Glucocorticoids

Question 1

Mechanism of GC action (2)

Answer 1

1. turns off COX2 synthesis

2. turns on synthesis of product that inhibits PLA2

Question 2

The long term administration of large doses of prednisone will cause the least reduction in the synthesis of….

a. cortisol
b. ACTH
c. CRF
d. Aldosterone
e. GH

Answer 2

D. aldosterone

Question 3

GCs effects of vascular events?

Answer 3

reduced vasodilation

decreased fluid exudation

Question 4

GCs effects on cellular events?

Answer 4

decrease in accumulation / activation of inflammatory immune cells

Question 5

GCs effects on inflmmatory immune mediators

Answer 5

decrease

Question 6

GC block (immune elements?

Answer 6

T cell activation
Cytokine production
eosinophil mediator release
mast cell mediator release

Question 7

GC and 11 keto vs 11 hydroxyl?

Answer 7

11 keto can’t be topical because must be activate in liver to 11 hydroxyl

Question 8

which two glucocorticoids are 11keto

Answer 8

prednisone

cortisone

Question 9

A patient with dehydration and hyponatremia would most benefit from?

a. dexamethasone
b. prednisone
c. prenisolone
d. fludrocortisone
e. triamcinolone

Answer 9

fludrocortisone because increases MC activity

Question 10

liver GC metabolism?

Answer 10

activating converts cortisone to cortisol 11b-hsd1

Question 11

kidney GC metabolism

Answer 11

inactivating converts cortisol to cortisone 11b-hsd2

Question 12

fetus GC metabolism

Answer 12

only has 11B-HSD2 (inactivator)

Question 13

adverse effects of pharmacologic doses unlikely to be seen with dexamethasone but possible with prednisone are? (2)

Answer 13

fluid retention and
hypokalemia
because prednisone has some MC activity whereas dexamethasone has none

Question 14

hydrocortisone

GC effect? IS effect? Topical? MC? Potency? Forms?

Answer 14

hydrocortisone is basically cortisol
it’s anti-inflammatory effect is the reference - 1 GC/IS; it’s topical activity is 1; its salt retaining activity is 1; and its potency is 20;
comes in oral, injectable, and topical forms
thus must be 11ox

Question 15

cortisone relative to hydrocortisione?

Answer 15

slightly less AI (GC/IS) activity 0.8; no topical activity (11=o); slightly less MC 0.8; Potency 25eod; only oral

Question 16

prednisone relative to hydrocortisone?

Answer 16

4x AI (GC/IS)
No topical (11=O)
0.3 MC
Potency 5 eod (relative to 20)

Question 17

methylprednisone relative to hydrocortisone

Answer 17

5x AI (GC/IS)
5x topical (11-oh)
MC = 0
Potency = 4 relative to 20
oral/injectable

Question 18

triamicinolone relative to hydrocortisone

Answer 18

5X AI (GC/IS)
Topical 5^3
No MC
Potency 4 relative to 20
oral/injectable/topical

Question 19

dexmethasone

Answer 19

30x AI (GC/IS)
10x topical 
0 MC
potency 0.75 relative to 20
oral/injectable/topical

Question 20

fludrocortisone

what is it?

Answer 20

mineralocorticoid
10x AI (GC/IS)
0 topical
250 MC

Question 21

Cortisol
when used?
GC:MC?
Admin

Answer 21

physiologic doses –> replacement therapy - emergencies

GC:MC 1:1

Administered orally and parenterally

Question 22

Prednisone
when?
GC:MC
Admin?

Answer 22

Most commonly used oral agent for steroid burst therapy

GC:MC (5:1)

Activated to prednisolone in liver (no topical activity)

Question 23

Methylprednisolone
IV = 
Oral = 
use?
benefit?

Answer 23

IV = solu-medrol
Oral = medrol
for steroid burst
minimal MC action

Question 24

Dexamethasone
use?
GC:MC
Unique?

Answer 24

Most potent anti-inflammatory
use: cerebral edema; chemo nausea
minimal MC
Greatest suppression of ACTH

Question 25

Tramcinolone use? GC:MC?

Answer 25

potent systemic agent with excellent topical activity no MC action

Question 26

Wasp reaction; which corticosteroid admin would be appropriate?

Answer 26

Gradually decreasing doses over several days

Question 27

What is rationale behind alternate day schedule?

Answer 27

minimize adrenal suppression - anti-inflammatory action outlasts HPA suppression

Question 28

What is rationale behind gradual termination?

Answer 28

minimize disease rebound and potential for symptoms of adrenal insufficiency

Question 29

what is the primary clinical advantage to alternate day gc therapy?

Answer 29

minimizes gc block of acth release, which can reduce adrenal atrophy

Question 30

which two steroids we considered would not be appropriate for derm?

Answer 30

cortisone | prednisone

Question 31

adverse effects of GC use?

Answer 31

adrenal gland suppression iatrogenic cushings adverse mc effects

Question 32

adverse mc effects

Answer 32

hypertension hypokalemia metabolic alkalosis

Question 33

acute, short course, high dose mc effects

Answer 33

salt and water retention --> edema --> hypertension and hypokalemia

Question 34

acute, short course, high dose gc effects

Answer 34

glucose intolerance in diabeteics, mood changes, insomnia, gi upset

Question 35

high dose sustained therapy gc effects (4)

Answer 35

iatrogenic cushings hpa axis suppression mood disturbance impaired wound healing / increased susceptibilty to infection

Question 36

iatrogenic cushing?

Answer 36

hyperglycemia, protein wasting, lipid deposition, diabetes like state

Question 37

hpa-axis suppression -->

Answer 37

insufficient stress response more suppression with dexamethasone and betamethason may also cause decrease in acth, gh, tsh, lh, sex steroids

Question 38

osteoperosis is possible with large cumulative doses of GC, how would we treat?

Answer 38

bisphosphonates

Question 39

peptic ulcers are possible with large cumulative doses of GC, how would we minimize risk?

Answer 39

antacids

Question 40

which of the following is a pharmacologic effect of exogenous glucocorticoids? a. increased muscle mass b. hypoglycemia c. inhibition of leukotriene synthesis d. improved wound healing e. increased excretion of salt and water

Answer 40

c