Pharmacokinetic-pharmacodynamic modelling of the EEG effect of alfentanil in rats

Journal of Pharmacological and Toxicological Methods

Volumn 38, Issue 2, 1997, Pages 99-108

  Cox, Eugène H ^a   Van Hemert, Jeanine G N ^a   Tukker, Erica J ^a   Danhof, Meindert ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

Author keywords

Alfentanil; EEG; Hypothermia; Pharmacokinetic Pharmacodynamic modelling; Proconvulsant activity

Indexed keywords

ALFENTANIL; MIDAZOLAM; VECURONIUM;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; CONVULSION; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG CLEARANCE; ELECTROENCEPHALOGRAM; HALF LIFE TIME; HYPOTHERMIA; INTRAVENOUS DRUG ADMINISTRATION; MALE; MODEL; NONHUMAN; PHARMACODYNAMICS; RAT; RESPIRATION DEPRESSION;

ALFENTANIL; ANALGESICS, OPIOID; ANIMALS; AREA UNDER CURVE; BLOOD GAS ANALYSIS; BODY TEMPERATURE; CHROMATOGRAPHY, GAS; ELECTROENCEPHALOGRAPHY; MALE; MODELS, BIOLOGICAL; RATS; RATS, INBRED STRAINS; RATS, WISTAR; RESPIRATION, ARTIFICIAL; SEIZURES;

ANIMALIA;

EID: 0030656350     PISSN: 10568719     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1056-8719(97)00065-8     Document Type: Article

References (57)

