NSAIDs Flashcards
what do NSAIDs manage
pain and inflammation
what are eicosanoids
initiates inflammatory response - pro inflammatory
prostaglandins, thromboxanes and leukotrienes
discuss synthesis of eicosanoids
- membrane phospholipids broken by heat/disease/chemical
- cell membrane release phospholipids
- arachidonic acid created via phospholipase A2
- arachidonic acid enters 2 pathways:
- cyclooxygenase pathway: cyclic endoperoxides (prostaglandins and thromboxane
- lipoxygenase pathway: luekotrienes
discuss good prostaglandin
COX-1 pathway: normal/physiologic
renal homeostasis
gastric mucosal protection
platelet function
discuss bad prostaglandin
COX-2 pathway - inflammatory process
pain, inflammation, fever
limited homeostatic effects
discuss thromboxanes
synthesized by platelets - platelet aggregation
vasoconstriction to dec swelling and bleeding
can also cause bronchoconstriction
luekotrienes may lead to
bronchoconstriciton
allergic rhinitis
mucus production
discuss aspirin
gold standard NSAID
inhibits both good and bad prostaglandin - blocks cyclooxygenase = not allows prostaglandin and thromboxane
discuss anti-inflammatory effect of NSAIDs
interferes c prostaglandin synthesis
inhibits granulocyte adherence - clotting mechanism
stabilizes lysosomes
inhibits migration of leukocytes and macrocytes
discuss anti-pyretic effect of NSAIDs
prevents pyrogen-induced release of prostaglandins
vasodilation: dec temp d/t heat dissipation
discuss analgesic effect of NSAIDs
peripheral mechanism
mild to mod pain
discuss inhibition of platelet aggregation effect of NSAIDs
inhibits thromboxane
absorption of aspirin
small intestines and stomach - oral
peak plasma level: 1-2 hrs
protein binding: 80-90%
metabolism of aspirin
hydrolysis to acetic acid and salicylate
conjugation with glycine to form salicyluric acid
excretion of aspirin
urine alkalinization to inc rate
low dose: 1st order
- t1/2: 3-4 hrs
high doses: 0 order kinetics
- t1/2: 15 hrs
dosages of aspirin
children: 50-70 mg/kg/day
adults: 4 g/d
normal dapat liver and kidney
current move to dec to 2g/d
ASA intoxication ssx
salicysm - tinnitus, dec hearing, vertigo
hyperpnea and respi alkalosis
seizures if acidotic
management of ASA intoxication
gastric lavage
ventilatory assist
alkalize the urine
COX-2 inhib
bad prostaglandins inhibited but inflammatory process still allowed
-coxibs
indications for NSAIDs
anti-pyresis
inflammation
DVT
stroke - embolic
MI
