Module 3: COX-2 Inhibitors

Question 1

What is COX-1 described as?

Answer 1

A ‘housekeeping’ enzyme regulating normal cellular processes

Question 2

Where is COX-1 expressed?

Answer 2

In most tissues, but variably

Question 3

What is COX-2’s constitutive expression found in?

Answer 3

Brain, kidney, bone, and probably female reproductive system

Question 4

Fill in the blank: COX-1 is stimulated by _______.

Answer 4

hormones or growth factors

Question 5

True or False: COX-2 is not expressed in the brain.

Answer 5

False

COX-2 is constitutively expressed in the brain.

Question 6

What is COX-1 involved in?

Answer 6

COX-1 is involved in gastric cytoprotection, vascular homeostasis, platelet aggregation, and kidney function.

Question 7

COX-2 is stimulated by?

Answer 7

COX-2 expression increases during inflammation or in response to mitogenic stimuli.

Question 8

What is the therapeutic effect of COX-2 inhibitors?

Answer 8

Similar overall efficacy as analgesic, antiinflammatory, and antipyretic with reduced risk of gastroduodenal toxicity.

Question 9

What are pharmacokinetic considerations for COX-2 inhibitors?

Answer 9

A: GI tract

D: Plasma Albumin

M: Liver - P%) (CYP) 2C9 isoenzyme

E: Kidneys/feces - small amount

Onset: within 60 mins

Peak: approx 3 hours

Duration: 8-12 hours