Louis W J, Krum H, Conway E L
Department of Clinical Pharmacology and Therapeutics, Austin Hospital, Heidelberg, Victoria, Australia.
Drug Saf. 1994 Aug;11(2):86-93. doi: 10.2165/00002018-199411020-00003.
Carvedilol is a nonselective beta-adrenoceptor blocking vasodilator drug that may be a promising new agent in the management of cardiovascular disease. The rationale for the development of agents of this type is that the alpha-blocking component may overcome the direct vasoconstrictor consequence of beta 2-blockade, whilst the beta-blocker component may inhibit the reflex tachycardia that occurs following alpha-blockade. In clinical trials published to date, carvedilol has been demonstrated to be effective as an antihypertensive agent as monotherapy and also as additional therapy in those patients whose blood pressure cannot be controlled on other standard agents. It is also effective in the management of angina. Carvedilol has beneficial haemodynamic effects in patients with congestive heart failure. beta-Blocker vasodilator drugs of this type may be particularly useful in this condition as the vasodilator component of the drug may overcome the initial negative inotropy of the beta-blocker. In addition, carvedilol possess potentially useful pharmacological actions. In particular, the drug has antimitogenic and free radical scavenging effects that may make it a useful therapy in the long term management of atherosclerotic vascular disease. Its metabolic profile is also favourable, presumably on the basis of its alpha-blocking properties. Thus, beta 2-mediated adverse effects on peripheral vascular tone, glycaemic control and lipid status appear to be offset by the alpha-blocking property of the drug. Carvedilol thus far appears to be well tolerated, with postural dizziness the major adverse effect, especially in the elderly. As with nonselective beta-blockers, carvedilol is contraindicated in patients with asthma.
卡维地洛是一种非选择性β-肾上腺素受体阻断性血管扩张剂,可能是心血管疾病治疗中一种有前景的新药。开发这类药物的理论依据是,α阻断成分可克服β2阻断导致的直接血管收缩后果,而β阻断成分可抑制α阻断后出现的反射性心动过速。在迄今发表的临床试验中,已证明卡维地洛作为单一疗法的抗高血压药物有效,对于那些使用其他标准药物无法控制血压的患者,作为附加疗法也有效。它在心绞痛的治疗中也有效。卡维地洛对充血性心力衰竭患者有有益的血流动力学作用。这类β阻断性血管扩张剂在这种情况下可能特别有用,因为药物的血管扩张成分可克服β阻断剂最初的负性肌力作用。此外,卡维地洛具有潜在有用的药理作用。特别是,该药物具有抗有丝分裂和清除自由基的作用,这可能使其成为动脉粥样硬化性血管疾病长期治疗的有用疗法。其代谢情况也较好,大概是基于其α阻断特性。因此,药物的α阻断特性似乎抵消了β2介导的对外周血管张力、血糖控制和血脂状态的不良影响。到目前为止,卡维地洛似乎耐受性良好,体位性头晕是主要的不良反应,尤其是在老年人中。与非选择性β阻断剂一样,卡维地洛禁用于哮喘患者。