NSAIDs

Question 1

NSAIDs

Answer 1

ASPIRIN
Anti-inflammatory
Analgesic
Anti-pyretic

Question 2

Mediators of Acute Inflammation

Answer 2

Histamine
Bradykinin
PGs
Leukotrienes

Question 3

Mediators of Chronic Inflammation

Answer 3

*IL-1- MO + lymph activation
*TNFa- induction, PGs
*IL-6- induction, differentiation, fever
IL-2- induction, differentation
IFNs- activation of cytotoxic lymphocytes, antimicrobial
Chemokines

Question 4

Aspirin (NSAID) MOA

Answer 4

=NON selective, IRReversible COX Inhibitor, prevent metabolism of arachidonic acid to PGs and Thromboxanes.

Question 5

Aspirin Use

Answer 5

Analgesia, Antipyretic, Anti-inflammatory- musculoskeletal disorders.
Other- anti-thrombotic (angina, ischemic attacks)

Question 6

Aspirin Adverse Rxn

Answer 6

GI upset and bleeding (erosive) 
Tinnitus, decr hearing 
Vertigo 
Ince uric acid 
Anti-platelet 
REYES SYND (post viral + aspirin = swelling of liver and brain)

Question 7

Aspirin Pharm

Answer 7

rapid absorbed
in synovial fluid
CYP 450
renal excretion

Question 8

Acetaminophen Pharm

Answer 8

rapid absorption
uniform distribution
hepatic microsomal metabolism
complete excretion

Question 9

Acetaminophen MOA

Answer 9

= NSAID, weak COX inhibitor

anti-pyretic!

Question 10

Acetaminophen Use

Answer 10

FEVER 
\+ good for pts who can't take aspirin 
-ok for peptic ulcers 
-ok for pregnancy 
-no effect on platelets

Question 11

Acetaminophen Adverse Rxn

Answer 11

skin rash (allergy) 
HEPATOTOXICITY  via oxidative stress

Question 12

Acetaminophen OD

Answer 12

common
Supportive therapy
1. gastric lavage
2. N-acetylcysteine to replenish hepatic glutathione)

Question 13

List of common NSAIDs

Answer 13

Ibuprofen - good
Diclofenac - good
Naproxen- 14hr 1/2 life
Piroxicam - 57hr 1/2 life + anti inflamm
Indomethacin – more toxic + anti inflamm
Flurbiprofen- ocular/oral + anti inflamm
Ketorolac - post surgery pain

Question 14

COX1

Answer 14

• Expressed in most tissues
• Constitutively active
• Necessary for cytoprotection in GI tract

Question 15

COX2

Answer 15

• Produces prostanoid mediators of inflammation
• Induced in inflammatory cells
• Component of the pain response

Question 16

COX-2 Inhibitors

Answer 16

Celecoxib (Celebrex) 
more SELECTIVE for COX2 
short half life ~1hr 
(+) fewer GI rxn 
(+) low platelet effect

Question 17

Celecoxib Adverse Rxn

Answer 17

CARDIO- MI, htn, edema
CNS- headache, fever
GI- diarrhea, nausea
RESP- URI, cough