Scott B T
Optometry Clinic, West Roxbury VA Medical Center, Massachusetts.
Optom Vis Sci. 1994 May;71(5):332-8. doi: 10.1097/00006324-199405000-00005.
Systemically administered carbonic anhydrase inhibitors lower intraocular pressure (IOP) by decreasing aqueous production. Their clinical usefulness is limited, however, because they often cause ill-tolerated side effects, and on occasion may be associated with serious adverse reactions. In the past, attempts at topical formulations of carbonic anhydrase inhibitors did not achieve desired results. Recent modifications to improve pharmacokinetics have lead to the development of topical carbonic anhydrase inhibitors that decrease IOP with minimal side effects. Thus, this class of drugs may soon become an additional therapy for treating open-angle glaucoma. This paper discusses the development of topical carbonic anhydrase inhibitors, including both unsuccessful and promising endeavors. It also summarizes the current understanding of the chemistry, mechanisms of action, pharmacokinetics, and side effects of these future glaucoma therapy adjuvants.
全身给药的碳酸酐酶抑制剂通过减少房水生成来降低眼压(IOP)。然而,它们的临床应用受到限制,因为它们常常会引起难以耐受的副作用,有时还可能与严重不良反应相关。过去,碳酸酐酶抑制剂局部用药制剂的尝试未取得理想效果。近期为改善药代动力学所做的改进已促成局部碳酸酐酶抑制剂的研发,这类抑制剂能以最小的副作用降低眼压。因此,这类药物可能很快会成为治疗开角型青光眼的一种额外疗法。本文讨论了局部碳酸酐酶抑制剂的研发情况,包括未成功的和有前景的尝试。它还总结了目前对这些未来青光眼治疗辅助药物的化学性质、作用机制、药代动力学及副作用的认识。