Busulfan

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[edit] BRAND NAMES

[edit] STRUCTURE

Busulfan.jpg

[edit] MECHANISM OF ACTION

Busulfan is a bifunctional alkylating agent in which two labile methanesulfonate groups are attached to opposite ends of a four carbon alkyl chain. In aqueous media, busulfan hydrolyzes to release the methanesulfonate groups. This produces reactive carbonium ions that can alkylate DNA. DNA damage is thought to be responsible for much of the cytotoxicity of busulfan.

Busulfan depresses both normal and abnormal myeloid tissue.

Busulfan was the mainstay of the chemotherapeutic treatment of chronic myeloid leukemia (CML) until it was displaced by imatinib, though it is still in use to a degree as a result of the drug's relative low cost.

[edit] INDICATIONS

Busulfan is used in combination with cyclophosphamide as a conditioning regimen prior to allogeneic hematopoietic progenitor cell transplantation for chronic myelogenous leukemia.

Busulfan produces prolonged remission in polycythaemia vera. It is especially useful in cases resistant to radiophosphorus (32 P) and where there is marked thrombocytosis.

Busulfan is useful in selected cases of essential thrombocythaemia and myelofibrosis

[edit] DOSAGE

[edit] CONTRAINDICATIONS

[edit] PRECAUTIONS

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

[edit] SIDE EFFECTS

Adrenal insufficiency, bone marrow suppression ( particularly thrombocytopenia), pulmonary fibrosis, skin pigmentation

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES