Abstract
Methods: The area under the plasma concentration-time curves (AUC) and the maximum concentration (Cmax) of fluticasone propionate and budesonide after a single inhaled dose of each drug were compared in 12 healthy control subjects and 12 subjects with moderately severe asthma.
Results: Peak plasma levels of budesonide occurred much earlier and were approximately 20-fold higher than those of fluticasone propionate in both healthy and asthmatic subjects. The AUC and Cmax for fluticasone propionate were lower by 307 (95% CI 62 to 522) pg/ml/h or 43% (p=0.02) and 52 (95% CI –11 to 115) pg/ml or 39% (p=0.1) in subjects with asthma compared with healthy control subjects. In contrast, the AUC and Cmax for budesonide were almost identical between the two groups (mean differences 826 (95% CI –1493 to 3143) pg/ml/h (p=0.5) and 157 (95% CI –1026 to 1339) pg/ml (p=0.8).
Conclusions: Following inhalation, healthy subjects have higher plasma levels of fluticasone propionate than subjects with asthma whereas budesonide plasma levels are similar in the two groups of subjects. Comparing the systemic effects of budesonide and fluticasone propionate in healthy subjects is unlikely to be relevant to subjects with asthma.
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Selected References
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- Bisgaard H., Klug B., Sumby B. S., Burnell P. K. Fine particle mass from the Diskus inhaler and Turbuhaler inhaler in children with asthma. Eur Respir J. 1998 May;11(5):1111–1115. doi: 10.1183/09031936.98.11051111. [DOI] [PubMed] [Google Scholar]
- Boorsma M., Andersson N., Larsson P., Ullman A. Assessment of the relative systemic potency of inhaled fluticasone and budesonide. Eur Respir J. 1996 Jul;9(7):1427–1432. doi: 10.1183/09031936.96.09071427. [DOI] [PubMed] [Google Scholar]
- Brutsche M. H., Brutsche I. C., Munawar M., Langley S. J., Masterson C. M., Daley-Yates P. T., Brown R., Custovic A., Woodcock A. Comparison of pharmacokinetics and systemic effects of inhaled fluticasone propionate in patients with asthma and healthy volunteers: a randomised crossover study. Lancet. 2000 Aug 12;356(9229):556–561. doi: 10.1016/S0140-6736(00)02581-2. [DOI] [PubMed] [Google Scholar]
- Donnelly R., Williams K. M., Baker A. B., Badcock C. A., Day R. O., Seale J. P. Effects of budesonide and fluticasone on 24-hour plasma cortisol. A dose-response study. Am J Respir Crit Care Med. 1997 Dec;156(6):1746–1751. doi: 10.1164/ajrccm.156.6.9703003. [DOI] [PubMed] [Google Scholar]
- Harrison T. W., Wisniewski A., Honour J., Tattersfield A. E. Comparison of the systemic effects of fluticasone propionate and budesonide given by dry powder inhaler in healthy and asthmatic subjects. Thorax. 2001 Mar;56(3):186–191. doi: 10.1136/thorax.56.3.186. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Martin Richard J., Szefler Stanley J., Chinchilli Vernon M., Kraft Monica, Dolovich Myrna, Boushey Homer A., Cherniack Reuben M., Craig Timothy J., Drazen Jeffrey M., Fagan Joanne K. Systemic effect comparisons of six inhaled corticosteroid preparations. Am J Respir Crit Care Med. 2002 May 15;165(10):1377–1383. doi: 10.1164/rccm.2105013. [DOI] [PubMed] [Google Scholar]
- Melchor R., Biddiscombe M. F., Mak V. H., Short M. D., Spiro S. G. Lung deposition patterns of directly labelled salbutamol in normal subjects and in patients with reversible airflow obstruction. Thorax. 1993 May;48(5):506–511. doi: 10.1136/thx.48.5.506. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Möllmann H., Wagner M., Meibohm B., Hochhaus G., Barth J., Stöckmann R., Krieg M., Weisser H., Falcoz C., Derendorf H. Pharmacokinetic and pharmacodynamic evaluation of fluticasone propionate after inhaled administration. Eur J Clin Pharmacol. 1998 Feb;53(6):459–467. doi: 10.1007/s002280050407. [DOI] [PubMed] [Google Scholar]
- Nielsen L. P., Dahl R. Therapeutic ratio of inhaled corticosteroids in adult asthma. A dose-range comparison between fluticasone propionate and budesonide, measuring their effect on bronchial hyperresponsiveness and adrenal cortex function. Am J Respir Crit Care Med. 2000 Dec;162(6):2053–2057. doi: 10.1164/ajrccm.162.6.9912072. [DOI] [PubMed] [Google Scholar]
- Wong C. A., Walsh L. J., Smith C. J., Wisniewski A. F., Lewis S. A., Hubbard R., Cawte S., Green D. J., Pringle M., Tattersfield A. E. Inhaled corticosteroid use and bone-mineral density in patients with asthma. Lancet. 2000 Apr 22;355(9213):1399–1403. doi: 10.1016/S0140-6736(00)02138-3. [DOI] [PubMed] [Google Scholar]