红霉素对卡马西平转化为其活性10,11 - 环氧化代谢物的抑制作用。
Inhibition by erythromycin of the conversion of carbamazepine to its active 10,11-epoxide metabolite.
作者信息
Barzaghi N, Gatti G, Crema F, Monteleone M, Amione C, Leone L, Perucca E
机构信息
Department of Internal Medicine and Therapeutics, University of Pavia, Italy.
出版信息
Br J Clin Pharmacol. 1987 Dec;24(6):836-8. doi: 10.1111/j.1365-2125.1987.tb03257.x.
Abstract
The serum levels of carbamazepine (CBZ) and its 10,11-epoxide metabolite (CBZ-E) were determined in seven subjects after a single dose of CBZ (400 mg) in the control state and during co-administration of erythromycin (500 mg three times daily for 10 days). Erythromycin treatment was associated with a decrease in CBZ clearance and a prolongation of CBZ half-life, while CBZ-E levels were markedly reduced. These data provide evidence that erythromycin inhibits the conversion of CBZ to its epoxide metabolite.
摘要
在7名受试者中，测定了他们在对照状态下单次服用卡马西平（CBZ，400mg）以及在联合使用红霉素（每日3次，每次500mg，共10天）期间血清中卡马西平（CBZ）及其10,11 - 环氧化代谢物（CBZ - E）的水平。红霉素治疗与卡马西平清除率降低及卡马西平半衰期延长有关，而CBZ - E水平则显著降低。这些数据证明红霉素可抑制卡马西平向其环氧化代谢物的转化。
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