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    Loprazolam molecular structure

    Loprazolam Stats & Data

    Depressant Benzodiazepine
    Dormonoct
    PubChem CID 3033860
    NPS DataHub
    MW464.91
    FormulaC23H21ClN6O3
    CAS61197-73-7
    IUPAC(2''Z'')-6-(2-Chlorophenyl)-2-[(4-methyl-1-piperazinyl)methylene]-8-nitro-2,4-dihydro-1''H''-imidazo[1,2-''a''][1,4]benzodiazepin-1-one
    SMILESCN1CCN(CC1)C=C1N=C2CN=C(c3ccccc3Cl)c3cc(N(=O)=O)ccc3N2C1=O
    InChIKeyUTEFBSAVJNEPTR-RGEXLXHISA-N
    Chemical Class Imidazobenzodiazepine
    Psychoactive Class Depressant

    Pharmacology

    DrugBank

    Description

    Loprazolam is an imidazobenzodiazepine with anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. It is indicated for the short-term treatment of insomnia including difficulty in falling asleep and/or frequent nocturnal awakenings. Loprazolam is recommended as a short-term therapy only, due to adverse events associated with the drug including dependence and withdrawal symptoms. It is a positive modulator of GABA-A receptor that enhances the inhibitory neurotransmission. It is not an FDA-approved drug.

    Toxicity

    PubChem

    Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor.

    Carcinogenicity

    No indication of carcinogenicity to humans (not listed by IARC).

    Tolerance & Pharmacokinetics

    drugs.wiki

    No tolerance chart. Our decay curves for these drugs were estimates, and a curve can make tolerance look longer-lasting than it is, which is the dangerous direction.

    How fast tolerance to these drugs fades after a break has not been measured well enough to draw, so don't count on a dose you used to take still being safe: after time off, start with a much smaller amount and don't use alone. Mixing sedatives with each other, with alcohol or with opioids sharply raises the risk of a fatal overdose. If you've been using regularly, don't stop suddenly: withdrawal from benzodiazepines, alcohol or GHB/GBL can cause seizures or delirium, so get medical help to cut down gradually.

    Sources: FRANK: benzodiazepines · Alcohol and Drug Foundation: GHB · FDA 2020: benzodiazepine boxed warning · FDA 2019: gabapentinoids and breathing · NHS: alcohol use disorder

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