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Delorazepam

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Collated from TripSit, Pharmacology, DrugCentral. Where sources differ (e.g. dosing), Compare shows them side by side.

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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

ThresholdLightCommonStrongHeavy
0.25–0.5 mg0.5–1.5 mg1.5–2 mg2 mg+
02.5 mg
LightCommonStrongHeavy
Onset30–60 minutes
Total12–16 hours
After-effects72 hours
OnsetCome-upPeakOffset

🧬 Receptor activityDC

TargetActionAffinitySource
GABA-A receptor alpha-1/beta-2/gamma-2 (GABRA1)8.745 IC50DRUGCENTRAL
GABA-A receptor; anion channel (GABRP)8.55 IC50DRUGCENTRAL
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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 when to take Delorazepam — see where onset, peak and comedown land on the clock

Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.