Springer, Private Bag 65901, Mairangi Bay 0754, Auckland, New Zealand,
Drugs. 2015 May;75(8):911-22. doi: 10.1007/s40265-015-0409-7.
Diquafosol ophthalmic solution 3 % (Diquas(®)) is a P2Y2 receptor agonist that promotes tear fluid and mucin secretion and is currently approved in Japan and South Korea for the treatment of dry eye. In randomized, double-blind, multicentre trials in patients with dry eye, significantly greater improvements in fluorescein and rose bengal staining scores were seen with diquafosol ophthalmic solution 3 % than with placebo, and diquafosol ophthalmic solution 3 % was noninferior to sodium hyaluronate ophthalmic solution 0.1 % in terms of the improvement in the fluorescein staining score and more effective than sodium hyaluronate ophthalmic solution 0.1 % in terms of the improvement in the rose bengal staining score. The efficacy of diquafosol ophthalmic solution 3 % in the treatment of dry eye was maintained in the longer term, with improvements also seen in subjective dry eye symptoms, and was also shown in a real-world setting. Diquafosol ophthalmic solution 3 % also demonstrated efficacy in various specific dry eye disorders, including aqueous-deficient dry eye, short tear film break-up time dry eye, obstructive meibomian gland dysfunction, dry eye following laser in situ keratomileusis surgery and dry eye following cataract surgery, as well as in contact lens wearers and visual display terminal users. Diquafosol ophthalmic solution 3 % was generally well tolerated in patients with dry eye, with eye irritation the most commonly reported adverse event. In conclusion, diquafosol ophthalmic solution 3 % is a useful option for the treatment of dry eye.
3%地夸磷索滴眼溶液（Diquas(®)）是一种 P2Y2 受体激动剂，可促进泪液和黏液分泌，目前已在日本和韩国获批用于治疗干眼症。在干眼症患者的随机、双盲、多中心试验中，与安慰剂相比，3%地夸磷索滴眼溶液在改善荧光素和孟加拉玫瑰红染色评分方面有显著改善，且在改善荧光素染色评分方面非劣效于 0.1%玻璃酸钠滴眼溶液，在改善孟加拉玫瑰红染色评分方面优于 0.1%玻璃酸钠滴眼溶液。3%地夸磷索滴眼溶液治疗干眼症的疗效在长期内得以维持，且患者的主观干眼症状也有所改善，在真实环境中也观察到了该疗效。3%地夸磷索滴眼溶液还在各种特定的干眼症中显示出疗效，包括水液缺乏性干眼症、泪膜破裂时间短的干眼症、阻塞性睑板腺功能障碍、激光原位角膜磨镶术后干眼症和白内障手术后干眼症，以及接触镜佩戴者和视频显示终端使用者。3%地夸磷索滴眼溶液在干眼症患者中通常具有良好的耐受性，最常报告的不良事件是眼部刺激。总之，3%地夸磷索滴眼溶液是治疗干眼症的一种有效选择。
