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NSAIDS kgima

Pharmacology

DrugUseToxicityMetabolismSpecial Qualities
Aspirin Antipyresis, Analgesia, anti-inflammatory, Rheumatoid Arthritis, propholaxis treatment for platelet hyperaggregability Salicylism, and common to all NSAIDS: GI dyspesea and bleeding, increased bleeding, nephrotoxicity and hepatotoxicity good oral absorption and distribution, prot. Bound, metab. By cellular esterase (Saturatable) only irreversible inhibitor
Ibuprofen Antipyresis, Analgesia, anti-inflammatory, NSAIDS toxicities, + rash, pruritus, tinnitus, dizziness, headache Liver CYP2C9, 8 OTC
Diclofenac Antipyresis, Analgesia, anti-inflammatory, GI bleeding common (20%) reason for misoprostal combo, renal and hepatotoxicity (rare) Liver CYP2C9, 3A4 to inactive metab. more liver function abnormalities, post operative ophthalmic inflammation
Diflunisal " + cancer pain " + pseudoporhpyria metabolism Saturatable, cleared via renal excretion, use cancer pain w/ bone metastases, may cause pseudoporphyria
Etodolac similar to ibuprofen Similar to Ibuprofen (blank) slight COX 2 specificity
Fenoprofen similar to ibuprofen Similar to Ibuprofen (blank) associated w/ interstitial nephritis
Flurbiprofen similar to ibuprofen NSAIDS tox. + cogwheel rigidity, ataxia, tremor and myoclonus extensive liver available in topical ointment, intraoperative miosis
Indomethacin " + popular for rheumatic conditions More severe NSAIDS effects, CNS disturbances (Hallucinations, confusion, depression) ext Hepatic metab and enterohepatic recirculation. probenicid inh. Ren. Exc. rheumatic conditions, gout, ankylosing spondylitis, PDA
Ketoprofen similar to ibuprofen Similar to Ibuprofen liver glucoronidation, probenicid prolongs t1/2 OTC, also inhibits lipoxygenase
Ketorolac High analgesic efficacy Similar to other NSAIDS but increased peptic ulceration and renal impairment IV, IM of PO, ext. Hep. Metab. acute post-surgical pain (good short term analgesic)
Meclofenamate similar to ibuprofen perhaps more toxic than other NSAIDS 58% excreted in urine contraindicated in pregnancy, analgesia, little A-Infl. No child.
Mefenamic Acid similar to ibuprofen perhaps more toxic than other NSAIDS (blank) contraindicated in pregnancy, analgesia, little A-Infl. No child.
Nabutamone similar to ibuprofen " + pseudoporhpyria non acid prodrug, slightly less GI toxicity, long half life
Naproxen similar to ibuprofen NSAIDS toxicities, + rare cases: allergic pneumonitis, vasculitis and pseudoporphyria Liver CYP2C9, 8 OTC,
Oxaprozin similar to ibuprofen (blank) (blank) long half life = qd, mildly uricosuric
Piroxicam similar to ibuprofen Similar to Ibuprofen, more GI tox extensive liver metab once-daily dose or every other
Sulindac similar to ibuprofen " + Stevens-Johnson epidermal ncerolysis, thrombocytopenia, agranulocytosis enterohepatic cycling may have less renal COX inh, similar liver effects as diclofenac
Tolmetin similar to ibuprofen " + allergic IgM-related thrombocytopenic purpura (blank) half life too short
Celecoxib similar to ibuprofen (better for older patients and patients susceptible to GI bleeding) Similar to other NSAIDS with less GI tox liver CYP2C9 Cox 2 selective = less GI toxicity and no platelet effects
Meloxicam similar to ibuprofen (better for older patients and patients susceptible to GI bleeding) Similar to other NSAIDS with less GI tox (blank) once-daily, likes COX 2 more
Rofecoxib similar to ibuprofen (better for older patients and patients susceptible to GI bleeding) Similar to other NSAIDS with less GI tox CYP3A4 metab. Cox 2 selective = less GI toxicity and no platelet effects
Valdecoxib similar to ibuprofen (better for older patients and patients susceptible to GI bleeding) Similar to other NSAIDS with less GI tox (blank) plus serious reactions may occur in sulfonamide sensitive patients
Acetaminophen patients who cannot tolerate aspirin, children, patients with bleeding disorders dose dependent hepatotoxicity See figure 4-4, Phase 2 low doses, phase 1 high doses producing hepatotoxic metabolite antipyretic (children), analgesic, No anti-inflammatory effects
Created by: kgima
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