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Nitrazepam

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🧬 Receptor activity

TargetActionAffinitySource
UncheckedKi 44.6 nMCHEMBL
Lysine-specific demethylase 4CKi 200000 nMCHEMBL
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Mechanism of action

Nitrazepam belongs to a group of medicines called benzodiazepines. This drug affects central benzodiazepine receptors, which are associated with inhibitory GABA (gamma amino butyric acid)receptors, leading to enhanced GABA binding activity. GABA is a major neurotransmitter in the brain, which causes somnolence, relaxation of muscles, a decrease in anxiety and general central nervous system depression. Nitrazepam has anticonvulsant properties that may be attributed to its ability to bind to voltage-dependent sodium channels. Sustained repetitive firing seems to be limited by benzodiazepines effect of slowing recovery of sodium channels from inactivation.

Pharmacodynamics

Nitrazepam is a type of benzodiazepine drug. It is a powerful hypnotic drug which possesses strong sedative, anxiolytic, amnestic, anticonvulsant, and skeletal muscle relaxant properties. Nitrazepam shortens the time required to fall asleep and lengthens the duration of sleep. It is also useful for the management of myoclonic seizures.

Pharmacokinetics

Half-life

15-38 hours (mean elimination half life 26 hours).

Absorption

Bioavailability is 53-94% following oral administration.

Metabolism

It is long acting, is lipophilic and is metabolised hepatically via oxidative pathways. [Wikipedia]
Half Life: 15-38 hours (mean elimination half life 26 hours).

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