Cloxazolam
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3 sources
🧬 Receptor activity
| Target | Action | Affinity | Source | |
|---|---|---|---|---|
| Aldo-keto reductase family 1 member C3 | — | Ki 1500 nM | CHEMBL | TargetAldo-keto reductase family 1 member C3 Action— AffinityKi 1500 nM SourceCHEMBL |
| Aldo-keto reductase family 1 member C2 | — | Ki 10000 nM | CHEMBL | TargetAldo-keto reductase family 1 member C2 Action— AffinityKi 10000 nM SourceCHEMBL |
| Aldo-keto reductase family 1 member C1 | — | Ki 10000 nM | CHEMBL | TargetAldo-keto reductase family 1 member C1 Action— AffinityKi 10000 nM SourceCHEMBL |
Mechanism of action
Cloxazolam is a long acting benzodiazepine. It acts as a prodrug, with pharmacologically active metabolites, which bind to to the GABAa receptor, which other benzodiazepines bind to, to illicit a physiological response.
Pharmacodynamics
Studies have shown a superiority of 4mg/day of cloxazepam to 12mg/day of bromazepam in terms of anxiety, depressed mood, and sleep; an insignificant difference in terms of sedative effect; and less muscle relaxant effects. [3] Cloxazolam, administered as a single oral dose of 3mg, when compared to a single 5 mg dose of diazepam in one study, showed similar subjective measures; however, there cloxazolam caused more fatigue, and less mood improvement. Cloxazolam also induced a significant increase in heart rate in the control group of this study. [3]
Pharmacokinetics
Half-life
65 hours
Absorption
Renal elimination.
Metabolism
Cloxazolam is metabolised by the liver into the active metabolite chlordesmethyldiazepam (delorazepam). [5]
Cloxazolam is metabolised by the liver into the active metabolite chlordesmethyldiazepam (delorazepam). [5]
Route of Elimination: Renal elimination.
Half Life: 65 hours
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