Mulki L, Foster C S
Massachusetts Eye Research and Surgery Institution, Harvard Medical School, Boston, MA, USA.
Drugs Today (Barc). 2011 May;47(5):327-33. doi: 10.1358/dot.2011.47.5.1590791.
Uveitis is the third leading cause of preventable blindness in the U.S. Topical administration of corticosteroids remains the mainstay in the management of acute autoimmune anterior uveitis. Difluprednate 0.05% ophthalmic emulsion is a potent new topical corticosteroid that exhibits enhanced penetration, better bioavailability, rapid local metabolism and strong efficacy, with a low incidence of adverse effects. In June 2008, difluprednate ophthalmic emulsion 0.05% gained FDA approval in the U.S. for the treatment of postoperative ocular inflammation and pain. Recently, a multicenter, randomized clinical trial showed difluprednate to be noninferior to prednisolone acetate 1% dosed twice as often, the current standard of care for the acute management of endogenous uveitis in the U.S. Furthermore, difluprednate proved to have a comparable safety profile. Here, we review difluprednate pharmacokinetics, ocular indications, animal studies, as well as the results of the clinical trials conducted to date in the U.S.
葡萄膜炎是美国可预防失明的第三大主要原因。局部应用皮质类固醇仍然是急性自身免疫性前葡萄膜炎治疗的主要手段。0.05%的地氟泼尼龙眼用乳剂是一种强效的新型局部皮质类固醇，具有增强的穿透力、更好的生物利用度、快速的局部代谢和强大的疗效，且不良反应发生率低。2008年6月，0.05%的地氟泼尼龙眼用乳剂在美国获得FDA批准，用于治疗术后眼部炎症和疼痛。最近，一项多中心随机临床试验表明，地氟泼尼龙并不劣于1%醋酸泼尼松龙，后者给药频率为前者的两倍，而1%醋酸泼尼松龙是美国目前内源性葡萄膜炎急性治疗的标准护理药物。此外，地氟泼尼龙被证明具有相当的安全性。在此，我们综述地氟泼尼龙的药代动力学、眼部适应症、动物研究以及美国迄今为止进行的临床试验结果。
