L35- Steroid Pharmacology (corticosteroid antagonists) Flashcards
list the corticosteroid antagonists
Gluco: Mifepristone
Mineralo: Spironolactone
Spironolactone MOA
competes with aldosterone for renal receptors
Spironolactone uses
- aldosteronism (Dx, Tx)
- diuretic
- hirsutism in women –> androgen antagonist
Spironolactone AEs
- hyperkalemia
- cardiac arrhythmia
- menstrual abnormalities
- gynecomastia
- sedation
- HAs
- GI issues
- skin rashes
Mifepristone MOA
antagonist at glucocorticoid receptors and progesterone receptors
Mifepristone uses
inoperable ectopic ACTH syndrome or adrenal carcinoma
list the steroid synthesis inhibitors
- ketoconazole
- aminoglutethimide
- metyrapone
Aminoglutethimide:
- (1) MOA
- (2) uses
1- blocks cholesterol to pregnenolone –> reduces synthesis of all steroid hormones
2- adrenal cancer adjunct with hydrocortisone / dexamethasone
Ketoconazole:
- (1) MOA
- (2) uses
1- potent non-selective inhibitor of adrenal and gonadal steroid synthesis
2- Cushing’s syndrome, Prostate cancer
Metyrapone MOA
selective inhibitor of steroid 11 hydroylation –> interferes with cortisol and corticosterone (–> aldosterone) synthesis
Metyrapone uses
tests adrenal function
Cushing’s syndrome in pregnancy
Metyrapone AEs
- salt / water wasting
- hirsutism
- transient disease
- GI disturbances