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It busulfan falls in the categories of immunosuppressive Agents, Antineoplastic Agents, Alkylating agents and Myeloablative Agents. It works by interupting replication of DNA and transcription of RNA ultimately causing disruption in the nucleic acid functions. In the end it induces irreversible apoptosis and therefore disrupts the spread of cancerous cells. Busulfan is used therapeutically in synergy with cyclophosphamide to produce a conditioning course of therapy before progenitor cell transplant protocols in Chronic Myelogenous Leukaemia.
The drug is also used widely in the used as part of the pre-transplant preparations for those patients requiring bone marrow transplants for advanced Myeloid LeuKaemia as well as other conditions that are non-malignant. This is therefore a very important chemotherapeutic agent in the management of Myeloid Leukaemia and other non-malignant cancers due its apoptosis causing effects on target cancerous cells. The drug is in three forms i.e. 2mg tablets; 25 mg capsules a liquid injection. Delivery of the drug is therefore possible through the oral and intravenous routes.
When used in the treatment of Chronic Myeloid leukaemia, the drug should be given as follows; the patient should first be pre-medicated with anti-convulsion drugs followed by an initial busulfan dose of 60 mcg/kg/day or 1.8 mg/m²; 4-8 mg PO qDay. Maintenance doses should be given subsequently at 1-4 mg/day to 2 mg/week PO. The patient is closely monitored and once the white blood cell count is 50,000/mcl the initial dosage should be resumed. When given in combination with cyclophosphamide, an intravenous dose of 0.
8 mg/kg at intervals of 6 hours for four days until WBC count reaches 15,000/mm3. When preparing an intravenous injection dose the preferred diluents are NS or and D5W. It should be prepared with diluents volume being 10 times that of busulfan until the desirable concentration of >0.5 mg/ml is attained. The preparation is then prepared through
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