Corticosteroid antagonists Flashcards
Corticosteroid antagonists (2 groups)
Corticosteroid receptor antagonists
Corticosteroid synthesis inhibitors
Corticosteroid receptor antagonists (3 drugs)
Spironolactone
Eplerenone
Mifepristone
Spironolactone - indications
DOC: Primary hyperaldosteronism
Hirsutism
Secondary hyperaldosteronism (pt with heart failure and Bartter syndrome)
Diuresis (potassium sparing)
Spironolactone - Adverse effects
Hyperkalemia Cardiac arrhythmias Gynecomastia Menstrual abnormalities Sedation
Corticosteroid receptor antagonist used for hypertension
Eplerenone
Cushing caused by inoperable adrenal carcinoma or ectopic ACTH secretion can be treated with
Mifepristone
Corticosteroid synthesis inhibitors (4 drugs)
Ketoconazole
Fluconazole
Aminoglutethimide
Metyrapone
Antifungal drugs - MOA as corticosteroid antagonists
Ketoconazole and fluconazole inhibits steroid production by inhibiting cytochrome P450 enzymes (β-hydroxylase inhibition)
Ketoconazole and fluconazole - indications as corticosteroid antagonists
Adrenal carcinoma, hirsutism, breast and prostate cancer.
Aminoglutethimide - MOA
Inhibits synthesis of all hormonally active steroids
Corticosteroid synthesis inhibitor used for malignant steroid-producing adrenocortical cancer
Aminoglutethimide
Aminoglutethimide - interactions
Increases metabolism of dexamethasone
Metyrapone - MOA
Inhibits cortisol synthesis by selectively inh steroid 11β-hydroxylation, shifts production to adrenal androgens
Only drug that can be used in pregnant women with Cushing syndrome
Metyrapone
Metyrapone - adverse effects
Salt and water retention
Hirsutism