Clomethiazole
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Collated from TripSit, Pharmacology, DrugCentral. Where sources differ (e.g. dosing), Compare shows them side by side.
Structurally related to Thiamine (vitamin B1), but with binding potential at the GABAa site, which causes it to produce effects most like those of a barbiturate: an effective sedative and hypnotic. Originally developed by Hoffman-LaRoche in the 1930s, it has seen use as a treatment for acute alcohol withdrawal.TS
Oral
Route dataTripSit
| Threshold | Light | Common | Strong | Heavy |
|---|---|---|---|---|
| 100 mg | 100–150 mg | 150–200 mg | — | 200 mg+ |
| Onset | 15–40 minutes |
|---|---|
| Total | 5–8 hours |
| After-effects | 1–16 hours |
🧬 Receptor activityDC
Mechanism of actionPH
clomethiazole interacts with the GABAA receptor complex. It inhibits the binding of [35S]butyl-bicyclophosphorothionate (TBPS), an effect indicative of GABAA receptor-channel activation, by increasing the rate of [35S]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
Pharmacokinetics
MetabolismPH
Clomethiazole has known human metabolites that include NLA-715.
Plan a dose of Clomethiazole
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