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Back to Oncology Drug index
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.
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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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