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乙醇导致人和分离的大鼠肝细胞中药物乙酰化增加。

Ethanol-induced increase in drug acetylation in man and isolated rat liver cells.

作者信息

Olsen H, Mørland J

出版信息

Br Med J. 1978 Nov 4;2(6147):1260-2. doi: 10.1136/bmj.2.6147.1260.

Abstract

Sixteen healthy volunteers took part in a cross-over study examining the effect of ethanol on the rate of sulphadimidine acetylation (blood ethanol concentration about 1 g/1). In both rapid and slow acetylators the apparent half life of the drug decreased by about 20% after ethanol (mean reduction 39 +/- SE 8 min) and the amount of drug acetylated, measured in blood and urine, increased. In three slow acetylators the rate of acetylation in blood increased so noticeably after ethanol that they would otherwise have been classified as rapid acetylators. Suspensions of isolated rat liver cells showed an increase of about 30% in the rate of sulphadimidine acetylation after the addition of ethanol (2 g/1). Patients' usual alcohol consumption should be taken into account in determining their acetylator status.

摘要

16名健康志愿者参与了一项交叉研究,该研究检测了乙醇对磺胺二甲嘧啶乙酰化速率的影响(血液乙醇浓度约为1g/1)。在快速乙酰化者和慢速乙酰化者中,服用乙醇后药物的表观半衰期均缩短了约20%(平均缩短39±标准误8分钟),且血液和尿液中测得的药物乙酰化量增加。在3名慢速乙酰化者中,服用乙醇后血液中的乙酰化速率显著增加,否则他们会被归类为快速乙酰化者。添加乙醇(2g/1)后,分离的大鼠肝细胞悬液中磺胺二甲嘧啶的乙酰化速率提高了约30%。在确定患者的乙酰化状态时应考虑其日常饮酒量。

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