NSAIDs Flashcards
3 Categories of NSAIDs
Salicylates (Aspirin), Traditional, COX-2 Specific
General Mechanism
NSAIDs competitively inhibit COX enzymes from converting arachidoic acid to PGs (Aspirin irreversible, Necolexin only to COX-2) in order to prevent the prostaglandins and thromboxane in order to stop pain, fever and inflammation from happening.
NSAID Purpose
Pain Relief
Fever Reduction
Reduce Inflammation
Aspirin Purpose
Moderate pain of muscle, joints, headache, dental
Inflammatory diseases like arthritis
Small doses prevent stroke/MI
Pain, Fever, Inflammation
Aspirin Mechanism
Aspirin acetylates the active binding pocket of COX-1 and COX-2 and therefore stopping prostaglnadin formation.
Inhibition of COX-2 is less potent
Aspirin Specific Toxicity
Reye’s Syndrome- Aspirin to a child or adolecent with a fever from a febrile virus can kill them due to encephalitis
Acute Gouty Attack- By preventing the elimination of uric acid in the kidneys
Aspirin and CVD
81 mg/day can act as primary or secondayr prevention of MI/Stroke or treat an occlusive stroke by acetylating COX-1 in platelets to permanently shut down TXA2 formation while maintaining endothelial COX-1 production of PGI2 –> this creates an anti-thrombotic state
Other Salicylates
Less Potent/Less risky NSAIDs than aspirin and better for patients with GI symptoms or bleeding problems
IND- pain, fever or inflammation
Toxicity = salicylate intox and can lead to respiratory depression and death
Traditional NSAIDs
Ibuprofen, naproxen, oxaproxin. indomethacin, diclofenac, keterolac
T-NSAID MEchanisms
Competitively inhibit both COX-1 and COX-2 to stop inflammation, pain and fever
T-NSAID Indications
Moderate pain, arthritis, fever
Ibuprofen
Rapid onset and good for ACUTE pain
Naproxen
Rapid onset and long half life (14 hrs)
Oxaproxin
Long half life (once a day)
Indomethacin
Potent anti-inflammatory
Treat Patent Ductus Arteriosis
