European Journal of Clinical Pharmacology

, Volume 22, Issue 6, pp 523–529

Topical and systemic glucocorticoid potencies of budesonide and beclomethasone dipropionate in man

  • S. -Å. Johansson
  • K. -E. Andersson
  • R. Brattsand
  • E. Gruvstad
  • P. Hedner
Originals

Summary

Topical anti-inflammatory (cutaneous “vasoconstriction”) and systemic glucocorticoid (depression of plasma cortisol and changes in differential WBC count) potencies of the two glucocorticoids budesonide and beclomethasone dipropionate (BDP) were compared in human volunteers. After topical application, budesonide was 2–3 times more potent than BDP in inducing “vasoconstriction”. After oral administration, on the other hand, budesonide was 2–4 times less potent than BDP in depressing plasma cortisol and changing the total or differential WBC. After inhalation, too, significant differences in favour of budesonide were noted, but the divergence between the drugs was less pronounced. The improved relationship between the topical and systemic glucocorticoid effects of budesonide makes it a promising alternative for aerosol treatment in asthma.

Key words

beclomethasone diproprionate budesonide glucocorticoids aerosol plasma cortisol differential WBC topical effect topical administration 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Andersson P, Edsbäcker S, Ryrfeldt Å (1982) In vitro biotransformation of budesonide, triamcinolonacetonide and hydrocortisone in liver and skin from man, rat and hairless mouse. J Steroid Biochem 16: 787–796PubMedCrossRefGoogle Scholar
  2. Armitage P (1974) Statistical methods in clinical research. Blackwell, OxfordGoogle Scholar
  3. Björkander J, Formgren H, Johansson SÅ, Millquist E (1982) Methodological aspects on clinical trials with inhaled corticosteroids: Results of two comparisons between two steroid aerosols in patients with asthma. Eur J Respir Dis Suppl 122 (Vol 63) 108–117Google Scholar
  4. Brattsand R, Thalén A, Roempke K, Källström L, Gruvstad E (1982) Influence of 16α, 17a-acetal substitution and steroid nucleus fluorination on the topical to systemic activity of glucocorticoids. J Steroid Biochemistry 16: 779–786CrossRefGoogle Scholar
  5. Brown MH, Storey G (1973) Beclomethasone dipropionate steroid aerosol in treatment of perennial allergic asthma in children. Br Med J 3: 161–164PubMedGoogle Scholar
  6. Brown MH, Storey G, George WHS (1972) Beclomethasone dipropionate: A new steroid aerosol for the treatment of allergic asthma. Br Med J 1: 585–590PubMedCrossRefGoogle Scholar
  7. Brown MH, Storey G (1975) Treatment of allergy of the respiratory tract with beclomethasone dipropionate steroid aerosol. Postgrad Med J 51 (Suppl 4): 59–64PubMedGoogle Scholar
  8. Buniva G, Dubini A, Sassella D (1979) Human bioassay of corticotropin-suppressing eosinopenic and hyperglycaemic potencies of deflazacort and prednisone. Curr Ther Res 26: 69–81Google Scholar
  9. Claman HN (1975) How corticosteroids work. J Allergy Clin Immunol 55: 145–51PubMedCrossRefGoogle Scholar
  10. Clark THJ (1972) The effect of beclomethasone trpropionate delivered by aerosol in patients with asthma. Lancet 1: 1361–1364PubMedCrossRefGoogle Scholar
  11. Ellul-Micallef R, Hansson E, Johansson SÅ (1980) Budesonide A new corticosteroid in bronchial asthma. Eur J Respir Dis 61: 167–173PubMedGoogle Scholar
  12. Finney DJ (1952) Statistical method in biological assay. Hafner, New YorkGoogle Scholar
