Skip to main content
SpringerLink
Log in

The pharmacokinetics after intravenous and oral administration in man of theα 2-adrenoreceptor antagonist idazoxan (RX781094)

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

Summary

A high performance liquid chromatographic method was developed for the quantitative determination of idazoxan in plasma. The assay was used to study the disposition of the drug after intravenous infusion and oral administration to five normal subjects. After i.v. administration the kinetics could be described by a two compartment model with a mean elimination half life of 4.20 h. The mean calculated volume of distribution during the elimination phase was 3.20 l/kg−1 and the mean plasma clearance was 824 ml min−1.

After oral administration a lag period before onset of absorption was observed in all five volunteers, the plasma levels declining monoexponentially from the peak concentration with a mean elimination half life of 5.58 h. The absolute availability varied between 26% and 41% with a mean value of 34%. Invitro measurements produced a blood/plasma ratio of 1.3 for idazoxan.

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

Access this article

Log in via an institution

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

Instant access to the full article PDF.

Institutional subscriptions

References

  • Chapleo CB, Doxey JC, Myers PL, Roach AG (1981) RX781094, a new potent, selective antagonist ofα 2-adrenoreceptors. Proceedings of the British Pharmacological Society 16th–18th September 1981. Br J Pharmacol 74: 842P

  • Dettmar PW, Lynn AG, Tulloch IF (1981) Neuropharmacological evaluation of RX781094, a new selective α2-adrenoreceptor antagonist. Proceedings of the British Pharmacological Society 16th–18th September 1981. Br J Pharmacol 74: 843P

  • Gibaldi M, Boyes RN, Feldman S (1971) Influence of first pass effects on availability of drugs on oral administration. J Pharm Sci 60: 1338–1340

    Google Scholar 

  • Gibaldi M, Perrier D (1975) Drugs and the pharmaceutical sciences, vol 1: Pharmacokinetics. Marcel Dekker, New York, pp 45–55

    Google Scholar 

  • Hannah JM, Hamilton CA, Reid JL (1983) RX781094, a new potent α2-adrenoreceptor antagonist. In-vivo and in-vitro studies in the rabbit. Naunyn Schmiedeberg's Arch Pharmacol 322: 221–227

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Pharmaceutical Division, Reckitt and Colman, Dansom Lane, Hull, UK

    N. C. Muir, J. G. Lloyd-Jones, J. D. Nichols & J. M. Clifford

Authors
  1. N. C. Muir
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. J. G. Lloyd-Jones
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. J. D. Nichols
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. J. M. Clifford
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Muir, N.C., Lloyd-Jones, J.G., Nichols, J.D. et al. The pharmacokinetics after intravenous and oral administration in man of theα 2-adrenoreceptor antagonist idazoxan (RX781094). Eur J Clin Pharmacol 29, 743–745 (1986). https://doi.org/10.1007/BF00615972

Download citation

  • Received:

  • Revised:

  • Accepted:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF00615972

Key words

Search

Navigation