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Over-the-Counter Ocular Decongestants in the United States – Mechanisms of Action and Clinical Utility for Management of Ocular Redness

机译:美国过度柜台上的眼镜剂 - 用于管理眼红的行动机制和临床效用

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To manage ocular redness effectively, health-care practitioners require an understanding of the pathophysiology, clinical features and differential diagnosis of ocular redness, as well as comprehensive knowledge of medical therapies available and their pharmacologic properties. This review aims to provide a clinically relevant summary of the current literature on the mechanism of action, efficacy, and safety of current over-the-counter (OTC) decongestants available for reduction of ocular redness due to minor irritations. Currently marketed OTC products indicated for such use in the United States include topical solutions of tetrahydrozoline 0.05%, naphazoline 0.012% to 0.03%, and brimonidine 0.025%. All 3 agents are adrenergic receptor agonists but vary in their receptor-binding profiles: tetrahydrozoline is a selective α 1 receptor agonist; naphazoline is a mixed α 1/α 2 receptor agonist; and brimonidine is a selective α 2 receptor agonist. These OTC decongestants produce vasoconstriction of conjunctival blood vessels, which results in a rapid reduction in ocular redness. In general, ocular adverse events reported in published studies of these OTC decongestants were minimal, mild, and transient, with no significant adverse systemic effects. However, ocular decongestants with α 1-adrenergic receptor agonist activity can be associated with loss of effectiveness with continued use (ie, tachyphylaxis) and rebound redness upon treatment discontinuation. In clinical trials of the selective α 2-adrenergic receptor agonist brimonidine 0.025%, tachyphylaxis was not observed, and rebound redness was rarely reported.
机译:为了有效地管理眼红,保健从业者需要了解眼红的病理生理学,临床特征和鉴别诊断,以及可用医疗治疗的全面知识及其药理学性质。该审查旨在提供目前关于当前文献的临床相关摘要,即当前的柜台(OTC)逆分体的动作,疗效和安全机制(OTC)因患者因轻微刺激而降低眼睛发红。目前销售的OTC产品在美国此类使用,包括四羟基唑啉的局部解决方案0.05%,甘唑啉0.012%至0.03%,二氧化碳辛0.025%。所有3种剂都是肾上腺素能受体激动剂,但在其受体结合谱中变化:四羟基唑啉是一种选择性α1受体激动剂;萘唑啉是混合α1/α2受体激动剂;和溴胺是一种选择性α2受体激动剂。这些OTC减料剂产生结膜血管的血管收缩,这导致眼红的快速降低。一般来说,在这些OTC减速物的公开研究中报告的眼部不良事件最小,轻度和瞬态,无明显不良全身效应。然而,具有α1-肾上腺素能受体激动剂活性的眼镜剂可以与持续使用的有效性丧失有关,并且治疗停止后反弹发红。在选择性α2-肾上腺素能受体激动剂溴胺的临床试验中,未观察到Tachyphylaxis,很少报道反弹发红。

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