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Methotrexate (MTX)

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General information

Class/mechanism: Folate analog, antimetabolite, interferes with DNA synthesis. Methotrexate inhibits dihydrofolic acid reductase, which catalyzes reactions that produce tetrahydrofolates, which are used in purine nucleotide and thymidylate synthesis.[1][2][3][4][5][6][7]
Route: IV, PO, IM, IT, SC, intraarterial
Extravasation: inflammitant

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Toxicity

Monitoring of plasma levels

  1. Stoller RG, Hande KR, Jacobs SA, Rosenberg SA, Chabner BA. Use of plasma pharmacokinetics to predict and prevent methotrexate toxicity. N Engl J Med. 1977 Sep 22;297(12):630-4. link to original article PubMed

Reversal agents

  • Glucarpidase (Voraxaze) can be used to treat toxic plasma methotrexate concentrations (greater than 1 micromole per liter) in patients with delayed methotrexate clearance due to impaired renal function

Diseases for which it is used

Patient drug information

History of changes in FDA indication

  • 12/7/1953: Initial FDA approval

Also known as

  • Generic names: amethopterin, MTX
  • Brand names:
Synonyms
Abitrexate Alltrex Antifolan Artrait Biometrox Biotrexate Caditrex Cytotrexate
Ebetrexat Emthexat Emthexate Ervemin Farmitrexat Fauldmetro Folex PFS Folitrax
Hextrate Ifamet Imutrex Ledertrexate Ledertrexato Lumexon Matrex Maxtrex
Medsatrexate Merex Metex Methobax Methoblastin Methorex Methotrexaat Methotrexat
Methotrexato Methotrexatum Meticil Metolate Metotressato Metotrexate Metotrexato Metotrexol
Metrex Metrexan Metrexato Metrotex Mexate Miantrex CS Neometho Neotrexate
Novatrex Oncotrex O Trexat Pharmatrexate Remtrex Reumatrex Rextop Rheumatrex
Tecnomet Texate Texorate Tratoben Tremetex Trexall Trexan Trexeron
Trixilem Unitrexate Zexate

References