Abstract

To review the possible association between methotrexate (MTX) intake and increased toxicity. A MEDLINE literature search MEDLINE (1980-August 2014) was performed using the search terms MTX, antifolate, MTX toxicity, glucarpidase, and leucovorin. Additional references were identified from a review of literature citations. All English-language observational studies and case reports were considered. Methotrexate (meth oh trex' ate) is an antifolate and antimetabolite that is used extensively in the therapy of leukemia, lymphoma, and several solid organ tumors. It also has potent activity against psoriasis and has immunomodulatory activity against inflammatory bowel disease and the inflammatory arthritidies. It exhibits a wide range of toxic effects profile. Leucovorin is indicated to diminish the toxicity and counteract the effect of inadvertently administered overdosages of MTX. In post marketing experience, overdose with MTX has generally occurred with oral and intrathecal administration, although intravenous and intramuscular overdose have also been reported. Supporting care strategies, extracorporeal measures, and glucarpidase are some of the means to overcome MTX overdosage. At present, pharmacogenomics tends to contribute toward the emergence of adverse effects following the widespread use of MTX for various indications.

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