Goa K L, Benfield P, Sorkin E M
ADIS Drug Information Services, Auckland, New Zealand.
Drugs. 1989 May;37(5):583-627. doi: 10.2165/00003495-198937050-00002.
Since labetalol was first reviewed in the Journal (1978), its scope of therapeutic use has expanded and become better defined. Labetalol is an adrenoceptor blocking drug with combined alpha- and beta-blocking properties. These result in a more favourable haemodynamic profile for labetalol compared with 'pure' beta-blockers or pure alpha-blockers, but also contribute to a wider range, but not an overall increased incidence, of adverse effects. The drug is effective and well-tolerated in patients with all grades of hypertension, but is of particular value in special subgroups such as Black patients, the elderly and patients with renal hypertension. While comparative studies are not extensive, available data show that the drug reduces blood pressure to a similar extent, and in a similar proportion of patients, as 'pure' beta-blockers such as propranolol, pure alpha-blockers such as prazosin, calcium antagonists (nifedipine, verapamil), and centrally acting drugs (clonidine and methyldopa). Labetalol is very effective in hypertensive pregnant women and in hypertensive crises, where it provides good control of blood pressure without serious adverse effects, and where few therapeutic options exist. Few controlled studies have investigated the use of labetalol in deliberate induction of hypotension or prevention of hypertension during anaesthesia, and also in patients with ischaemic heart disease. However, available evidence suggests a role for labetalol in these indications and further studies should aid in clarification of its efficacy in these areas. Thus, with its broad scope of therapeutic use in hypertension labetalol remains an important therapeutic option, and the drug may well find an additional place in the treatment of myocardial ischaemia if further evidence confirms encouraging preliminary findings.
自拉贝洛尔于1978年首次在本刊发表综述以来，其治疗用途范围不断扩大且定义更加明确。拉贝洛尔是一种具有α和β受体阻滞双重特性的肾上腺素能受体阻滞剂。与“单纯”β受体阻滞剂或单纯α受体阻滞剂相比，这些特性使拉贝洛尔具有更有利的血流动力学特征，但也导致不良反应的范围更广，不过总体发生率并未增加。该药物对各级高血压患者均有效且耐受性良好，但在特殊亚组如黑人患者、老年人及肾性高血压患者中具有特殊价值。虽然比较研究并不广泛，但现有数据表明，该药物降低血压的程度和比例与“单纯”β受体阻滞剂如普萘洛尔、单纯α受体阻滞剂如哌唑嗪、钙拮抗剂（硝苯地平、维拉帕米）及中枢作用药物（可乐定和甲基多巴）相似。拉贝洛尔对高血压孕妇和高血压危象非常有效，能很好地控制血压且无严重不良反应，而此时治疗选择很少。很少有对照研究调查拉贝洛尔在麻醉期间用于故意诱导低血压或预防高血压以及在缺血性心脏病患者中的应用。然而，现有证据表明拉贝洛尔在这些适应证中具有一定作用，进一步研究应有助于明确其在这些领域的疗效。因此，鉴于拉贝洛尔在高血压治疗中广泛的治疗用途，它仍然是一种重要的治疗选择，如果进一步证据证实初步的令人鼓舞的发现，该药物很可能在心肌缺血治疗中找到新的应用领域。
