Clorazepate
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| TripSit | Pharmacology | DrugCentral | ||
|---|---|---|---|---|
| Classification | ||||
| Class / category | — | — | ||
| Also known as | tranxenenovo-clopatetranzene | — | — | |
| Safety | ||||
| Dose · Oral | ||||
| Light | 5–10 mg | — | — | |
| Common | 10–20 mg | — | — | |
| Strong | 20–40 mg | — | — | |
| Duration | ||||
| Onset | 20–80 minutes | — | — | |
| Total | 8–12 hours | — | — | |
| After-effects | 1–8 hours | — | — | |
| Pharmacology | ||||
| Receptor activity | — | — | GABRA1GABRG2 | |
| Half-life | — | The serum half-life of clorazepate is approximately 2 days. Nordiazepam, the primary metabolite, quickly appears in the blood and is eliminated from the plasma with an apparent half-life of about 40 to 50 hours. PLASMA HALF-LIFE ... 53 HR ... . PRIMARY METABOLITE, NORDIAZEPAM, ... PLASMA HALF-LIFE IS ABOUT 24 HR. N-DIMETHYLDIAZEPAM, METABOLITE OF CHLORAZEPATE: MEAN HALF-LIFE 62 HR. CLORAZEPATE ADMIN IM TO PREGNANT & NONPREGNANT WOMEN. ELIMINATION HALF-LIFE WERE 1.3 HR IN PREGNANT WOMEN & 2.0 HR IN NONPREGNANT WOMEN. ITS METABOLITE, NORDIAZEPAM, REACHED PEAK CONCN WITHIN 12 HR. HALF-LIFE OF ELIMINATION FOR METABOLITE WAS 180 IN PREGNANT & 60 HR IN NONPREGNANT WOMEN. Elimination half-lives for metabolites: desmethyldiazepam (30-200 hr) and oxazepam (3-21 hr) | — | |
| Protein binding | — | The protein binding of nordiazepam (active metabolite of clorazepate) in plasma is high (97-98%). | — | |
TripSit summary
Is a prodrug for Desmethyldiazepam which is responsible for most of the therapeutic effects. Has a long half life, with the addition of Desmethyldiazepam as the main metabolite, which makes it much longer.
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