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49 Cards in this Set

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