BiCNU (Carmustine) Drug Information: Clinical Pharmacology

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May 25, 2012

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Cancer is the uncontrolled growth of abnormal cells anywhere in a body. The abnormal cells are termed cancer cells, malignant cells, or tumor cells. Many cancers and the abnormal cells that compose the cancer tissue are further identified by the name of the tissue that the abnormal cells originated from (for example, breast cancer, lung cancer, colon cancer). Cancer is not confined to humans; animals and other living organisms can get cancer. Below is a schematic that shows normal cell division and how when a cell is damaged or altered without repair to its system, the cell usually dies. Also shown is what can occur when such damaged or unrepaired cells do not die and become cancer cells and proliferate with uncontrolled growth; a mass of cancer cells develop. Frequently, cancer cells can break away from this original mass of cells, travel through the blood and lymph systems, and lodge in other organs where they can again repeat the ...

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CLINICAL PHARMACOLOGY

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.

Intravenously administered carmustine is rapidly degraded, with no intact drug detectable after 15 minutes. However, in studies with ¹⁴C-labeled drug, prolonged levels of the isotope were detected in the plasma and tissue, probably representing radioactive fragments of the parent compound.

It is thought that the antineoplastic and toxic activities of carmustine may be due to metabolites. Approximately 60% to 70% of a total dose is excreted in the urine in 96 hours and about 10% as respiratory CO₂. The fate of the remainder is undetermined.

Because of the high lipid solubility and the relative lack of ionization at physiological pH, carmustine crosses the blood-brain barrier quite effectively. Levels of radioactivity in the CSF are ≥50% of those measured concurrently in plasma.

Last reviewed on RxList: 5/5/2011
This monograph has been modified to include the generic and brand name in many instances.