de Arruda Mello Paulo Augusto, Yannoulis Natalia C, Haque Reza M
Department of Ophthalmology, Federal University of Sao Paulo-Paulista School of Medicine and Director Residency Training, Sao Paulo, Brazil.
Drug Saf. 2002;25(8):583-97. doi: 10.2165/00002018-200225080-00004.
This review summarises the safety of unoprostone isopropyl (both at the 0.12 and 0.15% concentrations) instilled twice daily in patients with primary open-angle glaucoma (POAG) or ocular hypertension (OH). For unoprostone 0.15%, combined data from two 12-month comparative monotherapy studies are reported, as well as data from three adjunctive therapy studies and two special population studies. With unoprostone monotherapy, most adverse events were mild or moderate and transient in nature. Less than 7% of unoprostone-treated patients discontinued therapy due to an adverse event. The most common adverse events associated with unoprostone were burning/stinging, burning/stinging directly upon drug instillation, ocular itching, and conjunctival hyperaemia. Unoprostone had no clinically notable effects on vital signs, laboratory profiles, or comprehensive ophthalmic examinations. One of 659 unoprostone 0.15%-treated patients had a change in iris colour after 12 months of monotherapy. Except for a higher incidence of burning/stinging and burning/stinging upon instillation, unoprostone was comparable to timolol 0.5% twice daily and betaxolol 0.5% twice daily. No safety concerns were raised with use of unoprostone as adjunctive therapy. Unoprostone had no significant effect on exercise-induced heart rate in healthy subjects or on pulmonary function in patients with mild-to-moderate asthma. The safety profile of unoprostone 0.15% was consistent with published information on the 0.12% formulation. In conclusion, unoprostone has an excellent safety profile in patients with POAG or OH.
本综述总结了原发性开角型青光眼（POAG）或高眼压症（OH）患者每日两次滴注异丙前列素（浓度为0.12%和0.15%）的安全性。对于0.15%的异丙前列素，报告了两项为期12个月的比较单一疗法研究的合并数据，以及三项辅助疗法研究和两项特殊人群研究的数据。使用异丙前列素单一疗法时，大多数不良事件性质轻微或中度且为短暂性。因不良事件而停止治疗的接受异丙前列素治疗的患者不到7%。与异丙前列素相关的最常见不良事件为烧灼感/刺痛感、滴药时直接出现的烧灼感/刺痛感、眼部瘙痒和结膜充血。异丙前列素对生命体征、实验室检查指标或全面眼科检查无临床上显著的影响。659例接受0.15%异丙前列素治疗的患者中有1例在单一疗法治疗12个月后虹膜颜色发生改变。除了滴注时烧灼感/刺痛感和烧灼感/刺痛感的发生率较高外，异丙前列素与每日两次使用的0.5%噻吗洛尔和每日两次使用的0.5%倍他洛尔相当。使用异丙前列素作为辅助疗法未引发安全担忧。异丙前列素对健康受试者运动诱发的心率或轻度至中度哮喘患者的肺功能无显著影响。0.15%异丙前列素的安全性与已发表的关于0.12%制剂的信息一致。总之，异丙前列素在POAG或OH患者中具有出色的安全性。
