Generic
Busulphan
1 brands available in the market
At a glance
Busulphan is an anti-cancer medication used in the treatment of chronic myeloid leukemia (CML) and as a conditioning regimen prior to hematopoietic progenitor cell transplantation (HPCT). It works by damaging the genetic material (DNA and RNA) of cancer cells, stopping their growth and multiplication.
Description
Busulphan is an alkylating agent used in the palliative treatment of chronic myeloid leukemia (CML) and as a conditioning regimen prior to hematopoietic progenitor cell transplantation (HPCT).
Busulphan reacts with the N-7 position of guanosine and interferes with DNA replication and RNA transcription by alkylating and cross-linking the DNA strands. It damages the genetic material (DNA and RNA) of cancer cells, stopping their growth and multiplication.
Indications
- Chronic myeloid leukemia (CML) - palliative treatment
- Conditioning regimen prior to hematopoietic progenitor cell transplantation (HPCT)
- Polycythemia vera
- Essential thrombocythemia
Therapeutic class
Antineoplastic Agent
Pharmacological class
Alkylating Agent (Busulfan)
Pharmacology
Busulphan reacts with the N-7 position of guanosine and creates intra- and inter-strand crosslinks between DNA strands. This disrupts DNA replication and RNA transcription, leading to cell cycle arrest and cancer cell death.
Mechanism of action
Busulphan attaches alkylating groups to DNA, creating crosslinks between DNA strands, which disrupts DNA replication and RNA transcription, leading to cancer cell death.
Dosage
Chronic Myeloid Leukemia (CML) - Palliative: 60 mcg/kg/day. Maintenance: 0.5-2 mg/day. Max: 4 mg/day.
Polycythemia Vera: 4-6 mg/day for 4-6 weeks (with blood count monitoring).
Essential Thrombocythemia: 2-4 mg/day.
Bone Marrow Transplantation Conditioning: 3.5-4 mg/kg/day in divided doses for 4 days, total 14-16 mg/kg. Usually used with cyclophosphamide.
Hepatic impairment: Limited information; caution required.
Renal impairment: Probably safe; dose adjustment may not be needed.
Administration
Take as advised by your doctor. Swallow tablets whole; do not chew, crush, or break. May be taken with or without food, preferably at a fixed time each day.
Missed dose
If you miss a dose, take it as soon as you remember. Skip the missed dose if it is almost time for your next dose. Do not double the dose.
Side effects
Common side effects: Decreased blood cells (red cells, white cells, platelets), abdominal pain, anxiety, nausea, vomiting, loss of appetite, decreased magnesium, decreased potassium, diarrhea, fever, headache, increased glucose, insomnia, stomatitis (mouth inflammation).
Serious: Bone marrow suppression, pulmonary fibrosis (with long-term use), adrenal insufficiency, hyperpigmentation, veno-occlusive disease (VOD), seizures.
Precautions & warnings
- Busulphan can lower blood clotting ability and infection resistance; seek immediate medical attention if unusual bruising/bleeding or signs of infection (fever, chills, body aches) occur.
- Inform your doctor if you have thalassemia, gout, or history of radiotherapy.
- Do not receive live vaccines; avoid contact with individuals who have recently received live vaccines.
- Do not use during pregnancy and lactation (Category D).
- Use effective contraception during and after treatment.
- Regular monitoring of CBC, kidney, liver, and cardiac function is required.
- Inform your doctor if you develop dry cough or shortness of breath (pulmonary toxicity).
Contraindications
- Pregnancy and lactation
- Hypersensitivity to busulphan
Drug interactions
- Cyclophosphamide and itraconazole: May decrease clearance.
- Phenytoin: May increase clearance.
- Vaccines: May reduce response; risk of generalized infections with live vaccines.
- Thioguanine: May result in esophageal varices and abnormal liver function tests.
- Cytotoxic agents: May increase risk of pulmonary toxicity (potentially fatal).
Food interactions
It is not known whether it is safe to consume alcohol with Busulphan. Please consult your doctor.
Use in pregnancy
Unsafe during pregnancy (Category D). Definite evidence of risk to the developing baby. May be prescribed rarely in life-threatening situations if benefits outweigh risks.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Unsafe during breastfeeding. Data suggests the drug may cause toxicity to the baby.
Pediatric use
Safety and effectiveness in pediatric patients have not been established; limited use in conditioning regimens.
Geriatric use
Dose adjustment may be required for elderly patients; dose determined by the physician based on patient condition.
Renal / hepatic impairment
Hepatic impairment: Limited information available; caution required. Consult your doctor.
Overdose effects
Overdose symptoms: Bone marrow suppression (severe pancytopenia), pulmonary fibrosis, seizures, veno-occlusive disease. Consult your doctor immediately if overdose is suspected.
Storage conditions
Store below 30°C, away from light and moisture. Keep out of reach of children.
Chemical structure
Busulphan (Alkylating Agent)