Cm. Spencer et Lr. Wiseman, TOPICAL FLUTICASONE PROPIONATE - A REVIEW OF ITS PHARMACOLOGICAL PROPERTIES AND THERAPEUTIC USE IN THE TREATMENT OF DERMATOLOGICAL DISORDERS, Biodrugs, 7(4), 1997, pp. 318-334
Fluticasone propionate is a fluoromethyl androstane 17 beta-carbiothio
ate that is classified for dermatological use as a moderate potency co
rticosteroid. It is available in 0.05% cream and 0.005% ointment formu
lations for the treatment of patients with inflammatory dermatoses res
ponsive to corticosteroids. Although it demonstrates greater activity
than other corticosteroids of similar potency in vasoconstrictor assay
s in humans, fluticasone propionate demonstrates low potential to caus
e significant systemic effects such as suppression of the hypothalamop
ituitary-adrenal (HPA) axis. This is because it has a high affinity So
r the glucocorticoid receptor and high lipophilicity, and the small am
ount of drug that is absorbed is rapidly metabolised to the inactive c
arboxylic acid derivative in the liver (i.e. it has low systemic bioav
ailability). In clinical trials, the efficacy of fluticasone propionat
e cream at 4 weeks did not differ significantly from that of hydrocort
isone butyrate 0.1% cream in patients with moderate to severe atopic d
ermatitis and betamethasone valerate 0.1% cream in patients with moder
ate to severe psoriasis. Likewise, after 4 weeks, the ointment form of
fluticasone propionate had similar efficacy to betamethasone dipropio
nate 0.05% in patients with psoriasis or atopic dermatitis, although t
he latter agent may have a faster onset of activity in patients with a
topic dermatitis. Fluticasone propionate ointment was generally more e
ffective than hydrocortisone butyrate ointment in patients with psoria
sis. A sustained response was usually observed after about I week's ap
plication of fluticasone propionate, and although once and twice daily
administration had similar efficacy, a twice daily regimen may have a
slightly faster onset of effect In trials which included both adults
and children, the only adverse events reported were local cutaneous re
actions (most frequently, pruritus). Thus, fluticasone propionate, wit
h its low potential for systemic toxicity and possible advantage of on
ce daily administration is a useful addition to the topical corticoste
roids available for the treatment of psoriasis and atopic dermatitis.