Skip to main content
Log in

Pharmacokinetics of fentanyl in man and the rabbit

  • Originals
  • Published:
European Journal of Clinical Pharmacology Aims and scope Submit manuscript

Summary

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.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  • Bray, G.A.: A simple efficient liquid scintillator for countting aqueous solutions in a liquid scintillation counter. Analytical Biochemistry1, 279–285 (1960).

    Google Scholar 

  • 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 

  • 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 

  • 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 

  • 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 

  • Henschel, W.F.: Die Neuroleptanalgesie. Der Landarzt36, 1613–1623 (1966).

    Google Scholar 

  • 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 

  • 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 

  • 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 

  • Kreuscher, H., Frey, R., Madijdi, A.: Die Neuroleptanalgesie. Dtsch. med. Wschr.16, 721–725 (1965).

    Google Scholar 

  • Maruyama, Y., Hosoya, E.: Studies on the fate of fentanyl. Keio J. Med.18, 59–70 (1969).

    Google Scholar 

  • 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 

  • 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 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Hess, R., Stiebler, G. & Herz, A. Pharmacokinetics of fentanyl in man and the rabbit. Eur J Clin Pharmacol 4, 137–141 (1972). https://doi.org/10.1007/BF00561135

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF00561135

Key words

Navigation