Busulfan
Class: Antineoplastic Agents
- Alkylating Agents
VA Class: AN100
CAS Number: 55-98-1
Brands: Busulfex, Myleran
Warning
- Hematologic Toxicity
Highly toxic drug with a low therapeutic index.
Possible severe bone marrow hypoplasia; discontinue therapy temporarily or reduce dosage at the first sign of abnormal bone marrow depression. In some cases, bone marrow examination may be necessary in addition to blood counts.
- Experience of Supervising Clinician
Use under constant supervision of a qualified clinician experienced in therapy with antineoplastic agents.
Clinicians supervising the administration of IV busulfan also should be experienced in hematopoietic stem cell transplantation and in the management of patients with severe pancytopenia.
Introduction
Antineoplastic agent; bifunctional alkylating agent.
Uses for Busulfan
Chronic Myelogenous Leukemia
Used IV in combination with cyclophosphamide: as a conditioning regimen prior to allogeneic hematopoietic progenitor cell transplantation in patients with chronic myelogenous leukemia (CML) (designated an orphan drug by US FDA for this use).
Also administered orally† as a component of a conditioning regimen prior to allogeneic transplantation.
Rarely, used as an alternative agent for palliative treatment of CML. Not curative, but approximately 90% of patients in the chronic phase of CML treated with the drug obtain remissions.
Pretransplant Regimens
Component of pretransplant conditioning regimens in patients undergoing bone marrow transplantation for acute myeloid leukemia and nonmalignant diseases (e.g., sickle cell disease)†.
Busulfan Dosage and Administration
General
Consult specialized references for procedures for proper handling and disposal of antineoplastics.
Individualize oral dosage carefully according to clinical and hematologic response and tolerance of the patient in order to obtain optimum therapeutic results with minimum adverse effects.
Prophylactic administration of phenytoin is recommended in all patients receiving IV busulfan; also may be considered in patients receiving oral busulfan. (See Nervous System Effects under Cautions.)
All patients should should receive antiemetics prior to the first dose of IV busulfan and on a fixed schedule throughout therapy. (See GI Effects under Cautions.)
Blood Sample Collection for Therapeutic Drug Monitoring for Pediatric Patients
Base AUC calculations on blood samples collected at specified time points; record actual sampling times.
Following the initial dose of IV busulfan, collect blood samples at 2 hours (the end of the infusion), 4 hours, and 6 hours (immediately prior to the next scheduled dose). For doses other than the first dose, collect blood samples prior to the infusion (baseline), and then at 2 hours (the end of the infusion), 4 hours,
