Plasma levels of chlorodesmethyldiazepam in humans

  title={Plasma levels of chlorodesmethyldiazepam in humans},
  author={L. Dal Bo and Franca Marcucci and Emilio Mussini and D Perbellini and Alessandro Castellani and Paola Fresia},
  journal={Biopharmaceutics \& Drug Disposition},
Chlorodesmethyldiazepam (I) concentrations were followed for 72 h in the plasma of four volunteers given 2 mg of the drug orally. The drug appears to be well absorbed, reaching peak plasma levels of 20–30 ng ml−1 1–2 h after administration; 72 h after administration, plasma concentrations are still measurable (5 ng ml−1). 

Pharmacokinetics of chlordesmethyldiazepam after single-dose oral administration in humans

The pharmacokinetics of chlordemethyldiazepam in healthy subjects after administration of a single oral dose of 2 mg, was studied and only conjugated lorazepam could be found its 96 hour excretion reaching about 15% of the administered dose of parent drug.

Pharmacokinetics and bioavailability of intravenous and oral chlordesmethyldiazepam in humans

SummarySix healthy, fasting volunteers were given single doses of chlordesmethyldiazepam by 1 mg i. v., or as drops or tablets. Chlordesmethyldiazepam and its metabolite, lorazepam, in multiple

Characterization of the designer benzodiazepine diclazepam and preliminary data on its metabolism and pharmacokinetics.

Based on this study, diclazepam has an approximate elimination half-life of 42 h and is metabolized into the pharmacologically active benzodiazepines delorazepAm, lorazEPam, and lormetazep am which can be detected in urine for 6, 19, and 11 days, respectively, when applying the presented LC-MS/MS method.

Quantification of chlordesmethyldiazepam by liquid chromatography-tandem mass spectrometry: application to a cloxazolam bioequivalence study.

A rapid, sensitive and specific LC-MS/MS method was developed and validated for quantifying chlordesmethyldiazepam (CDDZ or delorazepam), the active metabolite of cloxazolam, in human plasma and indicated bioequivalence since all ratios were as proposed by FDA and ANVISA.

Designer Benzodiazepines: Another Class of New Psychoactive Substances.

This chapter describes the phenomenon of designer benzodiazepines and summarizes the available data on pharmacokinetics and pharmacodynamics as well as analytical approaches for their detection.



Concentration‐effect relationships with major and minor tranquilizers

  • S. Curry
  • Psychology
    Clinical pharmacology and therapeutics
  • 1974
A brief review is presented of the current status of studies of the relationship between concentration and effect for these compounds, including glutethimide, nordiazepam, and chlorpromazine.

Electron-capture GLC determination of blood levels of 7-chloro-1,3-dihydro-5-(2'-chlorophenyl)-2H-1,4-benzodiazepin-2-one in humans and its urinary excretion as lorazepam determined by differential pulse polarography.

The clinical utility of a previously published electron-capture GLC assay in the measurement of blood levels of 7-chloro-1,3-dihydro-5-(2'-chlorophenyl)-2 H -1,4-benzodiazepin-2-one in humans following a single oral 4-mg dose is demonstrated.

Biliary excretion of conjugated hydroxyl benzodiazepines after administration of several benzodiazepines to rats, guinea pigs, and mice.

The fact that hydroxylated metabolites are excreted as conjugated derivatives more by mice and guinea pigs than by rats may suggest the hypothesis of a more extensive enterohepatic circulation of these compounds in mice and Guinea pigs than in rats.

Hydroxylation of three benzodiazepines in vitro.

Three structurally related benzodiazepines were studied as substrates for hydroxylation by liver microsomal enzymes of rats and mice and yielded two pharmacologically active metabolites, oxazepam and lorazepAM, respectively.