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在奎尼丁治疗期间,异喹胍的广泛代谢者会变成慢代谢者。

Extensive metabolizers of debrisoquine become poor metabolizers during quinidine treatment.

作者信息

Brøsen K, Gram L F, Haghfelt T, Bertilsson L

出版信息

Pharmacol Toxicol. 1987 Apr;60(4):312-4. doi: 10.1111/j.1600-0773.1987.tb01758.x.

Abstract

Seven male patients (age 55-75 years) were debrisoquine-tested immediately before and after one week of treatment with quinidine sulphate (200 mg X 3-4 day-1). Before quinidine all patients were classified as extensive metabolizers (metabolic ratio 0.1-3.6). During quinidine the formation of 4-OH-debrisoquine was practically abolished and the phenotype of the patients was altered to PM (metabolic ratio 15-51). This is probably due to an inhibition of debrisoquine hydroxylation by quinidine. Inhibition of 4-OH-debrisoquine formation was associated with a disproportionate increase in debrisoquine excretion.

摘要

七名男性患者(年龄55 - 75岁)在接受硫酸奎尼丁(200毫克×3 - 4天⁻¹)治疗一周前后立即进行了去甲异喹胍检测。在服用奎尼丁之前,所有患者均被归类为快代谢型(代谢比值0.1 - 3.6)。在服用奎尼丁期间,4 - 羟基去甲异喹胍的形成几乎被消除,患者的表型转变为慢代谢型(代谢比值15 - 51)。这可能是由于奎尼丁对去甲异喹胍羟基化的抑制作用。4 - 羟基去甲异喹胍形成的抑制与去甲异喹胍排泄的不成比例增加有关。

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