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13 Cards in this Set

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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
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
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
COX-I

Piroxicam
Meloxicam
Long half-life permits once a day dosing
Long term treatment of Ram osteoarthritis, acute gout
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
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
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

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
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
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
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
Hyperurecemia/Gout Drugs

Allopurinol
Competitively inhibits xanthine oxidase (catalyses last stem in uric acid formation) reducing uric acid levels Well tolerated
Indication:
Hyperuricemia , Chronic gout

S/E
Avoid in acute gout attacks
Cautious use in renal/hepatic impairment
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

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!