Adrenal corticosteroid pharm

Question 1

What is the MOA of Aminoglutethimide?

Answer 1

Blocks the conversion of cholesterol to pregnenolone

Use for adrenocortical cancer

Question 2

MOA of Spironolactone? Use?

Answer 2

Aldosterone receptor antagonist, also androgen receptor antagonist
Used for primary hyperaldosteronism (and as a diuretic)

Question 3

MOA of Eplerenone? Use?

Answer 3

Competitive antagonist of aldosterone at mineralocorticoid receptors
Used as a diuretic for HTN, HF

Question 4

MOA of mifepristone? Clinical use?

Answer 4

Glucocorticoid and progesterone receptor antagonist

Used for hypercortisolism and medical abortion

Question 5

MOA of metyrapone? Use?

Answer 5

Inhibition of steroid-11 hydroxylation–> surpasses cortisol and corticosteroid formation
Use for Cushing syndrome

Question 6

MOA of fludrocortisone? Use?

Answer 6

Synthetic aldosterone analog–> acts as mineralocorticoid replacement for adrenal insufficiency (addison, 21-hydroxylase wi/salt wasting)

Question 7

MOA of Ketoconazole? What is it used for?

Answer 7

CYP450 inhibition–> prevents synthesis of adrenal and sex hormones. Used for Cushing syndrome

Question 8

What influences the effects of CBG (transcortin)?

Answer 8

High during pregnancy, and hyperthyroid

Low in liver disease (cirrhosis)

Question 9

What electrolyte abnormalities can spironolactone and eplerenone cause?

Answer 9

Hyperkalemia

Question 10

If 11B-HSD is inactivated, what will happen?

Answer 10

Apparent mineralocorticoid excess–> HTN, excessive cortisol activation at MR–> HTN, edema

Question 11

What are the steroid synthesis inhibitors?

Answer 11

-Aminoglutethimide
– Ketoconazole
– Metyrapone
-Mitotane