Antimetabolites
DANGEROUS DRUG
PREGNANCY CATEGORY D
Therapeutic Actions
Antimetabolites are antineoplastic drugs that inhibit DNA polymerase. They are cell-cycle-phase–specific to S phase (stage of DNA synthesis), causing cell death for cells in the S phase; they also block progression of cells from G1 to S in the cell cycle.
Indications
Induction and maintenance of remission in acute myelocytic leukemia (higher response rate in children than in adults), chronic lymphocytic leukemia
Treatment of acute lymphocytic leukemia, chronic myelocytic leukemia and erythro-leukemia, meningeal leukemia, psoriasis and rheumatoid arthritis (methotrexate)
Palliative treatment of GI adenocarcinoma, carcinomas of the colon, rectum, breast, stomach, pancreas
Part of combination therapy for treatment of non-Hodgkin’s lymphoma in children
Contraindications and Cautions
Contraindicated with allergy to the drug, pregnancy, lactation, premature infants.
Use cautiously with hematopoietic depression secondary to radiation or chemotherapy; impaired liver function.
Adverse Effects
CNS: Neuritis, neural toxicity
Dermatologic: Fever, rash, urticaria, freckling, skin ulceration, pruritus, conjunctivitis, alopecia
GI: Anorexia, nausea, vomiting, diarrhea, oral and anal inflammation or ulceration; esophageal ulcerations, esophagitis, abdominal pain, hepatic impairment (jaundice), acute pancreatitis
GU: Renal impairment, urine retention
Hematologic: Bone marrow depression, hyperuricemia
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