Glucocorticoids

Question 1

Cortisol

• glucocorticoid activity
• mineralocorticoid activity
• duration

Answer 1

-1
-1
short

Question 2

Prednisone

• glucocorticoid activity
• mineralocorticoid activity
• duration

Answer 2

• 4
• 0.3
• medium

Question 3

Triamcinolone

• glucocorticoid activity
• mineralocorticoid activity
• duration

Answer 3

• 5
• 0
• intermediate

Question 4

Betamethasone

• glucocorticoid activity
• mineralocorticoid activity
• duration

Answer 4

• 25
• 0
• long-acting

Question 5

Dexamethasone

• glucocorticoid activity
• mineralocorticoid activity
• duration

Answer 5

• 30
• 0
• long-acting

Question 6

What are the cellular effects of glucocorticoids? (3)

Answer 6

1) decrease leukocyte migration (decreased integrins)
2) increase lysosomal membrane stability (decreased phagocytosis)
3) decrease capillary permeability

Question 7

What are the biochemical effects of glucocorticoids (4)

Answer 7

1) inhibit PLA2 via increased lipocortin expression > decreased PGs and LTs
2) decreased expression of COX2
3) Decreased platelet-activating factor
4) decreased interleukins (esp IL2)

Question 8

use of glucocorticoids

Answer 8

anti-inflammatory, immunosuppression

Question 9

Side effects of glucocorticoids

Answer 9

increased cortisol

Question 10

Glucocorticoid effect on pituitary

Answer 10

Suppress ACTH release > could cause a shock like syndrome if stopped abruptly

Question 11

Glucocorticoid effect on adrenal gland

Answer 11

iatrogenic cushingoid syndrome

Question 12

Glucocorticoid effect on blood sugars

Answer 12

hyperglycemia due to increased gluconeogenesis from induced PEPCK > decreased wound healing and increased infection > increased risk glaucoma and cataracts due to sorbitol build up

Question 13

Glucocorticoid effect on bone

Answer 13

Increased osteoclastic activity > osteoporosis and decreased skeletal growth in children

Question 14

Glucocorticoid effect on GI system

Answer 14

increased gastric acid and pepsin release > ulcers

Question 15

Glucocorticoid effect on kidneys

Answer 15

Increased ACTH > Increase RAAS > Na/H2O retention, edema, HTN

Question 16

Which steroids are used to treat primary adrenal insufficiency? Which is the emergency treatment?

Answer 16

Hydrocortisone, dexamethasone***, fludrocortisone

Question 17

What drug is used as the suppression test in Dx of cushing’s syndrome

Answer 17

dexamethasone

Question 18

What steroids are used for primary aldosteronism? what is their mechanism of action?

Answer 18

spironolactone and eplerenone > aldo receptor antagonists

Question 19

Aminoglutethide

• use
• mechanism

Answer 19

• treat Cushing’s

- blocks conversion of cholesterol to pregnenolone

Question 20

Ketoconazole

• use
• mechanism

Answer 20

• treat Cushing’s

- potent, nonselective inhibitor of adrnal and gonadal steroid synthesis

Question 21

Mitotane

• use
• mechanism

Answer 21

• treat Cushing’s but not really because it is DDT

- non-selective cytotoxin to adrenal cortex

Question 22

Mifopristone

• use
• mechanism
• side effects

Answer 22

• Control in Cushing’s hyperglycemia
• progesterone receptor antagonist; GR antagonist at high concentrations
• fatigue, nausea, hypokalemia, arthralgia

Question 23

Pasireotide

• use
• mechanism

Answer 23

• treat Cushing’s

- somatostatin analog, blocks release of ACTH

Question 24

Metyrapone

• use
• mechanism

Answer 24

• treat Cushing’s

- Relatively selective inhibitor of 11-hydroxylation > interferes with cortisol and corticosterone synthesis

Question 25

Which steroid is used as a mineralocorticoid replacement therapy with adrenal insufficiency

Answer 25

fludrocortisone

Question 26

How do you combat the risk of glucocorticoid induced osteoporosis

Answer 26

give Ca, Vit D, and bisphosphonates