Dooley M, Goa K L
Adis International Limited, Auckland, New Zealand.
Drugs. 1998 Nov;56(5):929-55. doi: 10.2165/00003495-199856050-00016.
Urapidil is a peripheral postsynaptic alpha 1-adrenoceptor antagonist with central agonistic action at serotonin 5-HT1A receptors. It reduces blood pressure by decreasing peripheral vascular resistance. Oral urapidil decreases blood pressure in patients with mild to moderate essential hypertension and associated risk factors such as hyperlipidaemia or type 2 (non-insulin-dependent) diabetes mellitus with no effect on heart rate. The antihypertensive efficacy of urapidil is similar to that of most comparators in patients with mild to moderate essential or secondary hypertension and no concomitant risk factors. However, the antihypertensive efficacy of urapidil was lower than that of hydrochlorothiazide in a well designed trial. Lipid levels and glucose metabolism are not adversely affected and may improve with urapidil in patients with lipid or glucose abnormalities. Urapidil can be safely combined with other antihypertensive agents such as hydrochlorothiazide and nifedipine and improves blood pressure control in previous nonresponders to monotherapy. Intravenous urapidil reduces blood pressure in patients with pre-eclampsia or hypertension in pregnancy and in patients with hypertensive crises or peri- or postoperative hypertension. The decrease in blood pressure is similar to that observed after nifedipine, enalaprilat, sodium nitroprusside and dihydralazine, greater than that of ketanserin according to 1 larger study, and greater than that of sublingual nitroglycerin in 1 trial in patients with nonsurgical hypertensive crises and pulmonary oedema. However, more patients responded to treatment with urapidil than with enalaprilat or nifedipine. Heart rate is less likely to be altered by urapidil than with some comparator drugs. Urapidil appears to be well tolerated, with most adverse events being mild and transient. The incidence of adverse events with urapidil is similar to that with prazosin, metoprolol, atenolol, sodium nitroprusside and hydrochlorothiazide and less than that with nifedipine and clonidine. Urapidil may not be as well tolerated as captopril and, in 1 study, more urapidil than nitrendipine recipients discontinued treatment because of adverse events.
urapidil reduces blood pressure without altering heart rate. The oral formulation is an effective choice in patients with hypertension and concomitant dyslipidaemia or type 2 diabetes mellitus, in whom the drug does not adversely affect and may improve lipid profiles and glucose metabolism. The intravenous formulation is effective in controlling various hypertensive crises and hypertension associated with pregnancy or surgery and is similar to or better than other first-line agents used in these conditions. Thus, urapidil may be a useful alternative to currently available antihypertensive agents.
乌拉地尔是一种外周突触后α1肾上腺素能受体拮抗剂，对5-羟色胺5-HT1A受体具有中枢激动作用。它通过降低外周血管阻力来降低血压。口服乌拉地尔可降低轻度至中度原发性高血压患者以及伴有高脂血症或2型（非胰岛素依赖型）糖尿病等相关危险因素患者的血压，对心率无影响。在轻度至中度原发性或继发性高血压且无伴随危险因素的患者中，乌拉地尔的降压疗效与大多数对照药物相似。然而，在一项设计良好的试验中，乌拉地尔的降压疗效低于氢氯噻嗪。脂质水平和糖代谢不会受到不利影响，对于脂质或糖代谢异常的患者，乌拉地尔可能会改善这些情况。乌拉地尔可安全地与其他降压药物如氢氯噻嗪和硝苯地平联合使用，并可改善先前对单一疗法无反应患者的血压控制。静脉注射乌拉地尔可降低先兆子痫或妊娠高血压患者以及高血压危象或围手术期或术后高血压患者的血压。血压下降情况与硝苯地平、依那普利拉、硝普钠和双肼屈嗪治疗后观察到的情况相似，根据一项更大规模的研究，比酮色林的降压效果更好，在一项针对非手术性高血压危象和肺水肿患者的试验中，比舌下含服硝酸甘油的降压效果更好。然而，与依那普利拉或硝苯地平相比，更多患者对乌拉地尔治疗有反应。与某些对照药物相比，乌拉地尔引起心率改变的可能性较小。乌拉地尔似乎耐受性良好，大多数不良事件为轻度且短暂。乌拉地尔不良事件的发生率与哌唑嗪、美托洛尔、阿替洛尔、硝普钠和氢氯噻嗪相似，低于硝苯地平和可乐定。乌拉地尔的耐受性可能不如卡托普利，并且在一项研究中，因不良事件而停药的乌拉地尔使用者比尼群地平使用者更多。
乌拉地尔降低血压而不改变心率。口服制剂是高血压合并血脂异常或2型糖尿病患者的有效选择，该药物不会对脂质谱和糖代谢产生不利影响，反而可能改善这些情况。静脉制剂对控制各种高血压危象以及与妊娠或手术相关的高血压有效，与这些情况下使用的其他一线药物相似或更好。因此，乌拉地尔可能是现有降压药物的一种有用替代药物。
