NSAIDS and COX inhibitors

Question 1

What is COX?

Answer 1

Cyclooxygenase (COX) is an enzyme that catalyzes the synthesis of prostaglandins from arachidonic acid

Question 2

Where is COX-1 located and what are its functions?

Answer 2

Located in gastric mucosa, platelets and renal parenchyma

Regulate GI mucosal integrity, platelet aggregation, and renal function

Question 3

What is the function of COX 2?

Answer 3

Pain inducing enzyme
mediates inflammation, pain, fever and carcinogenesis
Released in response to injury, illness and diet

Question 4

What is the MOA of NSAIDS?

Answer 4

Block both COX enzymes without specifity

Question 5

What happens when the recommended dose of NSAIDs are exceeded?

Answer 5

due to the ceiling effect it will only increase risk of toxicity

Question 6

How are NSAIDS absorbed from GI?

Answer 6

Well absorbed from GI with limited 1st pass hepatic extraction

Question 7

What is the pK of NSAIDS?

Answer 7

3-5

Question 8

What are advantages of NSAIDS?f

Answer 8

Decrease activation and sensitization of peripheral nociceptors
Attenuate inflammatory response
Absence of dependence or addiction
Synergistic with opioids
Preemptive analgesia
NO depression of ventilation
Less N/V
Long duration of action
Less variability
No pupil changes
Absence of cognitive effects

Question 9

What are disadvantages of NSAIDS?

Answer 9

Inhibition of platelet aggregation
Gastric ulceration
Renal dysfunction
Hepatocellular injury
Asthma exacerbation
Allergic reactions
Bone healing
Drug Interactions

Question 10

What are GI effects of NSAIDS

Answer 10

Dyspepsia
N/V
pain 
peptic ulcer
GI hemorrhage

Question 11

How does ASA work?

How long does it affect platelet dysfunction?

Answer 11

Irreversible acetylation of COX enzyme.

Since the life of a platelet is 7-10 days, platelet dysfunction will be affected for 7-10 days

Question 12

What are the clinical uses of ASA?

Answer 12

low intensity analgesic
1st line antipyretic
Antiplatelet function-even at low doses

Question 13

What are the side effects of ASA?

Answer 13

GI upset
prolonged bleeding and PT
Anspirin induced asthma
Others
-CNS toxicity
-minimal renal effects
-prolong labor and postpartum hemorrhage
-Rare allergic reaction
-Reyes syndrome

Question 14

What is reyes syndrome

Answer 14

Seen in some children given aspirin for viral infections.
Causes fatty liver with encephalopathy
rash, vomiting, and liver damage

Question 15

What are the clinical uses for acetominophen?

Answer 15

Analgesic
anti-pyretic
It is not an anti inflammatory
It is an alternative to aspirin for pediatric patients and those with peptic ulcers

Question 16

What is dose of IV acetominophen?

Answer 16

1000mg q 6 hours-max 4g q 24 hours

Question 17

How does acetominophen compare to ASA in gastric irritation and platelet aggregation?

Answer 17

No gastric irritation and no platelet effects, however considerable renal and hepatic toxicity

Question 18

How is toradol for analgesia and inflammation?

Answer 18

potent analgesic and minimal antiinflammatory

Question 19

What is dosage for toradol?

Answer 19

Adult: 30 mg IV/IM q 6 hours
Peds: 0.5 mg/kg IM/IV q 6
Also can be given PO

Question 20

What is indomethacin used for?

Answer 20

Used in babies to inhibit prostoglandins that keep PDA open

Question 21

What common drug is proprionic acid derivative?

Answer 21

Naproxen

Question 22

What are three NSAIDs used in the treatment of gout?

Answer 22

Phenlbutazone
colchicine
allopurinol

Question 23

HOw do saturated and unsaturated fat intake affect COX-2?

Answer 23

increases

Question 24

What disease states have increased COX-2?

Answer 24

Alzheimers
cancer
kidney disease
osteoporosis
rheumatic and osteoarthritis