Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2019 Publisher: medac, Gesellschaft für klinische Spezialpräparate mbH, Theaterstr. 6, 22880 Wedel, Germany
Pharmacotherapeutic group: cytostatics, alkylating agents
ATC code: L01AD02
The mode of action is believed to be partly as an alkylating agent and partly by inhibition of several steps in the synthesis of nucleic acid and inhibition of the repair of single strand breaks in DNA chains.
Lomustine “medac” is readily absorbed from the intestinal tract. A maximum plasma concentration of 0.5–2 ng/ml is reached after 3 hours following an oral dose of 30–100 mg/m².
The plasma disappearance of the chloroethyl-group follows by a single phased course with a half-life of 72 hours. The cyclohexyl-group disappears according to a twofold plasma disappearance with half-lives of 4 hours (t½α) and 50 hours (t½β). After oral application of radioactive marked lomustine the blood-brain-barrier is passed. Approximately 15 to 30% of the measured radioactivity in the plasma can be detected in the cerebrospinal fluid.
Lomustine “medac” is rapidly metabolised and metabolites are excreted mainly via the kidneys. Lomustine “medac” cannot be detected in its active form in the urine at any time.
Lomustine is embryotoxic and teratogenic in rats and embryotoxic in rabbits at dose levels equivalent to the human dose.
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