Back to Antimetabolites
Methotrexate
Amethopterin, MTX
Folex PFS, Rheumatrex Dose Pak (treatment of psoriasis or rheumatoid
arthritis)
Pregnancy Category X
Drug classes
Antimetabolites
Antineoplastics
Mechanism of action
Inhibits folic acid reductase, leading to inhibition of DNA synthesis and inhibition of cellular replication; selectively affects the most rapidly dividing cells (neoplastic and psoriatic cells).
Indications
- Treatment of gestational choriocarcinoma, chorioadenoma destruens, hydatidiform mole
- Treatment and prophylaxis of meningeal leukemia
- Symptomatic control of severe, recalcitrant, disabling psoriasis
- Management of severe, active, classical, or definite rheumatoid arthritis
Unlabeled uses: high-dose regimen followed by leucovorin rescue for adjuvant therapy of nonmetastatic osteosarcoma (orphan drug designation); to reduce corticosteriod requirements in patients with severe corticosteroid-dependent asthma.
Contraindications
- Allergy to methotrexate
- Lactation
- Proriasis with renal or hepatic disorders
- Pregnancy or childbearing age
Use caution in the presence of hematopoietic depression; leukopenia, thrombocytopenia, anemia, severe hepatic or renal disease, infection, peptic ulcer, ulcerative colitis, debility.
Adverse effects
- CNS: Headache, drowsiness, blurred vision, aphasia, hemiparesis, paresis, seizures, fatigue, malaise, dizziness
- GI: Ulcerative stomatitis, gingivitis, pharyngitis, anorexia, nausea, vomiting, diarrhea, hematemesis, melena, GI ulceration and bleeding, enteritis, hepatic toxicity
- Respiratory: Interstitial pneumonitis, chronic interstitial obstructive pulmonary disease
- Hematologic: Bone marrow depression, increased susceptibility to infection
- GU: Renal failure, effects on fertility (defective oogenesis, defective spermatogenesis, transient oligospermia, menstrual dysfunction, infertility, abortion, fetal defects)
- Dermatologic: Erythematous rashes, pruritus, urticaria, photosensitivity, depigmentation, alopecia, ecchymosis, telangiectasia, ance, furunculosi
- Hypersensitivity: Anaphylaxis, sudden death
- Other: Chills and fever, metabolic changes (diabetes, osteoporosis), cancer
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