NSAIDs Flashcards
What NSAID is used predominantly for pain?
Parecoxib
What is the usual action of prostaglandins?
Pro-inflammatory, pyretic, hyperalgesic, inhibit gastric acid, platelet aggregation, contract the uterus and increase renal blood flow
What is the action of aspirin?
Antipyretic, anti-inflammatory, analgesic,GI side-effects, anti-platelet effect, delays labour and can cause kidney problems
Which form of COX is elevated in joint inflammatory disorders?
COX-2
Which types of COX are present in the stomach?
COX-1 in the crypts to protect the mucosa, and small amounts of COX-2 in the superficial mucosa
What physiological molecule prevents platelet aggregation?
Prostacyclin produced by endothelial cells
What physiological molecule promotes platelet aggregation?
Thromboxane from platelets
Which type of COX enzyme is involved in nociceptive transmission?
COX-2
Where is COX-2 present in the kidney?
Macula densa, increases in numbers when there is salt deprivation
What are the complications of COX-1 inhibition?
Loss of gastric protection, ulcers and bleeding
What is the best-tolerated NSAID for those with cardiovascular problems?
Naproxen
How does aspirin work?
Rapid reversible binding followed by covalent binding (irreversible)
How does diclofenac work?
Rapid, lower-affinity, reversible binding followed by time-dependent higher affinity, slowly reversible binding of COX-1 and COX-2
How does ibuprofen work?
Rapid competitive binding of COX-1 and COX-2