Classes
DEA Class; Rx
Common Brand Names; Myleran, Busulfex
- Antineoplastics, Alkylating;
- Immunosuppressives, PHD
Description
A bifunctional alkylating agent
IV formulation used in combination with cyclophosphamide as a conditioning regimen prior to allogeneic hematopoietic stem-cell transplantation in patients with chronic myelogenous leukemia (CML); oral tablet formulation used for palliative treatment of CML
Black box warning for myelosuppression
Indications
Indicated for the palliative treatment of chronic myelogenous leukemia (CML).
Contraindications
Hypersensitivity, resistance to busulfan
Patients without definitive diagnosis of CML
Adverse Effects
- Neutropenia (nearly 100%)
- Myelosuppression (nearly 100%)
- Thrombocytopenia (98%)
- Nausea (97%)
- Stomatitis (96%)
- Anorexia (80%)
- Diarrhea (80%)
- Fever (80%)
- Insomnia (80%)
- Lymphopenia (79%)
- Hypomagnesemia (77%)
- Headache (69%)
- Hyperglycemia (66%)
- Hypokalemia (64%)
- Abdominal pain (62%)
- Anemia (62%)
- Asthenia (52%)
- Hypocalcemia (49%)
- Chills (47%)
- Dyspepsia (44%)
- Tachycardia (44%)
- Pain (41%)
- Constipation (38%)
- Hypertension (36%)
- Hypersensitivity (32%)
- Edema (27%)
- Thrombosis (27%)
- Dry mouth (26%)
- Vasodilation (25%)
Warnings
Bone marrow depression may occur
Seizures reported with use; initiate anticonvulsant prophylactic therapy prior to treatment with busulfan; monitor patients with history of seizure disorder, head trauma or receiving epileptogenic drugs
Cardiac temponade reported in children with thalassemia in combination with cyclophosphamide
Ovarian failure may occur
Secondary malignancies reported
Antiemetics may be recommended to prevent nausea and vomiting
Increased risk of developing hepatic veno-occlusive disease (HVOD) at AUC greater than 1,500 μM•min; monitor serum transaminases, alkaline phosphatase and bilirubin daily
Bronchopulmonary dysplasia with pulmonary fibrosis reported and can be fatal; toxicity may be additive if used with other agents that cause pulmonary toxicity; discontinue therapy if busulfan toxicity develops
Avoid pregnancy; can cause fetal harm; advise of potential risk to a fetus and use of effective contraception
Pregnancy and Lactation
Can cause fetal harm when administered to a pregnant woman based on animal data
Advise females of reproductive potential to use effective contraception during treatment and for 6 months following cessation of therapy
Maximum Dosage
8 mg/day PO; 1 mg/kg PO every 6 hours for 16 doses has been studied as part of a conditioning regimen prior to stem-cell transplantation.
0.8 mg/kg IV every 6 hours for 16 doses; 1 mg/kg IV every 6 hours for 16 doses has been studied as part of a conditioning regimen prior to stem-cell transplantation.
8 mg/day PO; 1 mg/kg PO every 6 hours for 16 doses has been studied as part of a conditioning regimen prior to stem-cell transplantation.
0.8 mg/kg IV every 6 hours for 16 doses; 1 mg/kg IV every 6 hours for 16 doses has been studied as part of a conditioning regimen prior to stem-cell transplantation.
60 mcg/kg or 1.8 mg/m2 PO per day.
60 mcg/kg or 1.8 mg/m2 PO per day.
60 mcg/kg or 1.8 mg/m2 PO per day.
60 mcg/kg or 1.8 mg/m2 PO per day.
How supplied
Busulfan
injectable solution
- 6mg/mL
tablet
- 2mg