Busulfan, an alkyl sulfonate, has historically been used to treatchronic myelogenous leukemia, polycythemia vera (increased red blood cell mass and increased number of WBCs and platelets), and other myeloproliferative (pertaining to an overactive bone marrow) disorders. It’s also used for treatment of leukemia during bone marrow transplant procedures.
Busulfan is rapidly well absorbed from the GI tract. Little is known about its distribution.
Busulfan is extensively metabolized in the liver before urinary ex-cretion. Its half-life is 2 to 3 hours.
As an alkyl sulfonate, busulfan forms covalent bonds with the DNA molecules in alkylation.
Busulfan primarily affects granulocytes (a type of WBC) and, to a lesser degree, platelets. Because of its action on granulocytes, ithas been used for treating chronic myelogenous leukemia and asadjunct therapy before and after bone marrow transplantation.
Busulfan is also effective in treating polycythemia vera, although other drugs are usually used to treat it because busulfan can cause severe myelosuppression (halting of bone marrow function).
There’s an increased risk of bleeding when busulfan is taken with anticoagulants or aspirin. Concurrent use of busulfan and thioguanine may cause liver toxicity, esophageal varices (enlarged, swollen veins in the esophagus), or portal hypertension (increased pressure in the portal vein of the liver). (See Adversereactions to busulfan.)