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

青光眼药物中防腐剂的毒性: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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Abstract

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.

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