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. Binding to DNA is believed to play a role in its mode of action , and di - guanyl  derivative has been isolated ,but intersatrand crosslinking has not been conclusively  demonstrated . The basic for the uniquely selective effects of  busulfan on granulocytopoiesis  is not fully understood.

DOSE :- 2-6 mg/day (0.06mg/kg/day) orally.

SIDE EFFECTS:- 

Common side effects are:- 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, or yellow eyes and skin.

USED:- used treat a certain type of chronic myelogenous leukemia (CML; a type of cancer of the white blood cells). Busulfan is in a class of medications called alkylating agents. It works by slowing or stopping the growth of cancer cells in your body.