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Original

Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles

, Ph.D. & , Ph. D.
Pages 60-79 | Received 10 Jul 1983, Published online: 07 Sep 2010

References

  • Achtert G., Hausleiter H. J. Pharmacokinetics and biotransformation of metaclazepam. 13th CINP-Congress, Jerusalem, Israel. 1982; 2, Abstracts
  • Allonen H., Ziegler G., Klotz U. Midazolam kinetics. Clin. Pharmacol. Ther. 1981; 30: 653–662
  • Alvan G., Odar-Cederlof I. The pharmacokinetic profile of oxazepam. Acta Psychiatr: Scand. 1978; 274: 47–55
  • Alvan G., Siwers B., Vessman J. Pharmacokinetics of oxazepam in healthy volunteers. Acta Pharmacol. Toxicol. (Copenh.) 1977; 40(Suppl. 1)40–51
  • Amrein R., Bovey F., Cano J. P., Eckert M., Ziegler W. H., Coassolo Ph., Schalch E., Burckhardt J. Pharmacokinetics and pharmacodynamics of flurazepam in man. Part II. Drugs Exp. Clin. Res. 1983; 9: 85–99
  • Aucamp A. K. Aspects of pharmacokinetics and pharmacodynamics of benzodiazepines with particular reference to clobazam. Drug Dev. Res. Suppl. 1982; 1: 117–126
  • Bond A., Lader M. A comparison of the psychotropic profiles of tofisopam and diazepam. Eur. J. Clin. Pharmacol. 1982; 22: 137–142
  • Borland R. G., Nicholson A. N. Comparison of the residual effects of two benzodiazepines (nitrazepam and flurazepam hydrochloride) and pentobarbital sodium on human performance. Br. J. Clin. Pharmacol. 1975; 2: 9–17
  • Breimer D. D., Danhof M. Interindividual variation in pharmacokinetics and drug metabolism. “Towards Better Safety of Drugs and Pharmaceutical Products”, D. D. Breimer. Elsevier/North Holland Biomedical Press, Amsterdam 1980; 117–142
  • Breimer D. D., Jochemsen R. Pharmacokinetics of hypnotic drugs. “Psycho-pharmacology of Sleep”, D. Wheatley. Raven Press, New York 1981; 135–152
  • Breimer D. D., Jochemsen R., Von Albert H.-H. Pharmacokinetics of benzodiazepines. Short-acting versus long-acting. Arzneim. Forsch. 1980; 30: 875–881
  • Carskadon M. A., Seidel W. F., Greenblatt D. J., Dement W. C. Daytime carry-over of triazolam and flurazepam in elderly insomniacs. Sleep 1982; 5: 361–371
  • Dement W., Seidel W., Carskadon M. Daytime alertness, insomnia and benzodiazepines. Sleep 1982; 5: S28–S45
  • Divoll Allen M., Greenblatt D. J., Arnold J. D. Single and multiple dose pharmacokinetics of estazolam, a triazolo-benzodiazepine. Psychopharmacology 1979; 66: 267–274
  • Divoll Allen M., Greenblatt D. J., Harmatz J. S., Shader R. I. Desmethyl-diazepam kinetics in the elderly after oral prazepam. Clin. Pharmacol. Ther. 1980; 28: 196–202
  • Divoll Allen M., Greenblatt D. J., Harmatz J. S., Shader R. I. Effect of age and gender on disposition of temazepam. J. Pharm. Sci. 1981; 70: 1104–1108
  • Eckert M., Ziegler W. H., Cano J. P., Bovey P., Amrein R., Coassola Ph., Schalch E., Burckhardt J. Pharmacokinetics and pharmacodynamics of flurazepam in man. Part I. Drugs Exp. Clin. Res. 1983; 9: 77–84
  • Fabre L. F., McLendon D. M. A. A double-blind study comparing the efficacy and safety of alprazolam with imipramine and placebo in primary depression. Curr. Ther. Res. 1980; 27: 474–482
  • Greenblatt D. J., Allen M. D., MacLaughlin D. S., Huffman D. H., Harmatz J. S., Shader R. I. Single- and multiple-dose kinetics of oral lorazepam in humans: the predictability of accumulation. J Pharmacokin. Biopharm. 1979; 7: 159–179
  • Greenblatt D. J., Divoll M., Abernethy D. R., Shader R. I. Benzodiazepine hypnotics: kinetic and therapeutic options. Sleep 1982; 5: S18–S27
  • Greenblatt D. J., Divoll M., Abernethy D. R., Moschitto L. J., Smith R. B., Shader R. I. Alprazolam kinetics in the elderly: relation to antipyrine disposition. Arch. Gen. Psychiatry 1983; 40: 287–290
  • Greenblatt D. J., Divoll M., Abernethy D. R., Harmatz J. S., Shader R. I. Antipyrine kinetics in the elderly-prediction of age-related changes in benzodiazepine oxidizing capacity. J. Pharmacol. Exp. Thes. 1982; 220: 120–126
