Busulfan (Intravenous)

Busulfan is an anticancer drug that stops cancer cells from growing and spreading in the body.


Busulfan is in a group of drugs called alkylating agents. It apparently works by interfering with bone marrow function. As Busulfan may also affect the growth of body cells, other effects will occur as well. Some of them could be serious and you must report them to your physician. Other effects may cause concern but may not be that serious. Some effects might not occur after months or years of Busulfan use.

Before you start Busulfan treatment, make sure to talk to your doctor about the benefits and risks of taking this medication.

This medication is only given by a doctor or under his/her direct supervision.

Before using Busulfan, you should consider the following factors. You and your doctor will have to weigh the risks of the medication against the positives it will bring.

  • Allergies—inform your doctor about any allergic or unusual reaction you may have had to Busulfan or any other medicine. Also inform your doctor if you're allergic to other things, including foods, animals, preservatives, or dyes. For nonprescription drugs, be sure to read the package or label ingredients carefully.
  • Children—appropriate studies haven't been done on the link between Busulfan injection effects and age in the kids' population. The medication's safety and efficacy has also not been established.
  • The elderly—appropriate studies done so far haven't shown geriatric-specific issues that would restrict the efficacy of Busulfan solution in older adults.
  • Pregnancy—studies in pregnant females have shown that Busulfan use can put the fetus at risk. The benefits of Busulfan treatment for a serious disease or life-threatening situation, however, may outweigh the possible risk.
  • Breastfeeding—there aren't enough studies done on women to determine infant risk when taking Busulfan during breastfeeding. Make sure to weigh the possible benefits against the possible risk of this medication before taking it while breastfeeding.

Conditions treated:

  • Chronic myeloid leukemia/CML
  • Other cancers requiring a stem cells/bone marrow transplant

Type of medicine:

  • Alkylating Agent

Side effects:

Diarrhea, nausea, vomiting, constipation, mouth sores, loss of appetite, dizziness, abdominal/stomach pain, swelling of ankles/hands/feet, headache, trouble sleeping, or flushing may occur. Be sure to inform your pharmacist/doctor right away if any of the effects mentioned persist or get worse.

Vomiting and nausea may be severe. Sometimes your doctor can prescribe some medicine to relieve or prevent vomiting and nausea. You can relieve vomiting and nausea by limiting your activities, eating small meals at several intervals, or not eating prior to treatment.

Many people using Busulfan get serious side effects. Nevertheless, your physician prescribed Busulfan because he/she concluded that its benefits to you outweigh the possible risks. Your doctor can lower your risk of side effects through careful monitoring.

Tell your physician as soon as possible if you suffer any severe side effects, such as signs of liver problem (e.g. persistent vomiting or nausea, yellowing of skin/eyes, dark urine, severe abdominal/stomach pain), mood or mental changes (e.g. depression, confusion, anxiety, hallucinations), muscle cramps, increased urination or thirst, irregular or fast heartbeat, bloody urine, coughing up blood, seizures, fainting, or swelling/pain/redness at injection site.

Busulfan rarely causes very serious (potentially fatal) lung disease. Inform your doctor at once if you have symptoms of lung infection, including shortness of breath, persistent cough, and chest pain.

Busulfan can cause other kinds of cancer like acute leukemia and tumors. Talk to your physician to get more information. Tell your doctor at once if you develop any cancer symptoms, including weight loss and unusual lumps.

Busulfan may affect your ovaries, potentially causing hormonal changes (e.g. missed menstrual periods) and reducing fertility. For more information, have a chat with your doctor.

This medication can shrink the testicles and reduce sperm production, effects that may decrease fertility in men. For more information, speak to your doctor.

Busulfan rarely causes a severe allergic reaction. However, seek medical help at once if you have any of these symptoms of a severe allergic reaction, such as rash, itching or swelling (especially of your face, tongue, or throat), troubled breathing, or severe dizziness.

This list of potential Busulfan side effects is not complete. If you notice any other effects not mentioned above, get in touch with your pharmacist or physician right away.

If you live in the US, contact your physician for medical advice regarding side effects. You can report all side effects to the FDA at www.fda.gov/medwatch or call FDA at 1-800-FDA-1088.


Busulfan injection is administered through central IV (i.e. a needle put into an upper chest vein). You'll receive Busulfan in a healthcare facility setting. You'll also be given other medicines to prevent some Busulfan side effects. Dosage is determined by your medical condition, response to treatment, weight, and lab test results.

Busulfan injection is normally given every six hours for four consecutive days. The medication must be administered slowly via the IV, and it may take at least two hours to complete each injection.

Busulfan can reduce blood cells that enable your body to fight infections. This may make you easily fall ill from being around sick people or more likely to bleed from any injury.

To ensure your blood cells don't reduce too much, you will need blood tests every week or month. You may also need liver function tests regularly. Busulfan can leave lasting effects on the body. Make sure to not miss any follow-up appointments with your physician for urine or blood tests.

Contact your physician immediately if you develop these signs of infection: fever, chills, flu symptoms, sore throat, easy bleeding or bruising (bleeding gums, nosebleeds), weight loss, unusual weakness, or mouth sores.

To get the most out of Busulfan, it's important to get each scheduled Busulfan dose as instructed. If you've missed a dose, contact your healthcare professional to set a new dosing program.

If you suspect a Busulfan overdose, call your emergency room or poison control center immediately. If you are in the US, call your poison control agency at 1-800-222-1222. If you're in Canada, you should call your provincial poison control agency.


