Classification: Antineoplastic, miscellaneous
See Also: See also Antineoplastic Agents.
Action/Kinetics: The mechanism of action is unknown, although metabolism of the drug is required for cytotoxicity. Well absorbed following PO ingestion; undergoes rapid demethylation in the liver, yielding the principal metabolites-pentamethylmelamine and tetramethylmelamine. Peak plasma levels: 0.5-3 hr. t 1/2: 4.7-10.2 hr. Metabolites are excreted mainly through the kidney.
Uses: Used alone in the palliative treatment of persistent or recurrent ovarian cancer after first-line cisplatin- or alkylating agent-based combination therapy.
Contraindications: Preexisting bone marrow depression or severe neurologic toxicity, although the drug has been used safely in clients with preexisting cisplatin neuropathies. Lactation.
Special Concerns: Safety and effectiveness have not been determined in children. High daily doses may result in gradual onset of N&V.
Side Effects: GI: N&V (most common). Neurologic: Peripheral sensory neuropathy, fatigue, anorexia, seizures. CNS: Mood disorders, disorders of consciousness, ataxia, dizziness, vertigo. Hematologic: Leukopenia, thrombocytopenia, anemia. Miscellaneous: Hepatic toxicity skin rash, pruritus, alopecia.
Laboratory Test Alterations: Serum creatinine, BUN, alkaline phosphatase.
Drug Interactions: Use with MAO inhibitors may cause severe orthostatic hypotension, especially in clients over the age of 60 years.
How Supplied: Capsule: 50 mg