Brands, Medical Use, Clinical Data
Drug Category
Dosage Forms
- Powder for solution
- Wafer
Brands / Synonyms
BCNU; Becenun; Bi CNU; Bicnu; Bischlorethylnitrosourea; Bischlorethylnitrosurea; Carmubris; Carmustin; Gliadel; Gliadel Wafer; Nitrumon
Indications
For the treatment of brain tumors, multiple myeloma, Hodgkin's disease and Non-Hodgkin's lymphomas.
Pharmacology
Carmustine is one of the nitrosoureas indicated as palliative therapy as a single agent or in established combination therapy with other approved chemotherapeutic agents in treatment of brain tumors, multiple myeloma, Hodgkin's disease, and non-Hodgkin's lymphomas. Although it is generally agreed that carmustine alkylates DNA and RNA, it is not cross resistant with other alkylators. As with other nitrosoureas, it may also inhibit several key enzymatic processes by carbamoylation of amino acids in proteins.
Mechanism of Action
Carmustine causes cross-links in DNA and RNA, leading to the inhibition of DNA synthesis, RNA production and RNA translation (protein synthesis). Carmustine also binds to and modifies (carbamoylates) glutathione reductase. This leads to cell death.
Absorption
5 to 28% bioavailability
Toxicity
The oral LD50s in rat and mouse are 20 mg/kg and 45 mg/kg, respectively. Side effects include leukopenia, thrombocytopenia, nausea. Toxic effects include pulmonary fibrosis (20-0%) and bone marrow toxicity.
Biotrnasformation / Drug Metabolism
Hepatic and rapid with active metabolites. Metabolites may persist in the plasma for several days.
Contraindications
BiCNU should not be given to individuals who have demonstrated a previous hypersensitivity to it.
Drug Interactions
No information provided.
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