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拉坦前列素。原发性开角型青光眼和高眼压症治疗中其药理特性、临床疗效及耐受性的综述。

Latanoprost. A review of its pharmacological properties, clinical efficacy and tolerability in the management of primary open-angle glaucoma and ocular hypertension.

作者信息

Patel S S, Spencer C M

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs Aging. 1996 Nov;9(5):363-78. doi: 10.2165/00002512-199609050-00007.

Abstract

Latanoprost is an ester prodrug analogue of prostaglandin F2 alpha which effectively reduces intraocular pressure (IOP) by increasing uveoscleral outflow rather than altering conventional trabeculo-canalicular) aqueous outflow. The IOP-lowering effect of latanoprost lasts for 20 to 24 hours after a single dose, which allows a single daily dosage regimen. Data from 4 randomised double-masked multicentre studies indicate that a once daily dose of topical latanoprost 0.005% is as effective as timolol 0.5% twice daily in the treatment of patients with primary open-angle glaucoma or ocular hypertension. A number of studies also demonstrate that latanoprost enhances IOP-lowering effects when applied in combination with other antiglaucoma agents. Latanoprost is well tolerated with no, or barely detectable, conjunctival hyperaemia, and, unlike timolol, is not associated with systemic adverse effects. However, 3 to 10% of patients treated with latanoprost 0.005% have shown increased iris pigmentation after 3 to 4.5 months' treatment. In summary, the available data show that latanoprost is a potent IOP-lowering agent with a number of positive features including a single daily dosage regimen, a novel mechanism of action that enhances the IOP-lowering effect of contemporary agents, and a lack of systemic adverse effects. These properties suitably poise latanoprost for a prominent position in the management of patients with primary open-angle glaucoma and ocular hypertension.

摘要

拉坦前列素是前列腺素F2α的酯前药类似物,它通过增加葡萄膜巩膜外流而非改变传统的小梁-小管房水外流来有效降低眼压(IOP)。单次给药后,拉坦前列素的降眼压作用可持续20至24小时,这使得可以采用每日一次的给药方案。来自4项随机双盲多中心研究的数据表明,每日一次局部应用0.005%的拉坦前列素在治疗原发性开角型青光眼或高眼压症患者方面与每日两次应用0.5%的噻吗洛尔效果相当。多项研究还表明,拉坦前列素与其他抗青光眼药物联合应用时可增强降眼压效果。拉坦前列素耐受性良好,无结膜充血或仅有轻微的结膜充血,而且与噻吗洛尔不同,它不会引起全身不良反应。然而,接受0.005%拉坦前列素治疗的患者中有3%至10%在治疗3至4.5个月后出现虹膜色素沉着增加。总之,现有数据表明,拉坦前列素是一种强效降眼压药物,具有许多积极特性,包括每日一次的给药方案、一种可增强当代药物降眼压效果的新作用机制以及无全身不良反应。这些特性使拉坦前列素在原发性开角型青光眼和高眼压症患者的治疗中占据显著地位。

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