Integrated pharmacokinetics and pharmacodynamics of Ro 48-6791, a new benzodiazepine, in comparison with midazolam during first administration to healthy male subjects

British Journal of Clinical Pharmacology

Volumn 44, Issue 5, 1997, Pages 477-486

  Dingemanse, J ^a,c   Van Gerven, J M A ^b   Schoemaker, R C ^b   Roncari, G ^a   Oberye J J L ^b   Van Oostenbruggen, M F ^b   Massarella, J ^a   Segala, P ^a   Zell, M ^a   Cohen, A F ^b  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b CENTRE FOR HUMAN DRUG RESEARCH   (Netherlands)

^c Jacon Research   (Switzerland)

Author keywords

Benzodiazepine; Midazolam; Pharmacodynamics; Pharmacokinetics; Ro 48 6791

Indexed keywords

3 (5 DIPROPYLAMINOMETHYL 1,2,4 OXADIAZOL 3 YL) 8 FLUORO 5,6 DIHYDRO 5 METHYL 4H IMIDAZO[1,5 A][1,4]BENZODIAZEPIN 6 ONE; BENZODIAZEPINE DERIVATIVE; MIDAZOLAM; PLACEBO; UNCLASSIFIED DRUG; RO 48 8684;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG SAFETY; ELECTROENCEPHALOGRAM; HUMAN; HUMAN EXPERIMENT; INTRAVENOUS DRUG ADMINISTRATION; MALE; NORMAL HUMAN; PHARMACODYNAMICS; PHARMACOKINETICS; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SACCADIC EYE MOVEMENT; VOLUNTEER; DOSE RESPONSE;

ADULT; ANTI-ANXIETY AGENTS; BENZODIAZEPINES; CROSS-OVER STUDIES; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; ELECTROENCEPHALOGRAPHY; HUMANS; INFUSIONS, INTRAVENOUS; MALE; MIDAZOLAM; OXAZOLES; PLACEBOS; SACCADES;

EID: 9844226779     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2125.1997.t01-1-00612.x     Document Type: Article

References (36)

