Levy O, Labbé A, Borderie V, Laroche L, Bouheraoua N
Service d'ophtalmologie 5, centre hospitalier national d'ophtalmologie des Quinze-Vingts, 28, rue de Charenton, 75012 Paris, France; Université Pierre-et-Marie-Curie, Paris VI, 75012 Paris, France.
Université Pierre-et-Marie-Curie, Paris VI, 75012 Paris, France; Service d'ophtalmologie 3, centre hospitalier national d'ophtalmologie des Quinze-Vingts, 28, rue de Charenton, 75012 Paris, France; Université de Versailles Saint-Quentin-en-Yvelines, 78000 Versailles-Saint-Quentin-en-Yvelines, France; Service d'ophtalmologie, hôpital Ambroise-Paré, AP-HP, 9, avenue Charles-De-Gaulle, 92100 Boulogne-Billancourt, France; Inserm, U968, 75012 Paris, France; Université UPMC Paris VI, UMR S 968, Institut de la Vision, 75012 Paris, France; CNRS, UMR 7210, 75012 Paris, France.
J Fr Ophtalmol. 2016 Mar;39(3):292-307. doi: 10.1016/j.jfo.2015.11.008. Epub 2016 Mar 17.
Cyclosporine A (CsA) is a cyclic undecapeptide, which is an immunosuppressive drug in the calcineurin inhibitor class. CsA was initially used as a systemic immunosuppressant to minimize rejection of solid organ transplants. In ophthalmology, topically applied CsA was first used to inhibit corneal allograft rejection in the 1980s and later in various inflammatory ocular surface disorders (OSD). Currently, topical ophthalmic CsA is available as a licensed commercial emulsion or is prepared by hospital pharmacies with concentration ranging from 0.05 to 2%. Many of its pharmacological effects on the ocular surface are direct consequences of its ability to inhibit T ciclosporine activation and apoptosis. Topical CsA differs from topical steroids in its favourable local and systemic tolerability at the concentrations used. Most clinical studies have evaluated topical CsA in moderate to severe dry eye disease (DED) and demonstrated its efficacy for improvement of signs and symptoms, thus providing the sole indication for market approval and treatment protocols. For the other indications - corneal graft rejection, blepharitis, allergic or viral keratitis, and ocular surface disease due to graft versus host disease or post-operative DED - evidence-based medicine remains unclear due to the lack of major randomized controlled trials. Despite the lack of standardized protocols or market approval for these conditions, numerous studies suggest clinical efficacy.
环孢素A（CsA）是一种环状十一肽，属于钙调神经磷酸酶抑制剂类免疫抑制药物。CsA最初用作全身免疫抑制剂，以尽量减少实体器官移植的排斥反应。在眼科领域，局部应用的CsA于20世纪80年代首次用于抑制角膜移植排斥反应，后来用于各种炎症性眼表疾病（OSD）。目前，局部用眼科CsA有已获许可的商业乳剂形式，或由医院药房配制，浓度范围为0.05%至2%。它对眼表的许多药理作用是其抑制T细胞激活和凋亡能力的直接结果。局部用CsA在所用浓度下具有良好的局部和全身耐受性，这与局部用类固醇不同。大多数临床研究评估了局部用CsA在中重度干眼症（DED）中的应用，并证明其对改善体征和症状有效，从而为市场批准和治疗方案提供了唯一依据。对于其他适应症——角膜移植排斥反应、睑缘炎、过敏性或病毒性角膜炎，以及移植物抗宿主病或术后DED引起的眼表疾病——由于缺乏大型随机对照试验，循证医学证据仍不明确。尽管针对这些病症缺乏标准化方案或市场批准，但众多研究表明其具有临床疗效。
