Holló Gábor, Bozkurt Banu, Irkec Murat
Department of Ophthalmology, Semmelweis University, 1083 Budapest, Tömö U. 25-29, Hungary.
Expert Opin Pharmacother. 2009 Aug;10(12):2015-24. doi: 10.1517/14656560903124388.
For the treatment of open-angle glaucoma, the most frequent cause of irreversible visual loss, fixed combinations of different topical intraocular pressure (IOP) lowering molecules have gained an important role in recent years. The use of fixed combinations reduces the number of daily instillations, which promotes adherence to the prescribed medication and diminishes the exposition of the ocular surface to preservatives. The fixed combination of brinzolamide and timolol was recently approved by the European Medicines Agency (EMEA) and is now available in several countries in Europe. It contains two molecules widely used to treat glaucoma: timolol 0.5% (5 mg/ml) and brinzolamide 1% (10 mg/ml) in ophthalmic suspension formulation. This fixed combination is approved for twice-daily instillation to reduce elevated IOP in open-angle glaucoma and ocular hypertension. The brinzolamide/timolol fixed combination provides an approximately 30-33% IOP reduction from the untreated baseline IOP of 25-27 mmHg; thus, it is more potent than either of its ingredients alone. It is similarly effective but better tolerated than the dorzolamide/timolol fixed combination, which consists of molecules from the same pharmacological classes. The brinzolamide/timolol fixed combination can be used by itself as a separate therapy, but owing to the additivity of its ingredients to IOP-lowering drugs belonging to other classes, it may also be administered adjunctive to other IOP-reducing molecules, most importantly topical prostaglandin analogues. The ocular and systemic tolerance of the brinzolamide/ timolol fixed combination was reported favorable in Phase III studies, but no long-term clinical experience with this preparation is available at present.
对于开角型青光眼(不可逆视力丧失的最常见原因)的治疗,近年来,不同局部降眼压(IOP)分子的固定组合发挥了重要作用。使用固定组合可减少每日滴眼次数,这有助于提高对规定药物的依从性,并减少眼表接触防腐剂的机会。布林佐胺和噻吗洛尔的固定组合最近已获欧洲药品管理局(EMEA)批准,目前在欧洲多个国家上市。它含有两种广泛用于治疗青光眼的分子:0.5%(5mg/ml)噻吗洛尔和1%(10mg/ml)布林佐胺的眼用混悬液制剂。该固定组合被批准每日滴眼两次,以降低开角型青光眼和高眼压症患者升高的眼压。布林佐胺/噻吗洛尔固定组合可使眼压从未治疗时的25 - 27mmHg基线水平降低约30 - 33%;因此,其降眼压效果比单独使用任何一种成分都更强。它与多佐胺/噻吗洛尔固定组合效果相似,但耐受性更好,后者由同一药理类别的分子组成。布林佐胺/噻吗洛尔固定组合可单独作为一种治疗方法使用,但由于其成分与其他类别的降眼压药物具有相加作用,它也可与其他降眼压分子(最重要的是局部前列腺素类似物)联合使用。在III期研究中,布林佐胺/噻吗洛尔固定组合的眼内和全身耐受性表现良好,但目前尚无该制剂的长期临床经验。