III. Mechanism

  1. See Alkylating Agent
  2. Synthetic derivative of dimethane-sulfonate with antineoplastic properties
  3. In vivo, generates carbonium ions which alkylate DNA, inhibiting DNA Replication and transcription

IV. Medications

  1. Busulfan Tablets (Myleran): 2 mg
  2. Busulfan Injection (Busulfex)

V. Dosing

  1. See other references for disease specific dosing protocols

VI. Adverse Effects

  1. Adrenal Insufficiency
  2. Alopecia
  3. Bone Marrow Suppression (severe)
  4. Hepatic Sinusoidal Obstruction Syndrome (Veno-occlusive Disease)
  5. Hyperuricemia
    1. Consider startic Allopurinol for prophylaxis prior to starting Busulfan
    2. Maintain adequate hydration
  6. Impaired future fertility
  7. Pulmonary Fibrosis
  8. Secondary Malignancy (and cellular dysplasia)
  9. Seizures
    1. Seizure Prophylaxis initiated prior to starting Busulfan
  10. Tooth Hypoplasia

VII. Safety

  1. Avoid in Lactation
  2. Avoid in pregnancy (contraindicated in all trimesters)
    1. Teratogenic and adverse outcomes
    2. Use reliable Contraception
  3. Monitoring
    1. Complete Blood Count
    2. Liver Function Tests

VIII. Drug Interactions

  1. Drugs that increase Busulfan levels (decreased clearance)
    1. Acetaminophen
    2. Itraconazole
  2. Drugs that decrease Busulfan levels (increased clearance)
    1. Phenytoin

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Related Studies

Ontology: Busulfan (C0006463)

Definition (NCI_NCI-GLOSS) An anticancer drug that belongs to the family of drugs called alkylating agents.
Definition (NCI) A synthetic derivative of dimethane-sulfonate with antineoplastic and cytotoxic properties. Although its mechanism of action is not fully understood, busulfan appears to act through the alkylation of DNA. Following systemic absorption of busulfan, carbonium ions are formed, resulting in DNA alkylation and DNA breaks and inhibition of DNA replication and RNA transcription. (NCI04)
Definition (CSP) alkylating agent having a selective immunosuppressive effect on bone marrow; has been used in the palliative treatment of chronic myeloid leukemia.
Definition (MSH) An alkylating agent having a selective immunosuppressive effect on BONE MARROW. It has been used in the palliative treatment of chronic myeloid leukemia (MYELOID LEUKEMIA, CHRONIC), but although symptomatic relief is provided, no permanent remission is brought about. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), busulfan is listed as a known carcinogen.
Definition (PDQ) A synthetic derivative of dimethane-sulfonate with antineoplastic and cytotoxic properties. Although its mechanism of action is not fully understood, busulfan appears to act through the alkylation of DNA. Following systemic absorption of busulfan, carbonium ions are formed, resulting in DNA alkylation and DNA breaks and inhibition of DNA replication and RNA transcription. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41947&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41947&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C321" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109) , Hazardous or Poisonous Substance (T131)
MSH D002066
SnomedCT 2571007, 387138002
LNC LP18783-8, MTHU004760
English Busulphan, busulfan, 1,4-Butanediol, dimethanesulfonate, 1,4-Bis(methanesulfonoxy)butane, 1,4-Bitanediol Dimethanesulfonate Esters, 1,4-Di(methanesulfonyloxy)butane, 1,4-Di(methylsulfonyloxy)butane, 1,4-Butanediol Dimethylsulfonate, Methanesulfonic Acid Tetramethylene Ester, Sulfabutin, Tetramethylene Bis(methanesulfonate), Busulfanum, Bussulfam, Myeleukon, busulfan (medication), BUSULFAN, Busulfan [Chemical/Ingredient], bsf, Tetramethylene bis[methanesulfonate], 1, 4-Bis[methanesulfonoxy]butane, Methanesulfonic acid, tetramethylene ester, Busulfan (product), Busulfan (substance), BSF, busulphan, BU, BUS, Busulfan
Swedish Busulfan
Czech busulfan
Finnish Busulfaani
Russian MIELOSAN, BUSUL'FAN, БУСУЛЬФАН, МИЕЛОСАН
Japanese ブスルファン
Croatian BUSULFAN
Spanish busulfán, busulfano (sustancia), busulfán (sustancia), Busulfán, busulfano (producto), busulfano, Busulfano
Polish Busulfan
French Busulfan
German Busulfan, Busulphan
Italian Busulfano
Portuguese Bussulfano