The effects of certain medications can change when you take them with other medications or herbal products. This can make your medications not work properly or increase the likelihood of side effects. These medication interactions can occur, but don't always happen. Your doctor/pharmacist can normally manage or prevent interactions by close monitoring or changing how you take your medicines.

To help your healthcare providers give you great medical care, make sure to tell them about all the medication products you're using, such as prescription and nonprescription drugs, vitamins, minerals, and herbal products, before commencing treatment with Busulfan. While using Busulfan, don't change, start, or stop the dose of any other drugs you're taking without your physician's knowledge.

Some medications that might interact with Busulfan include acetaminophen, thioguanine, itraconazole, and nalidixic acid.

Of course there are many other possible drug interactions with Busulfan. Have a list of all medications you take. Be sure to give your healthcare providers this list to reduce your chances of suffering serious drug problems.


It is vitally important for your progress to be regularly checked by your doctor to ensure that Busulfan is working well. You may require blood tests to rule out unwanted effects.

Taking Busulfan while pregnant can put your unborn child at risk. Use an effective birth control method to prevent pregnancy during or after Busulfan treatment. If you suspect you've gotten pregnancy while taking Busulfan, tell your physician at once.

Busulfan can reduce white blood cell levels in your blood, making you more likely to get an infection. It also can reduce your platelets, which are essential for effective blood clotting. There are some precautions you should take if this happens to reduce the chances of bleeding or infection.

If possible, stay away from people with infections. Consult your doctor at once if you feel you're developing an infection or you have fever or chills, lower side/back pain, cough or hoarseness, or difficult or painful urination.

Don't take Busulfan if you have allergies to it.

See your doctor at once if you experience any unusual bruising/bleeding, tarry stools, pinpoint red marks on your skin, or blood in the stools or urine.

Take care when using a dental floss, toothpick, or regular toothbrush. Your healthcare providers may recommend other methods to clean your gums and teeth. Before having any form of dental treatment, consult your medical doctor.

Don't touch your eyes or inside your nose if you've touched something else or you've not washed your hands.

Be careful to not cut yourself when using sharp objects like a toenail or fingernail cutter or safety razor.

Avoid contact sports as well as other situations where injury or bruising may occur.

Busulfan can cause HVOD (hepatic veno-occlusive disease). This normally happens if you receive excess Busulfan, receive Busulfan before radiotherapy, or if you have had progenitor cell transplant. Contact your doctor at once if you suffer a bloated stomach or abdomen, upper right stomach/abdominal pain, yellow eyes/skin, or weight gain.

While you're receiving Busulfan treatment, and after you finish treatment, don't take any vaccinations (immunizations) without your doctor's knowledge. Busulfan can reduce the body's resistance and possibly cause the infection the vaccination is supposed to prevent.

In addition, other members of your household shouldn't receive oral polio vaccine as they might infect you with the polio virus. In addition, avoid people who've had an oral polio vaccination in the past several months. Don't get near them, and don't stay with them in the same place for too long. If you can't observe these precautions, then consider putting on a protective mask that covers your mouth and nose.

Before you take any medical exams, tell the doctor attending to you that you're taking Busulfan. The results of certain studies on body tissues might be affected by Busulfan.

If you want to have children, talk to your medical doctor before taking Busulfan. Some men who take Busulfan become infertile (childless).

Don't use other medications unless you've discussed them with your physician. This includes over-the-counter medicines, prescription medicines, vitamin supplements, or herbal products.


Not applicable. Busulfan isn't kept at home since it is administered in a hospital.


Some people develop new kinds of cancer after receiving Busulfan. Discuss the specific benefits and risks of you taking Busulfan with your doctor.

Stay away from people with infections or those who are sick. Tell your healthcare provider promptly if you have signs of infection.

This medicine is only to be given by your doctor or under his or her direct supervision.

Keep Busulfan tablets away from excess heat and moisture and at room temperature.

Don't take Busulfan if you're pregnant or become pregnant as it could endanger the unborn child. Use effective methods of birth control and let your doctor know if you get pregnant during treatment.

Busulfan may affect your ability to get children, whether you're male or female. This problem may be reversed but it may not in some cases. Speak to your doctor.

Before you receive this medication, tell your physician if you have a seizure disorder (e.g. epilepsy), weak immune system (e.g. bone marrow depression), history of breathing or lung problems or head injury, or if you've recently used other cancer medicines or have had radiotherapy.

Busulfan can reduce your white blood cell count. This can make you more vulnerable to infections. You'll need weekly or monthly blood tests. You may also require regular liver function tests. Busulfan can leave long-term effects on the body. Honor all follow-up appointments with your physician for urine or blood exams.

While taking Busulfan, avoid a “live” vaccine and don't get close to anybody who has had a live vaccine recently. There's a possibility that you could catch a virus. Live vaccines include oral polio, measles, mumps, smallpox, rotavirus, yellow fever, typhoid, chickenpox (varicella), H1N1 influenza, rubella (MMR), nasal flu vaccine, and BCG (Bacillus Calmette-Guerin).

Contact your healthcare professional immediately if you have signs of infection like fever, chills, flu symptoms, persistent sore throat, weight loss, unusual weakness, mouth sores, pale skin, or easy bruising or bleeding (e.g. bleeding gums or nosebleeds).

Last Reviewed:
December 25, 2017
Last Updated:
April 04, 2018