Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1     Pharmacodynamic properties

Pharmacotherapeutic Group: Antineoplastic medicine, alkylating agent, nitrosourea ATC-Code: L01AD01

Carmustine alkylates DNA and RNA, has also been shown to inhibit several enzymes by carbamoylation of amino acids in proteins. It is thought that the antineoplastic and toxic activities of Carmustine may be due to metabolites.

Pharmacokinetic Properties

5.2     Pharmacokinetic properties

Distributio n
Intravenously administered Carmustine is rapidly degraded, with no drug intact detectable after 15 minutes. Because of the good lipid solubility and the lack of ionization at the physiological pH, Carmustine is very well transferred through the blood-brain barrier. Levels of radioactivity in the CSF are at least 50% higher than those measured concurrently in plasma.
The kinetic of carmustine in humans is characterized by a two-chamber model. After the intravenous infusion over 1 hour, the carmustine-plasma level drops in a biphasic manner. The half life α accounts to 1-4 minutes and the half life β accounts to 18-69 minutes.

Metabolism
It is presumed that the metabolites of carmustine causes its antineoplastic and toxic activity.

Eliminatio n

Approximately 60-70% of a total dose is excreted in the urine in 96 hours and about 10% as respiratory CO2. The fate of remainder is undetermined.