降眼内压药消旋噻吗心安的药理研究

摘要: 用国产0.5%消旋噻吗心安与同浓度国外左旋品相比较,前者降眼内压药效可达后者86%;与国产(江苏医药工业研究所合成)左旋品比较,消旋品药效可达95%。用两种家免模型进行试验,结果基本一致。根据消旋品的浓度效应曲线,可以配制与现有左旋品制剂药效相同的消旋品制剂。经 LD_(50)测定,消旋品的静注及口服急性毒性分别比国产左旋品低15%及32%。对眼结膜的急性和亚急性刺激性试验,未发现消旋品对眼结膜的刺激性。考虑到消旋品的β阻断副作用较轻,且价格低廉,因此认为用消旋品代替左旋品作为眼科用药具有其特有的优点。

Abstract: The effect of (±)timolol and (—) timolol were compared after topical administration in water loaded and anesthetized normotensive rabbits. (±) Timolol had about 86-95% potency of lowering the intraocular pressure as compared with(-)timolol. The i.v. and p. o. LD50 in mouse of (±)timolol were 15% and 32% larger than that of (—) timolol respectively. Application of (±) timolol eye drops for two weeks did not exhibit any local irritation in eyes. Experiment data indicated that application of (±) timolol in treatment of glaucoma might be promising.