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局部用眼科β受体阻滞剂:一项比较性综述。

Topical ophthalmic beta blockers: a comparative review.

作者信息

Zimmerman T J

机构信息

Department of Ophthalmology and Visual Sciences, University of Louisville School of Medicine, Kentucky Lions Eye Research Institute.

出版信息

J Ocul Pharmacol. 1993 Winter;9(4):373-84. doi: 10.1089/jop.1993.9.373.

Abstract

Topically administered beta blockers are the preferred medical therapy for glaucoma. These agents reduce intraocular pressure (IOP), thereby preventing damage to the optic nerve and the subsequent loss of vision. Timolol, betaxolol, levobunolol, metipranolol, and carteolol are the topical beta blockers available in the U.S. They have similar IOP-lowering efficacy, but differ in other pharmacological properties. Topically administered beta blockers are generally well tolerated. They undergo systemic absorption, however, and can adversely affect cardiovascular and bronchopulmonary function in patients with existing diseases such as heart failure, sinus bradycardia, chronic obstructive airways disease, or asthma. Betaxolol, which is beta 1-selective, and carteolol, which has intrinsic sympathomimetic activity (ISA), may have systemic tolerability profiles superior to the traditional nonselective, non-ISA beta blockers. These hypotheses require confirmation in controlled clinical trials. Local adverse effects associated with beta blockers include stinging, burning, red eye, itching, tearing and loss of corneal sensitivity. Stinging upon instillation is a particularly frequent finding with betaxolol (up to 30% to 40% of patients). Preliminary evidence suggests that carteolol has the best local tolerability profile of these drugs.

摘要

局部应用的β受体阻滞剂是青光眼的首选药物治疗方法。这些药物可降低眼压(IOP),从而防止对视神经的损害以及随后的视力丧失。噻吗洛尔、倍他洛尔、左布诺洛尔、美替洛尔和卡替洛尔是美国可用的局部β受体阻滞剂。它们降低眼压的疗效相似,但在其他药理特性上有所不同。局部应用的β受体阻滞剂通常耐受性良好。然而,它们会被全身吸收,并且可能对患有心力衰竭、窦性心动过缓、慢性阻塞性气道疾病或哮喘等现有疾病的患者的心血管和支气管肺功能产生不利影响。具有β1选择性的倍他洛尔和具有内在拟交感神经活性(ISA)的卡替洛尔,其全身耐受性可能优于传统的非选择性、无ISA的β受体阻滞剂。这些假设需要在对照临床试验中得到证实。与β受体阻滞剂相关的局部不良反应包括刺痛、烧灼感、眼红、瘙痒、流泪和角膜敏感性丧失。滴入时刺痛在倍他洛尔中尤为常见(高达30%至40%的患者)。初步证据表明,卡替洛尔在这些药物中具有最佳的局部耐受性。

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