眼用-受体阻滞剂:比较回顾。

T J Zimmerman
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引用次数: 112

摘要

局部使用受体阻滞剂是青光眼的首选药物治疗。这些药物可降低眼压(IOP),从而防止视神经受损和随后的视力丧失。替马洛尔、倍他洛尔、左旋布诺尔、美特萘洛尔和卡替洛尔是在美国可用的外用β受体阻滞剂。它们具有相似的降低眼压的功效,但在其他药理特性上有所不同。局部使用受体阻滞剂通常耐受性良好。然而,它们会被全身吸收,并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疾病的患者的心血管和支气管肺功能产生不利影响。倍他洛尔具有β 1选择性,而卡替洛尔具有内在的拟交感神经活性(ISA),它们的系统耐受性可能优于传统的非选择性、非ISA β受体阻滞剂。这些假设需要在对照临床试验中得到证实。与受体阻滞剂相关的局部不良反应包括刺痛、灼烧、红眼、瘙痒、撕裂和角膜敏感性丧失。注射时刺痛是倍他洛尔特别常见的发现(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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Topical ophthalmic beta blockers: a comparative review.

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.

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