Departments of Ophthalmology, Gifu University, Gifu *Osaka Medical College, Osaka daggerNiigata University daggerYamanashi Medical College paragraph signUniversity of Tokyo, Tokyo **Kobe University School of Medicine, Kobe daggerdaggerHiroshima University School of Medicine, Hiroshima double daggerdouble daggerKumamoto University the Divisions of Ophthalmology, section signAichi Prefectural Hospital ||University of Tokyo, Tokyo section sign section signDepartment of Agricultural Chemistry, Kinki University, Japan.
J Glaucoma. 1994 Winter;3(4):275-9.
We investigated the dose-response relationship of the intraocular pressure-lowering activity of dorzolamide, a novel topical carbonic anhydrase inhibitor previously known as MK-507. A double-masked, randomized, multicenter study of 113 patients with either primary open-angle glaucoma or ocular hypertension was conducted; dorzolamide (0.2, 0.5, 1, or 2%) was administered three times daily for 14 days. All of the dorzolamide concentrations substantially lowered intraocular pressure from baseline measurements. The percentage change in baseline intraocular pressure with 0.5, 1, and 2% dorzolamide 2, 4, and 6 h after dosing on day 14 ranged from 12.0 to 17.0% on average, which was greater than after treatment with 0.2% dorzolamide. No dose response was seen for 0.5, 1, or 2% dorzolamide. The most frequently reported ocular symptom was transient smarting, which occurred in 35.6-74.1% of every treatment group. Smarting and mild hyperemia were most frequent with 2% dorzolamide (74.1 and 18.5%, respectively). The present results indicate that the 0.5, 1, and 2% concentrations of dorzolamide are almost equally effective and that 2% concentrations may be less well-tolerated than 0.5 or 1% concentrations.
我们研究了一种新型局部碳酸酐酶抑制剂多佐胺（先前称为 MK-507）的降眼压活性的剂量反应关系。一项针对 113 例原发性开角型青光眼或高眼压症患者的双盲、随机、多中心研究进行了；多佐胺（0.2%、0.5%、1%或 2%）每天给药 3 次，共 14 天。所有多佐胺浓度均从基线测量值显著降低了眼压。第 14 天给药后 2、4 和 6 小时，0.5%、1%和 2%多佐胺的基线眼压的百分比变化平均为 12.0%至 17.0%，这大于 0.2%多佐胺的治疗效果。对于 0.5%、1%或 2%的多佐胺，未观察到剂量反应。最常报告的眼部症状是短暂刺痛，每个治疗组中有 35.6%-74.1%的患者出现这种症状。刺痛和轻度充血最常见于 2%多佐胺（分别为 74.1%和 18.5%）。目前的结果表明，0.5%、1%和 2%浓度的多佐胺几乎同样有效，并且 2%浓度可能不如 0.5%或 1%浓度耐受良好。
