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    Clomethiazole molecular structure

    Clomethiazole Stats & Data

    Chemical Class medicine
    Psychoactive Class Depressant

    Pharmacology

    DrugBank
    State Solid

    Description

    Clomethiazole is a well-established γ-aminobutyric acid (GABAA)-mimetic drug. It is a sedative and hypnotic that is widely used in treating and preventing symptoms of acute alcohol withdrawal. It is a drug which is structurally related to thiamine (vitamin B1) but acts like a sedative, hypnotic, muscle relaxant and anticonvulsant. It is also used for the management of agitation, restlessness, short-term insomnia and Parkinson's disease in the elderly.

    Mechanism of Action

    clomethiazole interacts with the GABAA receptor complex. It inhibits the binding of butyl-bicyclophosphorothionate (TBPS), an effect indicative of GABAA receptor-channel activation, by increasing the rate of TBPS dissociation and decreasing the binding affinity. Gamma-aminobutyric acid (GABA), acting at GABAA receptors, is the main fast inhibitory neurotransmitter in mammalian central nervous system

    Indication

    Investigated for use/treatment in strokes.

    Effect Profile

    Curated
    Opioid 4.7

    Moderate euphoria with mild sedation

    Euphoria / Warmth×3
    6
    Analgesia×2
    0
    Sedation / Relaxation×1
    5
    Itching / Nausea×1
    0

    Tolerance & Pharmacokinetics

    drugs.wiki

    Tolerance Decay

    Full tolerance 1d Half tolerance 21d Baseline ~35d
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