Sm. Holliday et al., INHALED FLUTICASONE PROPIONATE - A REVIEW OF ITS PHARMACODYNAMIC AND PHARMACOKINETIC PROPERTIES, AND THERAPEUTIC USE IN ASTHMA, Drugs, 47(2), 1994, pp. 318-331
Fluticasone propionate is an androstane carbothioate glucocorticostero
id with almost twice the topical anti-inflammatory potency of beclomet
hasone dipropionate. Importantly, it is not appreciably absorbed from
the gastrointestinal tract. However, the fraction of active drug absor
bed from the lungs after inhalation, and therefore total systemic avai
lability has yet to be determined. Inhaled fluticasone propionate admi
nistered at dosages of 1500 mu g/day for 1 year or 2000 mu g/day for 6
weeks did not cause clinically significant pituitary-adrenal suppress
ion. Preliminary data from 2 published trials also indicate no signifi
cant effect on growth in children. However wider clinical experience i
s needed to clarify the effects of long term administration on pituita
ry-adrenal function, bone metabolism and attainment of adult height in
children. In clinical studies, inhaled fluticasone propionate was at
least as effective as beclomethasone dipropionate or budesonide when a
dministered at half the dosage of the comparators in patients with mil
d to moderate or severe asthma. Limited data suggest that fluticasone
propionate also has considerable potential in the management of childh
ood asthma. In trials of up to 1 year in duration, fluticasone propion
ate appeared to be well tolerated by both adults and children. Whether
an improved tolerability profile compared with other corticosteroids
is a major clinical benefit of the extremely low oral bioavailability
of inhaled fluticasone propionate requires confirmation. Nevertheless,
on the basis of available data from initial clinical trials of mostly
limited duration, inhaled fluticasone propionate offers an effective
treatment option for the management of asthma, with the potential of a
n enhanced safety profile.