢曲嗪在妊娠前半期的胎儿体内分布广泛。