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Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

Terms in this set (40)

What was the first NON-SALICYLATE to be available OTC?
Ibuprofen
NSAIDs are primarily used to treat:
MSK disorders
Also
Pain
Inflammation
Fever
Primary mechanism of action of NSAIDs is?
In the periphery via blocking transmission or perception. They serve to inhibit the biosynthesis of prostaglandins by blocking COX 1 (Nonselective (both)constitutional and always on; cytoprotective) and COX2 (Selective, inducible and on when turned on; inflammatory).
Structural differences between cox 1 and cox 2
Cox 1: just a hydrophobic channel

Cox 2: hydrophilic side pocket

Depends on both structure and affinity.
Know the specific highlighted in the categories.
Why have most of the selective COX2 inhibitors been discontinued?
Because of serious cardiovascular toxicity. Celecoxib is the only one available
How do NSAIDs act as an analgesic?
By reducing prostaglandin levels. Reduce of headach is due to prostaglandin-mediated vasodilation.
How do NSAIDs act as anti inflammatory?
Decrease in vasodilator prostaglandins (PGE2, PGI2)=less vasodilation=less edenma.

Inhibition of adhesion molecules
How are NSAIDs antipyretic?
Decrease in prostaglandin (PGE2) elevate the hypothalamic set-point associated in autonomic responses. Alters temperature control.
Why NSAID vs Opioid?
No respiratory depression, and induce cooling mech for reducing fever
Why NOT NSAIDs vs opioid?
NO EFFECT on the perception o f pain.
GI Adverse Effects of NSAIDS?
Nausea and vomiting
GI ulceration. H+ secretion and mucus production. Back diffusion--> acid gets back diffused in to mucus of epithelial lining.


MUST *******HAVE COX1 blockage, COX2 blockage AND epithelial damage to have GI injury.
Anti-coagulant effect of NSAID:
Inhibits the synthesis of TxA2.

COX2 inhibits platelet aggregation through prostacyclin
Renal injury in NSAIDs:
Inhibition of PGI2 (renal homeostatic mechanisms and stimulation of renin angiotensin system for K secretion)

Inhibition of PGE2 (regulates sodium and water retention, higher BP)

===Peripheral edema and increased BP
Adverse pregnancy effects of NSAIDs:
PGE2 and PGF2alpha

The COX inhibitors inhibit arachidonic acid-->PGF2alpha.
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