Delorazepam
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3 sources
Collated from TripSit, Pharmacology, DrugCentral. Where sources differ (e.g. dosing), Compare shows them side by side.
Also known as nordiclazepamTS
Also known as chlordesmethyldiazepam, this uncommon benzodiazepine compound is primarily used for treatment of anxiety and alcohol withdrawal, due to its long half-life (60-140 hours). It is also the active metabolite of diclazepam and cloxazolam.TS
Oral
Route dataTripSit
| Threshold | Light | Common | Strong | Heavy |
|---|---|---|---|---|
| — | 0.25–0.5 mg | 0.5–1.5 mg | 1.5–2 mg | 2 mg+ |
| Onset | 30–60 minutes |
|---|---|
| Total | 12–16 hours |
| After-effects | 72 hours |
🧬 Receptor activityDC
| Target | Action | Affinity | Source | |
|---|---|---|---|---|
| GABA-A receptor alpha-1/beta-2/gamma-2 (GABRA1) | — | 8.745 IC50 | DRUGCENTRAL | TargetGABA-A receptor alpha-1/beta-2/gamma-2 (GABRA1) Action— Affinity8.745 IC50 SourceDRUGCENTRAL |
| GABA-A receptor; anion channel (GABRP) | — | 8.55 IC50 | DRUGCENTRAL | TargetGABA-A receptor; anion channel (GABRP) Action— Affinity8.55 IC50 SourceDRUGCENTRAL |
Pharmacokinetics
Half-lifePH
Very long elimination half life of 80-115 hours, varying with age. Elimination is slower as age increases. [1] Liver disease also impacts elimination half life, with impairment resulting in half lives up to 395 hours.
AbsorptionPH
77-87% oral bioavailability, with a relatively slow absorption rate. Reaches peak plasma levels within 1-2 hours of administration. Food may slow absorption, however other pharmacokinetic variables remain unchanged. After multiple doses delorazepam accumulates, although accumulation is slower in younger patients.
Renally eliminated.
140 L/kg apparent volume of distribution in 11 patients with normal renal function; 47 L/kg in 11 patients with renal failure and on regular hemodialysis. In another study, apparent volume of distribution was 65 L/kg in 8 patients with liver disease and 118.4 L/kg in 12 healthy controls.
Still detectable 72 hours after dosing in healthy patients. Patients with liver disease experienced a reduction in clearance from 0.13 to 0.25 ng/mLh.
MetabolismPH
Delorazepam is metabolized at a relatively slow pace by the liver. The major metabolite (15-34% of the parent drug) is lorazepam. Older patients metabolize delorazepam slower than younger patients.
Protein bindingPH
>90% protein bound.
Plan a dose of Delorazepam
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Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.