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