Display options
Cite
Pacifici GM, Cuoci L, Placidi GF. Disposition, distribution, plasma protein binding and biliary excretion of pinazepam after i.p. administration to rat. Eur J Drug Metab Pharmacokinet. 1983;8(3):209-17doi: 10.1007/BF03188750.
Pacifici, G. M., Cuoci, L., & Placidi, G. F. (1983). Disposition, distribution, plasma protein binding and biliary excretion of pinazepam after i.p. administration to rat. European journal of drug metabolism and pharmacokinetics, 8(3), 209-17. https://doi.org/10.1007/BF03188750
Pacifici, G M, et al. "Disposition, distribution, plasma protein binding and biliary excretion of pinazepam after i.p. administration to rat." European journal of drug metabolism and pharmacokinetics vol. 8,3 (1983): 209-17. doi: https://doi.org/10.1007/BF03188750
Pacifici GM, Cuoci L, Placidi GF. Disposition, distribution, plasma protein binding and biliary excretion of pinazepam after i.p. administration to rat. Eur J Drug Metab Pharmacokinet. 1983 Jul-Sep;8(3):209-17. doi: 10.1007/BF03188750. PMID: 6418547.
Copy Download .nbib Format: NLM
Share it on

Eur J Drug Metab Pharmacokinet. 1983 Jul-Sep;8(3):209-17. doi: 10.1007/BF03188750.

Disposition, distribution, plasma protein binding and biliary excretion of pinazepam after i.p. administration to rat.

European journal of drug metabolism and pharmacokinetics

G M Pacifici, L Cuoci, G F Placidi

PMID: 6418547 DOI: 10.1007/BF03188750

Abstract

The pharmacokinetics, distribution, plasma protein binding and the biliary excretion of pinazepam were studied in the rat. The drug was administered (5 mg/kg) by i.p. injection. The chemical analysis of pinazepam and its metabolites was carried out by a gas-chromatographic method. The parent compound was rapidly absorbed, accumulated into the tissues and converted into N-desmethyldiazepam. The highest plasma levels of the parent compound (367 +/- 13 ng/ml) were found 3 min after administration. The volume of distribution and the clearance of the drug were 1315 ml and 7.23 ml/min respectively. The metabolite was detected in the plasma and tissues 3 min after administration. At this sampling time its concentrations were 76 +/- 16 ng/ml in the plasma and 1081 +/- 68 ng/g in the liver. The decay curve of both pinazepam and N-desmethyldiazepam in the plasma, liver, lung, heart, kidney, brain, and gastrochemius muscle were characterized for their Kel, t 1/2, and AUC values. The tissue AUC to plasma AUC ratios indicated a preferential accumulation of pinazepam over its metabolite in the tissues. The plasma protein binding of pinazepam was measured by dialysis at the equilibrium. Rat plasma proteins bound 89.17 +/- 0.20 percent of the drug. The association constant was 2.60 X 10(3) l/mole and the number of sites 0.44 X 10(-6) sites/g. The biliary excretion of pinazepam and N-desmethyldiazepam was poor.

References

  1. Acta Pharmacol Toxicol (Copenh). 1975 Sep;37(3):242-9 - PubMed
  2. J Chromatogr. 1975 Jul 16;110(2):309-19 - PubMed
  3. Arch Biochem Biophys. 1968 Jun;125(3):858-64 - PubMed
  4. Drug Metab Dispos. 1974 Sep-Oct;2(5):429-32 - PubMed
  5. Clin Pharmacokinet. 1978 Jan-Feb;3(1):72-91 - PubMed
  6. Eur J Clin Pharmacol. 1982;22(3):225-8 - PubMed
  7. J Pharm Sci. 1968 Jun;57(6):895-918 - PubMed
  8. Annu Rev Pharmacol Toxicol. 1978;18:81-96 - PubMed
  9. Acta Physiol Scand. 1975 Sep;95(1):1-5 - PubMed
  10. J Chromatogr. 1977 May 11;135(1):133-9 - PubMed
  11. Res Commun Chem Pathol Pharmacol. 1970 Jan;1(1):43-56 - PubMed
  12. Eur J Drug Metab Pharmacokinet. 1982;7(2):119-22 - PubMed
  13. Drug Metab Dispos. 1982 Mar-Apr;10(2):180-2 - PubMed
  14. Life Sci. 1975 Sep 1;17(5):813-8 - PubMed
  15. J Pharmacol Exp Ther. 1976 Oct;199(1):67-73 - PubMed
  16. Farmaco Sci. 1977 Apr;32(4):278-85 - PubMed
  17. Eur J Clin Pharmacol. 1979 Sep;16(2):141-7 - PubMed
  18. Eur J Clin Pharmacol. 1977 Nov 14;12(3):209-12 - PubMed
  19. Pharmacol Res Commun. 1974 Apr;6(2):193-202 - PubMed
  20. Naunyn Schmiedebergs Arch Pharmacol. 1973;280(3):229-37 - PubMed
  21. Biochem Pharmacol. 1963 Jun;12:591-3 - PubMed
  22. J Pharm Sci. 1972 Jun;61(6):965-6 - PubMed
  23. Biochem Pharmacol. 1976 Jan 15;25(2):141-5 - PubMed
  24. Drug Metab Rev. 1976;5(1):43-140 - PubMed
  25. Drug Metab Rev. 1979;9(1):21-41 - PubMed

Substances

MeSH terms

Publication Types