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35 Cards in this Set
- Front
- Back
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celebrex
- anti inflammatory, analgesic, antipyretic arthritis, long t1/2, bid or qd - a-oxidation at CH3-->CH2OH-->ADH--> CO2H - P2 glucuronidation |
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ASA
81mg=antithrombotic pain, inflam, fever - 2-acetyloxyinteract with serine and transfer to Me-OH to irreversibly inhibit COX1 (6-7d - ester hydrolysis, AA conjugation, glucuronide |
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magensium salicylate
-arthritis, back pain less GI irritation |
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salsalate
- salicylate NSAID - ASA dimer --> SI --> hydrolysis --> 2ASA - not irreversible COX1 - less irritation |
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diflunisal
- salicylate NSAID - pain, arthritis - not antipyretic bc no CNS bc Fs create highly ionized CO2- - only P2 metabolism - no metabolism to ASA.. only a derivative |
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MESALAMINE
- salicylate NSAID - chronic IBS, UC - works in colon topically bc acrylic resin coated and slowly dissolve |
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SULFASALAZINE
- salicylate NSAID - IBS, UC - mesalamine derivative - 2/3 to colon bacteria -> nitroreductase -> 5asa(antiinflammatory) and sulfapyridine(N/V, upset stomach) |
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OSALAZINE
- salicylate NSAID - IBS, UC - bacterial azoreductase --> 2x mesalamine |
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BALSALAZIDE
- salicylate NSAID - UC, IBS - bacterial azoreductase - metabolite has less ADRs vs sulfasalazine |
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FENOPROFEN
- arylacetic acid NSAID - arthritis, pain.. maybe fever - para-hydroxylation --> glucuronide - COOH conjugation to glucuronide |
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IBUPROFEN
- arylacetic acid NSAID - pain, fever, inflammation, arthritis - COOH conjugation - CH3 = omega-oxidation --> primary OH - CH = omega(-1)oxidation--> tertiary OH |
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KETOPROFEN
- arylacetic acid NSAID - arthritis, pain - no Ar-OH bc carbonyl - ketone reduced to alcohol - P2 COOH glucuronidation |
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NAPROXEN
- arylacetic acid NSAID - pain, fever, arthritis - t1/2 =13hr - O-demthylation-->6phenol-->conjugated -COOH-glucuronide |
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INDOMETHACIN
- arylacetic acid NSAID - potent analgesic - GI distress, ulcer - amide hydrolysis-->indole + 4chlorobenzoic - a-oxidation (2sites) --> glucuronide - O-demethylation --> glucuronide |
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SULINDAC
- arylacetic acid NSAID - prodrug - S4 --> oxidized to sulfone (inactive) - S4 --> reduced to Me-Sulfide (activee) - a-oxidation (2sites) --> glucuronide - double bond oxidation to diol |
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TOLMENTIN
- arylacetic acid NSAID - arthritis - a-oxidation to OH --> ADH --> COOH --> P2 |
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KETOROLAC (ACULAR)
- arylacetic acid NSAID - severe pain (similar to opiods) - <5d otherwise severe gastric bleeding and ulcers - eye drops for seasonal conjunctivitis or inflammation post-cataract sx - ketone reduction-->secondary OH - p2 |
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DICLOFENAC (VOLTAREN)
- arylacetic acid NSAID - para-OH @ 5' |
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BROMFENAC (XIBROM)
- arylacetic acid NSAID - opthlamic inflammation, cataracts |
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NEPAFENAC
- arylacetic acid NSAID - opthalmic |
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FLURBIPROFEN (OCUFEN)
- arylacetic acid NSAID - the sodium salt is opthalmic - para-OH - P2 |
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ETODOLAC
- arylacetic acid NSAID - arthritis pain - low GI effects |
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OXAPROZIN
- arylacetic acid NSAID - 2x paraOH - P2 |
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MEFANAMIC ACID
- arylacetic acid NSAID - pain, post-dental extraction - not good anti-inflammatory - CH3-->CH2OH-->COOH |
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MECLOFENAMATE
- arylacetic acid NSAID - arthritis, pain, antiinflammatory - only P2 metab |
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PIROXICAM
- arthritis - long lasting, better tolerated vs ASA - amide hydrolysis --> COOH + 2-aminopyridine - OH on pyridine - N-demethylation |
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MELOXICAM
- arthritis - long lasting, better tolerated vs ASA - amide hydrolysis - N-demethylation |
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NABUMETONE
- prodrug 1/3 of dose becomes active - arthritis - not an acid = less GI - similar to naproxen (no a-CH3) - |
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LEFLUNOMIDE
- arthritis - teratogenic = Preg X - amide hydrolysis - CH3-->OH |
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APAP
- not antiinflammatory - no inhibition of platelets, less GI - OH-->oxidative--> amidoquinone, which is an electrophile and then can bind nucleophiles (bind proteins and nucleotides, hepatotoxic, nephrotoxin) + GSH (detox, small amount) at the 2 position |
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NAC
- sulfide works as nucleophile |
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PROBENECID
- uricosuric agent - increases excretion - inhibits renal tubule, increasing levels and DOA of PCN and NSAIDs - drink water otherwise kidney stones from uric acid |
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ALLOPURINOL
- XOI via hypoxanthine analog - chronic gout - used in chemo regimens |
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FEBUXOSTAT
- XOI via blocking active site - chronic gout |
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COLCHICINE
- natural product that inhibit leukocyte migration into the joints - acute gout - ADR = BM, anemia, diarrhea |