1. Kanto J, Klotz U. Intravenous benzodiazepines as anaesthetic agents : pharmacokinetics and clinical consequences. Acta Anaesthesiol Scand 1982; 26: 554-569.
2. Bell GD. Premedication and intravenous sedation for upper gastrointestinal endoscopy. Aliment Pharmacol Ther 1990; 4: 103-122.
3. Amrein R, Hetzel W, Allen SR. Co-induction of anaesthesia: the rationale. Eur J Anaesthesiol 1995; 12(suppl 12): 5-11.
4. Shafer A, White PF, Urquhart ML, Doze VA. Outpatient premedication: use of midazolam and opioid analgesics. Anesthesiology 1989; 71: 495-501.
5. Shelly MP, Sultan MA, Bodenham A, Park GR. Midazolam infusions in critically ill patients. Eur J Anaesthesiol 1991; 8: 21-27.
6. Dundee JW, Halliday NJ, Harper KW, Brogden RN. Midazolam: a review of its pharmacological properties and therapeutic use. Drugs 1984; 28: 519-543.
7. Haefely W. Pharmacology of the allosteric modulation of GABA-A receptors by benzodiazepine receptor ligands, In Allosteric modulation of amino acid receptors: therapeutic implications, eds Barnard EA, Costa E. New York: Raven Press, 1989: 47-69.
8. Van Steveninck AL, Mandema JW, Tuk B, et al. A comparison of the concentration effect relationships of midazolam for EEG-derived parameters and saccadic peak velocity. Br J Clin Pharmacol 1993; 36: 109-115.
9. Sutherland LR, Goldenberg E, Hershfield N, Price L, MacCarrell K, Schaffer E. Midazolam in upper gastrointestinal endoscopy: a single-blind dose-finding study. Clin Invest Med 1989; 12: 99-103.
10. Heizmann P, Eckert M, Ziegler WH. Pharmacokinetics and bioavailability of midazolam in man. Br J Clin Pharmacol 1983; 16: 43S-49S.
11. Van Steveninck AL, van Berckel BNM, Schoemaker HC, Breimer DD, Cohen AF. The sensitivity of pharmacodynamic tests of CNS effects of drugs to the effects of sleep deprivation. Br J Clin Pharmacol 1993; 35: 551P (Abstract).
12. Griffiths AN, Marshall RW, Richens A. Saccadic eye movement analysis as a measure of drug effects on human psychomotor performance. Br J Clin Pharmacol 1984; 18: 73S-82S.
13. Van Steveninck AL, Schoemaker HC, Pieters MSM, Kroon R, Breimer DD, Cohen AF. A comparison of the sensitivities of adaptive tracking, eye movement analysis and visual analog lines to the effects of incremental doses of temazepam in healthy volunteers. Clin Pharmacol Ther 1991; 50: 172-180.
14. Mandema JW, Danhof M. Electroencephalogram effect measures and relationships between pharmacokinetics and pharmacodynamics of psychotropic drugs. Clin Pharmacokinet 1992; 23: 191-215.
15. Gibaldi M, Perrier D. Pharmacokinetics. 2nd revised ed. New York: Marcel Dekker Inc., 1982.
16. Heinzel G, Woloszczak W, Thomann P. TOPFIT version 2.0: Pharmacokinetic and pharmacodynamic data analysis system. Stuttgart: Gustav Fischer Verlag, 1993.
17. Sachs L. Applied statistics, seventh edition. Berlin: Springer Verlag, 1992.
18. Greenblatt DJ, Harmatz JS. Kinetic-dynamic modeling in clinical psychopharmacology. J Clin Psychopharmacol 1993; 13: 231-234.
19. Holford NHG, Sheiner LB. Understanding the dose-effect relationship: clinical application of pharmacokinetic-pharmacodynamic models. Clin Pharmacokinet 1981; 6: 429-453.
20. Bates DM, Watts DG. Nonlinear regression analysis and its applications. New York: Wiley & Sons, 1988: 103-104.
21. Verotta D, Beal SL, Sheiner LB. Semiparametric approach to pharmacokinetic-pharmacodynamic data. Am J Physiol 1989; 256: R1005-1010.
22. Kroboth PD, Schmith VD, Smith RB. Pharmacodynamic modelling. Application to new drug development. Clin Pharmacokinet 1991; 20: 91-98.
23. Lemmens HJM, Dyck JB, Shafer SL, Stanski DR. Pharmacokinetic-pharmacodynamic modeling in drug development: application to the investigational opioid trefentanil. Clin Pharmacol Ther 1994; 56: 261-271.
24. Peck CC, Barr WH, Benet LZ, et al. A. Opportunities for integration of pharmacokinetics, pharmacodynamics, and toxicokinetics in rational drug development. Clin Pharmacol Ther 1992; 51: 465-473.
25. Crevoisier Ch, Ziegler WH, Eckert M, Heizmann P. Relationship between plasma concentration and effect of midazolam after oral and intravenous administration. Br J Clin Pharmacol 1983; 16: 51S-61S.
26. Dingemanse J, Danhof M, Breimer DD. Pharmacokinetic-pharmacodynamic modelling of CNS drug effects: an overview. Pharmacol Ther 1988; 38: 1-52.
27. Allonen H, Ziegler G, Klotz U. Midazolam kinetics. Clin Pharmacol Ther 1981; 30: 653-661.
28. Smith MT, Eadie MJ, O'Rourke Brophy T. The pharmacokinetics of midazolam in man. Eur J Clin Pharmacol 1981; 19: 271-278.
29. Ball DM, Glue P, Wilson S, Nutt DJ. Pharmacology of saccadic eye movements in man. I. Effects of the benzodiazepine receptor ligands midazolam and flumazenil. Psychopharmacology 1991; 105: 361-367.
30. Van Steveninck AL, Schoemaker RC, Den Hartigh J, et al. Effects of intravenous temazepam (I); saccadic eye movements and EEG following fast and slow infusion to pseudo steady state. Clin Pharmacol Ther 1994; 55: 535-545.
31. Santamaria J, Chiappa KH. The EEG of drowsiness in normal adults. J Clin Neurophysiol 1987; 4: 327-382.
32. Greenblatt DJ, Ehrenberg BL, Gunderman J, et al. Pharmacokinetic and electroencephalographic study of intravenous diazepam, midazolam, and placebo. Clin Pharmacol Ther 1989; 45: 356-365.
33. Bührer M, Maitre PO, Crevoisier C, Stanski DR. Electroencephalographic effects of benzodiazepines II. Pharmacodynamic modeling of the electroencephalographic effects of midazolam and diazepam. Clin Pharmacol Ther 1990; 48: 555-567.
34. Ariano RE, Kassum DA, Aronson KJ. Comparison of sedative recovery time after midazolam versus diazepam administration. Crit Care Med 1994; 22: 1492-1496.
35. Stanski DR. Pharmacodynamic modeling of anesthetic EEG drug effects. Ann Rev Pharmacol Toxicol 1992; 32: 423-447.
36. Mastey V, Donati F, Varin F. Early pharmacokinetics of midazolam. Sampling site and schedule considerations. Clin Drug Invest 1995; 9: 131-140.