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BUSULFAN

  BUSULFAN BRAND NAME:- MYLERAN, BUSUPHAN 2mg tab. BUSULFAN is highly specific for myeloid elements; granulocyte precursors being the most sensitive, followed by  those of platelets and RBC . It produces little effect on lymphoid tissue and g.i.t. Hyperuricaemia is common; Pulmonary fibrosis and skin pigmentation are the specific adverse effects. Sterility also occurs. It is the drug of choice for chronic myeloid leukaemia.  PHARMACODYNAMIC:- Busulfan is an alkylsulfonate. It is an alkylating agent that forms DNA-DNA interstrand crosslinks between the DNA bases guanine and adenine and between guanine and guanine.[7] This occurs through an SN2 reaction in which the relatively nucleophilic guanine N7 attacks the carbon adjacent to the mesylate leaving group. DNA crosslinking prevents DNA replication. Because the intrastrand DNA crosslinks cannot be repaired by cellular machinery, the cell undergoes apoptosis.  MECHANISM OF ACTION:- Busulfan is an alkylsulfonate agent. ...