The antiprogestin mifepristone acts as a glucocorticoid receptor antagonist as well. In Cushing’s syndrome, it can suppress the manifestations of corticosteroid excess, but blockade of feedback ACTH inhibition leads to oversecretion of ACTH → more hydrocortisone is produced, which tends to annul the GR blocking action of mifepristone.
GLUCOCORTICOID ANTAGONIST
The antiprogestin mifepristone acts as a glucocorticoid receptor antagonist
as well. In Cushing’s syndrome, it can suppress the manifestations of
corticosteroid excess, but blockade of feedback ACTH inhibition leads to
oversecretion of ACTH → more hydrocortisone is produced, which tends to annul
the GR blocking action of mifepristone. It is indicated only for inoperable
cases of adrenal carcinoma and in patients with ectopic ACTH secretion.
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