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Pinazepam: A precursor of N-desmethyldiazepam

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Summary

The plasma profile of a single oral dose of pinazepam 10 mg was studied in 6 healthy male volunteers, aged 26 to 31 years. The concentrations of the parent compound and of its metabolite in plasma were measured by gas-chromatography. The peak plasma levels of pinazepam was 36.8±5.1 ng/ml and of N-desmethyldiazepam 150±13.3 ng/ml. The plasma concentration of the metabolite become higher than that of the parent compound shortly after administration, suggesting that pinazepam acts as a prodrug.

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References

  • Allen MD, Greenblatt DJ, Harmatz JS, Shader RI (1980) Desmethyldiazepam kinetics in the elderly after oral prazepam. Clin Pharmacol Ther 28: 196–202

    Google Scholar 

  • Biscaldi GP, Hattab J, Montanaro N, Scoz R (1971) Quantitative polygraphic evaluation of emotional tension in the study of a new benzodiazepine. Curr Ther Res 13: 606–615

    Google Scholar 

  • Corni L, Palmir R, Gervasi GB, Comi V, Fossati A (1976) Cinetica ematica e prove di accumolo nell'uomo di una nuova benzodiazepina (pinazepam) dopo somministrazione orale. Clin Ter 78: 111–122

    Google Scholar 

  • De Lisio G, Cassano GB, Castrogiovanni P, Maggini C, Sarteschi P, Wittenborn JR (1975) Therapy in psychosomatic medicine. The influence of benzodiazepine on psychomotor and intellectual activities. Pinazepam effects on performance of normal volunteers. F Antonelli (ed), pp 183–188. Luigi Pozzi Rome

  • Gomeni R, Gomeni C (1979) AUTOMOD: a polygraphic method for an integrated analysis of linear pharmacokinetic models comput. Biol Med 9: 39–48

    Google Scholar 

  • Greenblatt DJ, Shader RI (1974) Benzodiazepines in clinical practice, Raven Press, New York, p 17

    Google Scholar 

  • Greenblatt DJ, Shader RI (1979) Single-dose kinetics of oral prazepam. Clin Pharmacol Ther 25: 211–212

    Google Scholar 

  • Kaplan SA, de Silva JAF, Jack ML, Alexander K, Strojny N, Weinfeld RE, Puglisi CV, Weissman L (1972) Blood level profile in man following chronic oral administration of flurazepam hydrochloride. J Pharm Sci 62: 1932–1935

    Google Scholar 

  • Klotz U, Müller-Seydlitz P (1979) Altered elimination of desmethyldiazepam in the elderly. Br J Clin Pharmacol 7: 119–120

    Google Scholar 

  • Mahon WA, Inaba T, Stone RM (1977) Metabolism of flurazepam by the small intestine. Clin Pharmacol Ther 22: 228–233

    Google Scholar 

  • Mandelli M, Tognoni G, Garattini S (1978) Clinical pharmacokinetics of diazepam. Clin Pharmacokinet 3: 72–91

    Google Scholar 

  • Pacifici GM, Cuoci L, Placidi GF (1978) Role of the gestational age on the distribution of pinazepam and its metabolite N-desmethyldiazepam in rabbit embryo, fetus and mother. 7th International Congress of Pharmacology, Paris, France

  • Pacifici GM, Placidi GF (1981) First pass effect of pinazepam in the rabbit liver. Eur J Drug Metab Pharmacokinet (In press)

  • Pacific GM, Cuoci L, Placidi GF (1981a) Disposition, distribution and first-pass effect of pinazepam in rats. Drug Metab Dispos (In press)

  • Pacifici GM, Placidi GF (1977) Rapid and sensitive electron-capture gaschromatographic method for the determination of pinazepam and its metabolites in human plasma urine and milk. J Chromatogr 135: 133–139

    Google Scholar 

  • Pacifici GM, Cuoci L, Placidi GF, Fornaro P, Gomeni R (1981b) Elimination kinetics of N-desmethyldiazepam in two young and elderly subjects. Eur J Drug Metab Pharmacokinet (In press)

  • Post C, Lindgren S, Bertler A, Malmgren H (1977) Pharmacokinetics of N-desmethyldiazepam in healthy volunteers after single daily dose of dipotassium Chlorazepate. Psychopharmacology 53: 105–109

    Google Scholar 

  • Schartz MA, Postma E (1970) Metabolism of flurazepam, a benzodiazepine, in man and dog. J Pharm Sci 59: 1800–1806

    Google Scholar 

  • Scrollini F, Caliari S, Romano P, Torchio P (1975) Toxicological and pharmacological investigations of pinazepam (7-Chloro-1-propargyl-5-phenyl-3H-1,4-benzodiazepin-2-one) a new psychotherapeutic agent. Arzneim Forsch 25:934–940

    Google Scholar 

  • Scrollini F, Pizzi A, Amigoni S (1978) The psychopharmacological properties of pinazepam, a new benzodiazepine derivative. Arzneim Forsch 28:423–426

    Google Scholar 

  • Smith MT, Evans LEJ, Eadie MJ, Tyrer JH (1979) Pharmacokinetics of prazepam in man. Eur J Clin Pharmacol 16:141–147

    Google Scholar 

  • Tansella M, Burti L, Siciliani O, Zimmerman C, Schiavon M, Gerna M, Tognoni G, Morselli PL (1975) N-desmethyldiazepam and amylobarbitone sodium as hypnotics in anxions patients. Plasma levels, Clinical efficacy and residual effects. Psychopharmacologia 41:81–85

    Google Scholar 

  • Tognoni G, Gomeni R, De Maio D, Alberti GG, Franciosi P, Scieghi G (1975) Pharmacokinetics of N-desmethyldiazepam in patients suffering from insomnia and treated with nortriptyline. Br J Clin Pharmacol 2:227–232

    Google Scholar 

  • Tosi GC, Tosi GC, Hattab JR (1973) The use of N-desmethyldiazepam in out patients suffering from insomnia. Curr Ther Res 15:460–464

    Google Scholar 

  • Trebbi A, Gervasi GB, Comi V (1975) Determination of pinazepam and its metabolites in serum, urine and brain of animals and man by gaschromatography and mass spectrometry. J Chromatogr 110:309–319

    Google Scholar 

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Pacifici, G.M., Placidi, G.F., Fornaro, P. et al. Pinazepam: A precursor of N-desmethyldiazepam. Eur J Clin Pharmacol 22, 225–228 (1982). https://doi.org/10.1007/BF00545219

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  • DOI: https://doi.org/10.1007/BF00545219

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