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噻吗洛尔:其药理特性及在心绞痛和高血压治疗中的疗效初步报告。

Timolol: a preliminary report of its pharmacological properties and therapeutic efficacy in angina and hypertension.

作者信息

Brogden R N, Speight T M, Avery G S

出版信息

Drugs. 1975;9(3):164-77. doi: 10.2165/00003495-197509030-00002.

Abstract

Timolol (MK 950) is a new beta-adrenergic receptor blocking drug. It has little or no membrane stabilising ('quinidine-like') or partial agonist (intrinsic sympathomimetic) activity and thus resembles sotalol. On a weight for.weight basis, timolol is more potent than sotalol or propranolol. A 2.5 mg dose of timolol causes about the same reduction in resting heart rate as 20mg of propranolol. Results of placebo-controlled and of comparative trials with other beta-adrenergic receptor blocking drugs, have shown that timolol effectively lowers blood pressure without producing orthostatic or exercise hypotension. Findings of an international multicentre trial in angina pectoris, indicate that timolol is effective in reducing the frequency of anginal attacks and the consumption of glyceryl trinitrate for their relief.

摘要

噻吗洛尔(MK 950)是一种新型β-肾上腺素能受体阻滞剂。它几乎没有或完全没有膜稳定作用(“奎尼丁样”)或部分激动剂(内在拟交感神经)活性,因此与索他洛尔相似。按重量计算,噻吗洛尔比索他洛尔或普萘洛尔更有效。2.5毫克剂量的噻吗洛尔降低静息心率的程度与20毫克普萘洛尔大致相同。安慰剂对照试验以及与其他β-肾上腺素能受体阻滞剂的对比试验结果表明,噻吗洛尔能有效降低血压,且不会引起体位性或运动性低血压。一项关于心绞痛的国际多中心试验结果表明,噻吗洛尔可有效减少心绞痛发作的频率以及缓解心绞痛时硝酸甘油的消耗量。

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