Langtry H D, Mammen G J, Sorkin E M
ADIS Drug Information Services, Auckland, New Zealand.
Drugs. 1989 Dec;38(6):900-40. doi: 10.2165/00003495-198938060-00005.
Urapidil is a postsynaptic alpha 1-adrenoceptor antagonist with a pharmacodynamic profile similar to prazosin. Unlike prazosin, however, urapidil also has some central activity which may explain the apparent improved tolerability of urapidil, including the absence of first-dose syncope. In clinical trials urapidil therapy resulted in significant reductions in blood pressure in patients with mild to severe essential hypertension, with little influence on heart rate. It is an effective antihypertensive when administered as monotherapy or in combination with beta-blockers and thiazide diuretics. In the few patients with cardiac dysfunction who have been studied to date, urapidil has improved myocardial oxygen consumption, systemic vascular resistance, left ventricular function, cardiac output and pulmonary capillary wedge pressure; however, further study is needed to assess the full therapeutic potential of urapidil in these patients. Urapidil has also been used successfully in the treatment of hypertensive emergencies, including eclampsia and pre-eclampsia, hypertensive crisis and hypertension occurring during general and cardiac surgery, rapidly lowering blood pressure without altering heart rate. Urapidil does not affect lipid or glucose metabolism, nor does it impair renal function. In addition, urapidil may be beneficial to patients with pulmonary hypertension, in whom it dilates pulmonary vascular beds to a greater extent than systemic vasculature, although therapeutic trials have not examined this effect. The most common adverse effects associated with urapidil therapy are dizziness, nausea, headache, fatigue and palpitations; however, these tend to be mild and transient and usually do not require discontinuation of treatment. Thus, urapidil offers a useful alternative to currently available drugs for the treatment of mild to severe hypertension, either as monotherapy or in combination with other antihypertensive drugs.
乌拉地尔是一种突触后α1肾上腺素能受体拮抗剂，其药效学特征与哌唑嗪相似。然而，与哌唑嗪不同的是，乌拉地尔还具有一些中枢活性，这可能解释了乌拉地尔耐受性明显改善的原因，包括无首剂晕厥现象。在临床试验中，乌拉地尔治疗可使轻至重度原发性高血压患者的血压显著降低，而对心率影响较小。作为单一疗法或与β受体阻滞剂及噻嗪类利尿剂联合使用时，它都是一种有效的抗高血压药物。在迄今为止研究的少数心脏功能不全患者中，乌拉地尔改善了心肌耗氧量、全身血管阻力、左心室功能、心输出量和肺毛细血管楔压；然而，需要进一步研究以评估乌拉地尔在这些患者中的全部治疗潜力。乌拉地尔还成功用于治疗高血压急症，包括子痫和先兆子痫、高血压危象以及普通外科手术和心脏手术期间出现的高血压，能迅速降低血压而不改变心率。乌拉地尔不影响脂质或葡萄糖代谢，也不损害肾功能。此外，乌拉地尔可能对肺动脉高压患者有益，在这类患者中，它对肺血管床的扩张程度大于体循环血管，尽管治疗试验尚未研究这种作用。与乌拉地尔治疗相关的最常见不良反应是头晕、恶心、头痛、疲劳和心悸；然而，这些不良反应往往较轻且短暂，通常不需要停药。因此，无论是作为单一疗法还是与其他抗高血压药物联合使用，乌拉地尔都为目前可用药物治疗轻至重度高血压提供了一种有用的替代选择。
