Pharmacologic study of the glucocorticoid activity of flunisolide compared with other steroids in the rat].

D Philibert, F Bouchoux, E Cerede, F Corallo, J M Allaire

Allergie et immunologie 1993 Feb

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Flunisolide (FLU), beclomethasone dipropionate (BDP) and its pulmonary metabolites beclomethasone monopropionate (BMP) and beclomethasone (B) were studied in rat for: their relative binding affinity (RBA) for the 5 classes of steroid receptors, their in vitro glucocorticoid activity on rat thymocytes, their in vivo glucocorticoid activity by oral route. These compounds displayed a strong RBA for rat lung, thymus and liver glucocorticoid receptors (FLU > or = BMP > BDP > or = B). They were also shown to have a moderate RBA for both mineralocorticoid and progestin receptors, while being devoid of any binding to androgen and oestrogen receptors. On rat thymocytes FLU exhibited the highest glucocorticoid activity (FLU > B > or = BMP > BDP). In rat oral FLU displayed a strong glucocorticoid activity with a slight first-pass metabolism as opposed to what has been reported in human.

Citation

D Philibert, F Bouchoux, E Cerede, F Corallo, J M Allaire. Pharmacologic study of the glucocorticoid activity of flunisolide compared with other steroids in the rat]. Allergie et immunologie. 1993 Feb;25(2):77-81