Plasma concentrations of fluticasone propionate and budesonide following inhalation: effect of induced bronchoconstriction

Article date: October 2007

By: Kevin J. Mortimer, Anne E. Tattersfield, Yufei Tang, Kai Wu, Sarah Lewis, Gunther Hochhaus, Tim W. Harrison, in Volume 64, Issue 4, pages 439-444

What is already known about this subject

Aims

To determine whether and to what extent bronchoconstriction affects plasma concentrations of fluticasone and budesonide following inhalation.

Methods

Twenty people with mild asthma inhaled 1000 µg fluticasone (Accuhaler®) plus 800 µg budesonide (Turbohaler®) on two visits. On one occasion, prior to drug inhalation, FEV1 was decreased by at least 25% using inhaled methacholine. Plasma drug concentrations were measured for each drug over 5 h and area under the plasma concentration‐time curve (AUC(0,5 h)) compared between visits.

Results

The mean difference in FEV1 prior to drug inhalation on the 2 days was 33%. AUC(0,5 h) values for fluticasone and budesonide were lower by a median of 60% (IQR 36–75) and 29% (IQR 2–44), respectively, when administered following bronchoconstriction; the reduction was greater for fluticasone than for budesonide, P = 0.007.

Conclusions

The lower plasma concentrations of fluticasone and, to a lesser extent, budesonide seen when the drugs were inhaled following induced bronchoconstriction, is likely to reflect variations that will occur with fluctuations in airway caliber in asthma.

DOI: 10.1111/j.1365-2125.2007.02856.x

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