European Journal of Clinical Pharmacology

, Volume 10, Issue 1, pp 1–7 | Cite as

The fate of3H-terbutaline sulphate administered to man as an aerosol

  • H. T. Nilsson
  • B. G. Simonsson
  • B. Ström


Six asthmatic patients and two healthy volunteers inhaled tritiated terbutaline sulphate delivered by a pressurized aerosol inhaler. Spirometric measurements were performed and the amounts of total radioactivity in plasma, urine and faeces were determined. The analysis of urine included determination of radioactivity due to metabolized drug. Depending on the amount of drug inhaled the peak plasma level varied from undetectable to 3.8 ng/ml. An early plasma peak was found in 7 out of 8 subjects. The main plasma peaks were observed 1 – 6 hours after administration. The results of urinalysis showed a metabolic profile similar to that after parenteral administration. Disregarding the amount of inhaled drug and sampling time, 3 – 35% of the delivered drug was recovered in the urine and 2 – 37% in the faeces. Immediately after treatment 4 subjects rinsed their mouths with water and it was found to contain 14.5 – 50% of the delivered dose. The adapters from the aerosol canisters contained 14 – 27.5% of the delivered dose of drug.

Key words

3H-terbutaline sulphate aerosol man absorption excretion spirometry 


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. 1.
    Arner, B.: A comparative clinical trial of different subcutaneous doses of terbutaline and orciprenaline in bronchial asthma. Acta med. scand. Suppl.512 45–48 (1970)Google Scholar
  2. 2.
    Arner, B., Bertler, Å., Karlefors, T., Westling, H.: Bronchodilator effect of a new sympathomimetic receptor-stimulating agent, terbutaline, given subcutaneously to asthmatic patients. Acta med. scand. Suppl.512 41–43 (1970)Google Scholar
  3. 3.
    Da Costa, J.L., Goh, B.K.: Studies of new sympathomimetic β-receptor stimulating drugs in asthmatic patients. I. The bronchodilator and circulatory effects of subcutaneous terbutaline. Singapore med. J.14 120–123 (1973)Google Scholar
  4. 4.
    Da Costa, J.L., Goh, B.K.: A comparative trial of subcutaneous terbutaline, Th 1165a, and adrenaline in bronchial asthma. Med. J. Aust.2 588–590 (1970)Google Scholar
  5. 5.
    Da Costa, J.L., Hedstrand, U.: The effect of new sympathomimetic β-receptor stimulating drug (terbutaline) on arterial blood gases in bronchial asthma. Scand. J. resp. Dis.51 212–217 (1970)Google Scholar
  6. 6.
    Cotes, J.E., Houston, K., Saunders, M.J.: Interpretation of aerosol recovery curves following inhalation of monodispersed particles. J. Physiol. (Lond.)213, 22–23 p (1971)Google Scholar
  7. 7.
    Davies, D.S.: Metabolism of isoprenaline and other bronchodilator drugs in man and dog. Bull. Physiopathol. respir.8 679–682 (1972)Google Scholar
  8. 8.
    Espinoza, R.: Klinisk komparativt försök mellom terbutalin- og isoprenalinaerosol. Nord. Med.85 729 (1971)Google Scholar
  9. 9.
    Formgren, H.: A clinical comparison of the effect of oral terbutaline and orciprenaline. Scand. J. resp. Dis.51 195–202 (1970)Google Scholar
  10. 10.
    Freedman, B.J.: Trial of a terbutaline aerosol in the treatment of asthma and a comparison of its effects with those of a salbutamol aerosol. Brit. J. Dis. Chest66 222–229 (1972)Google Scholar
  11. 11.
    Huhti, E.: Clinical comparison of terbutaline and isoprenaline administered by inhalation. Ann. clin. Res.4 152–164 (1972)Google Scholar
  12. 12.
    Lin, C., Magat, J., Calesnick, B., Symchowitz, S.: Absorption, excretion and urinary metabolic pattern of3H-albuterol aerosol in man. Xenobiot.2 507–515 (1972)Google Scholar
  13. 13.
    Morrow, P.E.: Dynamics of dust removal from the lower airways, measurements and interpretation based upon radioactive aerosols. In: Airway dynamics (Ed. A. Bouhuys) pp. 299–312, Springfield, Ill.: C.C. Thomas 1970Google Scholar
  14. 14.
    Muir, D.C.F.: The effect of airways obstruction on the single breath aerosol curve. In: Airway dynamics (Ed. A. Bouhuys) pp. 319–325, Springfield, Ill.: C.C. Thomas 1970Google Scholar
  15. 15.
    Nilsson, H.T., Persson, K., Tegnér, K.: The metabolism of terbutaline in man. Xenobiot.2 363–373 (1972)Google Scholar
  16. 16.
    Paterson, J.W., Conolly, M.E., Davies, D.S., Dollery, C.T.: Isoprenaline resistance and the use of pressurized aerosols in asthma. Lancet1968 II 426–429Google Scholar
  17. 17.
    Persson, K., Persson, K.: The metabolism of terbutalinein vitro by rat and human liver O-methyltransferase and monoamine oxidase. Xenobiot.2 375–382 (1972)Google Scholar
  18. 18.
    Rossum, J.M. van: Pharmacokinetics of inhalation medication. Int. J. clin. Pharmacol. Suppl.4 28–36 (1971)Google Scholar
  19. 19.
    Simonsson, B.G., Stiksa, J., Ström, B.: Double-blind trial with increasing doses of salbutamol and terbutaline aerosols in patients with reversible airways obstruction. Acta med. scand.192 371–376 (1972)Google Scholar
  20. 20.
    Svedmyr, N., Malmberg, R., Thiringer, G.: The effect of a new adrenergic β2-receptor stimulating agent (Rimiterol, R 798) in patients with chronic obstructive lung disease. Scand. J. resp. Dis.53 302–313 (1972)Google Scholar
  21. 21.
    Svensson, L.Å., Sörenby, L.: Personal communicationGoogle Scholar

Copyright information

© Springer-Verlag 1976

Authors and Affiliations

  • H. T. Nilsson
    • 1
  • B. G. Simonsson
    • 1
  • B. Ström
    • 1
  1. 1.Research and Development Laboratories and Department of Lung Medicine, LasarettetAB DracoLundSweden

Personalised recommendations