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12 Cards in this Set
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- Back
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aspirin
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irreversibly inhibits cyclooxygenase by covalent binding, which decreases synthesis of both thromboxane and prostaglandins.
use: low dose (<300 mg/day): decreased platelet aggregation. intermediate dose (300-2400 mg/day): antipyretic and analgesic. high dose (2400-4000 mg/day): anti-inflammatory. toxicity: gastric upset. chronic use can lead to acute renal failure, interstitial nephritis, and upper GI bleed. Reye's syndrome in children with viral infections. |
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NSAIDs
ibuprofen, naproxen, indomethacin, ketorolac |
reversibly inhibit COX 1/2. block PG synthesis.
use: antipyretic, analgesic, anti-inflammatory. Indomethacin is used to close a PDA. toxicity: renal damage, fluid retention, aplastic anemia, GI distress, ulcers. |
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COX 2 inhibitors
celecoxib |
reversibly inhibit COX 2, found in inflammatory cells and vascular endothelium and mediates inflammation and pain; spares COX 1, which helps maintain the gastric mucosa. thus should not have the corrosive effects of other NSAIDs on the GI lining.
use: rheumatoid and osteoarthritis. toxicity: increased risk for thrombosis. sulfa allergy. less toxicity to GI mucosa (lower incidence of ulcers, bleeding than NSAIDS). |
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acetaminophen
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reversibly inhibits COX, most in CNS. inactivated peripherally.
use: antipyretic, analgesic, but lacking anti-inflammatory properities. used instead of aspirin to prevent Reye's syndroem in children with viral infection. toxicity: OD produces hepatic necrosis; acetaminephen metabolites depletes glutathione and forms toic tissue adducts in liver. N acetylcysteine is antidote - regenreates glutathione. |
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comparison of OTC analgesics
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acetaminophen = NSAID w/o anti-inflammatory activity.
aspirin = NSAID with antiplatelet activity |
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bisphosphonates
etidronate, pamidronate, alendronate, risedronate |
inhibit osteoclastic activity, reduces both formationa nd resorption of hydroxyapatite.
use: malignancy-associated hypercalcemia, Paget's disease of bone, postmenopausal osteoporsis. toxicity: corrosive esophagitis, nausea, diarrhea. |
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colchicine
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acute gout. binds and stabilizes tubulin to inhibit polymerization, impairing leukocyte chemotaxis and degranulation.
GI side effets especially if given orally. Indomethacin is less toxic, also used in acute gout. |
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probenecid
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chronic gout. inhibit reabsorption of uric acid in PCT (also inhibits secretion of penicillin)
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allopurinol
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chronic gout. inhibits xanthine oxidase, decreased conversion of xanthine to uric acid. also used in lymphoma and leukemia to prevent tumor lysis-associated urate nephropathy.
increased concentration of azathioprine and 6-MP (both normally metabolized by xanthine oxidase). |
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etanercept
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recombinant form of human TNF receptors that binds TNF.
use: RA, psoriasis, ankylosing spondylitis. toxicity: infection, hypersensitivity, injection site reaction. etanerCEPT is a TNF decoY REceptOR. |
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infliximab
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anti-TNF ab.
use: crohn's disease, RA, ankylosing spondylitis. toxicity: predisposes to infections (reactvation of latent TB). |
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adalimumab
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directly binds TNF-a receptor sites
use: Ra, psoriasis, ankylosing spondylitis |
