Cloxazolam
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3 sources
Collated from TripSit, Pharmacology, DrugCentral. Where sources differ (e.g. dosing), Compare shows them side by side.
Benzodiazepine derivate that is metabolised into Delorazepam. Which is where most of its effects come from.TS
Oral
Route dataTripSit
| Threshold | Light | Common | Strong | Heavy |
|---|---|---|---|---|
| — | 1.5–3 mg | 3–6 mg | 6–12 mg | —+ |
| Onset | 15–45 minutes |
|---|---|
| Total | 7–12 hours |
| After-effects | 4–12 hours |
🧬 Receptor activityPHDC
| 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 |
| Aldo-keto reductase family 1 member C3 (AKR1C3) | — | 5.82 Ki | DRUGCENTRAL | TargetAldo-keto reductase family 1 member C3 (AKR1C3) Action— Affinity5.82 Ki SourceDRUGCENTRAL |
Mechanism of actionPH
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.
PharmacodynamicsPH
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-lifePH
65 hours
AbsorptionPH
Renal elimination.
MetabolismPH
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
Plan a dose of Cloxazolam
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