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Topical ophthalmic NSAIDs: a discussion with focus on nepafenac ophthalmic suspension

机译:局部眼用非甾体抗炎药:以尼帕芬酸眼用混悬剂为重点的讨论

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摘要

The removal of diclofenac sodium ophthalmic solution as a viable pharmaceutical entity in September 1999 from the US market spurred considerable interest in the general safety and effectiveness of topical ophthalmic NSAIDs for treatment of anterior segment inflammation. In late 1999 the use of topical ocular NSAIDs declined in the US as a result of incidents involving corneal melts and toxicity surrounding use of generic diclofenac. However, since the removal of diclofenac sodium ophthalmic solution from the marketplace, ophthalmic NSAIDs have regained use as viable pharmacotherapeutic entities. Moreover, several new ophthalmic NSAID products have recently been introduced for commercial use in the US including the novel chemical entity nepafenac. The purpose of this report is to revisit the use of topical ophthalmic NSAIDs for the treatment of surgically induced anterior segment inflammation with a particular focus on nepafenac. Nepafenac is unique among ophthalmic NSAIDs in that it is a prodrug deaminated to amfenac, a highly effective non-selective cyclooxygenase inhibitor. In the case of topical ophthalmic NSAIDs, practitioners should carefully weigh the cost-benefit of implementing “highly potent” new drug products because perturbations in pharmacodynamic response due to the inherent novelty in terms of chemical designs may outweigh the demonstrated replicative pharmacologic action of all topical ophthalmic NSAIDs.
机译:1999年9月从美国市场上撤出双氯芬酸钠眼用溶液作为可行的药物实体,引起了人们对局部眼用NSAID治疗前段炎症的一般安全性和有效性的关注。在1999年末,由于涉及角膜融化和使用通用双氯芬酸的毒性事件,在美国局部使用眼用非甾体抗炎药的情况有所下降。然而,由于从市场上去除了双氯芬酸钠眼药水,眼科NSAIDs已经重新用作可行的药物治疗实体。此外,最近已经在美国引入了几种用于商业用途的新型眼科NSAID产品,包括新型化学实体奈帕芬酸。本报告的目的是重新探讨局部眼用NSAIDs在外科手术引起的前节段炎症的治疗中的应用,特别关注奈帕芬酸。 Nepafenac在眼用非甾体抗炎药中是独特的,因为它是一种与高效非选择性环氧化酶抑制剂amfenac脱氨基的前药。就局部眼用非甾体抗炎药而言,从业人员应仔细权衡实施“高效”新药的成本收益,因为化学设计固有的新颖性引起的药效学反应紊乱可能超过所有局部用药的已证实的复制药理作用。眼用非甾体抗炎药。

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