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an alkylating agent that acts selectively on the bone marrow, depressing granulocyte formation, and is therefore used in the treatment of myelogenous leukemias. It is also used for the treatment of myeloproliferative disorders, including polycythemia vera and myeloid metaplasia. Administered orally or intravenously. Side effects include nausea and vomiting, and heavy doses may lead to excessive bone marrow depression. Complete blood counts (including platelet counts) must be done frequently while the drug is being administered and are used as a guide to dosage and effects on bone marrow production. Because of its effects on bone marrow, it is used at high doses in lieu of whole body irradiation in bone marrow transplantation.
Miller-Keane Encyclopedia and Dictionary of Medicine, Nursing, and Allied Health, Seventh Edition. © 2003 by Saunders, an imprint of Elsevier, Inc. All rights reserved.


Busilvex (UK), Busulfex, Myleran

Pharmacologic class: Alkylating agent

Therapeutic class: Antineoplastic

Pregnancy risk category D

FDA Box Warning

• Drug causes profound myelosuppression at recommended dosage. Give under supervision of physician experienced in allogeneic hematopoietic stem cell transplantation, cancer chemotherapy, and management of severe pancytopenia, in facility with adequate diagnostic and treatment resources.


Unclear. Thought to interfere with bacterial cell-wall synthesis by cross-linking strands of DNA and disrupting RNA transcription, which causes cell to rupture and die. Exhibits minimal immunosuppressant activity.


Injection: 6 mg/ml in 10-ml ampules

Tablets: 2 mg

Indications and dosages

Chronic myelogenous leukemia

Adults: 4 to 8 mg P.O. daily until white blood cell (WBC) count decreases to 15,000/mm3; then discontinue drug until WBC count rises to 50,000/mm3, and then resume as needed.

Children: 0.06 to 0.12 mg/kg/day P.O. or 1.8 to 4.6 mg/m2/day P.O. Adjust dosage to maintain WBC count at approximately 20,000/mm3. Drug should be withheld when WBC count decreases to approximately 15,000/mm3.

Allogenic hematopoietic stem cell transplantation

Adults: 0.8 mg/kg I.V. q 6 hours for 4 days. Starting 6 hours after 16th dose of busulfan injection, give cyclophosphamide 60 mg/kg/day I.V. over 1 hour for 2 days.

Off-label uses

• Adjunctive therapy in ovarian cancer

• Bone marrow transplantation


• Hypersensitivity to drug

• Patients not definitively diagnosed with chronic myelogenous leukemia

• Pregnancy or breastfeeding


Use cautiously in:

• active infections, decreased bone marrow reserve, chronic debilitating disease, depressed neutrophil and platelet counts, seizure disorders, obesity

• patients receiving concurrent myelosuppressive or radiation therapy

• females of childbearing age.


• Give oral doses on empty stomach.

• When administering I.V., withdraw dose from ampule using 5-micron filter needle. Remove filter needle and use new needle to add busulfan to diluent.

• Dilute for injection using dextrose 5% in water or normal saline solution.

• Infuse I.V. dose over 2 hours, using an infusion pump.

• Flush I.V. catheter before and after each infusion with 5 ml D5W or normal saline solution.

Be aware that drug is highly toxic and has a narrow therapeutic index.

• Maintain vigorous hydration to reduce risk of renal toxicity.

• Handle patient gently to avoid bruising.

Adverse reactions

CNS: anxiety, confusion, depression, dizziness, headache, insomnia, weakness, encephalopathy, seizures, cerebral hemorrhage, coma

CV: chest pain, hypotension, hypertension, tachycardia, ECG changes, heart block, left-sided heart failure, thrombosis, pericardial effusion, ventricular extrasystole, atrial fibrillation, arrhythmias, cardiac tamponade, cardiomegaly

EENT: cataracts, ear disorders, epistaxis, pharyngitis

GI: nausea, vomiting, diarrhea, constipation, abdominal pain, dyspepsia, abdominal enlargement, pancreatitis, hematemesis, dry mouth, stomatitis, anorexia

GU: dysuria, hematuria, sterility, gyne-comastia, oliguria

Hematologic: febrile neutropenia, thrombotic microangiopathy, profound myelosuppression

Hepatic: hepatitis, hepatomegaly

Metabolic: hypokalemia, hypomagnesemia, hypophosphatemia, hyperuricemia, hyperglycemia

Musculoskeletal: arthralgia, myalgia, back pain

Respiratory: hyperventilation, dyspnea, pulmonary fibrosis

Skin: pruritus, rash, acne, alopecia, erythema nodosum, exfoliative dermatitis, hyperpigmentation

Other: allergic reactions, chills, fever, injection site infection or inflammation; severe bacterial, viral, fungal infections; sepsis; tumor lysis syndrome


Drug-drug. Anticoagulants, aspirin, nonsteroidal anti-inflammatory drugs: increased risk of bleeding

Live-virus vaccines: decreased antibody response to vaccine, increased risk of adverse reactions

Myelosuppressants: additive bone marrow depression

Nephrotoxic and ototoxic drugs (such as aminoglycosides, loop diuretics): additive nephrotoxicity and ototoxicity

Thioguanine: increased risk of hepatotoxicity

Drug-diagnostic tests. Alkaline phosphatase, aspartate aminotransferase, bilirubin, nitrogenous compounds (urea): increased levels

Hemoglobin, WBCs: decreased values

Patient monitoring

• Monitor patient closely for adequate hydration.

