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Preservative toxicity in glaucoma medication: clinical evaluation of benzalkonium chloride-free 0.5 timolol eye drops

机译:青光眼药物的防腐毒性:不含苯扎氯铵的0.5%噻吗洛尔滴眼液的临床评价

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摘要

Timolol (generic name) is a frequently used medication for the control of glaucoma. Benzalkonium chloride (BAK) is a commonly used preservative in ophthalmic solutions with a broad range of antimicrobial activity; however, this nonspecificity can result in toxicity. Adverse effects attributed to BAK, including conjunctival inflammation and fibrosis, tear film instability, corneal cytotoxicity, anterior chamber inflammation, trabecular meshwork cell apoptosis, cataract development, macular edema, and even systemic effects, have been well documented. These effects can lead to ocular discomfort, poor intraocular pressure control, glaucoma surgery failure, and decreased patient compliance. BAK use in topical medications has decreased recently as newer and less toxic preservatives have become available. Yet these preservatives still exert some toxic effects, especially in patients with chronic eye disease who use multiple drops over extended periods of time. Thus, attempts to reduce overall preservative loads for patients are important, whether it be decreasing the amount of preservative, decreasing the total number of drops patients use, or eliminating preservatives entirely. A preservative-free formulation of timolol, TIMOPTIC® in OCUDOSE®, is available in unit-dose vials. Preservative-free unit-dose vials minimize toxic adverse effects and are a good option for patients with ocular surface disease, on long-term multidrop therapy, or who simply do not tolerate the effects of preservatives due to discomfort.
机译:替米洛尔(通用名)是控制青光眼的常用药物。苯扎氯铵(BAK)是眼科溶液中常用的防腐剂,具有广泛的抗菌活性;但是,这种非特异性会导致毒性。众所周知,BAK的不良反应包括结膜炎症和纤维化,泪膜不稳定,角膜细胞毒性,前房炎症,小梁网细胞凋亡,白内障发展,黄斑水肿,甚至全身性作用。这些影响会导致眼部不适,眼内压控制不良,青光眼手术失败和患者顺应性下降。随着新型和毒性较小的防腐剂的问世,BAK在局部药物中的使用近来有所减少。然而,这些防腐剂仍具有一定的毒性作用,特别是对于长期使用多滴眼药的慢性眼病患者。因此,减少患者总体防腐剂负荷的尝试很重要,无论是减少防腐剂的用量,减少患者使用的滴剂总数还是完全消除防腐剂。蒂莫洛尔的无防腐剂TIMOPTIC®inOCUDOSE®可在单位剂量的药瓶中使用。不含防腐剂的单位剂量药水瓶可最大程度地减少毒副作用,对于长期接受多滴治疗或因不适而不能耐受防腐剂作用的眼表疾病患者而言,是一个不错的选择。

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