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Generic Name: Methotrexate
Brand Name(s): Trexall®
IUPAC: (2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanedioic acid
FDA Approval: yes
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Usage: Methotrexate is used to treat a variety of ailments, including cancer and skin diseases. Malignancies for which methotrexate is used include: Choriocarcinoma, Acute lymphocytic
leukemia, Large cell
lymphoma, High grade lymphoma, Head and neck cancers, Breast cancers, Bladder cancers, Osteogenic Cancers.
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Methotrexate is also notable for its use in inflammatory disease, rheumatoid arthritis, dermatological disorders, and to treat some gynecological conditions. The dosage used varies with the condition being treated. For example, high dosages are used for cancer patients, whereas skin disorders require lower dosages.
Mechanism: Methotrexate inhibits folic acid reductase, causing inhibition of
DNA synthesis and of cellular
replication.
Side Effects: Methotrexate is very toxic at high doses. Leucovorin (brand name: Wellcovorin®.) may be administered along with the methotrexate to reduce anemia resulting from treatment with methotrexate. The toxicity of methotrexate depends more on the duration of treatment than the amount present in the blood at any given time. It is especially toxic within the bone marrow and lining of the digestive tract and oropharnyx (part of the throat). Hematological (of blood and blood generating organs) status must be closely monitored during treatment. Symptoms of this toxicity can include nausea, anorexia, mild diarrhea to severe ulceration and bleeding. Hepatotoxicity (damaging effects on the liver) is possible at high or low dosage concentrations of the drug. Reversible pulmonary syndrome is another possible outcome.
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