Warning:
JavaScript is turned OFF. None of the links on this page will work until it is reactivated.
If you need help turning JavaScript On, click here.
This Concept Map, created with IHMC CmapTools, has information related to: Pain, inflammation, RA, gout, Migraines Prevent NSAIDs-naproxen -block TXA2->block plt agg ->reduce 5-HT release -can take 1wk before, up to menses to prevent beta-blockers Ca++ channel blockers -least helpful 5-HT2 antagonists -METHYSERGIDE, Migraines Abort 5-HT_1D/1B agonists MOA-in trigem neurovasc ->vasoconstriction ->no throbbing ->inhibit peptide release ->no dilation, inflam, pain ->prevent activation in brainstem DIHYDROERGOTAMINE (DHE) -intranasal, injectable -can->N/V/D, mm cramps, vertigo -Periph vasoconstriction->cold skin -don't use if heart problem Ergotamine-all routes but nasal -give early in attack -excessive dosing->rebound HA, Nonselective ASPIRIN IBUPROFEN NAPROXEN KETOROLAC ketoprofen sulindac nabumetone -all w/ diff doses, T1/2 Specific Drugs ASA-irreversible -transfers acetyl group -plts more sens than vessel ->analgesic, anti-inf, antipyretic ->antiplt-cardioprotective-LDA ->inhibit cataract development ->counter-irritant ->decrease colorectal CA risk ->decrease ALZHEIMERS risk IF OD: -induce vomiting/gavage -NaHCO3 IV, Nonselective ASPIRIN IBUPROFEN NAPROXEN KETOROLAC ketoprofen sulindac nabumetone -all w/ diff doses, T1/2 Specific Drugs ACETAMINOPHEN =ASA for analgesic, antipy MOA-inhibit COX-3??? NOT anti-inflammatory -inactivated by peroxides in inflamed tissue ADRs-no GI/HA -well tolerated-mostly conjugated -HEPATOTOXICITY -CYP450->toxic intermed -no more glutathione ->attack hep cell->necrosis Interactions: warfarin(inc INR), EtOH->inc'd P450, dec'd glutathi ->more toxic metabolites Treat OD: acetylcysteine (Mucomyst), Pain, Inflammation Drugs DMARDs Disease-Modifying Anti-Rheumatic Drugs -slow jt erosion -take wks-mos to kick in Gold Salts-parenteral & oral GOLD SODIUM THIOMALATE Toxicities: Hematologic, Dermatologic, GI, Renal -flushing, hypoTN, tachycard -skin rash, stomatitis, Migraines Prevent MISC: Gabapentin Feverfew/ginger Vitamin B2, Migraines Abort 5-HT_1D/1B agonists SUMATRIPTAN -intranasal faster than oral -oral relief = 2 hrs -subQ=1hr More lipophilic, oral only: Zolmatriptan Rizatriptan -both inhibit brainstem involvement more than suma Outcome-40% w/ same-day recurrence ADRs-chest tightness, weakness, tired-50% -tingling, burning in skin-benign -can -> angina, increased BP, Pain, Inflammation Drugs DMARDs Disease-Modifying Anti-Rheumatic Drugs -slow jt erosion -take wks-mos to kick in Glucocorticoids PREDNISONE-fastest of DMARDs ->formation of lipocortin ->inhibits phospholipase A2 ->no arach acid release, PGs ->inhibit cytokine production -ILs, TNF -ADRs, so long-term use limited -can use for flare-ups or before other DMARD kicks in, Pain, Inflammation Drugs NSAIDs Nonselective ASPIRIN IBUPROFEN NAPROXEN KETOROLAC ketoprofen sulindac nabumetone -all w/ diff doses, T1/2, Pain, Inflammation Drugs NSAIDs Selective COX-2 CELECOXIB rofecoxib valdecoxib ->anti-inflam ->LESS GI, renal, plt, CNS effects BUT-2.5x inc'd risk of CV event, Pain, Inflammation Drugs DMARDs Disease-Modifying Anti-Rheumatic Drugs -slow jt erosion -take wks-mos to kick in METHOTREXATE-Tx of choice -MOST EFFECTIVE DMARD -antineoplastic & immunomodulatory -MOA-decrease: folate reductase lymphocyte prolif cytokines, RF production WBC chemotaxis free rad/cytokine production ADRs -hepatotoxicity-LFTs in 15% -bone marrow suppression -teratogenic -pulm rxns Leflunamide-alternative to MTX -inhibit mononuc, T-cell prolif via inhib of pyrimidine synth, Migraines Abort MISC: Isometheptene Tramadol Butorphanol Acetaminophen/codeine Acetaminophen/caffeine/butalbital NSAIDS prochlorperazine, Pain, Inflammation Drugs Gout Prevent Attacks-excretion -reduce uric acid synth -decrease secretion -increase hypoxanthine sec tho ALLOPURINOL-oral purine analog -inhibit xanthine oxidase ->increase salvage pathway -also use along w/ CTX ADRs-N/V, hypersensitivity -hepatitis, skin rash -Stevens-Johnson, Migraines Pathogenesis Phase 1-cerebral vasoconstriction ->ischemia -via serotonin from CNS, plts (use 5-HT antags, antiplts) Phase 2-vasodilation, PAIN -longer than 1 -trigeminal nn key player -release substance P, CGRP ->dilation, pial/dural vessel inflam ->nociceptive trigem nn->PAIN, Pain, Inflammation Drugs DMARDs Disease-Modifying Anti-Rheumatic Drugs -slow jt erosion -take wks-mos to kick in Older Drugs SULFASALAZINE -MOA?? -SULFA ALLERGIES -Nausea, Rash -Leukopenia, Hepatitis D-penicillamine -MOA?? <=3mo onset ->reduces inflam cytokines -decreasing use, Pain, Inflammation Drugs NSAIDs COX-1 -constitutive (housekeeping) -constant in various tissues ->protection of GI tract ->TXA2->plt agg, hemostasis COX-2 -inducible (only high during inflam) -only in inflamed sites (eg synovitis) BOTH -renal homeostasis COX-3 -variant of COX-1 -inhibited by ACETAMINOPHEN, Pain, Inflammation Drugs DMARDs Disease-Modifying Anti-Rheumatic Drugs -slow jt erosion -take wks-mos to kick in Immunomodulators -inactivate TNF ETANERCEPT-THF-R+IgG1 complex INFLIXIMAB-anti-TNF AB adalimumab-anti-TNF AB -bind to and inactivate TNF, Pain, Inflammation Drugs NSAIDs ADRs GI-dyspepsia (PGE2-mediated mucus) Renal-PGE2 -analgesic nephropathy -inhibit renal PGs->vasoconstriction ->Na, water retention ->acute ischemic RF ->hyporeninemic hypoaldost Hypersensitivity -Asthma, Skin Rash, Anaphylaxis Resp - bronchospasm CNS -Tinnitus -HA, drowsiness, dizziness, fatigue -Reye syndrome (ASA)-kids w/ virus, Pain, Inflammation Drugs NSAIDs Actions Low-Dose->analgesia, antipyresis High-Dose->anti-inflam -for arthritis, injuries Won't Cause (unlike opioids): -resp depression -ileus, N/V/C -sedation, dizziness, Pain, Inflammation Drugs DMARDs Disease-Modifying Anti-Rheumatic Drugs -slow jt erosion -take wks-mos to kick in HYDROXYCHLOROQUINE -antimalarial -less toxic, but ɲmo onset ->dec'd lymphos, PMNs, superoxide radicals -G6PD def->hemolytic anemia -elderly->RETINAL DMG