Gunning F P, Greve E L, Bron A M, Bosc J M, Royer J G, George J L, Lesure P, Sirbat D
Glaucoma Center, Academic Medical Center, Amsterdam, The Netherlands.
Graefes Arch Clin Exp Ophthalmol. 1993 Jul;231(7):384-8. doi: 10.1007/BF00919645.
The ocular hypotensive activities of the two potent topical carbonic anhydrase inhibitors sezolamide (previously known as MK-417) and dorzolamide (previously known as MK-507 and L-671,152) were compared formulated in Gelrite vehicle, a novel ophthalmic drug delivery system. This was a four-center, double-blind, randomized, placebo-controlled, parallel study in 73 patients with a diagnosis of bilateral primary open-angle glaucoma or ocular hypertension and a morning intraocular pressure (IOP) of greater than 23 mmHg in both eyes following washout of ocular hypotensive medications. Parallel 12-h modified diurnal curves were performed prestudy and on day 6, with a 4-h IOP curve on day 1. On day 6 the peak mean percentage decrease in IOP from baseline occurred 4 h after the dose of dorzolamide (22.1%) and 6 h after the dose of sezolamide (21.3%). There were no significant differences between 2% dorzolamide and 1.8% sezolamide at any time point, although the decrease in IOP for sezolamide tended to be slightly greater than that for dorzolamide. Duration of action of both compounds was, at most, slightly prolonged by the use of Gelrite vehicle when compared with former studies on sezolamide and dorzolamide.
在一种新型眼科药物递送系统Gelrite载体中，比较了两种强效局部碳酸酐酶抑制剂西佐胺（以前称为MK-417）和多佐胺（以前称为MK-507和L-671,152）的降眼压活性。这是一项四中心、双盲、随机、安慰剂对照的平行研究，纳入73例诊断为双侧原发性开角型青光眼或高眼压症的患者，在停用降眼压药物后，双眼早晨眼压（IOP）均大于23 mmHg。在研究前和第6天进行平行的12小时改良昼夜曲线测量，第1天进行4小时眼压曲线测量。在第6天，多佐胺给药后4小时眼压从基线下降的平均峰值百分比为22.1%，西佐胺给药后6小时为21.3%。在任何时间点，2%多佐胺和1.8%西佐胺之间均无显著差异，尽管西佐胺的眼压下降幅度往往略大于多佐胺。与以前关于西佐胺和多佐胺的研究相比，使用Gelrite载体时，两种化合物的作用持续时间至多略有延长。