1. 2 reactivity in pigs anaesthesized with fentanyl, nitrous oxide and pancuronium. Acta Anaesthesiol Scand 37:85-93.
2. Akaike H (1974) A new look at the statistical model identification. IEEE Trans Automat Control AC-19:716-723.
3. Ambre JJ, Belknap SM, Nelson J, Ih Ruo T, Shin S, Atkinson AJJ (1988) Acute tolerance to cocaine in humans. Clin Pharmacol Ther 44:1-8.
4. Ausems ME, Hug Jr. CC, Stanski JR, Burm AGL (1986) Plasma concentrations of alfentanil required to supplement nitrous oxide anaesthesia for general surgery. Anesthesiology 65:362-373.
5. Bauer JA, Fung H (1990) Effects of chronic glyceryl nitrate on left ventricular haemodynamics in a rat model of congestive heart failure: demonstration of a simple animal model for the study of in-vivo nitrate tolerance. Cardiovasc Res 24:198-203.
6. Björkman S, Stanski DR, Verotta D, Harashima H (1990) Comparative physiological pharmacokinetics of fentanyl and alfentanil in humans predicted from tissue/blood partition data obtained in rats. Anesthesiology 72:865-873.
7. Björkman S, Stanski DR, Harashima H, Dowrie R, Harapat SR, Wada DR, Ebling WF (1993) Tissue distribution of fentanyl and alfentanil in the rat cannot be described by a blood flow limited model. J Pharmacokin Biopharm 21:255-279.
8. Björkman S, Wada DR, Stanski DR, Ebling WF (1994) Comparative physiological pharmacokinetics of fentanyl and alfentanil in rats and humans based on parametric single-tissue models. J Pharmacokin Biopharm 22:381-410.
9. Carlsson C, Smith DS, Keykhay MM, Englebach I, Harp JR (1982) The effects of high-dose fentanyl on cerebral circulation and metabolism in rats. Anesthesiology 57:375-380.
10. Chow MJ, Ambre JJ, Ih Ruo T, Atkinson AJJ, Bowsher DJ, Fischman MW (1985) Kinetics of cocaine distribution, elimination and chronotropic effects. Clin Pharmacol Ther 38:318-324.
11. Chugani HT, Ackermann RF, Chugani DC, Engel Jr J (1984) Opioid-induced epileptogenic phenomena: anatomical, behavioral, and electroencephalographic features. Ann Neurol 15:361-368.
12. Clark WG (1981) Effects of opioid peptides on thermoregulation. Fed Proc 40:2754-2759.
13. Danhof M, Mandema JW, Hoogerkamp A, Mathot RAA (1993) Pharmacokinetic-pharmacodynamic modelling in pre-clinical investigations: principles and perspectives. Eur J Drug Metab Pharmacokinet 18:41-47.
14. De Castro J, Van de Water A, Wouters L, Xhonneux R, Reneman R, Kay B (1979) Comparative study of cardiovascular, neurological ans metabolic side-effects of eight narcotics in dogs. Acta Anesthesiol Belg 30:6-99.
15. Dingemanse J, Sollie FAE, Breimer DD, Danhof M (1988) Pharmacokinetic modelling of the anticonvulsant response of oxazepam in rats using the pentylenetetrazol threshold concentration as pharmacodynamic measure. J Pharmacokin Biopharm 16:203-228.
16. Ebling WF, Danhof M, Stanski DR (1991) Pharmacodynamic characterization of the electroencephalographic effects of thiopental in rats. J Pharmacokin Biopharm 19:123-143.
17. Gårdmark M, Ekblom M, Bouw R, Hammarlund-Udenaes M (1993) Quantification of effect delay and acute tolerance development of morphine in the rat. J Pharmacol Exp Ther 267:1061-1067.
18. Gibaldi M, Perrier D (1982) Noncompartmental analysis based on statistical moment theory. In Pharmacokinetics 2nd ed. Ed. X. New York: Marcel Dekker, pp. 409-424.
19. Gilmore PC, Brenner RP (1981) Correlation of EEG, computerized tomography, and clinical findings. Study of 100 patients with focal delta activity. Arch Neurol 38:371-372.
20. Hammarlund MM, Odlind B, Paalzow LK (1985) Acute tolerance to furosemide diuresis in humans: pharmacokinetic-pharmacodynamic modelling. J Pharmacol Exp Ther 233:447-453.
21. James MK (1994) Remifentanil and anesthesia for the future. Exp Opin Invest Drugs 3:331-340.
22. Keykhay MM, Smith DS, Carlsson C, Safo Y, Englebach I, Harp JR (1985) Influence of sufentanil on cerebral metabolism and circulation in the rat. Anesthesiology 63:274-277.
23. Kofke WA, Graman RH, Tom WC, Rose ME, Hawkins RA (1993) Alfentanil-induced hypermetabolism, seizure, and histopathology in rat brain. Anesth Analg 75:953-964.
24. Lemmens HJM, Dyck JB, Shafer SL, Stanski DR (1994) Pharmacokinetic-pharmacodynamic modeling in drug development: application to the investigational opioid trefentanil. Clin Pharmacol Ther 56:261-271.
25. Levy G (1993) The case for preclinical pharmacodynamics. In Integration of Pharmacokinetics, Pharmacodynamics and Toxicokinetics in Rational Drug Development. Eds. A Yacobi, JP Skelly, VP Shah, and LZ Benet. New York: Plenum Press, pp. 7-13.
26. Lupica CR, Dunwiddie TV (1991) Differential effects of mu-and delta selective opioid agonists on feedforward and feedback GABAergic inhibition in hippocampal brain slices. Synapse 8:237-248.
27. Maekawa T, Tommasino C, Shapiro HM (1984) Local cerebral blood flow with fentanyl seizures. J Cereb Blood Flow Metab 4:88-95.
28. Mandema JW, Danhof M (1990) Pharmacokinetic-pharmacodynamic modelling of the CNS effects of heptabarbital using EEG analysis. J Pharmacokin Biopharm 18:459-481.
