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51 Cards in this Set
- Front
- Back
The COX pathway of arachidonate metabolism produces __________.
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Prostaglandins
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The lipoxygenase pathway of arachidonate metabolism yields __________.
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Leukotrienes
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Which COX isoform is believed to be homeostatic in nature?
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COX-1
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Which COX isoform is induced during inflammation and tends to facilitate the inflammatory response?
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COX-2
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True or False
Stimulation of the neutrophil membranes leads to the oxidation of molecular oxygen, which reacts with arachidonic acid to perpetuate the inflammatory response. |
False. Reduction.
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What is the only NSAID that is a ketone prodrug that is metabolized to the acidic active drug?
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Nabumetone.
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True or False
NSAID metabolism occurs primarily by CYP3A and CYP2C. |
True
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Which NSAID irreversibly acetylates and blocks platelet cyclooxygenase?
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Aspirin
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Selective COX-__ inhibitiors may increase the incidence of edema and HTN.
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2
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What are the only 2 COX-2 inhibitors marketed in the USA?
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Celecoxib and Meloxicam
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Which two groups of NSAIDs do not inhibit platelet aggregration?
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COX-2 selective agents
and Nonacetylated salicylates |
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What 3 major things do NSAIDs do?
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Decrease sensitivity to bradykinin and histamine.
Affect lymphokine production from T lymphocytes. Reverse the vasodilation of inflammation. |
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What are the 3 major adverse reactions associated with NSAIDs?
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GI ulcers, nephrotoxicity, and hepatotoxicity.
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True or False
NSAID associated nephrotoxicity is due to interference with the autoregulation of renal blood flow, which is modulated by leukotrienes. |
False. NSAID associated nephrotoxicity is due to interference with the autoregulation of renal blood flow, which is modulated by prostaglandins.
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This drug is a mild-moderate analgesic and inhibits platelet aggregation. It is used to prevent arterial and venous thrombosis, but may cause GI disturbances.
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Aspirin
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Which COX isozyme mediates platelet aggregation?
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COX-1
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A selective COX-2 inhibitor. May cause rashes, but does not affect platelet aggregation. A sulfonamide.
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Celecoxib.
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An enolcarboxamide that is a "preferentally selective" COX-2 inhibitor. Approved for the treatment of osteoporosis.
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Meloxicam
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Phenylacetic acid derivative that has less GI ulceration than other NSAIDs. Treats ophthalmic inflammation, intraocular lens implantation and strabismus surgery. Preemptive analgesic and postoperative anti-emetic.
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Diclofenac
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A salicylic acid derivative that undergoes an enterohepatic cycle. Effective treatment for cancer pain with bone metastases and for pain control in dental surgery.
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Diflunisal
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A racemic acetic acid derivative with an intermediate half-life.
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Etodolac
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A proprionic acid derivate; S - enanatiomer inhibits COX. It inhibits intraoperative miosis and is effective against perioperative analgesia in the minor ear, neck, and nose surgery.
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Flurbiprofen
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A simple derivative of phenpylpropionic acid. At lower doses it has analgesic but not anti-inflammatory properties. May limit cardioprotective effects of aspirin.
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Ibuprofen
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Indole derivative that may inhibit phospholipase A and C, reduce neutrophil migration, and decrease T-cell and B-cell proliferation. Popular for gout and ankylosing spondylitis.
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Indomethacin
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A propionic acid derivative that inhibits both COX and lipoxygenase. Major effects on GI and CNS.
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Ketoprofen
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Mainly used as an anti-inflammatory drug. An an effective analgesic that sometimes is used to replace morphine.
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Ketorolac
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A nonacid NSAID converted to the active acetic acid derivative. Once daily dosing.
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Nabumetone
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A naphthylproprionic acid derivative. Effective against rheumatologic disorders. Twice the incidence of upper GI bleeding.
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Naproxen
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A propionic acid derivative; mildly uricosuric, making it potentially more useful in gout.
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Oxaprozin
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An oxicam that inhibits polymorphonuclear leukocyte migration, decreases oxygen radical production, and inhibits lymphocyte function. Rheumatic indications.
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Piroxicam
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A sulfoxide prodrug. Rheumatic disease indications, suppresses familial intestinal polyposis and it may inhibit the development of colon, breast, and prostate cancer in humans.
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Sulindac
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Nonselective COX inhibitor with a short half-life. Treatment of gout.
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Tolmetin
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A costimulation modulator that inhibits the activation of T cells by binding to CD80 and 86 thereby inhibiting binding to CD28. Treats moderate to severe rheumatoid athritis.
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Abatacept
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6-thioguanine suppresses inosinic acid synthesis, B-cell and T-cell function, Ig production, and interleukin-2 secretion. Toxicity includes bone marrow suppression and GI disturbances.
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Azathioprine
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Used mainly in malaria and in the rheumatic diseases. Suppresses T-lymphocyte responses to mitogens, decreased leukocyte chemotaxis, stabilization of DNA and RNA synthesis, and the trapping of free radicals.
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Chloroquine and Hydroxychloroquine
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A phosphoramide mustard, which cross-links DNA to prevent cell replication.
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Cyclophosphamide
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Inhibits IL-1 and IL-2 receptor production secondarily inhibits macrophage-T-cell interaction and T-cell responsiveness. Significant nephrotoxicity.
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Cyclosporine
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Inhibits dihydroorotate dehydrogenase, ultimately inhibiting T-cell proliferation and production of autoantibodies by B cell.
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Leflunomide
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Inhibition of AICAR transformylase and thymidylate synthetase, with secondary effects on PMN chemotaxis.
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Methotrexate
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Inhibits cytosine monophosphate dehydrogenase and inhibits T-cell lymphocyte proliferation. Treats renal disease due to lupus.
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Mycophenolate mofetil
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A chimeric monoclonal antibody that targets CD20 B lymphocytes. Treats rheumatoid arthritis refractory to anti-TNF agents. About 30% of patients develop rash.
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Rituximab
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Decreases IgA and IgM rheumatoid factor; inhibits release of inflammatory cytokines, including those produced by monocytes or macrophages.
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Sulfasalazine
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Fully human IgG anti-TNF monoclonal antibody, which complexes with soluble TNF-alpha and prevents its interaction with p55 and p75. RA, AS
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Adalimumab
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IgG monoclonal antibody that binds with high affinity to soluble TNF-alpha. Treats RA, AS, Chron's
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Infliximab
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Recombinant fusion protein consisting of two soluble TNF p75 receptor moieties linked to the Fc portion of human IgG. Inhibits lymphotoxin- alpha.
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Etanercept
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IL-1 inhibitor in its investigational stages.
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Aakrina
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The active metabolite of phenacetin; a weak COX-1 and COX-2 inhibitor in peripheral tissues; lacks anti-inflammatory properties.
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Acetaminophen
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An alkaloid isolated from the autumn crocus. Alters metabolism or excretion of urates and w/o other analgesic effects. Inhibits leukocyte migration and formation of leukotriene B4. SE: diarrhea
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Colchicine
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Organic acids that act at the anion transport sites of the renal tubule. Decrease the net reabsorption of uric acid in the proximal tubule. Maintain a large urine volume to avoid development of stones.
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Uricosuric agents
(Probenecid and sulfinpyrazone) |
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Used between acute episodes by inhibiting xanthine oxidase, thereby decreasing the plasma urate level and the size of the urate pool.
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Allopurinol
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Nonpurine inhibitor of xanthine oxidase; extensively metabolized in the liver; SE: liver function abnormalities.
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Febuxostat
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