  • Greenblatt D. J., Divoll Allen M., Harmatz J. S., Shader R. I. Diazepam disposition determinants. Clin. Pharmacol. Thes. 1980; 27: 301–312
  • Greenblatt D. J., Divoll M., Harmatz J. S., Shader R. I. Oxazepam kinetics: effects of age and sex. J. Pharmacol. Exp. Ther. 1980; 215: 86–91
  • Greenblatt D. J., Divoll M., Harmatz J. S., MacLaughlin D. S., Shader R. I. Kinetics and clinical effects of flurazepam in young and elderly noninsomniacs. Clin. Pharmacol. Thes. 1981; 30: 475–486
  • Greenblatt D. J., Divoll M., Abernethy D. R., Ochs H. R., Shader R. I. Clinical pharmacokinetics of the newer benzodiazepines. Clin. Pharmacokin. 1983; 8: 233–252
  • Greenblatt D. J., Divoll M., Abernethy D. R., Ochs H. R., Shader R. I. Benzodiazepine kinetics. Implications for therapeutics and pharmacogeriatrics. Drug Metab. Rev. 1983; 14: 251–292
  • Greenblatt D. J., Divoll M., Puri S. K., Ho I., Zinny M. A., Shader R. I. Clobazam kinetics in the elderly. Br. J. Clin. Pharmacol. 1981; 12: 631–636
  • Greenblatt D. J., Shader R. I. Effects of age and other drugs on benzodiazepine kinetics. Arzneim. Forsch. 1980; 30: 886–890
  • Greenblatt D. J., Shader R. I., Divoll M., Harmatz J. S. Benzodiazepines: a summary of pharmacokinetic properties. Br. J. Clin. Pharmacol. 1981; 11: 11S–16S
  • Hailey D. M., Baird E. S. Plasma concentrations of medazepam and its metabolites after oral administration. Br. J. Anaesth. 1979; 51: 493–496
  • Hindmarch I., Clyde C. A. The effects of triazolam and nitrazepam on sleep quality, morning vigilance and psychomotor performance. Arzneim. Forsch. 1980; 30: 1163–1166
  • Hümpel M., Nieuweboer B., Milius W., Hanke H., Wendt H. Kinetics and biotransformation of lormetazepam. II. Radioimmunological determinations in plasma and urine of young and elderly subjects: first-pass effect. Clin. Pharmacol. Thes. 1980; 28: 673–679
  • Jochemsen R. Clinical pharmacokinetics of benzodiazepine hypnotics. University of Leiden, The Netherlands 1983, Ph.D. Thesis
  • Jochemsen R., Van der Graaff M., Boeijinga J. K., Breimer D. D. Influence of sex, menstrual cycle and oral contraception on the disposition of nitrazepam. Br. J. Clin. Pharmacol. 1982; 13: 319–324
  • Jochemsen R., Hogendoorn J. J. H., Dingemanse J., Hermans J., Boeijinga J. K., Breimer D. D. Pharmacokinetics and bioavailability of intravenous, oral and rectal nitrazepam in humans. J. Pharmacokin. Biopharm. 1982; 10: 231–245
  • Jochemsen R., Van Beusekom B. R., Spoelstra P., Janssens A. R., Breimer D. D. Effect of age and liver cirrhosis on the pharmacokinetics of nitrazepam. Br. J. Clin. Pharmacol. 1983; 15: 295–303
  • Jochemsen R., Joeres R. P., Wesselman J. G. J., Richter E., Breimer D. D. Pharmacokinetics of oral brotizolam in patients with liver cirrhosis. Br. J. Clin. Pharmacol. 1983, In press
  • Jochemsen R., Nandi K. L., Corless D., Breimer D. D. Pharmacokinetics of brotizolam in the elderly. Br. J. Clin. Pharmacol. 1983, In press
  • Jochemsen R., Wesselman J. G. J., Van Boxtel C. J., Hermans J., Breimer D. D. Comparative pharmacokinetics of brotizolam and triazolam in healthy subjects. Br. J. Clin. Pharmacol. 1983, In press
  • Jochemsen R., Van Boxtel C. J., Hermans J., Breimer D. D. Pharmacokinetics of 5 benzodiazepine hypnotics in the same panel of healthy subjects. Clin. Pharmacol. Ther. 1983, In press
  • Jochemsen R., Van Rijn P. A., Hazelzet T. G. M., Breimer D. D. Assay of midazolam and brotizolam in plasma by a gas chromatographic and a radioreceptor technique. Pharm. Weekbl. Sci. Ed. 1983, In press
  • Kales A., Scharf M. B., Bixler E. O., Schweitzer P. K., Jacoby J. A., Soldatos C. R. Dose-response studies of quazepam. Clin. Pharmacol. Thea 1981; 30: 194–200
  • Kales A., Soldatos C. R., Bixler E. O., Kales J. D. Early morning insomnia with rapidly eliminated benzodiazepines. Science 1983; 220: 95–97
  • Kangas L., Iisalo E., Kanto J., Lehtinen V., Pynnönen S., Ruikka J., Salminen J., Sillanpää M., Syvälathi E. Human pharmacokinetics of nitrazepam: effects of age and disease. Eur. J. Clin. Pharmacol. 1979; 15: 163–170
