Glucocorticoid receptor antagonist
- Cortisol cannot signal
- Controls hypercortisolism symptoms (Cushing syndrome)
- Treats hyperglycemia of Cushing syndrome
- Cortisol and ACTH levels RISE on therapy — follow the clinical picture, not the labs
- Adrenal insufficiency cannot be detected by cortisol levels
- ↑ cortisol spills onto mineralocorticoid receptors → hypokalemia, hypertension
Drugs with this mechanism (1)
- Mifepristone — Progesterone/glucocorticoid antagonist; medical abortion and Cushing-syndrome hyperglycemia.
Self-check
- Should cortisol/ACTH levels guide glucocorticoid-receptor antagonist response?
No; they rise. Follow the clinical picture. - Why can hypokalemia and hypertension occur despite glucocorticoid-receptor blockade?
Increased cortisol activates mineralocorticoid receptors.
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