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Nitrazepam

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Collated from TripSit, Pharmacology, DrugCentral. Where sources differ (e.g. dosing), Compare shows them side by side.

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BenzodiazepineHabit-formingDepressantTS

Also known as mogadon, baronite, dormin, dreem, enzed, gentravit, hypnonex, hypnoril, hypnotex, konit, nicare, nigap, nipam, nirosun, nitavan, nithraTS

Hypnotic Benzodiazepine, that is used for short term relief of anxiety and insomnia. It has a pronouced affect on respritory action.TS

Oral

Route dataTripSit

Dose
WeakerStronger
ThresholdLightCommonStrongHeavy
—2–5 mg5–15 mg15–20 mg20 mg+
025 mg
LightCommonStrongHeavy
Duration
ShorterLonger
Onset10–40 minutes
Total5–8 hours
After-effects6–12 hours
OnsetCome-upPeakOffset

🧬 Receptor activityPHDC

TargetActionAffinitySource
Unchecked—Ki 44.6 nMCHEMBL
Lysine-specific demethylase 4C—Ki 200000 nMCHEMBL
GABA-A receptor alpha-1/beta-2/gamma-2 (GABRA1)Positive allosteric modulator8 EC50DRUGCENTRAL
GABA-A receptor; anion channel (GABRA1)—7.42 IC50DRUGCENTRAL
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Mechanism of actionPH

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.

PharmacodynamicsPH

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-lifePH

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

AbsorptionPH

Bioavailability is 53-94% following oral administration.

MetabolismPH

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).

Plan when to take Nitrazepam — see where onset, peak and comedown land on the clock

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