II. Indications
- FDA approved
- Off-Label
III. Mechanism
- See Alkylating Agent
- Synthetic derivative of dimethane-sulfonate with antineoplastic properties
- In vivo, generates carbonium ions which alkylate DNA, inhibiting DNA Replication and transcription
IV. Medications
- Busulfan Tablets (Myleran): 2 mg
- Busulfan Injection (Busulfex)
V. Dosing
- See other references for disease specific dosing protocols
VI. Adverse Effects
- Adrenal Insufficiency
- Alopecia
- Bone Marrow Suppression (severe)
- Hepatic Sinusoidal Obstruction Syndrome (Veno-occlusive Disease)
-
Hyperuricemia
- Consider startic Allopurinol for prophylaxis prior to starting Busulfan
- Maintain adequate hydration
- Impaired future fertility
- Pulmonary Fibrosis
- Secondary Malignancy (and cellular dysplasia)
-
Seizures
- Seizure Prophylaxis initiated prior to starting Busulfan
- Tooth Hypoplasia
VII. Safety
- Avoid in Lactation
- Avoid in pregnancy (contraindicated in all trimesters)
- Teratogenic and adverse outcomes
- Use reliable Contraception
- Monitoring
VIII. Drug Interactions
- Drugs that increase Busulfan levels (decreased clearance)
- Drugs that decrease Busulfan levels (increased clearance)
IX. Resources
- Busulfan Injection (Busulfex, DailyMed)
- Busulfan Tablet (Myleran, DailyMed)