Busulphan

Indications
 Oral
Palliative treatment of chronic myeloid leukemia
Adult: 60 mcg/kg daily. Maintenance: 0.5-2 mg daily. Max: 4 mg daily.
Oral
Polycythemia vera
Adult: 4-6 mg daily continued for 4-6 wk with blood counts monitoring.
Oral
Essential thrombocythemia
Adult: 2-4 mg daily.
Oral
Conditioning regimens for bone marrow transplantation
Adult: 3.5-4 mg/kg daily in divided doses for 4 days up to a total dose of 14-16 mg/kg. Usually used with cyclophosphamide for ablation of recipient's bone marrow.
Intravenous
Conditioning regimens for bone marrow transplantation
Adult: When used with phenytoin, recommended dose: 3.2 mg/kg ideal body-weight/day for 4 days (total dose 12.8 mg/kg); actual body-weight is used for dose calculation if it is <the ideal weight. Daily dose is given as 4 infusions of 800 mcg/kg at 6-hrly intervals; each dose is diluted in sodium chloride 0.9% or glucose 5% to a final concentration of about 500 mcg/mL, given over 2 hr through a central venous catheter using an infusion pump. Start cyclophosphamide only at least 24 hr after last dose of busulfan.
Contraindications
 Pregnancy and lactation. Hypersensitivity.
Warnings / Precautions
 Prior treatment with other myelosuppressive drugs, patients predisposed to seizures. May cause secondary malignancies (tumors, acute leukaemias, ovarian failure). Previous irradiation/therapy. Monitor blood counts carefully during therapy. Discontinue if lung toxicity develops.
Adverse Reactions
 GI symptoms, anorexia, wt loss, weakness, hyperpigmentation, amenorrhoea, cataracts, cough or hoarseness, impaired fertility and gonadal function, dry skin, liver damage, gynaecomastia.
Potentially Fatal: Bone marrow depression manifesting as thrombocytopaenia, leucopaenia, anaemia. Interstitial pulmonary fibrosis (known as "busulfan lung" on prolonged treatment).
Drug Interactions
 Decreased clearance when used with cyclophosphamide and itraconazole. Increased clearance by phenytoin. May reduce response to vaccines, possibility of generalized infections with live vaccines. Combination with thioguanine results in oesophageal varices and abdominal liver function tests.
Potentially Fatal: Cytotoxic agents may increase risk of pulmonary toxicity.
See Below for More busulfan Drug Interactions
Mechanism of Actions
 Busulfan reacts with N-7 position of guanosine and interferes with DNA replication and RNA transcription by alkylating and cross-linking the DNA strands.
Absorption: Readily absorbed from the GIT (oral).
Distribution: Crosses the blood-brain barrier.
Metabolism: Extensively hepatic.
Excretion: Urine (as sulfur-containing metabolites); 2-3 hrs (elimination half-life).
Administration
 May be taken with or without food. (Take w/ chilled liqd, ensure adequate fluid intake.)
Storage Conditions
 Oral: Store below 25°C.
ATC Classification
 L01AB01 - busulfan ; Belongs to the class of alkylating agents, alkyl sulfonates. Used in the treatment of cancer.
Storage
 Oral: Store below 25°C.
Available As
  • Busulphan 2 mg
  • Busulphan 60 mg

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