Difference between revisions of "Methotrexate (MTX)"

Revision as of 14:19, 24 November 2021

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

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
Most recent package insert:
- Methotrexate is indicated in the treatment of gestational choriocarcinoma, chorioadenoma destruens and hydatidiform mole.
- In acute lymphocytic leukemia, methotrexate is indicated in the prophylaxis of meningeal leukemia and is used in maintenance therapy in combination with other chemotherapeutic agents.
- Methotrexate is also indicated in the treatment of meningeal leukemia.
- Methotrexate is used alone or in combination with other anticancer agents in the treatment of breast cancer, epidermoid cancers of the head and neck, advanced mycosis fungoides (cutaneous T cell lymphoma), and lung cancer, particularly squamous cell and small cell types.
- Methotrexate is also used in combination with other chemotherapeutic agents in the treatment of advanced stage non-Hodgkin’s lymphomas.
- Methotrexate in high doses followed by leucovorin rescue in combination with other chemotherapeutic agents is effective in prolonging relapse-free survival in patients with non- metastatic osteosarcoma who have undergone surgical resection or amputation for the primary tumor.

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

[insert-1] 1.0 ^1.1 Methotrexate (MTX) tablet package insert

[2] Methotrexate (MTX) tablet package insert (locally hosted backup)

[3] Methotrexate (MTX) injection package insert

[4] Methotrexate (MTX) injection package insert (locally hosted backup)

[Otrexup-5] 5.0 ^5.1 Methotrexate (Otrexup) subcutaneous injection package insert

[6] Methotrexate (Otrexup) subcutaneous injection package insert (locally hosted backup)

[7] Otrexup manufacturer's website

[8] Methotrexate (MTX) patient drug information (Chemocare)

[9] Methotrexate (MTX) patient drug information (UpToDate)

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 ==History of changes in FDA indication==
 * 12/7/1953: Initial FDA approval
+* Most recent package insert:
+**Methotrexate is indicated in the treatment of [[Gestational trophoblastic neoplasia|gestational choriocarcinoma, chorioadenoma destruens and hydatidiform mole]].
+**In [[:Category:Acute lymphoblastic leukemias|acute lymphocytic leukemia]], methotrexate is indicated in the prophylaxis of meningeal leukemia and is used in maintenance therapy in combination with other chemotherapeutic agents.
+**Methotrexate is also indicated in the treatment of [[CNS leukemia|meningeal leukemia]].
+**Methotrexate is used alone or in combination with other anticancer agents in the treatment of [[breast cancer]], [[Head and neck cancer|epidermoid cancers of the head and neck]], advanced [[Cutaneous T-cell lymphoma|mycosis fungoides (cutaneous T cell lymphoma)]], and lung cancer, particularly [[Non-small cell lung cancer, Squamous|squamous cell]] and [[Small cell lung cancer|small cell]] types.
+**Methotrexate is also used in combination with other chemotherapeutic agents in the treatment of advanced stage [[:Category:Non-Hodgkin lymphomas|non-Hodgkin’s lymphomas]].
+**Methotrexate in high doses followed by leucovorin rescue in combination with other chemotherapeutic agents is effective in prolonging relapse-free survival in patients with non- metastatic [[osteosarcoma]] who have undergone surgical resection or amputation for the primary tumor.
 ==Also known as==