Abstract

Methotrexate (MTX) is a folate analog widely used against a range of diseases including malignancies and autoimmune disorders. Its high effectiveness-price ratio also won extensive application in ophthalmology. On the other hand, although MTX has an excellent pharmacological efficacy, MTX associated side effects in clinical use, which vary from patient to patient, are nonnegligible. There is no comparatively systematic review on MTX associated side effects and its risk factors. This review aimed to reveal novel clinical approaches of MTX and its adverse effects in order to provide a reference for ophthalmic scholars in clinical application of MTX.

Highlights

  • Methotrexate (MTX) is an antifolate metabolite that inhibits DNA synthesis, repair, and cellular replication

  • Khalil et al [26] had 400 μg/0.1 ml of MTX intravitreal injection once monthly administrated to 20 adult Behcet’s disease (BD) patients suffering from BD-associated ocular inflammation with posterior segment involvement. eir results prove that intravitreal MTX improves visual acuity, reduces posterior segment manifestations associated with Behcet’s disease, and allows the reduction of corticosteroids and immunosuppressive drugs [26]. ese results supported Taylor and associates who conducted trials on 15 patients with unilateral uveitis and/or cystoid macular edema [27]. eir clinical trials suggest that intravitreal MTX may help patients with uveitis-associated posterior segment involvement to regain normal anatomical structure and allowed the reduction of immunosuppressive therapy

  • Mori et al supported the protective effect by demonstrating that patients treated with low-dose MTX without folate supplements were significantly associated with the development of myelosuppression and pancytopenia [113]

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Summary

Introduction

Methotrexate (MTX) is an antifolate metabolite that inhibits DNA synthesis, repair, and cellular replication. It was firstly used as one of the essential treatments of pediatric leukemia [1, 2]. While immediate and low-dose MTX is used to treat nonmalignant and immune-mediated disorders, high-dose MTX (HDMTX, more than 500 mg/m2/week) is widely used to treat malignancies. HD-MTX (with or without radiation therapy) is still the backbone of most modern chemotherapy regimens [6], as well as the prevention of systemic/central nervous system (CNS) lymphoma recurrence at a dose of 3 g/m2 per week [7]. MTX has been widely applied in ophthalmic diseases, systemically and locally. Published articles pay more attention to new clinical applications, routes of administration, and newly discovered side effects, which are foci of this review

Clinical Applications in Ophthalmology
New Approaches of Applications of MTX
The Pharmacogenetics of MTX
Findings
Discussion
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