29. Mandema JW, Tukker E, Danhof M (1991a) Pharmacokinetic-pharmacodynamic modelling of the EEG effects of midazolam in individual rats: influence of rate and route of administration. Br J Pharmacol 102:663-668.
30. Mandema JW, Sansom LN, Dios-Vièitez C, Hollander-Janssen M, Danhof M (1991b) Pharmacokinetic-pharmacodynamic modeling of the EEG effects of benzodiazepines. Correlation with receptor binding and anticonvulsant activity. J Pharmacol Exp Ther 257:472-478.
31. Mandema JW, Tuk B, Van Steveninck AL, Breimer DD, Cohen AF, Danhof M (1992a) Pharmacokinetic-pharmacodynamic modeling of the central nervous system effects of midazolam and its main metabolite alpha-hydroxymidazolam in healthy volunteers. Clin Pharmacol Ther 51:715-728.
32. Mandema JW, Heijligers-Feijen CD, Tukker E, De Boer AG, Danhof M (1992b) Modeling of the effect site equilibration kinetics and pharmacodynamics of racemic baclofen and its enantiomers using quantitative EEG effect measures. J Pharmacol Ther 261:88-95.
33. Mandema JW, Wada DR (1995) Pharmacodynamic model for acute tolerance development to the electroencephalographic effects of alfentanil in the rat. J Pharmacol Exp Ther 275:1185-1194.
34. Marshall DW, Brey RL, Morse MW (1988) Focal and/or lateralized polymorphic delta activity. Association with either normal or ''nonfocal' computed tomographic scans. Arch Neurol 45:33-35.
35. Meuldermans WEG, Hurkmans RMA, Heykants JJP (1982) Plasma protein binding and distribution of fentanyl, sufentanil, alfentanil and lofentanil in blood. Arch Int Pharmacodyn 257:4-19.
36. Nicoll RA, Alger BE, Jahr CE (1980) Enkephalin blocks inhibitory pathways in the vertebrate CNS. Nature 287:22-25.
37. Panel-Raymond D, Gotman J (1990) Can slow waves in the electrocorticogram (ECoG) help localize epileptic foci? Electroencephal Clin Neurophysiol 75:464-473.
38. Peck CC, Barr WH, Benet LZ, et al. (1992) Opportunities for integration of pharmacokinetics, pharmacodynamics and toxicokinetics in rational drug development. Clin Pharmacol Ther 51:465-473.
39. Porchet HC, Benowitz NL, Sheiner LB (1988) Pharmacodynamic model of tolerance: application to nicotine. J Pharmacol Ther 244:231-236.
40. Puig MM, Warner W, Tang CK, Laorden ML, Turndorf H (1987) Effects of temperature on the interaction of morphine with opioid receptors. Br J Anaesth 59:1459-1464.
41. Rekand T, Sulg IA, Bjaertnes L, Jolin A (1991) Neuromonitoring of hypothermia and in hypothermie hypoxia. Arctic Med Res 50(Suppl. 6):32-36.
42. Rosow C (1993) Remifentanil: a unique opioid analgesic. Anesthesiology 79:875-876.
43. Scollo-Lavizzari G, Eichhorn K, Wiggli U (1976) Computerized transverse axial tomography in the diagnosis of epilepsy; an electroencephalo-tomographic study. EEG-EMZ Z Electroenzephalogr Electromyogr Verwandte Geb 7:189-192.
44. Scott JC, Cooke JE, Stanski DR (1991) Electroencephalographic quantification of opioid effect: the comparative pharmacodynamics of fentanyl and sufentanil. Anesthesiology 74:34-42.
45. Scott JC, Ponganis KV, Stanski DR (1985) EEG quantification of narcotic effect: the comparative pharmacodynamics of fentanyl and alfentanil. Anesthesiology 62:234-241.
46. Shafer SL, Varvel JR (1991) Pharmacokinetics, pharmacodynamics and rational opioid selection. Anesthesiology 53-63.
47. Tommasino C, Maekawa T, Shapiro HM (1984) Fentanyl-induced seizures activate subcortical brain metabolism. Anesthesiology 60: 283-290.
48. Urea G, Frenk H, Liebeskind JC, Taylor AN (1977) Morphine and enkephalin: analgesic and epileptic properties. Science 197:83-86.
49. Voskuyl RA, Dingemanse J, Danhof M (1989) Determination of the threshold for convulsions by direct cortical stimulation. Epilepsy Res 3:120-129.
50. Wagner JG (1974) A safe method for rapidly achieving plasma concentration plateaus. Clin Pharmacol Ther 16:691-700.
51. Wauquier A, Van den Broeck WAE, Niemegeers CJE, Janssen PAJ (1981) Effects of morphine, fentanyl, sufentanil, and the short-acting morphine-like analagesic alfentanil on the EEG in dogs. Drug Dev Res 1:167-179.
52. Wauquier A, Bovill JG, Sebel PS (1984) Electroencephalographic effects of fetanyl-, sufentanil-and alfentanil anesthesia in man. Neuropsychobiology 11:203-206.
53. Wauquier A, De Ryck M, Van den Broeck W, Van Loon J, Melis W, Janssen P (1988) Relationships between quantitative EEG measures and pharmacodynamics of alfentanil in dogs. Electroencephal Clin Neurophysiol 69:550-560.
54. Werz MA, MacDonald RL (1982) Opiate alkaloids antagonize postsynaptic glycine and GABA responses: correlation with convulsant action. Brain Res 236:107-119.
55. Woestenborghs R, Michielsen L, Heykants J (1981) Rapid and sensitive gas chromatographic method for the determination of alfentanil and sufentanil in biological samples. J Chromatogr 224:122-127.
56. Young GA, Neistadt L, Khazan N (1981) Differential neuropharmacological effects on mu, kappa and sigma opioid agonists on cortical EEG power spectra in the rat. Res Commun Psychol Psychiat Behav 6:365-377.
57. Young ML, Smith DS, Grenberg J, Reivich M, Harp JR (1984) Effects of sufentanil on regional cerebral glucose utilization in rats. Anesthesiology 61:564-568.