Beresford R, Heel R C
Drugs. 1986 Jan;31(1):6-28. doi: 10.2165/00003495-198631010-00002.
Betaxolol is a relatively cardioselective beta-adrenoceptor blocking drug, with no partial agonist (intrinsic sympathomimetic) activity and weak membrane-stabilising (local anaesthetic) activity. Its pharmacokinetic properties of most interest include high bioavailability after oral administration, and a long elimination half-life. It has a narrow dose-response range, which obviates the need for dose titration, with 10 to 20 mg once daily being the usual dosage. This dose reduces systolic and diastolic blood pressures by about 15 mm Hg in most patients with mild to moderate hypertension. In a few comparative studies betaxolol 20 mg daily was as effective as atenolol and moderate doses of propranolol, and more effective than acebutolol, in reducing blood pressure in such patients. Betaxolol has been well tolerated in most patients. Thus, betaxolol is an effective alternative to other beta-blocking drugs in patients with essential hypertension, with properties that may offer advantages in some patients.
倍他洛尔是一种相对具有心脏选择性的β-肾上腺素受体阻断药，无部分激动剂（内在拟交感神经）活性，膜稳定（局部麻醉）活性较弱。其最受关注的药代动力学特性包括口服给药后生物利用度高，消除半衰期长。它的剂量反应范围较窄，无需进行剂量滴定，通常剂量为每日一次10至20毫克。该剂量可使大多数轻度至中度高血压患者的收缩压和舒张压降低约15毫米汞柱。在一些比较研究中，每日20毫克倍他洛尔在降低此类患者血压方面与阿替洛尔和中等剂量的普萘洛尔效果相当，且比醋丁洛尔更有效。大多数患者对倍他洛尔耐受性良好。因此，倍他洛尔是原发性高血压患者的一种有效替代其他β受体阻断药的药物，其特性可能在某些患者中具有优势。
