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β-肾上腺素能受体阻断药在甲状腺功能亢进症中的应用。

Use of beta-adrenoceptor blocking drugs in hyperthyroidism.

作者信息

Feely J, Peden N

出版信息

Drugs. 1984 May;27(5):425-46. doi: 10.2165/00003495-198427050-00003.

DOI:10.2165/00003495-198427050-00003
PMID:6144501
Abstract

There is an increasing use and variety of beta-adrenoceptor blocking agents (beta-blockers) available for the treatment of hyperthyroidism. Recent comparative studies suggest that atenolol (200mg daily), metoprolol (200mg daily); acebutolol (400mg daily), oxprenolol ( 160mg daily), nadolol ( 80mg daily) and timolol (20mg daily) produce a beneficial clinical response equal to that seen with propranolol ( 160mg daily). Most beta-blockers reduce resting heart rate by approximately 25 to 30 beats/min, although a lesser reduction is seen with those possessing intrinsic sympathomimetic activity such as oxprenolol and pindolol. While earlier studies employing large doses of intravenous propranolol concluded that beta-blockade reduced myocardial contractility, more recent non-invasive studies suggest that the predominant cardiac effect is on heart rate. In patients with cardiac failure, beta-blockers may, however, produce a profound fall in cardiac output. Nevertheless, in combination with digoxin they may be useful in controlling the atrial fibrillation of thyrocardiac disease. beta-Blockers improve nervousness and tremor (although to a lesser extent with cardioselective agents) and severe myopathy, and they also reduce the frequency of paralysis in patients with thyrotoxic periodic paralysis. There is often subjective improvement in sweating but usually no major effect on eye signs. Recent studies show a 10% reduction in oxygen consumption/basal metabolic rate with long term oral use of selective or nonselective beta-blockers. In addition, many agents (propranolol, metoprolol, nadolol and sotalol but not acebutolol, atenolol or oxprenolol) reduce circulating tri-iodothyronine (T3) concentration by between 10 and 40%, although the clinical significance of this effect (if any) is not established. beta-Blockers may also have endocrinological effects on gastrin, cyclic AMP, catecholamines and other hormone levels. Given in adequate dosage, propranolol has been shown to control thyrotoxic hypercalcaemia. Minor side effects (nausea, headaches, tiredness, etc.) are quite common but overall beta-blockers are well tolerated by the thyrotoxic patient. The major use of these drugs is in symptomatic control while awaiting definitive diagnosis or treatment. As an adjunct to antithyroid drugs or radioactive iodine, beta-blockers will produce a satisfactory clinical response in the weeks to months before these forms of therapy produce a euthyroid state. beta-Blockers are more convenient than antithyroid drugs in the control of patients receiving therapeutic radioiodine, in that continuous therapy and assessment of biochemical response is possible.(ABSTRACT TRUNCATED AT 400 WORDS)

摘要

用于治疗甲状腺功能亢进的β-肾上腺素能受体阻滞剂(β受体阻滞剂)的使用越来越广泛,种类也越来越多。最近的比较研究表明,阿替洛尔(每日200毫克)、美托洛尔(每日200毫克)、醋丁洛尔(每日400毫克)、氧烯洛尔(每日160毫克)、纳多洛尔(每日80毫克)和噻吗洛尔(每日20毫克)产生的有益临床反应与普萘洛尔(每日160毫克)相当。大多数β受体阻滞剂可使静息心率降低约25至30次/分钟,不过,具有内在拟交感活性的药物如氧烯洛尔和吲哚洛尔降低的幅度较小。虽然早期使用大剂量静脉注射普萘洛尔的研究得出结论,β受体阻滞会降低心肌收缩力,但最近的非侵入性研究表明,对心脏的主要作用是对心率的影响。然而,在心力衰竭患者中,β受体阻滞剂可能会使心输出量大幅下降。尽管如此,与地高辛联合使用时,它们可能有助于控制甲状腺性心脏病的房颤。β受体阻滞剂可改善紧张和震颤(尽管心脏选择性药物的改善程度较小)以及严重的肌病,还可减少甲状腺毒症性周期性麻痹患者的麻痹发作频率。出汗通常会有主观改善,但对眼部体征通常没有显著影响。最近的研究表明,长期口服选择性或非选择性β受体阻滞剂可使耗氧量/基础代谢率降低10%。此外,许多药物(普萘洛尔、美托洛尔、纳多洛尔和索他洛尔,但醋丁洛尔、阿替洛尔或氧烯洛尔除外)可使循环中的三碘甲状腺原氨酸(T3)浓度降低10%至40%,不过这种作用(如果有的话)的临床意义尚未确定。β受体阻滞剂对胃泌素、环磷酸腺苷、儿茶酚胺和其他激素水平也可能有内分泌作用。已证明,给予足够剂量的普萘洛尔可控制甲状腺毒症性高钙血症。轻微副作用(恶心、头痛、疲劳等)相当常见,但总体而言,甲状腺毒症患者对β受体阻滞剂耐受性良好。这些药物的主要用途是在等待明确诊断或治疗期间进行症状控制。作为抗甲状腺药物或放射性碘的辅助药物,在这些治疗方式使甲状腺功能恢复正常之前的数周或数月内,β受体阻滞剂将产生令人满意的临床反应。在控制接受治疗性放射性碘的患者方面,β受体阻滞剂比抗甲状腺药物更方便,因为可以进行持续治疗并评估生化反应。(摘要截选至400字)

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