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318 CH. 70

NSAIDs and Tylenol Cyclooxygenase inhibitors

What is cyclooxygenase? the enzyme responsible for synthesis of prostanoids (prostaglandins and related compounds)
what are cyclooxygenase inhibitors (NSAIDs/Tylenol) used for? suppression of inflammation (not tylenol). Pain relief, fever reduction
general side effects of cyclooxygenase inhibitors: GASTRIC ULCERATION/BLEEDING, renal impairment
What are the 4 NSAIDs? Aspirin, ibuprofen, celebrex, naproxen
what are the beneficial effects of inhibiting COX-1? protection against MI and stroke. (secondary to reduction of platelet aggregation)
what are the harmful effects of COX-1? gastric erosion and ulceration, bleeding tendencies, renal impairment.
what are the beneficial effects of inhibiting COX-2? suppression of inflammation, alleviation of pain, reduction of fever, protect against colorectal cancer.
what are the harmful effects of inhibiting COX-2? renal impairment, promotion of MI and stroke (Secondary to suppressing vasodilation
What are the first generation NSAIDs? which of the cyclooxygenase enzymes do they inhibit? the First generation NSAIDs are Aspirin, ibuprofen, Naproxen and Ketorolac (Toradol) They block BOTH COX-1 and COX-2!
what are the first generation NSAIDs used for? arthritis (osteo- and rheumatoid, alleviation of mild-moderate pain, suppression of fever, relieve dysmenorrhea
what are the adverse effects of First generation NSAIDs? gastric ulceration, bleeding, GI upset
what is acetylsalicylic acid (ASA) aspirin
what is the mechanism of action of Aspirin? NONSELECTIVE inhibition of COX (1&2)
what is aspirin used for? mild-moderate pain, fever, protect against thrombotic disorders, inflammation,suppression of platelet aggregation , dysmenorrhea, cancer prevention (colorectal)
who can NOT use aspirin? children - Reye's Syndrome, pt with peptic ulcer disease, bleeding disorders, hypersensitivity to aspirin, pregnancy
what are the adverse effects of Aspirin? GI distress/BLEEDING, n/heartburn, bleeding, Salicysm, Reye's Children
what are the s/s of Salicysm? what do you do if these s/s appear? tinnitus, sweating, headache, dizziness (withhold medication until s/s subside)
what are the s/s of Reye's syndrome? encephalopathy and fatty liver degeneration
what is Reye's syndrome linked to? aspirin and children with chickenpox/influenzae
what is a pregnant pt at risk for if taking aspirin? anemia dn postpartum hemorrhage. it also crosses placentae and can cause premature closure of ductus arteriosus
there are 5 drugs that interact with Aspirin, what are they? other blood thinners (Coumadin/heparin). Alcohol [increases GI bleed risk]. Ibuprofen [Reduce platelet effects of aspirin], ACE/ARBs [renal impairment], glucocorticoids [increase risk for Gastrick ulceration]
what are the lethal doses of Aspirin (child vs adult) child (4g), adult (20-25 g)
what are the s/s of acute poisoning of aspirin? initially, there is a compensated state of respiratory alkalosis. other s/s = acidosis, hyperthermia, sweating, dehydration, electrolyte imbalance, stupor and coma
what is the treatment for acute poisoning with Aspirin? acute medical emergency. IMMEDIATE THREATS TO LIFE = respiratory depression, hyperthermia, dehydration and acidosis. Treatment is SUPPORTIVE (mechanical vent if respirations are inadequate, external cooling, IV fluids for dehydration.)
what is the major difference between Aspirin and non-aspirin NSAIDS (mechanism of action)? Aspirin is IRREVERSIBLE and NSAIDs are REVERSIBLE inhibition of COX
which NSAID is superior in treating Dysmenorrhea? Ibuprofen
what is the different side effect that RARELY ibuprofen pts get? steven-johnson syndrome.
which of the first generation NSAIDs is SELECTIVE for COX-1? Naproxen
what is naproxen approved for? arthritis, bursitis, tendinitis, dysmenorrhea, fever, mild-moderate pain.
what are the adverse effects of Naproxen? GI disturbances, compromise renal function, may increase MI/stroke risk, can prolong bleeding time secondary to reversible inhibition of platelet aggregation
administration route of Ketorolac (Toradol) Oral, IM, IV
contraindicatinos of Ketorolac (Toradol) concurrent use with other NSAIDs, Peptic ulcer disease, Recent GI bleed, advanced renal impairment, confirmed or suspected intracranial bleeding, prior to major surgery, history of NSAID hypersensitivity, labor/delivery
which of the NSAIDs have all the contraindications? Ketorolac (Toradol)
What is the Second generation NSAID that is left? Celecoxib [Celebrex]
what is the mechanism of action for Celecoxib [Celebrex]? SELECTIVE inhibition of COX-2
administration route of Celecoxib [Celebrex] oral
what is the HUGE risk with second generation NSAIDS (Celecoxib) HUGE increase risk for MI/Stroke [black box label]
what is Celecoxib [Celebrex] used for? arthritis [osteo- and rheumatoid], ankylosing spondylitis, dysmenorrhea, acute pain
what are the side effects of Celecoxib [Celebrex] dyspepsia, abdominal pain, INCREASE RISK MI/STROKE, renal impairment, gastric bleeding,/ulcer, sulfamide allergy exacerbation
pregnancy and Celecoxib? NO
what drugs interact with Celecoxib [Celebrex]? Warfarin (BLEEDING RISK), Lasix/ACE (decrease diuretic effects)
what is distinct about Acetominophen [Tylenol] compared to NSAIDs? NO INFLAMMATORY effects!
what are the side effects of acetominophen? Well tolerated at low, regular doses. [4g/day = MAX] (pts with renal failure should not have more than 2g/day). There is a risk for hepatotoxicity if too much is taken.
s/s liver failure: jaundice, n/v/abdominal pain
what is the antidote for acetominophen [Tylenol] acetylcystine [Mucomyst
what should you avoid if on Acetominophen? anything that will further damage the liver (Alcohol)
Created by: 1398660434



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