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25 Cards in this Set
- Front
- Back
Aspirin MOA
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IRREVERSIBLY inhibits cyclooxygenase (1 & 2) by acetylation = DEC TXA2 and PGs
INC BT |
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Aspirin clinical use
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Low dose: DEC platelet aggregation
Int dose: antipyretic and analgesic High dose: anti-inflammatory |
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Aspirin TOX
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Gastric ulceration
Tinnitus (CN VIII) Chronic use: acute renal failure, interstital nephritis, and upper GI bleeding Reye's syndrome in children with viral illness Stimulates respiratory centers cuasing HYPERventilation and respiratory alkalosis |
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NSAIDs
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Ibuprofen (advil)
Naproxen (Aleve) Indomethacin Ketorolac Diclofenac |
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NSAIDs MOA
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REVERSIBLY inhibit Cox 1,2
Block PG synthesis |
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NSAIDs clinical use
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antipyretic, analgesic, anti-inflammatory
Indomethacin used to close PDA |
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NSAIDs TOX
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Interstital nephritis
Gastric ulcer (PGs protect against gastric mucosa) Renal ischemia (PGs vasodilate afferent arteriole) |
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COX-2 inhibitors
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Celecoxib
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Celecoxib MOA
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REVERSIBLY inhibit COX2 (found in inflammatory cells and vascular endothelium and mediates inflammation and pain)
Spares COX-1 which helps maintain gastric mucosa Spares platelet function as TXA2 prod is dep on COX1 |
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Celecoxib clinical use
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RA and osteoarthritis; patients with gastritis or ulcers
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Celecoxib TOX
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INC risk of thrombosis
Sulfa allergy |
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Acetaminophen MOA
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REVERSIBLY inhibit cyclooxygenase MOSTLY in CNS (inactivated peripherally)
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Aceaminophen clinical use
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Antipyretic, analgesic, NOT anti-inflammatory
Used instead of aspirin in children with viral infection to avoid Reye's syndrome |
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Acetaminophen TOX
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Hepatic necrosis
-metabolite depletes glutathione and forms toxic tissue adducts in liver N-acetylcysteine is anti-dote (regenerates glutathione) --also used as mucolytic in CF |
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Bisphosphonates MOA
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Pyrophosphate analogs; binds hyroxyapatite in bone inhibiting osteoclast activity
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Bisphosphonate clinical use
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Osteoporosis!
Hypercalcemia Paget's disease of bone |
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Bisphosphonate TOX
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Corrosive esophagitis (stay upright for atleast 30 min., NEVER before bedtime, NOT with other food or meds)
Osteonecrosis of jaw |
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Allopurinol
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Inhibits xanthine oxidase
DEC conversion of xanthine to uric acid Prevent tumor lysis syndrome (leuk/lymph) INC [Azathioprine] and [6-MP] ; both normally metabolized by xanthine oxidase |
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Febuxostat
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Inhibits xanthine oxidase
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Probenecid
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Inhiits reabsoprtion of uric acid in PCT
Inhibits secretion of penicillin |
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Colchicine
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Binds and stabilizes tubulin to inhibit polymerization, impairing leukocyte chemotaxis and degranulation
Low therapeutic dose GI SE |
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NSAIDs for Gout
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Naproxen, indomethacin
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TNF-a inhibitors
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Predispse to infection including reactivation of latent TV since TNF blockage prevents activation of macrophages and estruction of phagocytosed microbes
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Etanercept
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Fusion protein (receptor for TNF-a + IgG Fc), produced by recombinant DNA
TNF decoy receptor Use: RA, Psoriasis, ankylosing spondylitis |
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Infliximab, adalimumba
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Anti-TNF-a monoclonal ab
Crohn's, RA, ankylosing sponylitis, Psoriasis |