Meuldermans W, Woestenborghs R, Noorduin H, Camu F, van Steenberge A, Heykants J
Eur J Clin Pharmacol. 1986;30(2):217-9. doi: 10.1007/BF00614307.
Maternal and umbilical venous plasma was obtained at delivery from 8 mothers and their neonates after an i.v. bolus injection of alfentanil, and from 6 mothers and their neonates after epidural administration of sufentanil. Plasma levels of total (free + bound) alfentanil in neonates were about 3.4-times lower than in their mothers. At 33-55 min after 30 micrograms sufentanil, total drug levels in mothers were around the limit of detection of the radioimmunoassay (0.05 ng/ml); in one mother who had received 250 micrograms, the plasma level of total sufentanil was 2.6-times higher than in her neonate. Plasma protein binding of alfentanil was 88.2% in mothers and 67.2% in neonates. Plasma protein binding of sufentanil was 90.7% in mothers and 79.3% in neonates. For both drugs, plasma protein binding was significantly related to the alpha 1-acid glycoprotein (alpha 1-AGP) level, which was about 2.5-times lower in the infants. Free alfentanil levels in mothers and neonates were similar. Free levels of sufentanil in mothers and neonates differed less from each other than did the total drug levels.
在静脉推注阿芬太尼后,从8名母亲及其新生儿中于分娩时获取母体和脐静脉血浆;在硬膜外给予舒芬太尼后,从6名母亲及其新生儿中获取血浆。新生儿体内总(游离+结合)阿芬太尼的血浆水平比其母亲体内的低约3.4倍。在给予30微克舒芬太尼后33 - 55分钟,母亲体内的总药物水平约为放射免疫测定法的检测限(0.05纳克/毫升);在一名接受了250微克舒芬太尼的母亲中,总舒芬太尼的血浆水平比其新生儿高2.6倍。母亲体内阿芬太尼的血浆蛋白结合率为88.2%,新生儿为67.2%。母亲体内舒芬太尼的血浆蛋白结合率为90.7%,新生儿为79.3%。对于这两种药物,血浆蛋白结合率均与α1 - 酸性糖蛋白(α1 - AGP)水平显著相关,而婴儿体内的α1 - AGP水平约低2.5倍。母亲和新生儿体内游离阿芬太尼水平相似。母亲和新生儿体内舒芬太尼的游离水平彼此之间的差异小于总药物水平之间的差异。