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318 CH. 70
NSAIDs and Tylenol Cyclooxygenase inhibitors
| Question | Answer |
|---|---|
| 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) |
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