Robin A L
Johns Hopkins University School of Medicine, Baltimore, MD 21209-2226, USA.
Curr Opin Ophthalmol. 1997 Apr;8(2):42-9. doi: 10.1097/00055735-199704000-00008.
alpha-Agonists are a relatively old class of medications, the topical use of which lowers eye pressure. Clonidine was introduced for this use in 1966, brimonidine in 1974, and apraclonidine in 1978. Initial short-term attempts to use clonidine were complicated by problems with systemic hypotension. Apraclonidine is more polar and less lipophilic than clonidine. This probably allows less penetration into both the posterior segment of the eye and systemic circulation, allowing for an excellent therapeutic index. The prophylactic use of apraclonidine (1% and 0.5%) has dramatically changed the safety profile for many anterior segment laser procedures, cataract surgery, and vitrectomy. The role of alpha-agonists in the chronic treatment of glaucoma is still uncertain. Potential benefits of additional lowering of intraocular pressure must be weighed against the following potential disadvantages: tachyphalaxsis, posterior segment vasoconstriction, psychologic depression and fatigue, syncope and systemic hypotension, and a topical allergy-like syndrome.
α-激动剂是一类相对古老的药物，局部使用可降低眼压。可乐定于1966年开始用于此用途，溴莫尼定于1974年，阿可乐定于1978年。最初使用可乐定的短期尝试因系统性低血压问题而变得复杂。阿可乐定比可乐定极性更强且亲脂性更低。这可能使得其较少渗透到眼后段和体循环中，从而具有出色的治疗指数。预防性使用阿可乐定（1%和0.5%）已显著改变了许多眼前节激光手术、白内障手术和玻璃体切除术的安全性。α-激动剂在青光眼慢性治疗中的作用仍不确定。眼压进一步降低带来的潜在益处必须与以下潜在缺点相权衡：快速耐受、眼后段血管收缩、心理抑郁和疲劳、晕厥和系统性低血压，以及局部过敏样综合征。
