Morselli P L, Boutroy M J, Bianchetti G, Zipfel A, Boutroy J L, Vert P
Clinical Research Department, Synthelabo Recherche, Paris, France.
Eur J Clin Pharmacol. 1990;38(5):477-83. doi: 10.1007/BF02336687.
Betaxolol levels in blood were monitored in the perinatal period in 28 pregnant hypertensive women and in their babies. In the mothers betaxolol concentrations at delivery ranged from less than 1 to 115 ng.ml-1 after doses of 10 to 40 mg.day-1. The apparent blood half-life was 15.6 to 22.1 h mean (19 h). Umbilical cord levels indicated a rapid equilibrium between fetal and maternal units (ratio 0.93) within few hours after dosing. Milk betaxolol concentrations, measured in few cases, exceeded those in blood by a factor of 3. Amniotic fluid concentrations were similar to those observed in maternal venous blood and umbilical cord blood. In neonates, the blood betaxolol half-life ranged from 14.8 to 38.5 h, with a definite trend towards a negative correlation with gestational age. A 11-61% rise in the betaxolol concentration was observed in 64% of the neonates during the first 12 h of extrauterine life. The data indicate that betaxolol kinetics is not altered in pregnant women and they stress the need for careful and prolonged (72-96 h) intensive monitoring of neonates born to hypertensive mothers treated with beta-blocking agents.
对28名妊娠高血压妇女及其婴儿围产期的血液中倍他洛尔水平进行了监测。母亲们在每日服用10至40毫克剂量后，分娩时倍他洛尔浓度范围为小于1至115纳克/毫升。表观血液半衰期平均为15.6至22.1小时（19小时）。脐带水平表明给药后数小时内胎儿和母体单位之间迅速达到平衡（比率为0.93）。少数病例中测得的乳汁中倍他洛尔浓度超过血液中的浓度3倍。羊水浓度与母体静脉血和脐带血中观察到的浓度相似。在新生儿中，血液中倍他洛尔半衰期范围为14.8至38.5小时，与胎龄呈明显负相关趋势。64%的新生儿在宫外生活的前12小时内倍他洛尔浓度升高了11%至61%。数据表明倍他洛尔动力学在孕妇中未改变，强调了对接受β受体阻滞剂治疗的高血压母亲所生新生儿进行仔细且长时间（72至96小时）强化监测的必要性。
