Wu R, Spence J D, Carruthers S G
Eur J Clin Pharmacol. 1986;30(5):553-7. doi: 10.1007/BF00542414.
Endralazine, a novel vasodilator related to hydralazine, exhibits a longer half-life and is only minimally influenced by acetylator status. The antihypertensive action of once daily endralazine has been studied in 17 patients previously controlled with an antihypertensive regimen which included hydralazine and a beta-blocker. Hydralazine was discontinued but other medications were unchanged. Pre-study dosage of hydralazine ranged from 25 mg b.i.d. to 50 mg g.i.d., mean daily dose 126.5 mg. Endralazine was started at a dose of 10 mg o.d. and increased by 10 mg to a maximum of 40 mg o.d. until seated DBP was controlled below 95 mmHg. All 17 patients completed the study. Seated BP significantly decreased from 147.5/99.7 to 133.8/83.9 and standing BP from 145.8/99.2 to 133.6/87.3 mmHg. Ten patients (59%) were successfully controlled with endralazine once daily but 7 patients required twice daily dosage schedules because of lack of BP control at 24 h after dosing or excessive hypotension shortly after dosing. Other adverse effects were headache, palpitations and fatigue. There was a statistically insignificant average weight gain of 1 kg but pedal edema was not observed. Endralazine is an effective antihypertensive agent with adverse symptoms similar to those experienced with hydralazine.
恩屈嗪是一种与肼屈嗪相关的新型血管扩张剂,半衰期较长,乙酰化状态对其影响极小。在17例先前采用包括肼屈嗪和β受体阻滞剂的抗高血压方案控制血压的患者中,研究了每日一次服用恩屈嗪的降压作用。停用了肼屈嗪,但其他药物不变。研究前肼屈嗪的剂量范围为每日两次25毫克至每日四次50毫克,平均每日剂量126.5毫克。恩屈嗪起始剂量为每日一次10毫克,每次增加10毫克,最大剂量为每日一次40毫克,直至坐位舒张压控制在95毫米汞柱以下。所有17例患者均完成了研究。坐位血压从147.5/99.7显著降至133.8/83.9,站立位血压从145.8/99.2降至133.6/87.3毫米汞柱。10例患者(59%)每日一次服用恩屈嗪后血压得到成功控制,但7例患者由于给药后24小时血压控制不佳或给药后不久出现过度低血压,需要每日两次给药方案。其他不良反应包括头痛、心悸和疲劳。平均体重增加1千克,差异无统计学意义,且未观察到足踝水肿。恩屈嗪是一种有效的抗高血压药物,其不良反应与肼屈嗪相似。