Adrenal Drugs

Question 1

Hydrocortisone, cortisone, prednisone, prednisolone, dexamethazone

Answer 1

Acts on GC-R and GCREs to regulate transcription
Effects: hyperglycemia, fat deposits, protein catabolism, immunosuppression (macrophage), anti-inflammatory: affects leukocytes and cytokines
Tx: Replacement (Addison’s) and CAH
AE: growth retardation, osteoporosis, wasting, thin skin, poor wound healing, central obesity, hyperglycemia, DM, depression, anxiety, hypomania, insomnia, glaucoma, cataracts, androgenicity (hirsutism, sweating, acne)

Question 2

Fludrocortisone

Answer 2

Acts on MC-R and MCRE to regulate transcription
Promotes sodium and water retention, and potassium wasting with protons, maintain blood volume
Tx: Replacement (Addison), CAH
AE: hypertension, hypokalemia, alkalosis

Question 3

Ketoconazole, metyrapone

Answer 3

Ketoconazole: Inhibits CYPC17, C17,20-lyase, 3beta-hydroxy-steroid dehydrogenase and CYPC11
Metyrapone: Inhibit CYPC11
Inhibits MC and GC production
Tx: Cushing
AE: Ketoconazole: GI and hepatotoxicity
AE: Metyrapone: BP and ‘lytes, androgenic, N+V, GI

Question 4

Mifepristone

Answer 4

GC-R inhibitor
Treat Cushing’s
AE: menstrual abnormalities, nausea, fatigue, hypokalemia

Question 5

Cabergoline

Answer 5

Agonist at D2-R
Suppress pituitary ACTH
Tx Cushing’s
AE: Cardiac valvuloplasty, HA, light-headedness, OH, fatigue, psychosis

Question 6

Pasireotide

Answer 6

Agonist at SST-R
Suppress pituitary ACTH
Tx Cushing’s
AE: nausea, diarrhea, hyperglycemia, bradycardia, conduction disturbances

Question 7

Spironolactone, eplerenone

Answer 7

MC-R inhibitor
Diuretic effects and fixes aldosterone excess
Tx for hyperaldosteronism
AE: Spironolactone: hyperkalemia, cardiac arrhythmia, menstrual changes, gynecomastia
AE: Eplerenone: hyperkalemia

Question 8

Phenoxybenzamine, prazosin, terazosin, doxazosin

Answer 8

Antagonist at alpha1-R, phenoxybenzamine is irreversible
Lower BP
Tx: HTN with pheochromocytoma
AE: OH, tachycardia in phenoxybenzamine

Question 9

Atenolol, metoprolol, propranolol

Answer 9

Lower HR and BP
Tx: pheochromocytoma (with alpha block)
AE: bradycardia, fatigue, cold hands

Question 10

Metyrosine

Answer 10

Inhibit tyrosine hydroxylase
Lowers BP
Tx: HTN with pheo.
AE: EPS, OH, crystalluria