Revision Year: 2011 Publisher: RS & M Consulting GmbH, Industriestrasse 8, D-82194 Groebenzell, GERMANY
Pharmacotherapeutic class: 1,4-benzodiazepine derivative, hypnotic
ATC-Code: N05CD06
Lormetazepam is a psychotropic substance belonging to the class of 1,4-benzodiazepines with sedative and hypnotic properties. It also exerts tension relieving, excitation suppressing and anxiolytic effects. In addition, Lormetazepam has central muscle relaxant and anticonvulsive properties.
Lormetazepam has a high affinity for specific binding sites in the central nervous system. These benzodiazepine receptors display a close functional relationship to the receptors of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). As a benzodiazepine receptor agonist, Lormetazepam reinforces the GABA-ergic inhibition of the activity of distal neurons.
After intravenous administration, approximately 88% of the administered dose of Lormetazepam is bound to plasma proteins.
Biotransformation takes place in the liver by glucuronidation of the C3-hydroxyl group. Only a minor fraction is demethylated to form the active metabolite Lorazepam and inactivated immediately by glucuronidation. Since demethylation of Lormetazepam occurs slowly, the substance is not a prodrug of Lorazepam.
In the urine, more than 90 % of Lormetazepam is present as Lormetazepam-3-O-glucuronide and less than 10% as Lorazepam-glucuronide. After an oral dose of 2 mg Lormetazepam less than 6% was identified in the urine as Lorazepam-glucuronide. No free Lormetazepam was found.
The elimination half-life of Lormetazepam and its active metabolites is in average 9 hours (8–15 h).
The rate of inactivation and elimination of Lormetazepam is not affected by impaired hepatic function.
The pharmacokinetic properties of Lormetazepam remain largely unaffected in patients with renal impairment, because essentially only accumulation of the biologically inactive Lormetazepam-glucuronide occurs. As a rule, dose adjustment is not required.
Lormetazepam passes the placenta and is detectable in breast milk.
Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential and toxicity to reproduction.
Acute toxicity of Lormetazepam is low (see section 4.9 Overdose).
Studies of chronic toxicity in the rat and dog gave no indication of substance-specific toxic effects.
Lormetazepam has been sufficiently studied with regard to mutagenic effects.
In tumorigenicity long-term studies no indication of a tumorigenic effect of Lormetazepam was observed in animals.
Benzodiazepines pass the placenta. Experiments for Lormetazepam are not available. Animal experiments of toxicity to reproduction of Lormetazepam gave no indication of teratogenic effects.
There are indications of behavioural disorders in the progeny of mother animals exposed to benzodiazepines.
Sedalor 2 mg/10 ml solution for injection or for infusion does not contain any component which results in an additional hazard to the environment during storage, distribution, use and disposal.
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