III. Mechanism

  1. See Alkylating Agent
  2. Synthetic derivative of dimethane-sulfonate with antineoplastic properties
  3. In vivo, generates carbonium ions which alkylate DNA, inhibiting DNA Replication and transcription

IV. Medications

  1. Busulfan Tablets (Myleran): 2 mg
  2. Busulfan Injection (Busulfex)

V. Dosing

  1. See other references for disease specific dosing protocols

VI. Adverse Effects

  1. Adrenal Insufficiency
  2. Alopecia
  3. Bone Marrow Suppression (severe)
  4. Hepatic Sinusoidal Obstruction Syndrome (Veno-occlusive Disease)
  5. Hyperuricemia
    1. Consider startic Allopurinol for prophylaxis prior to starting Busulfan
    2. Maintain adequate hydration
  6. Impaired future fertility
  7. Pulmonary Fibrosis
  8. Secondary Malignancy (and cellular dysplasia)
  9. Seizures
    1. Seizure Prophylaxis initiated prior to starting Busulfan
  10. Tooth Hypoplasia

VII. Safety

  1. Avoid in Lactation
  2. Avoid in pregnancy (contraindicated in all trimesters)
    1. Teratogenic and adverse outcomes
    2. Use reliable Contraception
  3. Monitoring
    1. Complete Blood Count
    2. Liver Function Tests

VIII. Drug Interactions

  1. Drugs that increase Busulfan levels (decreased clearance)
    1. Acetaminophen
    2. Itraconazole
  2. Drugs that decrease Busulfan levels (increased clearance)
    1. Phenytoin

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