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13 Cards in this Set
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- Back
- 3rd side (hint)
COX-I
Indomethacin |
Potent NSAID – rapidly and completely absorbed form GI tract
Highly bound to plasma proteins, anti-inflammatory, antipyretic, analgesic Reduces polymorphonuclear leukocyte motility, development of cellular exudates and reduces vascular permeability in injured tissue |
Highly indicated in RA, acute gouty arthritis, osteoarthritis
Closure of patent ductus arteriosus |
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COX-I
Aspirin |
Non-selectively and irreversibly (acetyl group from ASA covalently binds the enzyme) inhibits both COX1/2 so inhibits prostaglandins and thromboxanes
Inhibitis granulocyte adherence to damaged vasculature and chemotaxis of polymorphonuclear leukocytes/macrophages Low dose=decreased platelet agg Intermediate dose= antipyretic and analgesic High=anti-inflamma Low dose = decreased ureic acid excretion High dose = increased ureic acid excretion Important in patient with hyperuricemia and gout since aspirin can block effects of probenecid |
Indicated:
Coronary Artery Disease MI DVT Unstable Angina S/E: Reyes Syndrome in children with viral infection Liver Dysfunction, Encephalopathy, upper GI bleeding Contraindicated in Children Careful in patients with gout/hyperuricemia |
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COX-I
Acetaminophen |
No anti inflammatory action
No antiplatelet activity, No significant GI side-effects Durg of choice for antipyresis in children Reversibly inhibits COX in CNs |
Temporary mild to moderate pain and fever reduction
S/E: Overdose=hepatic necrosis |
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COX-I
Piroxicam Meloxicam |
Long half-life permits once a day dosing
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Long term treatment of Ram osteoarthritis, acute gout
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COX-I
Ketolorac |
Potent analgesic action, moderate anti-inflammatory Alternative to opioids
Parenterna and oral formulation Strongest analgesic NSAID |
Short term treatment of moderate pain
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COX-I
Naproxene Ibuprofen |
Highly effective anti-inflammatory and analgesics
80% absorbed form GI tract |
Indication:
Gout, RA, Osteoarthritis S/E: Renal damage, Aplastic Anemia, GI distress |
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COX-I
Diclofenac |
Highly selective for COX2
Intermediate relase, delayed relase and extended release forms |
Indication:
Long term for osteoarthritis, ankylosing spondylitis Short term for acute musculoskeletal and postoperative pain |
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COX-I
Sulindac |
90% absorbed after oral administration,
Prodrug- transformed to sulfide metabolite in liver, Half-life Sulindac 7h Suflide metabolite 18h Highly potent COX inhibitor |
Indication:
Acute/long term RA, osteoarthritis, bursitis, acute gouty arthritis |
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COX-I
Diflusinal |
Releif of pain occurs through both peripheral and central mechanism
Low does irreversibly inhibits thromboxane production in platelets Half-life 8-12hrs and 4x potency of aspirin |
Effective analgesic in osteoarthritis and musculoskeletal sprains
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Hyperurecemia/Gout Drugs
Colchicine |
Binds to tubulin in mitotic spindles and arrest cell division, mobility, and release of chomotactic factors. Inhibits migration of granulocytes into inflamed area and decreases phagocytic activity, inhibits mast cell degranulaiton
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Indication:
Dramatic relief from acute attacks of gout, give in first few hrs of attack S/E: Diarrhea, nausea, vomiting and bone marrow suppression limit therapy If GI problems don’t use |
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Hyperurecemia/Gout Drugs
Allopurinol |
Competitively inhibits xanthine oxidase (catalyses last stem in uric acid formation) reducing uric acid levels Well tolerated
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Indication:
Hyperuricemia , Chronic gout S/E Avoid in acute gout attacks Cautious use in renal/hepatic impairment |
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Hyperurecemia/Gout Drugs
Probenecid |
Block proximal tubular reabsorption of uric acid
Oral twice daily combined with liberal fluid intake until uric acid level controlled |
Indication:
Chronic Gout |
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COX-2-Inhibitor
Celecoxib |
Less incidence of GI ulcers, less effect on platelets and bleeding time Half-life 11h
Very well absorbed and extensive hepatic metabolism |
Indicated:
Dysmnorrhea, osteoarthritis, RA, and post op pain Contraindicated: Contraindicated in pts with any hx of cardiovascular disease! |