Busulfan is an alkylating agent that forms DNA-DNA and DNA-protein cross-links to inhibit DNA replication. Oral busulfan is well absorbed, has a terminal half-life of 2 to 2.5 hours, and is eliminated primarily by metabolism. Busulfan has shown significant clinical activity in the treatment of acute myelogenous leukemia and chronic myelo-cytic leukemia. Side effects include bone marrow suppression, hyperpigmentation of skin creases, and rarely, pulmonary fibrosis. High doses used for bone marrow transplant preparatory regimens result in severe nausea and vomiting, tonic-clonic seizures, and sinusoidal obstruction syndrome (formerly known as veno-occlusive disease). Patients receiving high-dose busulfan should receive anticonvulsant prophylaxis.

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