• Check for signs and symptoms of local or systemic infections.

• Assess for bleeding and excessive bruising.

• Evaluate oral hygiene regularly.

• Monitor CBC and WBC and platelet counts daily if patient is receiving I.V. busulfan.

• Monitor renal and hepatic function.

Know that diffuse pulmonary fibrosis ("busulfan lung") is a rare but potentially life-threatening complication, with symptom onset as late as 10 years after therapy.

Patient teaching

• Inform patient that drug doesn't cure leukemia but may induce remission.

• Advise patient to drink plenty of fluids to avoid dehydration.

Instruct patient to immediately report inability to eat or drink. Prescriber may add another drug to improve appetite.

• Inform patient that he's at increased risk for infection. Advise him to avoid contact with people with known infections and to avoid public transportation, if possible.

• Tell patient he's at increased risk for bleeding and bruising.

• Advise patient to avoid activities that can cause injury and to use soft toothbrush and electric razor to avoid gum and skin injury.

• Inform patient that he'll undergo frequent blood testing to monitor drug effects.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved


An alkylating agent, C6H14O6S2, that is used as an antineoplastic drug in the treatment of chronic myelogenous leukemia.
The American Heritage® Medical Dictionary Copyright © 2007, 2004 by Houghton Mifflin Company. Published by Houghton Mifflin Company. All rights reserved.


An alkyl sulphonate, the sole antineoplastic activity of which is myelosuppression. At low doses, it suppresses granulocytopoiesis; at higher doses, it evokes pancytopenia. Bulsulfan was the standard therapy for chronic myeloid leukaemia (CML) until imatinib was developed for oncological therapy.
Adverse effects
Marrow suppression, pulmonary fibrosis, seizures, hepatic veno-occlusive disease, wasting syndrome, thrombocytopaenia.

Response rate
Segen's Medical Dictionary. © 2012 Farlex, Inc. All rights reserved.


BU, Myleran® Oncology An alkyl sulfonate, the sole antineoplastic activity of which is myelosuppression; at low doses, it suppresses granulocytopoiesis; at higher doses, evokes pancytopenia Indications CML Toxicity Confined to BM Response rate 85–90%
McGraw-Hill Concise Dictionary of Modern Medicine. © 2002 by The McGraw-Hill Companies, Inc.
References in periodicals archive ?
The company has introduced Busulfan Injection in 6mg/ml in 10ml vials through its collaborative partnership with Athenex Pharmaceuticals, Sungen Pharma and Chemwerth.
Busulfan, melphalan, or alkylating agents such as thiotepa, especially in the autologous setting, are among the risk factors for the late onset SOS (49,50).
"Busulfan is currently on American Society of Health System Pharmacists drug shortage list," he added.
Busulfan and cyclophosphamide as a preparative regimen for allogeneic blood and marrow transplantation in patients with non-Hodgkin's lymphoma.
High-dose busulfan, melphalan and thiotepa followed by autologous peripheral blood stem cell (PBSC) rescue in patients with advanced stage III-IV ovarian cancer.
Comparison of reduced conditionings combining fludarabine with melphalan or 3-day busulfan in patients allografted for myeloid neoplasms.
Myeloablative conditioning (MAC) regimens were based on cyclophosphamide with either busulfan or total body irradiation (TBI) or on melphalan, fludarabine, and alemtuzumab.
2003, Melphalan (NL) 35 PBSC retrospective [3] Busulfan (NL) ONR = 2 BSC Study Response EFS (number of pts) Rasper et al.
Anagrelide, on the other hand, is a phosphodiesterase 3 (PDE 3) inhibitor that is recommended as a 3rd-line treatment for ET after interferon-[alpha] (IFN-[alpha]) and busulfan [2].
Alkylating agents, specifically busulfan and melphalan, was reported to be associated with the development of FNH in preparation for bone marrow transplantation due to the formation of SOS [3 5].
The options of (A) conditioning with alemtuzumab, treosulfan, fludarabine, and thiotepa using a TCR-alpha and -beta depleted graft versus (B) using a T-cell replete marrow graft after cyclophosphamide 14, 5 mg/kg days -6 and -5, flu 30 mg/[m.sup.2] days -6 to -2 (5 days), and 200 cGy TBI day -1 [15] with the addition of busulfan 3.2 mg/kg/day, days -4 and -3 to achieve myeloablation [16] as conditioning and posttransplant cyclophosphamide 50 mg/kg days +3 and +4 and tacrolimus and mycophenolate mofetil as graft-versus-host-disease (GVHD) prophylaxis [15] were discussed.