Uchio Eiichi
Department of Ophthalmology, Fukuoka University School of Medicine, Fukuoka, Japan.
Clin Ophthalmol. 2008 Sep;2(3):525-31. doi: 10.2147/opth.s3294.
Olopatadine hydrochloride exerts a wide range of pharmacological actions such as histamine H(1) receptor antagonist action, chemical mediator suppressive action, and eosinophil infiltration suppressive action. Olopatadine hydrochloride 0.1% ophthalmic solution (Patanol((R))) was introduced to the market in Japan in October 2006. In a conjunctival allergen challenge (CAC) test, olopatadine hydrochloride 0.1% ophthalmic solution significantly suppressed ocular itching and hyperemia compared with levocabastine hydrochloride 0.05% ophthalmic solution, and the number of patients who complained of ocular discomfort was lower in the olopatadine group than in the levocabastine group. Conjunctival cell membrane disruption was observed in vitro in the ketotifen fumarate group, epinastine hydrochloride group, and azelastine hydrochloride group, but not in the olopatadine hydrochloride 0.1% ophthalmic solution group, which may potentially explain the lower discomfort felt by patients on instillation. Many other studies in humans have revealed the superiority of olopatadine 0.1% hydrochloride eye drops to several other anti-allergic eye drops. Overseas, olopatadine hydrochloride 0.2% ophthalmic solution for a once-daily regimen has been marketed under the brand name of Pataday((R)). It is expected that olopatadine hydrochloride ophthalmic solutions may be used in patients with a more severe spectrum of allergic conjunctival diseases, such as vernal keratoconjunctivitis or atopic keratoconjunctivitis, in the near future.
盐酸奥洛他定具有多种药理作用，如组胺H(1)受体拮抗作用、化学介质抑制作用和嗜酸性粒细胞浸润抑制作用。0.1%盐酸奥洛他定滴眼液（帕坦洛（R））于2006年10月在日本上市。在结膜过敏原激发（CAC）试验中，与0.05%盐酸左卡巴斯汀滴眼液相比，0.1%盐酸奥洛他定滴眼液能显著抑制眼部瘙痒和充血，且奥洛他定组主诉眼部不适的患者数量低于左卡巴斯汀组。在体外观察到富马酸酮替芬组、盐酸依匹斯汀组和盐酸氮卓斯汀组出现结膜细胞膜破坏，但0.1%盐酸奥洛他定滴眼液组未出现，这可能是患者滴药时不适感较低的潜在原因。许多其他人体研究表明，0.1%盐酸奥洛他定滴眼液优于其他几种抗过敏滴眼液。在海外，每日一次给药方案的0.2%盐酸奥洛他定滴眼液已以帕他迪（R）的品牌上市。预计在不久的将来，盐酸奥洛他定滴眼液可用于患有更严重过敏性结膜疾病谱的患者，如春季角结膜炎或特应性角结膜炎。