  • Kangas L., Kanto J., Pakkanen A., Mansikka M. Comparison of sedatory and anxiolytic properties of placebo, tofisopam and nitrazepam as oral premedicaments. 12th CINP-Congress, Göteborg. 1980; 197, Abstracts
  • Kanto J., Kangas L., Aaltonen L., Hilke H. Effect of age on the pharmacokinetics and sedative effect of flunitrazepam. Int. J. Clin. Pharmacol. Biopharm. 1981; 19: 400–404
  • Kaplan S. A., Jack M. L., Weinfeld R. E., Glover W., Weissman L., Cotler S. Biopharmaceutic and clinical pharmacokinetic profile of bromazepam. J. Pharmacokin. Biopharm. 1976; 4: 1–16
  • Klotz U., Avant G. R., Hoyumpa A., Schenker S., Wilkinson G. R. The effects of age and liver disease on the disposition and elimination of diazepam in adult man. J. Clin. Invest. 1975; 55: 347–359
  • Klotz U., Müller-Seydlitz P. Altered elimination of desmethyldiazepam in the elderly. Br. J. Clin. Pharmacol. 1979; 7: 119–120
  • Kraus J. W., Desmond P. V., Marshall J. P., Johnson R. F., Wilkinson G. R., Schenker S. The effects of ageing and liver disease on the disposition of lorazepam in man. Clin. Pharmacol. The. 1978; 24: 411–419
  • Li F-L., Achtert G. Binding properties of metaclazepam and its metabolites to benzodiazepine receptor and its pharmacology. 13th CINP-Congress, Jerusalem, Israel, 1982; 442, Abstracts
  • Lader M., Melhuish A., Harris P. Residual effects of repeated doses of 0.5 and 1 mg flunitrazepam. Eur. J. Clin. Pharmacol. 1982; 23: 135–140
  • Lippa A. S., Meyerson L. R., Beer B. Molecular substrates of anxiety: clues from the heterogeneity of benzodiazepine receptors. Life Sci. 1982; 31: 1409–1417
  • Morgan K., Oswald I. Anxiety caused by a short-life hypnotic. Br. Med. J. 1962; 284: 942
  • Nicholson A. N., Stone B. M. Activity of the hypnotics, flunitrazepam and triazolam, in man. Br. J. Clin. Pharmacol. 1980; 9: 533–541
  • Nicholson A. N., Stone B. M., Pascoe P. Studies on sleep and performance with a triazolo-1, 4-thienodiazepine (brotizolam). Br. J. Clin. Pharmacol. 1980; 10: 75–82
  • Nicholson A. N., Stone B. M. Imidazo-benzodiazepines: sleep and performance studies in man. J. Clin. Psychopharmacol. 1983; 3: 72–75
  • Pecknold J. C., McClure D. J., Fleury D., Chang H., Elie R. A controlled comparative study of halazepam in anxiety. Curr. Ther. Res. 1982; 32: 895–905
  • Perrier F. Bilan de l'étude coopérative du bromazepam portant stir 3401 observations de psychiatric ambulatoire et 8191 observations de médicine practicienne. Nouv. Press Méd. 1982; 11: 1747–1751
  • Róai S., Orosz E., Bolla K. Human pharmacokinetic data on Grandaxin. Ther. Hung. 1975; 23: 139–142
  • Ruhland M., Hell I., Muesch H. R., Rohle O. CNS-pharmacological properties of the new anxiolytic drug metaclazepam — animal studies with mice and rats. 13th CINP-Congress, Jerusalem, Israel, 1982; 632, Abstracts
  • Rupp W., Badian M., Christ O., Hadju P., Kulkarni R. D., Tacuber K., Uihlein M., Bender R., Vanderbeke O. Pharmacokinetics of single and multiple doses of clobazam in humans. Br. J. Clin. Pharmacol. 1979; 7: 51S–57S
  • Schacht U., Baecker G. Effects of clobazam in benzodiazepine-receptor binding assays. Drug Dev. Rex. 1982, Suppl. 1: 83–93
  • Schwartz H. J. Phatmacokinetics and metabolism of temazepam in man and several animal species. Br. J. Clin. Pharmacol. 1979; 8: 23S–29S
  • Sellers E. M., Greenblatt D. J., Giles H. G., Naranjo C. A., Kaplan H., MacLeod S. M. Chlordiazepoxide and oxazepam disposition in cirrhosis. Clin. Pharmacol. Ther. 1979; 26: 240–246
  • Shull H. J., Jr., Wilkinson G. R., Johnson R., Schenker S. Normal disposition of oxazepam in acute viral hepatitis and cirrhosis. Ann. Infern. Med. 1976; 84: 420–425
  • Wickstrom E., Amrein R., Haefelfinger P., Hartmann D. Pharmacokinetic and clinical observations on prolonged administration of flunitrazepam. Eur. J. Clin. Pharmacol. 1980; 17: 189–196

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