European Journal of Clinical Pharmacology

, Volume 4, Issue 3, pp 137–141 | Cite as

Pharmacokinetics of fentanyl in man and the rabbit

  • R. Hess
  • G. Stiebler
  • A. Herz


Plasma levels and urinary excretion of3H-fentanyl were studied in 5 human subjects after intravenous injection of this drug. After an initial rapid decline, the plasma level of fentanyl decreased slowly and approximately exponentially. The plasma concentration of metabolites remained almost steady from 1–3 h after injection. More than 60% of the administered radioactivity was excreted through the kidneys within 4 days. Only a small proportion of it was unchanged fentanyl. The rates of fall of plasma concentration and of urinary excretion were slower in man than in rabbits. — The time courses of plasma concentrations and of urinary excretion were simulated on an analogue computer. The results support the assumption that the different time courses of concentrations in man and rabbits are caused by slower metabolism in man. It seems likely that redistribution plays a dominant part in the short duration of action of fentanyl in man.

Key words

Fentanyl pharmacokinetics neuroleptanalgesia analogue computer 


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. Bray, G.A.: A simple efficient liquid scintillator for countting aqueous solutions in a liquid scintillation counter. Analytical Biochemistry1, 279–285 (1960).Google Scholar
  2. Cube, B. von, Teschemacher, Hj., Herz, A., Hess, R.: Permeation morphinartig wirksamer Substanzen an den Ort der antinociceptiven Wirkung im Gehirn in Abhängigkeit von ihrer Lipoidlöslichkeit nach intravenöser und nach intraventrikulärer Applikation. Naunyn-Schmiedebergs Arch. Pharmak.265, 455–473 (1970).Google Scholar
  3. Downes, J.J., Kemp, R.A., Lambertsen, C.J.: The magnitude and duration of respiratory depression due to fentanyl and meperidine in man. J. Pharmacol. exp. Ther.158, 416–420 (1967).Google Scholar
  4. Finch, J.S., de Kornfeld, T.J.: Clinical investigation of analgesic potency and respiratory depressant properties of fentanyl. J. clin. Pharma.7, 46–51 (1967).Google Scholar
  5. Gardocky, J.F., Yelnosky, J.: A study of some of the pharmacologic actions of fentanyl citrate. Toxicol. appl. Pharmacol.6, 48–62 (1964).Google Scholar
  6. Henschel, W.F.: Die Neuroleptanalgesie. Der Landarzt36, 1613–1623 (1966).Google Scholar
  7. Hess, R., Herz, A., Friedel, K.: Pharmacokinetics of fentanyl in rabbits in view of the importance for limiting the effect. J. Pharmacol. exp. Ther.179, 474–481 (1971).Google Scholar
  8. Holderness, M.C., Chase, P.E., Dripps, R.D.: A narcotic analgesic and a butyrophenone with nitrous oxide for general anaesthesia. Anaesthesiology24, 336–340 (1963).Google Scholar
  9. Janssen, P.A.J., Niemegeers, C.J.E., Dony, J.G.H.: The inhibitory effect of fentanyl and other morphine-like analgesics on the warm water induced tail withdrawal reflex in rats. Drug Research13, 502–507 (1963).Google Scholar
  10. Kreuscher, H., Frey, R., Madijdi, A.: Die Neuroleptanalgesie. Dtsch. med. Wschr.16, 721–725 (1965).Google Scholar
  11. Maruyama, Y., Hosoya, E.: Studies on the fate of fentanyl. Keio J. Med.18, 59–70 (1969).Google Scholar
  12. Schaer, H., Jenny, E.: Plasmakonzentration und Plasmaeiweißbindung von Droperidol und Fentanyl während der Neuroleptanalgesie beim Menschen. In: Neue Klinische Aspekte der Neuroleptanalgesie. W. F. Henschel, Ed. p. 15–20. Stuttgart: F.K. Schattauer Verlag 1970.Google Scholar
  13. Wijngaarden, I. van, Soudijn, W.: The metabolism and excretion of the analgesic fentanyl (R 4263) by wistar rats. Life Sciences7, (I) 1239–1244 (1968).Google Scholar

Copyright information

© Springer-Verlag 1972

Authors and Affiliations

  • R. Hess
    • 1
    • 2
  • G. Stiebler
    • 1
  • A. Herz
    • 1
  1. 1.Max-Planck-Institut für Psychiatrie und I. Frauenklinik der UniversitätMünchenGermany
  2. 2.Max-Planck-Institut für biophysikalische ChemieGöttingen-NikolausbergGermany

Personalised recommendations