Glucocorticoid Antagonist

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Chapter: Essential pharmacology : Corticosteroids

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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