Frampton James E
Wolters Kluwer Health, Adis, Auckland, New Zealand.
Drugs Aging. 2006;23(9):753-61. doi: 10.2165/00002512-200623090-00005.
A fixed combination of brimonidine (a highly selective alpha(2)-adrenergic agonist) and timolol (a non-selective beta-blocker) [brimonidine 0.2%/timolol 0.5% ophthalmic solution; brimonidine/timolol] is available for the topical treatment of glaucoma and ocular hypertension (OH). Brimonidine and timolol decrease elevated intraocular pressure (IOP) by complementary mechanisms of action and have an additive effect when coadministered to healthy volunteers and patients with glaucoma or OH. When assessed over a 3- or 12-month period in large, well designed clinical studies, brimonidine/timolol instilled twice daily (one drop in each eye) was superior to monotherapy with the individual components instilled two (brimonidine) or three (timolol) times daily, and noninferior to concomitant therapy with the individual components instilled twice daily, in lowering raised IOP in patients with glaucoma or OH. In small, randomised, comparative studies of 1 or 3 months' duration, the IOP-lowering effect of brimonidine/timolol twice daily was similar or superior to that of fixed combination dorzolamide 2%/timolol 0.5% ophthalmic solution (dorzolamide/timolol) twice daily (preliminary data). Brimonidine/timolol is generally well tolerated with a predictable local and systemic adverse event profile based on that of the individual components used alone and concomitantly. No unexpected or serious adverse events associated with the fixed combination were reported in key clinical trials. Brimonidine/timolol may be advantageous over dorzolamide/timolol with respect to ocular tolerability and comfort (preliminary data).
溴莫尼定(一种高选择性α₂肾上腺素能激动剂)和噻吗洛尔(一种非选择性β受体阻滞剂)的固定组合[溴莫尼定0.2%/噻吗洛尔0.5%滴眼液;溴莫尼定/噻吗洛尔]可用于局部治疗青光眼和高眼压症(OH)。溴莫尼定和噻吗洛尔通过互补的作用机制降低升高的眼压(IOP),在健康志愿者以及青光眼或高眼压症患者中联合使用时具有相加效应。在大型、设计良好的临床研究中,对患者进行3个月或12个月的评估时,每天两次(每只眼睛滴一滴)滴注溴莫尼定/噻吗洛尔,在降低青光眼或高眼压症患者升高的眼压方面,优于每天两次(溴莫尼定)或三次(噻吗洛尔)滴注单一成分的单药治疗,且不劣于每天两次滴注单一成分的联合治疗。在为期1个月或3个月的小型随机对照研究中,每天两次滴注溴莫尼定/噻吗洛尔的降眼压效果与每天两次滴注2%多佐胺/0.5%噻吗洛尔滴眼液(多佐胺/噻吗洛尔)相似或更优(初步数据)。基于单独使用和联合使用的单一成分的情况,溴莫尼定/噻吗洛尔通常耐受性良好,具有可预测的局部和全身不良事件谱。在关键临床试验中未报告与该固定组合相关的意外或严重不良事件。在眼部耐受性和舒适度方面,溴莫尼定/噻吗洛尔可能优于多佐胺/噻吗洛尔(初步数据)。