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恩屈嗪,一种新型外周血管扩张剂:乙酰化状态对其降压效果无影响。

Endralazine, a new peripheral vasodilator: absence of effect of acetylator status on antihypertensive effect.

作者信息

Holmes D G, Bogers W A, Wideroe T E, Huunan-Seppala A, Wideroe B

出版信息

Lancet. 1983 Mar 26;1(8326 Pt 1):670-1. doi: 10.1016/s0140-6736(83)91967-0.

Abstract

50 patients with confirmed hypertension were treated with endralazine, a new peripheral vasodilator, in addition to the beta-blocker, pindolol, to which they had not responded adequately. The blood pressure was lowered from 173/115 mm Hg to 143/87 mm Hg in the 34 slow acetylators and from 175/111 mm Hg to 140/84 mm Hg in the 16 fast acetylators. The dosages of both pindolol and endralazine were the same in both groups. It is concluded that the acetylator phenotype does not affect the therapeutic efficacy or dosage requirement of endralazine. It is suggested that this is because endralazine is metabolised mainly by hydrazone formation and only to a minor extent by acetylation.

摘要

50名确诊为高血压的患者在使用β受体阻滞剂吲哚洛尔治疗效果不佳后,加用了一种新型外周血管扩张剂恩屈嗪进行治疗。34名慢乙酰化者的血压从173/115毫米汞柱降至143/87毫米汞柱,16名快乙酰化者的血压从175/111毫米汞柱降至140/84毫米汞柱。两组中吲哚洛尔和恩屈嗪的剂量相同。结论是乙酰化者表型不影响恩屈嗪的治疗效果或剂量需求。有人认为,这是因为恩屈嗪主要通过腙的形成进行代谢,只有少量通过乙酰化代谢。

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