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Busulfan Prescription
Generic Name: busulfan (oral/injection) (bue SUL fan)
Brand Name: Busulfex, Myleran
Physician reviewed busulfan (oral/injection) (oral/injection) patient information - includes busulfan (oral/injection) description, dosage and directions.
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Busulfan Drug Information:

Busulfan oral (taken by mouth) is used to treat the symptoms of chronic myelogenous leukemia (a type of blood cancer). Busulfan is not a cure for leukemia. Busulfan injection is used together with a medicine called Cyclophosphamide, to prepare your body to receive a stem cell transplant from a donor's bone marrow. Busulfan may also be used for purposes not listed in this medication guide. Busulfan affects your immune system. You may get infections more easily, even serious or fatal infections. Call your doctor if you have a fever, chills, cough, mouth sores, or unusual bleeding or bruising. Learn more

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Busulfan Side Effects

For the Consumer

Applies to busulfan: intravenous solution


Intravenous route (Solution)

Busulfan causes severe or prolonged myelosuppression at recommended doses. Hematopoietic progenitor cell transplantation is required to prevent life-threatening or fatal complications of severe or prolonged myelosuppression.

Along with its needed effects, busulfan may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor or nurse immediately if any of the following side effects occur while taking busulfan:

More common

  • Black, tarry stools
  • bloated abdomen or stomach
  • blood in the urine or stools
  • blurred vision
  • chest pain
  • cough or hoarseness
  • dizziness
  • fast or irregular breathing
  • fast, pounding, or irregular heartbeat or pulse
  • fever or chills
  • headache
  • lower back or side pain
  • nervousness
  • pain and fullness in the upper abdominal or stomach
  • painful or difficult urination
  • pinpoint red spots on the skin
  • pounding in the ears
  • skin rash or itching
  • slow heartbeat
  • swelling of the eyes or eyelids
  • tightness in the chest
  • trouble breathing
  • unusual bleeding or bruising
  • weight gain
  • yellow eyes and skin

Incidence not known

  • seizures

Some side effects of busulfan may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  • Acid or sour stomach
  • back pain
  • belching
  • bloody nose
  • depression
  • diarrhea
  • difficulty having a bowel movement (stool)
  • fear
  • heartburn
  • indigestion
  • loss of appetite
  • lack or loss of strength
  • sneezing
  • stomach discomfort or upset
  • stuffy nose or runny nose
  • swelling or inflammation of the mouth
  • tenderness, pain, swelling, warmth, skin discoloration, and prominent superficial veins over affected area
  • trouble sleeping

For Healthcare Professionals

Applies to busulfan: intravenous solution, oral tablet


Very common (10% or more): Prolonged myelosuppression (i.e., severe granulocytopenia, leukopenia, thrombocytopenia, anemia, or any combination thereof) (100%)

Rare (less than 0.1%): Aplastic anemia

Frequency not reported: Prolonged prothrombin time

Postmarketing reports: Febrile neutropenia


Very common (10% or more): Rhinitis (44%), lung disorder (34%), cough (28%), epistaxis (25%), dyspnea (25%)

Rare (less than 0.1%): Bronchopulmonary dysplasia

Frequency not reported: Pneumonia, hyperventilation, alveolar hemorrhage, pharyngitis, hiccup, asthma, atelectasis, pleural effusion, hypoxia, hemoptysis, sinusitis, interstitial fibrosis


Very common (10% or more): Tachycardia (44%), hypertension (36%), chest pain (26%), vasodilation (25%)

Common (1% to 10%): Cardiac tamponade in patients with thalassemia (at high doses)

Frequency not reported: Arrhythmia, atrial fibrillation, ventricular extrasystoles, third degree heart block, thrombosis (all episodes were associated with the central venous catheter), hypotension, flushing and hot flashes, cardiomegaly, ECG abnormality, left-sided heart failure, pericardial effusion, cardiac tamponade

Postmarketing reports: Thrombotic microangiopathy (TMA)


Rare (less than 0.1%): Lens disorder and cataract (which may be bilateral), corneal thinning (reported after bone marrow transplantation preceded by high-dose therapy)


Very common (10% or more): Rash (57%), pruritus (28%)

Common (1% to 10%): Alopecia


Very common (10% or more): Hypomagnesemia (77%), hyperglycemia (66%), hypokalemia (64%), hypocalcemia (49%), hyperbilirubinemia (49%), edema (36%), serum glutamic pyruvic transaminase (SGPT) elevation (31%), creatinine increased (21%)

Frequency not reported: Hypervolemia, hypophosphatemia, hyponatremia


Very common (10% or more): SGPT Elevation

Common (1% to 10%): Hepatic veno-occlusive disease (HVOD)

Rare (less than 0.1%): Jaundice, abnormal hepatic function, biliary fibrosis

Frequency not reported: Alkaline phosphatase increase, jaundice, hepatomegaly

Nervous system

Very common (10% or more): Headache (69%), asthenia (51%), dizziness (30%)

Common (1% to 10%): Seizures

Very rare (less than 0.01%): Myasthenia gravis

Frequency not reported: Cerebral hemorrhage, coma, delirium, agitation, encephalopathy, confusion, hallucinations, lethargy, somnolence


Common (1% to 10%): Neoplasms benign, malignant, and unspecified (including cysts and polyps)

Postmarketing reports: Tumor lysis syndrome, cellular dysplasia


Very rare (less than 0.01%): Gynecomastia

Frequency not reported: Dysuria, oliguria, hematuria, hemorrhagic cystitis


Very common (10% or more): Nausea (98%), stomatitis (mucositis) (97%), vomiting (95%), anorexia (85%), diarrhea (84%), abdominal pain (72%), dyspepsia (44%), dry mouth (26%), rectal disorder (25%), abdominal enlargement (23%)

Frequency not reported: Esophagitis, ileus, hematemesis, pancreatitis, rectal discomfort

Postmarketing reports: Tooth hypoplasia


Very common (10% or more): Chills (46%), back pain (23%)

Frequency not reported: Myalgia, arthralgia


Frequency not reported: Graft-versus-host disease

Postmarketing reports: Severe bacterial, viral (e.g., cytomegalovirus viremia), fungal infections, sepsis


Very common (10% or more): Allergic reaction (26%)


Very common (10% or more): Injection site inflammation (25%)

Frequency not reported: Injection site pain


Frequency not reported: Blood urea nitrogen (BUN) increased

Editorial References and Review

Medically reviewed by USARx EDITORIAL TEAM Last updated on 1/27/2021.

Source: Drugs.com Busulfan (www.drugs.com/mtm/busulfan-oral-injection.html).