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14 Cards in this Set

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What is the mechanism of action for NSAIDs?
Inhibit cyclooxygenase (COX) activity to decrease the production of prostaglandins and thromboxanes.
What exactly does COX do?
One of three enzymes (CYP and LOX) that act on Arachidonic acid. COX will convert Arachidonic acid to Prostaglandins and Thromboxanes
COX-1 isoform constitutive where?
Present in most tissues, it affects blood vessels, stomach, kidneys, and platelets
COX-2 isoform constitutive where?
Present in Brain, Lung, GI, Kidneys.
Cox-2 is induced how?
Induced in inflammation/injury by cytokines and other mediators
What are the pharmacological actions of NSAIDs? x9
1. Anti-inflammatory
2. Anti-pyretic
3. Anti-thrombotic
4. Analgesia
5. Ductus Arteriosus closure
6. Dysmenorrhea
7. Colorectal CA protection
8. Alzheimer's retard
9. Tocolytic
What are the two major side effects of NSAIDs?
GI and renal
How are NSAIDs side effects of the GI caused?
NSAIDs inhibit production of PGs (which protect GI) causing acidic environment, leading to ulcers, dyspepsia, diarrhea, etc.
Can GI side effects with NSAIDs be prevented with H2 antagonists or antacids?
No
What can prevent NSAID damage of he GI?
Misoprostol
How are NSAIDs side effects of the renal caused?
NSAIDs inhibit production of PG that maintain renal blood flow, leading to nephritis and renal necrosis.
In compromised patients, NSAIDs can lead to what?
Acute renal failure
Describe absorption, metabolism, and excretion of NSAIDs.
Rapid, complete absorption
Highly protein bound
Mostly metabolized by CYP450 (hepatic)
Renal excretion
Describe effects of Aspirin on COX
Irreversibly inhibits COX-1 and COX-2