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Lormetazepam

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Mechanism of action

Lormetazepam, as a benzodiazepine, binds to the regulatory site between the α and γ subunits of γ-aminobutryic acid (GABA) A receptors with γ2 and α1, α2, α3, or α5 subunits. This facilitates the opening of the chloride channel allowing chloride ions to flow into the neuron resulting in hyperpolarization. Hyperpolarized neurons require greater simulation to reach their action potential threshold. The general inhibitory effect on neuronal depolarization produces the effects of lormetazepam.

Pharmacodynamics

Lormetazepam is a benzodiazepine which reduces central nervous system (CNS) activity. It produces anxiolytic, muscle relaxant, sedative and hypnotic effects. Because it is a short-acting benzodiapine, it does not produce significant sedation after waking.

Pharmacokinetics

Half-life

The terminal phase half life is 11 h.

Metabolism

Metabolised to an inactive metabolite via glucuronide conjugation

Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.