ABSTRACT

Introduction

Atropine is an old-known drug which is gaining increasing attention due to the myriad of therapeutic effects it may trigger on eye structures. Nevertheless, novel applications may require more adequate topical formulations.

Areas covered

This review aims to gather the existing knowledge about atropine and its clinical applications in the ophthalmological field when administered topically. Atropine ocular pharmacokinetics is paid a special attention, including recent evidences of the capability of the drug to access to the posterior segment. Ocular bioavailability and systemic bioavailability are counterbalanced. Finally, limitations of traditional dosage forms and potential advantages of under investigation delivery systems are analyzed.

Expert opinion

Mydriasis and cyclopegia have been widely exploited for eye examination, management of anterior segment diseases, and more recently as antidotes of chemical weapons. Improved knowledge on drug receptors and related pathways explains atropine repositioning as an outstanding tool to prevent myopia. The ease with which atropine penetrates ocular tissues is a double edged sword, that is, while it ensures therapeutic levels in the posterior segment, the unspecific distribution causes a wide variety of untoward effects. The design of formulations that can selectively deliver atropine to the target tissue for each specific application is an urgent unmet need.

中文翻译：

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用于治疗前段和后段眼部疾病的局部制剂中的阿托品

摘要

介绍

阿托品是一种古老的药物，由于它可能对眼睛结构产生无数的治疗作用，因此越来越受到关注。然而，新的应用可能需要更合适的局部制剂。

覆盖区域

本综述旨在收集有关阿托品及其在眼科领域局部应用的现有知识。阿托品眼部药代动力学受到特别关注，包括药物进入后段能力的最新证据。眼部生物利用度和全身生物利用度相互抵消。最后，分析了传统剂型的局限性和正在研究的递送系统的潜在优势。

专家意见

散瞳和散瞳已被广泛用于眼科检查、眼前节疾病的治疗，以及最近作为化学武器的解毒剂。对药物受体和相关途径的认识的提高解释了阿托品重新定位作为预防近视的杰出工具。阿托品容易穿透眼组织是一把双刃剑，也就是说，虽然它确保了后段的治疗水平，但非特异性分布会导致各种各样的不良影响。为每个特定应用设计可以选择性地将阿托品递送到目标组织的制剂是一个紧迫的未满足的需求。