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25 Cards in this Set
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Acetic Acid Class
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are equally efficacious
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indomethacin
sulindac nabumetone etodolac ketorolac diclofenac sodium |
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Indomethacin
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Acetic Acid
Extended realease qd Used to close ductus arteriousus in newborns |
Can get severe headache (esp with high doses)
drowsiness, dizziness, forgetfulness, and mental confusion |
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Sulindac
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Acetic Acid
Prodrug |
GI SE seen in 20% pts
nausea and ab pain |
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Nabumetone
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Acetic Acid
prodrug increased selectivity for COX2 |
Long half-life
qd |
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Etodolac
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Acetic Acid
Increased selectivity for COX2 |
Sustained-release
qd |
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Ketorolac
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Acetic Acid
Analgesic use Short term IM use (<5 days) |
Injectable
Can be used with opiods |
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Diclofenac Sodium
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Acetic Acid
Enteric coated For patients with high risk of ulcer development |
Diclofenac + Misoprostil + Arthrotec
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Propionic Acids Class
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Oxaprozin
Ibuprofen Naproxen Sodium Ketoprofen Fenoprofen |
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Oxaprozin
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Propionic Acids
long half-life qd |
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Ibuprofen
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Propionic Acid
OTC:advil and motrin IV admin approved |
mild/moderate pain in adults
used with opioids for mod/severe pain |
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Ketoprofen
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Propionic Acid
OTC available dissolution of coated pellets within capsules requires basic pH |
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Fenoprofen
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Propionic Acid
only NSAID not taken with food |
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Fenamic Acids
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Meclofenamate
Mefenamic Acid duration less than a week |
dyspepsia and severe diarrhea (~25%)
bowel irritation (possible colitis) |
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Oxicams
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Enolic acids (piroxicam (gi toxic), meloxicam(gi rare))
qd |
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Pyrazoles
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Phenylbutazone, oxyphenbutazone
very eff one of the strongest NSAIDs BUT more toxic, not used much |
aplastic anemia with mortality ~50%
agranulocytosis 1 week MAX with acute osteo attacks when not responding to other drugs |
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Diaryl Substituted Pyrazoles
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Celecoxib
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Celecoxib
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Diaryl sub pyrazole
selective cox2 inhibitor (>100 fold selectivity) bulky drug for osteo- and rheumatoid arthritis approved for familial adenomatous polyps (higher dose) |
less likely to produce ulcers
renal toxicity is possible consider cv implications (MI, stroke) has sulfonamide component cross-react in patients with allergy to sulfonamides |
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COX2 Inhibitor Recommendations
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Necessary?
For patients with high risk of GI bleeding |
AVOID patients with coronary artery disease
Use lowest eff dose Celebrex: 200mg osteo, 200-400mg RA, 400mg pain |
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Salicylates
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Aspirin
Magnesium choline salicylate, sodium salicylate, and salicylsalicylate Diflunisal |
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Aspirin - Uses and Kinetics
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Salicylate
Analgesis, antiinflammatory, antipyretic antiplatelet action, CV disorders decrease colon cancer risk |
hydrolyzed by tissue and blood esterases to acetic acid and salicylate
with large doses, saturation and small increase in aspirin dose results in large increase in plasma levels and half life |
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Aspirin - Doses and Consequences
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Salicylate
low dose (650mg)-1st order kinetics and half life of 3-5 hrs high antiinflam dose (3.6-4g)-0 order kinetics, half life >15 hrs |
Highly protein bound
might be drug interactions due to protein binding displacement reactions Large amnt= INC risk of gi bleeding and ulceration |
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Aspirin - Adverse Effs
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Like other NSAIDs: gi bleeding, impaired blood clotting, hypersensitivity
High doses: salicylism, tinnitus, decreased hearing, vertigo |
Overdose toxicity
hyperventilation, vasomotor collapse, and respiratory failure |
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Other Salicylates
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Mag choline salicylate, sod sal, and salicylsal
equal or less efficacy than aspirin (usually less) slower onset of action |
no aspirin hypersensitivity
no drug interactions less gi se: buffered, enteric coated very low incidence of platelet impairment |
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Diflunical
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Salicylate
not converted to salicylic acid little antipyretic action does not readily enter brain |
less gi and antiplatelet effs
less auditory se incidences of aspirin hypersensitivity has occured |
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Acetaminophen
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analgesic, antipyretic, extremely weak antiinflammatory effects
preferred to aspirin in children inhibition of COX in brain weak inhibition of cox in presence of peroxides |
normally metabed by glucuronide and sulfate conjugates
high doses result in increased production of reactive intermediate (from p450) hepatic/renal toxicity treated with n-acetylcysteine slight protein binding very little drug interactions Mild SE with normal dose no increased bleeding, no inhib of platelet agg, no gi bleeding, no ulcer incidence |
