氨己烯酸各对映体在癫痫未得到控制的新生儿中的药代动力学。
Pharmacokinetics of the individual enantiomers of vigabatrin in neonates with uncontrolled seizures.
作者信息
Vauzelle-Kervroëdan F, Rey E, Pons G, d'Athis P, Chiron C, Dulac O, Dumas C, Olive G
机构信息
Pharmacologie Clinique Périnatale et Pédiatrique, Université René Descartes, Hôpital Saint-Vincent de Paul (Assistance Publique-Hôpitaux de Paris, France.
出版信息
Br J Clin Pharmacol. 1996 Dec;42(6):779-81. doi: 10.1046/j.1365-2125.1996.00495.x.
The antiepileptic drug vigabatrin (VGB) is a selective irreversible inhibitor of GABA-transaminase. It is administered as a racemic R(-), S(+) mixture, but the pharmacological activity of vigabatrin resides in the S(+) enantiomer and the R(-) enantiomer is inactive. The pharmacokinetic parameters of the two enantiomers have been studied after administration of a single oral 125 mg dose of the racemate to six neonates. The mean values of Cmax and AUC of the S(+) enantiomer were significantly lower (Cmax: 14.0 +/- 4.3 mg l-1; AUC: 143 +/- 44 mg l-1 h) than those of the R(-) enantiomer (Cmax: 34.1 +/- 9.5 mg l-1; AUC: 231 +/- 88 mg l-1 h), whereas no significant difference in the time to reach Cmax (S(+): 2.1 +/- 1.1 h; R(-): 2.2 +/- 1 h) was observed between the two enantiomers. During chronic administration (125 mg twice daily over 4 days), there was no evidence of accumulation of either enantiomer.
抗癫痫药物氨己烯酸（VGB）是γ-氨基丁酸转氨酶的选择性不可逆抑制剂。它以消旋R(-)、S(+)混合物的形式给药，但氨己烯酸的药理活性存在于S(+)对映体中，而R(-)对映体无活性。在给6名新生儿单次口服125mg消旋体后，对两种对映体的药代动力学参数进行了研究。S(+)对映体的Cmax和AUC平均值显著低于R(-)对映体（Cmax：14.0±4.3mg·l-1；AUC：143±44mg·l-1·h）（R(-)对映体Cmax：34.1±9.5mg·l-1；AUC：231±88mg·l-1·h），而两种对映体达到Cmax的时间没有显著差异（S(+)：2.1±1.1h；R(-)：2.2±1h）。在长期给药期间（4天内每日两次，每次125mg），没有证据表明两种对映体有蓄积现象。
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