Busulfan

A mixture of 16.3 g of (2-chloro-5-methylphenyl)glycidic ether (from epichlorohydrin and 2-chloro-5-methylphenol) and 6.2 g of t-butylamine in 50 ml of ethanol is heated at reflux for 6 hours. The solvent is removed, the residue Is washed with water and then extracted with benzene. The dried extract is evaporated to give 1-t-butylamino-3-(2-chloro-5-methylphen-oxy)-2-propanol. Treatment of the free base in benzene solution with dry hydrogen chloride yields the hydrochloride salt. 

Chemical Name 1,4-butanediol dimethanesulfonate Common Name — 

Burroughs Wellcome Techni-Pharma Wellcome Wellcome 

6 grams of redistilled 1,4-butanediol were dissolved in 10 ml of pyridine and the solution was cooled in ice and water. 9.6 grams of redistilled methane-sulfonyl-chloride were added dropwise at such a rate that the temperature did not rise above 20°C. The solution was then allowed to stand at room temperature for 30 minutes, during which time the temperature rose to 60°C. A thick precipitate of pyridine hydrochloride was formed. 

Trade Name Manufacturer Coumry Year Introduced 

Betadrenol Betadrenol Bet ad ran Looser (Lucer) Panimlt Ophtorenin 

A mixture of 16.3 g of (2-chloro-5-methylphenyl)glycidic ether (from epichlorohydrin and 

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Burlington Biomedical Scientific Corporation, 220 Burnt umber, 28 Busulfan, 28... 

Mabertin - Temazepam Mablin - Busulfan Macasirool - Furosemide Macmiror - Nifuratel Macocyn - Dxytetracycline Macphenicol -Thiamphenicol Macrodantin - Nitrofurantoin Macro-Dil - Midecamycin Madaprox - Naproxen Madar - Nordazepam Madecitina - Metampicillin sodium Madelen - Drnidazole Madlexin - Cephalexin Madopar - Benserazide Madopark - Benserazide... 

British investigators (Haddow and Timmis 1951) synthesized and studied esters of the methanesulfonic acid. The most active derivative was the dimethylsulfonic ester of 1,4-butanedione, known as busulfan. Busulfan interacts with the thiol groups of proteins and amino acids some of its metabolites can alkylate the thiols of cysteine, peptides and proteins. Busulfan exerts selective cytotoxic activity in hematopoietic bone marrow cells and inhibits the formation of granulocytes and platelets. It slightly affects the lymphoid tissue. 

Busulfan was used for the treatment of chronic myeloid leukemia and polycytemia vera. 

The malignant cells appear to be more susceptible to the effects of the alkylating drugp. Examples of alkylating drag include busulfan (Myleran, Busulfex) and chlorambucil (Leukeran). 

Acute Pulmonary Inflammation Alkylating Agents Busulfan Cyc1ophosphamide... 

Bleomycin, busulfan, carmustine, cyclophosphamide, methotrexate, mitomycin, and radiation therapy... 

List the nonhematologic toxicity to high-dose chemotherapy used in myeloablative preparative regimens, specifically busulfan-induced seizures, hemorrhagic cystitis, gastrointestinal toxicities, and sinusoidal obstruction syndrome. 

The optimal myeloablative preparative regimen is challenging to study because several indications for HCT (e.g., SCID and thalassemia) are rare enough that it is not feasible or is cost-prohibitive to conduct clinical trials that are powered adequately to detect clinically relevant differences. The longterm outcomes of busulfan-cyclophosphamide (BU-CY) and... 

Seizures have been reported in both adult and pediatric patients receiving high-dose busulfan for HCT preparative regimens. Anticonvulsants are used to minimize the risk of... 

Busulfan Seizures, busulfan concentrations if being used with the BU-CY preparative regimen, number of vomiting episodes, nausea by patient self-report... 

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