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busulfan (Myleran)
Tradename: Myleran.
Indications:
1) chronic myelogenous leukemia
2) polycythemia vera
3) bone marrow ablation prior to bone marrow transplant (stem cell transplantation)*
* major, if not exclusive, use in 2015 [4]
Contraindications: Caution:
1) monitor for signs of bleeding
2) excellent oral hygiene is needed to minimize oral discomfort
Dosage:
1) adults 408 mg PO QD
2) maintenance dosage: 2-4 mg/week to 4 mg QD
3) bone marrow transplant: up to 8-16 mg/kg
Tabs: 2 mg.
Pharmacokinetics: well absorbed orally
Adverse effects:
1) common (> 10%)
- pancytopenia
- delayed effect, onset 7-10 days
- nadir 14-21 days
- recovery 28 days
- busulfan affects stem cells
2) less common (1-10%)
- amenorrhea, hyperpigmentation, nausea/vomiting, diarrhea, weakness, anorexia, weight loss
3) uncommon (< 1%)
- seizures, adrenal suppression (Addison-like syndrome), hepatic dysfunction, blurred vision, pulmonary fibrosis, hemorrhagic cystitis, gynecomastia, hyperuricemia,
4) other
- mucositis
- increased serum transaminases
- "Bulsulfan" lung (< 8%)
- fever/chills, rales, dyspnea
- 30 days to 1 year after exposure
- pulmonary fibrosis, pulmonary nodules, dependent consoligation
- treatment is generally supportive
- glucocorticoids may be of benefit [4]
Drug interactions:
1) thioguanine
2) in combination with probenecid results in increased serum & urine uric acid
Test interactions:
- may increase measurements of serum K+
Mechanism of action: alkylating agent
Interactions
drug adverse effects of alkylating agents
General
alkylating agent
Properties
MISC-INFO: elimination route LIVER
1/2life 2.5 HOURS
Database Correlations
PUBCHEM cid=2478
References
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Deprecated Reference
- Medical Knowledge Self Assessment Program (MKSAP) 17,
American College of Physicians, Philadelphia 2015