Anti-Inflammatories I NSAIDs + Acetaminophen Flashcards
General NSAID mechanism
inhibit COX: decrease PG + Tx synthesis. change gene expression: inhibit NFkB. inhibit leukocyte function/adhesion. increase endogenous cannabinoids, serotonin, NE analgesia
General NSAID therapies
pain: moderate, menstrual cramps, inflammation, smooth muscle contraction by COX metabolites. fever due to tissue damage, inflammation, disease. inflammation: AS, OA, RA. close ductus arteriosus. aspirin: prophylactic for thromoembolism, colon cancer
General NSAID adverse effects
gastric/intestinal irritation common. gastric/duodenal ulcers. overcome this with proton pump inhibitor, selective COX2 block. increased bleeding time, prolonged gestation, renal injury/failure
Salicylates (aspirin)
covalently acetylates Ser in active site of COX. COX1- prevents arachidonic acid binding. COX2- binds, but PGs not produced. irreversible. treat fever pain inflammation thrombotic events. additional adverse: CNS, tinnitus, Reye’s syndrome, asthma, poisoning - metabolic acidosis
Propionic Acid Derivatives (ibuproFEN)
reversibly inhibits COX. treat fever, pain, inflammation RA OA AS. better tolerated than aspirin. not for preg/breast feed. additional adverse: rash, tinnitus, peripheral edema
Acetic Acid Derivatives (-acin, -ac)
reversibly inhibit COX, inhibit neutrophil migration. treat inflammation more than pain/fever. additional adverse: severe headache. indomethacin- severe CNS. etodolac/ketorolac- perioperative pain
Selective COX2 Inhibitors (-coxib)
selectively inhibit COX2. treat OA RA, acute pain. decreased GI/platelet effects. not for 3rd trimester preg. additional adverse: CV events, skin reaction- toxic epidermal necrolysis
Acetaminophen (para-aminophenol derivative)
inhibit COX, weakly in presence of peroxides. treat pain (as effective as aspirin), fever. adverse: rash, allergic reaction, hepatic necrosis. chronic use- renal failure. no anti-inflammation, GI upset, platelet effect or bleeding time change
