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    Nitrazepam molecular structure

    Nitrazepam Stats & Data

    Arem Dreem Enzed Konit Nigap mogadon baronite dormin
    Chemical Class Benzodiazepine
    Psychoactive Class Depressant
    Half-Life 15–38 hours (mean ~26 h; may be longer with advanced age or liver impairment)

    Pharmacology

    DrugBank
    State Solid

    Description

    A benzodiazepine derivative used as an anticonvulsant and hypnotic.

    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.

    Absorption

    Bioavailability is 53-94% following oral administration.

    Toxicity

    An overdose of nitrazepam may lead to impaired breathing, dizziness, decreased cognition and balance, bluish nails and lips, slurred speech, and extreme somnolence, among others. In severe overdose, these symptoms may progress to a coma with a possibility of death.

    Indication

    Used to treat short-term sleeping problems (insomnia), such as difficulty falling asleep, frequent awakenings during the night, and early-morning awakening.

    Half-life

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

    Receptor Profile

    Receptor Actions

    Modulators
    GABA-A receptor positive allosteric modulator (benzodiazepine site)
    Voltage-gated sodium channel modulator (anticonvulsant effects)

    Receptor Binding

    Gamma-aminobutyric acid receptor subunit alpha-1 antagonist

    Effect Profile

    Curated
    Benzodiazepine 7.1

    Strong anxiolysis, cognitive impairment, and euphoria with mild sedation

    Anxiolysis×3
    10
    Sedation / Relaxation×2
    5
    Motor / Cognitive Impairment×1
    10
    Euphoria / Mood Lift×1
    10

    Tolerance & Pharmacokinetics

    drugs.wiki
    Half-Life
    15–38 hours (mean ~26 h; may be longer with advanced age or liver impairment)
    Addiction Potential
    Moderate to high. Nitrazepam, like other benzodiazepines, carries a risk of dependence and withdrawal symptoms with prolonged or high-dose use.

    Tolerance Decay

    Full tolerance 14d Half tolerance 28d Baseline ~56d

    Tolerance to hypnotic and sedative effects develops over days to weeks of regular use and decays over several weeks of abstinence. Cross‑tolerance is substantial across benzodiazepines and partial with non‑benzodiazepine 'Z‑drugs'. Estimates reflect aggregated clinical knowledge and HR guidance; individual variability is high.

    Cross-Tolerances

    Other benzodiazepines
    80% ●●○
    Z-drugs
    50% ●○○

    Harm Reduction

    drugs.wiki

    Identification and naming: Nitrazepam is a long-acting nitrobenzodiazepine; common brand name is Mogadon and synonyms include RO 5-3059 and RO 4-5360—use correct naming to avoid confusing it with flunitrazepam or other benzos. Residual impairment: Because the elimination half-life averages 26 hours (range ~15–38 h), next‑day psychomotor impairment and a 'hangover' effect are common, even if you feel subjectively sober. Driving or operating machinery should be avoided until fully recovered. Interindividual variability: Oral bioavailability spans ~53–94%, so two people given the same dose can have very different effects; titrate slowly and avoid stacking doses. Combination risks: Co‑use with opioids, alcohol, barbiturates or GHB/GBL markedly increases the risk of respiratory depression, loss of consciousness and fatal overdose; if any depressants are involved, do not use alone and have naloxone available when opioids are present. General CNS depressant stacking (e.g., Z‑drugs, sedating antihistamines, gabapentinoids) also increases blackout and breathing suppression risk—avoid or use only with strong safeguards. Caffeine and stimulants may mask sedation without restoring coordination or reaction time; DrugBank advises limiting caffeine and strictly avoiding alcohol while on nitrazepam. Tolerance/withdrawal: Regular use can produce tolerance within weeks and dependence; abrupt discontinuation can cause severe withdrawal including seizures—medical tapering is essential. Populations: Older adults and those with liver impairment are more prone to prolonged sedation, confusion, and falls—use lower doses with extra monitoring. Legality/access: Nitrazepam is not marketed in the United States (reducing legitimate supply there); in unregulated markets, counterfeit 'benzos' may contain more potent analogues—drug checking and conservative dosing are strongly advised. Therapeutic note: Beyond hypnotic use, nitrazepam has anticonvulsant properties (e.g., myoclonic seizures), but non-medical redosing to chase sedation can rapidly escalate risk due to delayed peaks and long half-life.

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