NSAIDs and Tylenol Cyclooxygenase inhibitors
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| What is cyclooxygenase? | the enzyme responsible for synthesis of prostanoids (prostaglandins and related compounds)
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| what are cyclooxygenase inhibitors (NSAIDs/Tylenol) used for? | suppression of inflammation (not tylenol). Pain relief, fever reduction
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| general side effects of cyclooxygenase inhibitors: | GASTRIC ULCERATION/BLEEDING, renal impairment
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| What are the 4 NSAIDs? | Aspirin, ibuprofen, celebrex, naproxen
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| what are the beneficial effects of inhibiting COX-1? | protection against MI and stroke. (secondary to reduction of platelet aggregation)
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| what are the harmful effects of COX-1? | gastric erosion and ulceration, bleeding tendencies, renal impairment.
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| what are the beneficial effects of inhibiting COX-2? | suppression of inflammation, alleviation of pain, reduction of fever, protect against colorectal cancer.
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| what are the harmful effects of inhibiting COX-2? | renal impairment, promotion of MI and stroke (Secondary to suppressing vasodilation
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| 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!
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| what are the first generation NSAIDs used for? | arthritis (osteo- and rheumatoid, alleviation of mild-moderate pain, suppression of fever, relieve dysmenorrhea
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| what are the adverse effects of First generation NSAIDs? | gastric ulceration, bleeding, GI upset
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| what is acetylsalicylic acid (ASA) | aspirin
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| what is the mechanism of action of Aspirin? | NONSELECTIVE inhibition of COX (1&2)
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| what is aspirin used for? | mild-moderate pain, fever, protect against thrombotic disorders, inflammation,suppression of platelet aggregation , dysmenorrhea, cancer prevention (colorectal)
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| who can NOT use aspirin? | children - Reye's Syndrome, pt with peptic ulcer disease, bleeding disorders, hypersensitivity to aspirin, pregnancy
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| what are the adverse effects of Aspirin? | GI distress/BLEEDING, n/heartburn, bleeding, Salicysm, Reye's Children
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| 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)
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| what are the s/s of Reye's syndrome? | encephalopathy and fatty liver degeneration
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| what is Reye's syndrome linked to? | aspirin and children with chickenpox/influenzae
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| 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
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| 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]
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| what are the lethal doses of Aspirin (child vs adult) | child (4g), adult (20-25 g)
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| 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
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| 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.)
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| what is the major difference between Aspirin and non-aspirin NSAIDS (mechanism of action)? | Aspirin is IRREVERSIBLE and NSAIDs are REVERSIBLE inhibition of COX
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| which NSAID is superior in treating Dysmenorrhea? | Ibuprofen
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| what is the different side effect that RARELY ibuprofen pts get? | steven-johnson syndrome.
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| which of the first generation NSAIDs is SELECTIVE for COX-1? | Naproxen
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| what is naproxen approved for? | arthritis, bursitis, tendinitis, dysmenorrhea, fever, mild-moderate pain.
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| 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
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| administration route of Ketorolac (Toradol) | Oral, IM, IV
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| 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
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| which of the NSAIDs have all the contraindications? | Ketorolac (Toradol)
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| What is the Second generation NSAID that is left? | Celecoxib [Celebrex]
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| what is the mechanism of action for Celecoxib [Celebrex]? | SELECTIVE inhibition of COX-2
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| administration route of Celecoxib [Celebrex] | oral
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| what is the HUGE risk with second generation NSAIDS (Celecoxib) | HUGE increase risk for MI/Stroke [black box label]
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| what is Celecoxib [Celebrex] used for? | arthritis [osteo- and rheumatoid], ankylosing spondylitis, dysmenorrhea, acute pain
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| what are the side effects of Celecoxib [Celebrex] | dyspepsia, abdominal pain, INCREASE RISK MI/STROKE, renal impairment, gastric bleeding,/ulcer, sulfamide allergy exacerbation
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| pregnancy and Celecoxib? | NO
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| what drugs interact with Celecoxib [Celebrex]? | Warfarin (BLEEDING RISK), Lasix/ACE (decrease diuretic effects)
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| what is distinct about Acetominophen [Tylenol] compared to NSAIDs? | NO INFLAMMATORY effects!
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| 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.
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| s/s liver failure: | jaundice, n/v/abdominal pain
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| what is the antidote for acetominophen [Tylenol] | acetylcystine [Mucomyst
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| what should you avoid if on Acetominophen? | anything that will further damage the liver (Alcohol)
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