NSAIDs & DMARDs Flashcards
NSAIDs act through _
inhibition of prostoglandins
cyclo-oxygenases (COX1/COX2)
synthesize prostoglandins and thromboxanes
prostoglandin effects
pain by lowering threshold of pain receptors, fever, inflammation
glucorticoids
induce lipocortin that inhibits PLA2 for broad anti-inflammatory response
COX1
constitutive activation; production of platelet clotting factors, parturition, stomach mucosa, ion excretion
COX2
activated by inflammatory stimulus and mostly transcribed in macrophages; causes inflammation, swelling, pain, redness
COX1 for _
prevention of cardiovascular events
COX2 for _
anti-inflammatory/analgesic reasons
NSAIDs three therapeutic actions
fever, pain, inflammation
acetaminophen lacks _
anti-inflammatory effects
analgesic action of NSAIDs
PGE2 sensitizes nerve endings to action of bradykinin, histamine, and other chemical mediators released by inflammatory process –> by decreasing PGE2, pain is decreased
ketorolac
can be used in severe pain for short duration
dose-dependent effects of salicylates
lower dose has an analgesic effect while higher dose has an anti-inflammatory effect
antipyretic (fever) action of NSAIDs
cytokines (mainly IL-1) stimulate hypothalamus to release PGE2 which leads to an increase in body temp –> decreasing PGE2 will inhibit this
low dose aspirin
selectively inhibits COX1 which reduces the production of TXA2 to prevent vasoconstriction and platelet aggregation
salicylic acid
topically to treat acne, corns, calluses, warts
methyl salicylate
used externally as a cutaneous counterirritant
diclofenac
topical treatment of osteoarthritis