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Brotizolam

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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 lendorminTS

Benzodiazepine analogue which is sedating, hypnotic and anxiolytic. It is available as prescription medicine in much of Europe, and is an extremely potent drug active at only 80ug. May cause amnesia and lowered inhibitions in overdose. Danger of respiratory depression when combined with other depressants. Short half life.TS

Oral

Route dataTripSit

ThresholdLightCommonStrongHeavy
80 µg200–400 µg—+
0400 µg
LightCommonStrongHeavy
After-effects1–4 hours

🧬 Receptor activityDC

TargetActionAffinitySource
Platelet-activating factor receptor (PTAFR)6.52 IC50DRUGCENTRAL
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Pharmacokinetics

Half-lifePH

4.4 hours.

AbsorptionPH

The plasma concentration profile of brotizolam can be described as a one compartmental open model with first-order absorption.
0.63 l/kg.
Total clearance: 109 ml/min.

MetabolismPH

There are two primary metabolites: 1-methyl-hydroxy- and the 4-hydroxy-derivatives (Eberts et al., 1981; Boehringer Ingelheim, product information). The 4-hydroxymetabolites have a pharmacological activity which is far less than that of the parent drugs, but the 1-methyl-hydroxymetabolites probably have comparable activity (Gall et al., 1978; Jochemsen et al., 1982; Sethy & Harris, 1982; Jochemsen et al., unpublished results). These active compounds are, however, not present in plasma in measurable amounts following a single dose of brotizolam to young healthy subjects (Jochemsen et al., 1982; Jochemsen et al., unpublished results).
Brotizolam has known human metabolites that include alpha-hydroxy-BRT and 6-hydroxy-BRT.

Protein bindingPH

The mean value of the free fraction (%): 8.4 ± 0.7.

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