Country: South Africa
Language: English
Source: South African Health Products Regulatory Authority (SAHPRA)
Bm_squib
BiCNU injection SCHEDULING STATUS: BiCNU S4 Diluent S1 PROPRIETARY NAME (and dosage form): BiCNU injection (Lyophilized powder in vial for reconstitution) Dehydrated Alcohol, injection USP COMPOSITION BiCNU is a lyophilized powder for injection containing 100 mg carmustine per vial. When reconstituted with 3 mL dehydrated alcohol and 27 mL sterile water for injection, each mL of the resulting solution will contain 3,3 mg of carmustine in 10% ethanol. Diluent contains 3 mL dehydrated alcohol. PHARMACOLOGICAL CLASSIFICATION BiCNU injection A 26 Cytostatic agents Diluent A 34 Other PHARMACOLOGICAL ACTION BiCNU (1,3 - bis(2 chloroethyl)-1-nitrosourea) is one of the nitrosoureas. The structural formula is: {illustrated here} BiCNU alkylates DNA and RNA and has been shown to inhibit several enzymes by carbamoylation of amino acids in proteins. BiCNU is not cross resistant with other alkylating agents. Intravenously administered BiCNU is rapidly degraded, with no intact drug detectable after 15 minutes. However in studies with C 14 labelled drug, prolonged levels of the isotope were observed in the plasma and tissue, probably representing radioactive fragments of the parent compound. It is thought that the antineoplastic and toxic activities of BiCNU may be due to metabolites. Approximately 60 to 70 percent of a total dose is excreted in the urine in 96 hours and about 10 percent as respiratory CO 2 . The fate of the remainder is undetermined. Because of high lipid solubility and the relative lack of ionization at a physiological pH, BiCNU crosses the blood brain barrier quite effectively. Levels of radioactivity in the CSF are greater than those measured concurrently in plasma. INDICATIONS BiCNU is indicated as palliative therapy as a single age Read the complete document