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拉坦前列素:其在青光眼和高眼压症治疗中的应用进展

Latanoprost : an update of its use in glaucoma and ocular hypertension.

作者信息

Perry Caroline M, McGavin Jane K, Culy Christine R, Ibbotson Tim

机构信息

Adis International Limited, Mairangi Bay, Auckland, New Zealand.

出版信息

Drugs Aging. 2003;20(8):597-630. doi: 10.2165/00002512-200320080-00005.

Abstract

Latanoprost (Xalatan) is an ester analogue of prostaglandin F2alpha that reduces intraocular pressure (IOP) by increasing uveoscleral outflow. The IOP-lowering efficacy of latanoprost 0.005% lasts for up to 24 hours after a single topical dose, which allows for a once-daily dosage regimen. In patients with ocular hypertension or open-angle glaucoma, a single drop of latanoprost 0.005% solution (about 1.5 microg) administered topically once daily reduced diurnal IOP by 22 to 39% over 1 to 12 months' treatment in well-controlled trials; efficacy was maintained during treatment periods of up to 2 years. At this dosage, latanoprost was significantly more effective than timolol 0.5% twice daily in 3 of 4 large, double-blind, randomised studies, was generally as effective as bimatoprost or travoprost, and was significantly more effective than dorzolamide, brimonidine or unoprostone. Furthermore, in patients whose IOP was poorly controlled with timolol, switching to latanoprost monotherapy was at least as effective at lowering IOP as adding dorzolamide or pilocarpine to the regimen. Latanoprost has also shown significant additive effects when used in combination with one or more other glaucoma medications. The fixed combination of latanoprost plus timolol was significantly more effective than either of its individual components in two double-blind randomised studies and more effective than the fixed combination of dorzolamide and timolol in a 3-month, evaluator-masked study. Data in patients with angle-closure glaucoma are limited, but in patients with elevated IOP after undergoing iridotomy, latanoprost 0.005% once daily was significantly more effective than timolol 0.5% twice daily at reducing IOP over 12 weeks of treatment in a large double-blind, randomised study. Latanoprost is generally well tolerated and, unlike timolol, induces minimal systemic adverse events. In well-controlled, 6-month trials, the most commonly occurring drug-related ocular events in latanoprost recipients were mild to moderate conjunctival hyperaemia (3 to 15%) and iris colour change (2 to 9%); these seldom required patient withdrawal although the latter may be permanent. Latanoprost 0.005% as a single daily drop has shown good IOP-lowering efficacy in patients with open-angle glaucoma or ocular hypertension and does not produce the cardiopulmonary adverse effects associated with beta-blockers. Thus, latanoprost is a valuable addition to the first-line treatment options for patients with open-angle glaucoma or ocular hypertension. In addition, adjunctive treatment with latanoprost in patients who are refractory to beta-blocker therapy is a viable, second-line treatment option. Although preliminary findings are promising, wider clinical experience is required to define the place of latanoprost in the treatment of angle-closure glaucoma.

摘要

拉坦前列素(适利达)是前列腺素F2α的酯类类似物,通过增加葡萄膜巩膜外流来降低眼压(IOP)。0.005%的拉坦前列素单次局部给药后,其降眼压疗效可持续长达24小时,这使得可以采用每日一次的给药方案。在高眼压症或开角型青光眼患者中,在精心控制的试验中,每日一次局部给予一滴0.005%的拉坦前列素溶液(约1.5微克),在1至12个月的治疗期间,日间眼压降低了22%至39%;在长达2年的治疗期间疗效得以维持。在此剂量下,在4项大型双盲随机研究中的3项中,拉坦前列素比每日两次使用的0.5%噻吗洛尔显著更有效,通常与比马前列素或曲伏前列素效果相当,且比多佐胺、溴莫尼定或乌诺前列酮显著更有效。此外,对于眼压用噻吗洛尔控制不佳的患者,改用拉坦前列素单药治疗在降低眼压方面至少与在治疗方案中加用多佐胺或毛果芸香碱一样有效。拉坦前列素与一种或多种其他青光眼药物联合使用时也显示出显著的相加作用。在两项双盲随机研究中,拉坦前列素加噻吗洛尔的固定组合比其任何一种单独成分都显著更有效,并且在一项为期3个月、评估者盲法的研究中比多佐胺和噻吗洛尔的固定组合更有效。闭角型青光眼患者的数据有限,但在一项大型双盲随机研究中,在接受虹膜切开术后眼压升高的患者中,每日一次使用0.005%的拉坦前列素在12周的治疗期间比每日两次使用0.5%的噻吗洛尔在降低眼压方面显著更有效。拉坦前列素一般耐受性良好,与噻吗洛尔不同,它引起的全身不良事件极少。在精心控制的6个月试验中,接受拉坦前列素治疗的患者中最常发生的与药物相关的眼部事件是轻度至中度结膜充血(3%至15%)和虹膜颜色改变(2%至9%);这些很少需要患者停药,尽管后者可能是永久性的。每日一滴0.005%的拉坦前列素在开角型青光眼或高眼压症患者中显示出良好的降眼压疗效,并且不会产生与β受体阻滞剂相关的心肺不良反应。因此,拉坦前列素是开角型青光眼或高眼压症患者一线治疗选择中的一个有价值的补充。此外,对于β受体阻滞剂治疗无效的患者,用拉坦前列素进行辅助治疗是一种可行的二线治疗选择。尽管初步研究结果很有前景,但需要更广泛的临床经验来确定拉坦前列素在闭角型青光眼治疗中的地位。

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