Lavol Mechanism of Action

Pharmacology: Mechanism of Action: Although Nimetazepam exhibits a spectrum of activity (harmless, sedative, muscle relaxant, stimulates and promotes sleep, anti-convulsant effects, etc.) similar to Nitrazepam, it is stronger and faster acting compared to Nitrazepam (in mice and rats). The mechanism of hypnotic action of nimetazepam is considered to be related to suppression of the emotional mechanisms of the limbic system and hypothalamus and suppression of the activating limbic system.
Pharmacokinetics: Nimetazepam appears rapidly in the blood after oral administration of 5 mg in healthy adult subjects and the blood concentration is 10.4 ng/ml at 1 hour after administration which is similar to the concentration (13.4 ng/mL) within 2-4 hours when the peak level is reached. Hence, Nimetazepam exhibits higher initial blood concentrations than Nitrazepam. The 1-desmethyl and 3-hydroxy forms were identified as blood metabolites but its blood level were quite low in comparing to blood concentrations of unchanged compounds.