PharmaLogic Development, Inc., San Rafael, CA, USA.
Department of Ophthalmology and Vision Science, School of Medicine, University of California, Davis, CA, USA.
J Clin Pharmacol. 2024 Sep;64(9):1068-1082. doi: 10.1002/jcph.2451. Epub 2024 May 6.
Treatment of ocular diseases presents unique challenges and opportunities for the clinician and for the clinical pharmacologist. Ophthalmic pharmaceuticals, typically given as liquids, require consideration of solubility, physiological pH, and osmolarity, as well as sterility and stability, which in turn requires optimal pharmaceutics. Ocular tissue levels are challenging to obtain in humans, and the clinical pharmacokinetics is typically blood levels, which are primarily related to safety, rather than efficacy. The eye is a closed compartment with multiple physiological barriers with esterases and transporters, but relatively little cytochrome oxidases. Delivery routes include topical, intravitreal, and systemic. Patient dosing involves not only adherence issues common to all chronic diseases, but also performance requirements on eye drop instillation. Therapeutically, ocular diseases and their pharmacological treatments include both those analogous to systemic diseases (e.g., inflammation, infection, and neuronal degeneration) and those unique to the eye (e.g., cataract and myopia).
治疗眼部疾病对临床医生和临床药理学家来说都具有独特的挑战和机遇。眼科药物通常为液体剂型，需要考虑溶解度、生理 pH 值和渗透压，以及无菌性和稳定性，这又需要最佳的药剂学。在人体中很难获得眼部组织水平，而临床药代动力学通常是血药水平，这主要与安全性相关，而不是疗效相关。眼睛是一个封闭的腔室，有多个生理屏障，包括酯酶和转运体，但相对较少的细胞色素氧化酶。给药途径包括局部、玻璃体内和全身给药。患者用药不仅涉及所有慢性病常见的依从性问题，还涉及滴眼剂滴注的操作要求。在治疗方面，眼部疾病及其药物治疗包括与全身疾病类似的疾病（例如炎症、感染和神经元变性），以及眼部特有的疾病（例如白内障和近视）。