  13. Harris DM (1980) In: Topical steroid treatment for asthma and rhinitis. Clark THJ and Mygind N (eds) Clinical Pharmacology of Beclomethasone dipropionate. Baillere-Tindall, London, pp 34–47Google Scholar
  14. Hartiala J, Uotila P, Nienstedt W (1979) Absorption and metabolism of intratracheally instilled cortisol and beclomethasone dipropionate in the isolated perfused rat lungs. Med Biol 57: 294–297PubMedGoogle Scholar
  15. Martin LE, Tanner RJN, Clark THJ, Cochrane GM (1974) Absorption and metabolism of orally administered beclomethasone dipropionate. Clin Pharmacol Ther 15: 267–275PubMedGoogle Scholar
  16. McKenzie AW, Stoughton RB (1962) Method for comparing percutaneous absorption of steroids. Arch Dermatol 86: 608–610Google Scholar
  17. Mygind M, Hansen J (1973) Beclomethasone dipropionate aerosol effect on the adrenals in normal persons. Acta Allergol 28: 211–218PubMedGoogle Scholar
  18. Place VA, Velazquez JG, Burdick KH (1970) Precise evaluation of topically applied corticosteroid potency. Arch Dermatol 101: 531–537PubMedCrossRefGoogle Scholar
  19. Rosenhall L, Lundquist G, Ädelroth E, Glennow C (1982) Comparison between inhaled and oral corticosteroids in patients with chronic asthma. Eur J Respir Dis Suppl 122 (Vol 63) 154–162Google Scholar
  20. Ryrfeldt Å, Andersson P, Edsbäcker S, Tönnesson M, Davies D, Pauwels R (1981) Pharmacokinetics of a selective glucocorticoid, budesonide. Proceedings of the Annual Meeting of European Academy of Allergology and Clinical Immunology, Clermont-Ferrand, France 704–708Google Scholar
  21. Ryrfeldt Å, Tönnesson M, Nilsson E, Wikby A (1979) Pharmacokinetics studies of a potent glucocorticoid (budesonide) in dogs by high performance liquid chromatography. J Steroid Biochem 10: 317–324PubMedCrossRefGoogle Scholar
  22. Scott M, Malmsten LÅ, Thelin J (1981) Effect on plasma cortisol level and urinary cortisol excretion, in helathy volunteers, after application of three different topical steroid ointments under occlusion. Acta Derm Venereol 61: 543–546PubMedGoogle Scholar
  23. Thalén A, Brattsand R (1979) Synthesis and Anti-inflammatory properties of budesonide, a new non-halogenated glucocorticoid with high local activity. Arzneim Forsch 29 (II), 11: 1687–1690Google Scholar
  24. Toogood JH, Lefcoe NH, Haines DSM, Jennings B, Errington M, Baksh L, Chuang L (1977a) A graded doseassessment of the efficacy of beclomethasone dipropionate aerosol for severe chronic asthma. J Allergy 59: 298–308Google Scholar
  25. Toogood JH, Lefcoe NH, Haines DSM, Chuang L, Jennings B, Errington N, Baksh L, Cauchi M (1978) Minimum dose requirements of steroid-dependent asthmatic patients for aerosol beclomethasone and oral prednisone. J Allergy 61: 355–364Google Scholar
  26. Wyatt R, Waschek J, Weinberger M, Sherman B (1978) Effects of inhaled beclomethasone dipropionate and alternateday prednisone on pituitary-adrenal function in children with chronic asthma. N Engl J Med 299 (No.25): 1387–1392PubMedCrossRefGoogle Scholar

Copyright information

© Springer-Verlag 1982

Authors and Affiliations

  • S. -Å. Johansson
    • 1
  • K. -E. Andersson
    • 2
  • R. Brattsand
    • 3
  • E. Gruvstad
    • 1
  • P. Hedner
    • 4
  1. 1.Medical DepartmentAB DracoLundSweden
  2. 2.Department of Clinical PharmacologyUniversity of LundLundSweden
  3. 3.R & D DepartmentAB DracoLundSweden
  4. 4.Medical DepartmentUniversity of LundLundSweden

Personalised recommendations