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Updated: Aug 2, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
Published on: March 28, 2017
Lorazepam is primarily metabolized into its glucuronide form in humans and several animal species. This metabolism study clarifies lorazepam
Area of Science:
- Pharmacology
- Drug Metabolism
- Toxicology
Background:
- Lorazepam is a widely used benzodiazepine medication.
- Understanding its metabolic pathways is crucial for clinical application and safety.
Purpose of the Study:
- To review and detail the metabolism of lorazepam in humans and four other animal species.
- To identify and quantify lorazepam and its metabolites in biological samples.
Main Methods:
- Thin-layer chromatography
- Gas chromatography
- Mass spectrometry
- Analysis of blood, urine, and feces samples
Main Results:
- The principal metabolite in humans, dogs, pigs, and cats is lorazepam glucuronide.
- Rats exhibit different metabolic profiles depending on dosage.
- Unconjugated lorazepam blood concentrations peak within 1-4 hours and persist for 24 hours.
- Approximately 95% of a lorazepam dose is excreted in urine and feces within 5 days.
- The excretory half-life of lorazepam is approximately 12 hours.
Conclusions:
- Lorazepam metabolism is consistent across several species, with glucuronidation being the primary pathway.
- Excretion and blood concentration data align with observed clinical effects of lorazepam.
- The findings support the safe and effective use of lorazepam in clinical practice.
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