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Pinazepam: a precursor of N-desmethyldiazepam
European Journal of Clinical Pharmacology
|January 1, 1982
Summary
Pinazepam, a medication, was studied in healthy males. Its metabolite, N-desmethyldiazepam, appeared in higher concentrations, suggesting pinazepam functions as a prodrug.
Area of Science:
- Pharmacology
- Clinical Pharmacy
- Drug Metabolism
Background:
- Pinazepam is a benzodiazepine derivative.
- Understanding its pharmacokinetic profile is crucial for therapeutic use.
Purpose of the Study:
- To investigate the plasma concentration profile of pinazepam and its metabolite after a single oral dose.
- To determine if pinazepam acts as a prodrug.
Main Methods:
- A single oral dose of 10 mg pinazepam was administered to 6 healthy male volunteers.
- Plasma concentrations of pinazepam and its metabolite, N-desmethyldiazepam, were quantified using gas-chromatography.
Main Results:
- Peak plasma levels of pinazepam reached 36.8 +/- 5.1 ng/ml.
- Peak plasma levels of N-desmethyldiazepam were significantly higher, reaching 150 +/- 13.3 ng/ml.
- The metabolite's concentration exceeded the parent drug's concentration shortly after administration.
Conclusions:
- Pinazepam appears to function as a prodrug.
- The rapid conversion to N-desmethyldiazepam influences its pharmacological activity.