European Journal of Clinical Pharmacology

, Volume 60, Issue 4, pp 265–268 | Cite as

Bioavailability of fluticasone propionate and mometasone furoate aqueous nasal sprays

  • P. T. Daley-Yates
  • R. L. Kunka
  • Y. Yin
  • S. M. Andrews
  • S. Callejas
  • C. Ng
Pharmacokinetics and Disposition



To compare the systemic exposure for intranasal mometasone furoate (MF) and fluticasone propionate (FP) aqueous nasal sprays (ANS) in terms of serum and urinary cortisol parameters and plasma pharmacokinetics.


Twelve healthy subjects completed this three-way, cross-over study. They received FPANS (50 μg/spray), MFANS (50 μg/spray) or placebo ANS, eight sprays per nostril every 8 h for 4 days. Cortisol measurements were made at baseline and day 4. FP and MF plasma concentrations were also measured on day 4.


MFANS produced similar mean plasma AUC (123 pmol/l h) to FPANS (112 pmol/l h). Despite the use of high doses, necessary to generate adequate pharmacokinetic data, only minor reductions in cortisol parameters were found, with no difference between FPANS and MFANS.


FP and MF have similar and very low systemic bioavailability when administered intranasally using a high-dose regimen. It is therefore unlikely that therapeutic doses of intranasal FP or MF will produce dissimilar or significant degrees of systemic exposure or systemic effects.


Fluticasone propionate Mometasone furoate Nasal bioavailability 


  1. 1.
    Dolovich J, O’Connor M, Stepner N, Smith A, Sharma RK (1994) Double-blind comparison of intranasal fluticasone propionate, 200 micrograms, once daily with 200 micrograms twice daily in the treatment of patients with severe seasonal allergic rhinitis to ragweed. Ann Allergy 72:435–440PubMedGoogle Scholar
  2. 2.
    Pedersen B, Dahl R, Richards DH (1995) Once daily fluticasone propionate aqueous nasal spray controls symptoms of most patients with seasonal allergic rhinitis. Allergy 50:794–799PubMedGoogle Scholar
  3. 3.
    Hebert JR, Nolop K, Lutsky BN (1996) Once-daily mometasone furoate aqueous nasal spray (Nasonex) in seasonal allergic rhinitis: an active- and placebo-controlled study. Allergy 51:569–576PubMedGoogle Scholar
  4. 4.
    Drouin M, Yang WH, Bertrand B (1996) Once daily mometasone furoate aqueous nasal spray is as effective as twice daily beclomethasone dipropionate for treating perennial allergic rhinitis patients. Ann Allergy Asthma Immunol 77:153–160PubMedGoogle Scholar
  5. 5.
    Daley-Yates PT, Baker R (2001) Systemic bioavailability of fluticasone propionate administered as nasal drops and the aqueous nasal spray formulations. Br J Clin Pharmacol 51:103–105CrossRefPubMedGoogle Scholar
  6. 6.
    McDowell JE, Mackie AE, Ventresca GP, Bye A (1997) Pharmacokinetics and bioavailability of intranasal fluticasone in humans. Clin Drug Invest 1:44–52Google Scholar
  7. 7.
    Schering-Plough Research Institute (1998) SCH 32088: single dose absolute bioavailability study of mometasone nasal spray in volunteers with evidence of allergic rhinitis. Study No. C93–196 (data on file)Google Scholar
  8. 8.
    Callejas S, Biddlecombe R, Jones A, Joyce K, Pereira A, Pleasance S (1998) Determination of the glucocorticoid fluticasone propionate in plasma by automated solid-phase extraction and liquid chromatography-tandem mass spectrometry. J Chromatogr 718:243–250Google Scholar
  9. 9.
    FDA Summary Basis of Approval (2000) NDA 20762, Nasonex Nasal Spray Medical Officer ReviewGoogle Scholar
  10. 10.
    Price AC, Daley-Yates PT, Wright AM, Callejas S (2000) Negligible absolute bioavailability and no HPA-axis effects after multiple 200 µg daily doses of Fluticasone propionate (FP) administered from the aqueous nasal spray (FPANS). Eur Resp J 16:279sGoogle Scholar
  11. 11.
    Daley-Yates PT, Price AC, Sisson JR, Pereira A, Dallow N (2001) Beclomethasone dipropionate: absolute bioavailability, pharmacokinetics and metabolism following intravenous, oral, intranasal and inhaled administration in man. Br J Clin Pharmacol 51:400–409CrossRefPubMedGoogle Scholar
  12. 12.
    Jeal W, Faulds D (1997) Triamcinolone acetonide. A review of its pharmacological properties and therapeutic efficacy in the management of allergic rhinitis. Drugs 53:257–280PubMedGoogle Scholar
  13. 13.
    Thorsson L, Borga O, Edsbaker S (1999) Systemic availability of budesonide after nasal administration of three different formulations: pressurized aerosol, aqueous pump spray and powder. Br J Clin Pharmacol 47:619–624CrossRefPubMedGoogle Scholar
  14. 14.
    Argenti D, Colligon I, Heald D (1994) Nasal mucosal inflammation has no effect on the absorption of intranasal triamcinolone acetonide. J Clin Pharmacol 34:854–858PubMedGoogle Scholar
  15. 15.
    Vargas R, Dockhorn RJ, Findlay SR, Korenblat PE, Field EA, Kral KM (1998) Effect of fluticasone propionate aqueous nasal spray versus oral prednisone on the hypothalamic-pituitary-adrenal axis. J Allergy Clin Immunol 102:191–197PubMedGoogle Scholar
  16. 16.
    Van As A, Bronsky E, Grossman J, Meltzer E, Ratner P, Reed C (1991) Dose tolerance study of fluticasone propionate aqueous nasal spray in patients with seasonal allergic rhinitis. Ann Allergy 67:156–162PubMedGoogle Scholar
  17. 17.
    Brannan MD, Seiberling M, Cutler DL (1996) Lack of systemic activity with intranasal mometasone furoate. J Allergy Clin Immunol 97:198Google Scholar
  18. 18.
    Brannan MD, Herron JM, Reidenberg P (1996) Lack of HPA axis suppression following 36 days of intranasal mometasone furoate. Ann Allergy Asthma Immunol 78:154Google Scholar
  19. 19.
    Crim C, Pierre LN, Daley-Yates PT (2001) A review of the pharmacology and pharmacokinetics of fluticasone propionate and mometosone furoate. Clin Therapeut 23:1339–1354CrossRefGoogle Scholar
  20. 20.
    Daley-Yates PT, Richards DH (2001) Pharmacokinetic and pharmacodynamic relationships for intranasal corticosteroids (INCS). J Allergy Clin Immunol 107:S313Google Scholar

Copyright information

© Springer-Verlag 2004

Authors and Affiliations

  • P. T. Daley-Yates
    • 1
  • R. L. Kunka
    • 2
  • Y. Yin
    • 2
  • S. M. Andrews
    • 2
  • S. Callejas
    • 3
  • C. Ng
    • 2
  1. 1.GlaxoSmithKline Research & DevelopmentClinical Pharmacology & Discovery MedicineGreenford, MiddlesexUK
  2. 2.GlaxoSmithKline Research & DevelopmentUSA
  3. 3.GlaxoSmithKline Research & DevelopmentWareUK

Personalised recommendations