NSAIDs Flashcards
COX-2 inhibitors: explain why COX-2 inhibitors have proved less successful than hoped
2 main iso-forms of COX
COX-1 and COX-2
cellular distributions of COX-1 and COX-2
different but overlapping
effect of most NSAIDs (e.g. ibuprofen) on both isoforms
reversibly inhibit
what does the coxib family (e.g. celecoxib) do
selectively reversibly inhibit COX-2
evidence that celecoxib is gastroprotective
fewer ulcerations
effect of celecoxib on CVD
increased risk than conventional NSAIDs
cardiovascular effects of COX-2 inhibitors: VSMCs and endothelial cells
platelet activation onto coronary plaques (thrombosis)
cardiovascular effects of COX-2 inhibitors: cardiomyocytes
decreased protection against arrhythmias and oxidative injury, increasing risk of heart failure
cardiovascular effects of COX-2 inhibitors: renal
decrease renal blood flow and GFR, and reduces Na+ and H2O excretion, increasing BP
what do dual COX and LOX inhibitors (reduce risk to asthma patients) injure
liver
another new NSAID which may be safer than COX-2 inhibitor
NO/H2S releasing NSAIDs (protective to GI and CVS)
COX-1 vs COX-2 affinity, and significance of ibuprofen
COX-1 selective causes increased GI risk, COX-2 causes increased CVD risk; ibuprofen reversible and in middle of affinity
