Anti-Inflammatories

Question 1

How does exogenous glucocorticoid administration impact the HPA axis?

Answer 1

inhibits release of CRH (hypothalamus) & ACTH (anterior pituitary)

long term exogenous admin = atrophy of adrenal cortex & decreased ability to manufacture endogenous cortisol

Question 2

List systemic effects of glucocorticoids

Answer 2

• carb, fat, protein metabolism
• maintenance of vascular integrity
• decreased inflammation
• maintain neuronal excitability
• can have mineralocorticoid effects (H2O/Na+/K+ impact)

Question 3

List some exogenous corticosteroids

Answer 3

prednisolone
prednisone
methylprednisolone
dexamethasone

Question 4

At the cellular level, how do glucocortioids work?

Answer 4

Diffuse into phospholipid bilayer. Bind receptors and then diffuse into nucleus. Bind DNA & result in alteration in mRNA transcription –> change in protein synthesis

Question 5

Do glucocorticoids or COX inhibitors have a greater impact on the immune system?

Answer 5

glucocorticoids

(inhibits via multiple pathways)

Question 6

Are adverse effects of glucocorticoids expected at pharmacologic doses?

Answer 6

yes

Question 7

are adverse effects of glucocorticoids expected at physiologic doses?

Answer 7

no

Question 8

List some adverse effects of high dose glucocorticoids

Answer 8

infection risk
adrenal insufficiency
osteoporosis
hyperglycemia
growth delay (children)
fluid/electrolyte disturbances
peptic ulcer disease
psych disturbances

Question 9

How to avoid hypotension after glucocorticoid drug discontinuation?

Answer 9

taper drug dose

Question 10

Why is stress dosing required for surgery/trauma/illness when a patient is on chronic glucocorticoids?

Answer 10

adrenal cortex has atrophied and cannot manufacture the necessary extra glucocorticoid secretion

Question 11

What does histamine do?

Answer 11

• vasodilation & increased cap permeability = swelling, redness
• hypotension/reflex tachycardia
• bronchoconstriction
• itching, pain
• CNS: cognition, memory, sleep/wake

Question 12

Where are histamine receptors located?

Answer 12

all tissues, but high concentrations in skin, lungs, GI tract

Question 13

What is the difference between the first and second generation H1 receptor antagonists?

Answer 13

1st generation can cross BBB = sedation
2nd generation cannot = no CNS effects

Question 14

List some first generation H1 receptor antagonists

Answer 14

diphenhydramine (Benadryl)
promethazine (Phenergan)
dimenhydrinate

Question 15

List some second generation H1 receptor antagonists

Answer 15

Fexofenadine (Allegra)
Certirizine (Zyrtec)
Loratadine (Claritin)
Desloratadine (Clarinex)

Question 16

Adverse effects of H1 receptor antagonists

Answer 16

• sedation (1st gen)
• dizziness, fatigue, confusion
• N/V, loss of appetite, constipation
• anticholinergic effects (some)
• resp depression (young/old patients)

Question 17

Main THERAPEUTIC effects of COX inhibitors

Answer 17

decreased inflammation
decreased pain
decreased fever

Question 18

Adverse effects of COX inhibitors

Answer 18

• increased gastric acid secretion
• decreased platelet aggregation
• decreased vasodilation (esp of renal artery!)

Question 19

How is acetaminophen different than other COX inhibitors?

Answer 19

centrally acting - only decreases pain & fever

doesn’t impact inflammation or have any of the side effects of the others

Question 20

What is the major risk with acetaminophen toxicity?

Answer 20

liver failure

Question 21

What is the antidote for acetaminophen overdose?

Answer 21

acetylcysteine