Latanoprost in the treatment of glaucoma.
Latanoprost in the treatment of glaucoma.
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DOI：
10.2147/opth.s59162
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发表时间：
2014
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通讯作者：
Alm A
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作者：
Alm A
前列腺素被欧洲青光眼协会指南批准为青光眼的一线治疗药物。本文重点介绍拉坦前列素，前列腺素(PG)F2α的酯前体药，它是目前可用于治疗青光眼或高眼压的第一个外用前列腺素F2α类似物，目前仍占处方的大部分。它比母体化合物更好地通过角膜吸收，活性药物的峰值浓度在局部给药(15-30 ng/mL)后1-2小时出现在房水中。新陈代谢主要发生在肝脏。拉坦前列素(0.005%)已经在临床试验和荟萃分析中得到了很好的研究，这些研究表明，它与其他PG类似物(比马前列酮、曲伏前列素和他氟前列素)一般一样有效，比噻吗洛尔、多唑胺和布里莫尼定更有效。拉坦前列素具有良好的短期和长期安全性和耐受性。与其他前列腺素一样，它缺乏全身性作用，但可导致眼部不良事件，如结膜充血、虹膜色素沉着、眼周皮肤或睫毛、多毛症、眼表影响或刺激。拉坦前列素的耐受性明显好于比马前列素或曲伏前列素。与服用其他药物的患者相比，接受拉坦前列素治疗的患者依从性更好，持续治疗的时间更长。最近开发了一种不含防腐剂苯扎氯铵的拉坦前列素的改进配方。它与传统的拉坦前列素一样有效，充血发生率较低，可以在室温下储存。综上所述，拉坦前列素是治疗青光眼的PG类似物中最好的疗效耐受率，并且具有良好的依从性和持久性。这些因素应该通过无防腐剂拉坦前列素的最新开发来进一步改善。
Prostaglandins are approved by the European Glaucoma Society guidelines as first-line treatment for glaucoma. This review focuses on latanoprost, an ester prodrug of prostaglandin (PG) F2α, which was the first of the currently available topical PGF2α analogs to be launched for glaucoma or ocular hypertension and which still accounts for the majority of prescriptions. It is better absorbed than the parent compound through the cornea, and peak concentration of the active drug is in the aqueous humor 1–2 hours after topical dosing (15–30 ng/mL). Metabolism occurs mainly in the liver. Latanoprost (0.005%) has been very well studied in clinical trials and meta-analyses that show it to be generally as effective as the other PG analogs (bimatoprost, travoprost, and tafluprost) and more effective than timolol, dorzolamide, and brimonidine. Latanoprost has good short- and long-term safety and tolerability profiles. In common with other prostaglandins, it lacks systemic effects, but can cause ocular adverse events such as conjunctival hyperemia, pigmentation of the iris, periocular skin or eyelashes, hypertrichosis, and ocular surface effects or irritation. Latanoprost is significantly better tolerated than either bimatoprost or travoprost. Patients treated with latanoprost have better compliance and persist with therapy longer than those that are given other drugs. An improved formulation of latanoprost without the preservative benzalkonium chloride has recently been developed. It is as effective as conventional latanoprost, has a lower incidence of hyperemia, and can be stored at room temperature. In conclusion, latanoprost has the best efficacy–tolerability ratio of the PG analogs available for glaucoma treatment, and has good compliance and persistence. These factors should be improved further by the recent development of preservative-free latanoprost.