Find & Manage Your Patient Assistance Programs
Estimated patient savings $600,000,000.00

Important Note

The following information is intended to supplement, not substitute for, the expertise and judgment of your physician, pharmacist or other healthcare professional. It should not be construed to indicate that use of the drug is safe, appropriate, or effective for you. Consult your healthcare professional before using this drug.




WARNING: This medication can lower the body's ability to fight an infection or cancer, as well as preventing normal blood clotting. Notify your doctor immediately if you develop any signs of an infection such as fever, chills, persistent sore throat; easy bruising/bleeding or unusual tiredness/fatigue.


Busulfan is used in combination with cyclophosphamide in the treatment of leukemia (chronic myelogenous leukemia) before stem cell transplant. It works by stopping cancer cells from multiplying, but also affects some normal cells, such as bone marrow cells.

How To Use

Give this medication by vein (IV) over 2 hours, diluted in a solution (e.g., saline, dextrose), usually 4 times daily for 4 days; or as directed by your doctor. To minimize side effects, you may be given other medications (e.g., anti-nausea, anti-seizure agents) to take in addition to this drug. Follow all directions for the proper use of other medications; consult your doctor or pharmacist. Drink plenty of fluids while using this medication, unless instructed otherwise. Follow all instructions for proper preparation, use, handling, and safe disposal of this medication. Ask your pharmacist if you have questions regarding busulfan. Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid.

Side Effects

Nausea, diarrhea or constipation, headache, skin darkening, flushing, trouble sleeping, pain or swelling at the injection site, or dry mouth may occur. If any of these effects persist or worsen, contact your doctor or pharmacist promptly. To relieve dry mouth, suck on (sugarless) hard candy or ice chips, chew (sugarless) gum, drink water, or use a saliva substitute. Tell your doctor immediately if any of these serious side effects occur: unusual tiredness, fast or irregular heartbeat, fever, persistent sore throat, easy bruising/bleeding, mental/mood changes, vomiting, increased thirst, blurred vision, muscle cramps or weakness, chest pain, seizures, sudden weight gain, stomach pain or swelling, change in amount or color of urine, mouth sores. Tell your doctor immediately if any of these unlikely but serious side effects occur: dizziness, fainting. Tell your doctor immediately if any of these highly unlikely but very serious side effects occur: dark urine, yellowing of the eyes/skin, coughing up blood, vision problems. An allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of an allergic reaction include: rash, itching, swelling, dizziness, trouble breathing. Rare, possibly fatal, lung problems may occur months to years after using busulfan. Symptoms include trouble breathing; or persistent cough or congestion. Report any symptoms promptly. Even though this is an anti-cancer drug, busulfan may infrequently cause a new cancer to develop. If you notice other effects not listed above, contact your doctor or pharmacist.


Tell your doctor your medical history, especially of: seizures, head injury, blood disorders (thalassemia), diabetes, lung disease, serious infections, any allergies you may have. Because this medication can lower your body's ability to fight an infection, do not touch your eyes or the inside of your nose without first washing your hands. Do not have immunizations/vaccinations without the consent of your doctor, and avoid contact with people who have recently received oral polio vaccine. Use caution with sharp objects like safety razors or nail cutters, and avoid activities that might cause injury. Caution is advised when using this drug in children because they may clear the drug from their system faster, and therefore may require special dosing and monitoring. This drug may also cause fertility problems. This medication is not recommended for use during pregnancy. Busulfan may cause fetal harm. Avoid becoming pregnant while using this drug. Consult your doctor for more details. It is not known whether this drug passes into breast milk. Because of the potential risk to the infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

Drug Interactions

Tell your doctor or pharmacist of all prescription and nonprescription drugs you may use, especially of: azole antifungals (e.g., itraconazole,), thioguanine, acetaminophen, drugs that can cause seizures (e.g., bupropion), drugs that can increase seizure risk (e.g., phenothiazines such as chlorpromazine), other drugs which affect the bone marrow/immune system (e.g., other anti-cancer drugs, cyclosporine). Check your prescription and nonprescription labels carefully for acetaminophen-containing products. If needed, use the products cautiously 3 days before and during therapy with busulfan. Acetaminophen may increase busulfan blood levels and side effects. If acetaminophen is used, do not exceed recommended daily doses. Do not start or stop any medicine without doctor or pharmacist approval.


If overdose is suspected, contact your local poison control center or emergency room immediately. Symptoms of overdose may include severe fatigue, persistent sore throat, fever; or easy bruising or bleeding.


Do not share this medication with others. Laboratory tests (e.g., blood, liver) will be performed to monitor your progress.

Missed Dose

If you miss a dose, or the dose is interrupted, contact your doctor or pharmacist immediately to establish a new dosing schedule.


Store the vials at refrigerator temperature between 36 and 46 degrees F (2 and 8 degrees C). Do not freeze. After mixing and dilution in correct IV fluids (consult your pharmacist for details), the drug is stable at room temperature for 8 hours. Discard any unused liquid. Busulfan diluted in saline solution is stable for up to 12 hours if refrigerated as noted above.

Medical Alert

Your condition can cause complications in a medical emergency. For enrollment information call MedicAlert at 1-800-854-1166 (USA), or 1-800-668-1507 (Canada).