https://wikimd.org/index.php?action=history&feed=atom&title=MethotrexateMethotrexate - Revision history2026-05-14T02:53:09ZRevision history for this page on the wikiMediaWiki 1.44.2https://wikimd.org/index.php?title=Methotrexate&diff=5540504&oldid=prevPrab at 12:11, 7 April 20242024-04-07T12:11:51Z<p></p>
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'''[[methotrexate]]''' is a drug that blocks the body’s ability to use folic acid, which is needed by growing cells such as those making up the skin, blood, digestive tract, and the cells that protect the body against infection and disease. Methotrexate is used to treat some types of [[cancer]], [[arthritis]], and severe skin disorders. It belongs to the group of drugs called [[antimetabolites]].<br />
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Methotrexate is an antineoplastic and immunosuppressive agent widely used in the therapy of [[leukemia]], [[lymphoma]], solid tumors, psoriasis and rheumatoid arthritis. <br />
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==Liver toxicity==<br />
When given in high intravenous doses, methotrexate can cause acute elevations in serum enzymes, and long term methotrexate therapy has been associated with frequent but mild elevations in serum [[liver enzymes]] and, more importantly, with development of chronic [[liver injury]], progressive fibrosis, cirrhosis and portal hypertension. <br />
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==Mechanism of action==<br />
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. Methotrexate is considered a disease modifying antirheumatic drug (DMARD) and used widely in rheumatoid arthritis and other autoimmune diseases. Methotrexate acts by inhibition of folate metabolism, blocking dihydrofolic acid reductase, thereby inhibiting synthesis of purines and pyrimidines and decreasing [[DNA]] and [[RNA]] synthesis. Recent results suggest that methotrexate also leads to increase and release of adenosine, which may mediate its immunosuppressive activity. <br />
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Folic acid antagonists (aminopterin) were developed in the late 1940s and introduced into clinical medicine shortly thereafter. Aminopterin was later replaced by methotrexate because of its better tolerance and lower rate of toxicity. Methotrexate was approved for use in cancer in the United States in 1955, for psoriasis in 1972 and rheumatoid arthritis in 1988 and is still widely used for these indications. <br />
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Methotrexate is available in generic forms and under the brand names of [[Rheumatrex]] and [[Trexall]] in tablets of 2.5, 5, 7.5, 10 and 15 mg, and in both powdered and liquid-for-injection forms in vials of various strengths for intravenous, intramuscular or intrathecal injection. The dose regimen varies by indication; high, short term doses being used in [[treatment]] of cancer and chronic, lower doses for autoimmune conditions. The typical maintenance dose used to treat psoriasis and rheumatoid arthritis is 7.5 to 25 mg once weekly either orally or by injection. <br />
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[[side effects]] are mostly dose related and include stomatitis, [[oral ulcers]], [[hair loss]], [[fatigue]], [[headache]], gastrointestinal upset, [[nausea]], [[diarrhea]] and [[bone marrow suppression]]. <br />
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{{Immunosuppressants}}<br />
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[[Category:Antifolates]]<br />
[[Category:Antirheumatic products]]<br />
[[Category:Benzamides]]<br />
[[Category:Chemotherapy]]<br />
[[Category:Hepatotoxins]]<br />
[[Category:IARC Group 3 carcinogens]]<br />
[[Category:Immunosuppressants]]<br />
[[Category:Mammalian dihydrofolate reductase inhibitors]]<br />
[[Category:Nephrotoxins]]<br />
[[Category:World Health Organization essential medicines]]<br />
[[Category:Orphan drugs]]</div>Prab