Gupta S K, Agarwal R, Galpalli N D, Srivastava S, Agrawal S S, Saxena R
Delhi Institute of Pharmaceutical Sciences and Research, New Delhi, India.
Methods Find Exp Clin Pharmacol. 2007 Dec;29(10):665-71. doi: 10.1358/mf.2007.29.10.1147765.
Intraocular pressure (IOP)-lowering effects of investigational antiglaucoma drugs often need comparison with existing drugs, but detailed data showing comparative efficacy of antiglaucoma drugs with different mechanism of action has not been reported so far. This study was designed to establish baseline information of the IOP-lowering effect of three currently used antiglaucoma drugs in three experimental models in rabbits, so that they act as a benchmark for the efficacy evaluation of the future experimental antiglaucoma drugs. The IOP-lowering effect of single-drop application of pilocarpine, timolol and latanoprost was studied in normotensive, water loading and steroid-induced models of glaucoma in rabbits. The noncontact tonometer was used for the first time to estimate IOP in rabbits. The peak IOP-lowering effect of pilocarpine, timolol and latanoprost in normotensive rabbit eye was 18.23%, 20% and 22.56%, respectively. In water-loading model, the maximum protection against the rise in IOP was shown by latanoprost (40.27%), followed by timolol (31.39%) and pilocarpine (28.91%). In steroid-pretreated rabbit eyes, peak IOP-lowering effects of pilocarpine, timolol and latanoprost were 25.65%, 34.21% and 35.06%, respectively. Therefore, the latanoprost was found to be most effective in all three models followed by timolol and pilocarpine. The results of this study can be used for future preclinical investigations for the assessment of IOP-lowering activity of potential antiglaucoma drugs.
研究性抗青光眼药物的降眼压作用通常需要与现有药物进行比较,但目前尚未有详细数据显示不同作用机制的抗青光眼药物的比较疗效。本研究旨在建立三种目前使用的抗青光眼药物在兔的三种实验模型中的降眼压作用的基线信息,以便它们作为未来实验性抗青光眼药物疗效评估的基准。在兔的正常眼压、水负荷和类固醇诱导的青光眼模型中,研究了毛果芸香碱、噻吗洛尔和拉坦前列素单滴应用的降眼压作用。首次使用非接触眼压计估计兔的眼压。毛果芸香碱、噻吗洛尔和拉坦前列素在正常眼压兔眼中的最大降眼压作用分别为18.23%、20%和22.56%。在水负荷模型中,拉坦前列素对眼压升高的最大保护作用为40.27%,其次是噻吗洛尔(31.39%)和毛果芸香碱(28.91%)。在类固醇预处理的兔眼中,毛果芸香碱、噻吗洛尔和拉坦前列素的最大降眼压作用分别为25.65%、34.21%和35.06%。因此,发现拉坦前列素在所有三种模型中最有效,其次是噻吗洛尔和毛果芸香碱。本研究结果可用于未来评估潜在抗青光眼药物降眼压活性的临床前研究。