A Review of Clinical Applications and Side Effects of Methotrexate in Ophthalmology

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.

Poly-Lysine Dendritic Nanocarrier to Target Epidermal Growth Factor Receptor Overexpressed Breast Cancer for Methotrexate Delivery

“…Methotrexate (MTX) is an FDA approved drug used in the treatment of many cancers, including breast cancer, but the adverse effects related to its folate antagonistic action remain as a constraint to use this drug clinically. The dose-limiting toxicity of this drug includes hepatotoxicity and nephrotoxicity, but mortality is due to the fact of pneumonitis or secondary infections [15]. A potential approach to strengthen the efficacy of the administered drug without causing any side effects is to develop capable targeted DDS.…”

Structural Deformation of MTX Induced by Nanodrug Conjugation Dictate Intracellular Drug Transport and Drug Efficacy

“…19,20 Although it has excellent therapeutic efficacy, long-term administration of MTX may cause serious side effects such as bone marrow suppression, hepatitis and infection. [21][22][23] Therefore, in order to reduce the side effects of repeated administration of high doses, it is necessary to adopt appropriate strategies to reduce the toxicity of anti-inflammatory drugs while effectively treating the symptoms of arthritis with minimal drug dose. One strategy for reducing the toxicity in the body from drug administration is to use nanomaterials as delivery systems specifically targeting cells or tissues.…”

miR-6315 Attenuates Methotrexate Treatment-Induced Decreased Osteogenesis and Increased Adipogenesis Potentially through Modulating TGF-β/Smad2 Signalling

“…A systematic review summarized the adverse effects of MTX in ophthalmology and it was found that, despite being considered well-tolerated and reversible, even the low-dose of MTX causes significant toxicity, such as central nervous system complications, mucositis, and hepatotoxicity, with substantial death rates [ 10 ]. Furthermore, MTX treatment has shown effects on blastocyst formation, resulting in dysmorphic features and neurologic defects during early pregnancy [ 10 ]. Furthermore, MTX treatment during childhood might lead to visual defects in patients [ 10 ].…”

“…Furthermore, MTX treatment has shown effects on blastocyst formation, resulting in dysmorphic features and neurologic defects during early pregnancy [ 10 ]. Furthermore, MTX treatment during childhood might lead to visual defects in patients [ 10 ]. Additionally, various clinical studies have demonstrated that intensive MTX treatment causes skeletal growth defects, such as reduced bone mass and increased marrow fat contents [ 11 , 12 ].…”

“…In order to prevent/reduce MTX-induced side effects, the supplementation of folate (folic acid or folinic acid) is common among patients treated with low-dose MTX [ 10 ]. Fan et al also observed that a folinic acid supplementation preserves the formation of the primary spongy bone and bone growth during long-term low-dose MTX therapy in rats [ 15 ].…”