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49 Cards in this Set
- Front
- Back
salicylates
prototype drug is? |
aspirin (acetylsalicylic acid, ASA)
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mechanism of action of ASA is inhibition of?
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prostaglandin (PG) synthesis by irriversibly inhibiting cyclooxygenase (COX) by acetylation
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therapeutic effects of ASA?
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1) analgesia
2) antipyresis 3) antiinflammatory 4) anti-plt 5) uricosuric |
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SE of ASA
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1) gastric ulceration and blddeing
2) intolerance (broncheal secretions, urticaria, angioedema, hypotension, shock) 3) cross sensitivity to other NSAIDs |
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all NSAIDS are contraindicated in pts with?
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ASA hypersensitivity
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SE of ASA
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1) < plt aggregation
2) hepatotoxicity (SLE, juvenile RA pts) 3) acute decrease in renal function |
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ASA use in kids with viral disease?
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association with Reye's syndrome
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ASA use in pregnancy?
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Do not use in last trimester
1) > gestation and labor 2) > blood loss at delivery 3) neonate intracranial hemorrhage 4) close ductus arteriosus prematurely |
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Salsalate (Disalcid, Salflex)
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1) dimer of salicyclic acid
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salicylates displace other drugs
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1) oral hypoglycemics
2) phenytoin 3) sulfonamides 4) methotrexate 5) other NSAIDs |
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drugs increase salicylate intoxication?
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1) alcohol
2) ototoxic agents 3) antacids 4) penicillin 5) acetazolamide |
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salicylates antagonize?
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1) diuretics
2) uricosurics |
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prototype of para-aminophenols?
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acetaminophen (Tylenol, Datril, Tempra, Panadol)
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effects of acetaminophen?
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1) analgesia
2) antipyresis 3) antiinflammatory (but not useful for RA) |
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SE of acetaminophen?
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hepatotoxicity
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Tx for acetaminophen intoxication?
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1) emesis or lavage followed with activated charcoal
2) sulfhydryl agents (Mucomyst) |
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other NSAIDS
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all reversibly inhibit COX1 and COX2 with effects on PGs and thromboxanes
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other NSAIDS are organic?
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anions and highly bound to plasma protein
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COX inhibitors
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1) for colon cancer
2) tx for Alzheimer's |
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most common complaints of other NSAIDS are?
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stomach pain, N/V
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Indomethacin (Indocin)
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1) most potent of the NSAIDs
2) for ankylosing spondylitis, OA, acute gout |
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SE of Indomethacin
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1) severe headache (most common)
2) dezziness 3) confusion 4) gastric intolerance |
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Indomethacin is more selective in inhibiting?
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COX-1
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Sulindac (Clinoril)
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1) prodrug
2) converted to the active sulfide metabolite 3) lower incidence of GI toxicity than indomethacin |
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lowest incidence of GI side effect?
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Etodolac (Lodine)
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Tolmetin (Tolectin)
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better tolerated than aspirin and equally effective
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Ketrolac (Toradol)
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1) 1st injectable NSAID
2) very potent analgesic 3) for allergic conjunctivitis |
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Ketrolac- do not use for more than?
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5 days
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Diclofenac (Voltaren, Cataflam)
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1) very potent antiinfla.
2) accumulates in synovial fluid 3) first-pass effects 4) for after cataract sx |
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Ibuprofen (Motrin)
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1) analgesic 200 mg
2) antiinfla 600 mg 3) increase serum digoxin conc. |
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Naproxen (Naprosyn)
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1) Aleve
2) long t1/2 14 hr |
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Fenoprofen (Nalfon)
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rapidly absorbed but incompletely
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Ketoprofen (Orudis, Oruvail)
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1) dose should be individualized
2) analgesia 3) dysmenorrhea 4) inhibit leukotriene synthesis |
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Flubiprofen (Ansaid)
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almost equally inhibits COX1 and COX2
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Oxaprozin (Daypro)
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very long t1/2 40-60 hr
once a day |
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Piroxicam (Feldene)
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t1/2 = 57 hr
once a day |
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Meloxicam (Mobic)
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t1/2 = 20 hr
for OA |
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Meclofenamate (Meclomen)
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not recommended for initial tx of RA or OA
cause hemolytic anemia |
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Mefenamic acid (Ponstel)
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1) only for analgesia
2) for dysmenorrhea 3) too toxic for chronic use |
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Nabumetone (Relafen)
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1) prodrug
2) converted to an active metabolite |
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Diflunisal (Dolobid)
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difluorophenyl derivative
but not metabolized to salicyclic acid |
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COX2 inhibitors
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1) selectively inhibit the COX2 enzyme
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COX2 enzyme found mainly in?
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tissues other than the GI tract
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benefit of COX2 inhibitors?
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GI ulceration and symptoms can be avoided
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COX2 inhibitors
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1) Celecoxib (Celebrex)
2) Rofecoxib (Vioxx) 3) Valdecoxib (Bextra) |
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COX2 inhibitors SE
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cardiovascular risks (MI, stroke)
kidney damage |
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CNS SE of other NSAIDs
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1) dizziness
2) tinnitus 3) headache 4) aplastic anemia 5) granulocytopenia |
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hepatotoxicities of other NSAIDs
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1) cholestatic jaundice
2) hepatic necrosis |
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nephrotoxicities of other NSAIDs
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1) Na and water retention
2) ARF 3) papillary necrosis 4) nephrotic syndrome |