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51 Cards in this Set

  • Front
  • Back
The COX pathway of arachidonate metabolism produces __________.
Prostaglandins
The lipoxygenase pathway of arachidonate metabolism yields __________.
Leukotrienes
Which COX isoform is believed to be homeostatic in nature?
COX-1
Which COX isoform is induced during inflammation and tends to facilitate the inflammatory response?
COX-2
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.
What is the only NSAID that is a ketone prodrug that is metabolized to the acidic active drug?
Nabumetone.
True or False

NSAID metabolism occurs primarily by CYP3A and CYP2C.
True
Which NSAID irreversibly acetylates and blocks platelet cyclooxygenase?
Aspirin
Selective COX-__ inhibitiors may increase the incidence of edema and HTN.
2
What are the only 2 COX-2 inhibitors marketed in the USA?
Celecoxib and Meloxicam
Which two groups of NSAIDs do not inhibit platelet aggregration?
COX-2 selective agents
and Nonacetylated salicylates
What 3 major things do NSAIDs do?
Decrease sensitivity to bradykinin and histamine.
Affect lymphokine production from T lymphocytes.
Reverse the vasodilation of inflammation.
What are the 3 major adverse reactions associated with NSAIDs?
GI ulcers, nephrotoxicity, and hepatotoxicity.
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.
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.
Aspirin
Which COX isozyme mediates platelet aggregation?
COX-1
A selective COX-2 inhibitor. May cause rashes, but does not affect platelet aggregation. A sulfonamide.
Celecoxib.
An enolcarboxamide that is a "preferentally selective" COX-2 inhibitor. Approved for the treatment of osteoporosis.
Meloxicam
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.
Diclofenac
A salicylic acid derivative that undergoes an enterohepatic cycle. Effective treatment for cancer pain with bone metastases and for pain control in dental surgery.
Diflunisal
A racemic acetic acid derivative with an intermediate half-life.
Etodolac
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.
Flurbiprofen
A simple derivative of phenpylpropionic acid. At lower doses it has analgesic but not anti-inflammatory properties. May limit cardioprotective effects of aspirin.
Ibuprofen
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.
Indomethacin
A propionic acid derivative that inhibits both COX and lipoxygenase. Major effects on GI and CNS.
Ketoprofen
Mainly used as an anti-inflammatory drug. An an effective analgesic that sometimes is used to replace morphine.
Ketorolac
A nonacid NSAID converted to the active acetic acid derivative. Once daily dosing.
Nabumetone
A naphthylproprionic acid derivative. Effective against rheumatologic disorders. Twice the incidence of upper GI bleeding.
Naproxen
A propionic acid derivative; mildly uricosuric, making it potentially more useful in gout.
Oxaprozin
An oxicam that inhibits polymorphonuclear leukocyte migration, decreases oxygen radical production, and inhibits lymphocyte function. Rheumatic indications.
Piroxicam
A sulfoxide prodrug. Rheumatic disease indications, suppresses familial intestinal polyposis and it may inhibit the development of colon, breast, and prostate cancer in humans.
Sulindac
Nonselective COX inhibitor with a short half-life. Treatment of gout.
Tolmetin
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.
Abatacept
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.
Azathioprine
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.
Chloroquine and Hydroxychloroquine
A phosphoramide mustard, which cross-links DNA to prevent cell replication.
Cyclophosphamide
Inhibits IL-1 and IL-2 receptor production secondarily inhibits macrophage-T-cell interaction and T-cell responsiveness. Significant nephrotoxicity.
Cyclosporine
Inhibits dihydroorotate dehydrogenase, ultimately inhibiting T-cell proliferation and production of autoantibodies by B cell.
Leflunomide
Inhibition of AICAR transformylase and thymidylate synthetase, with secondary effects on PMN chemotaxis.
Methotrexate
Inhibits cytosine monophosphate dehydrogenase and inhibits T-cell lymphocyte proliferation. Treats renal disease due to lupus.
Mycophenolate mofetil
A chimeric monoclonal antibody that targets CD20 B lymphocytes. Treats rheumatoid arthritis refractory to anti-TNF agents. About 30% of patients develop rash.
Rituximab
Decreases IgA and IgM rheumatoid factor; inhibits release of inflammatory cytokines, including those produced by monocytes or macrophages.
Sulfasalazine
Fully human IgG anti-TNF monoclonal antibody, which complexes with soluble TNF-alpha and prevents its interaction with p55 and p75. RA, AS
Adalimumab
IgG monoclonal antibody that binds with high affinity to soluble TNF-alpha. Treats RA, AS, Chron's
Infliximab
Recombinant fusion protein consisting of two soluble TNF p75 receptor moieties linked to the Fc portion of human IgG. Inhibits lymphotoxin- alpha.
Etanercept
IL-1 inhibitor in its investigational stages.
Aakrina
The active metabolite of phenacetin; a weak COX-1 and COX-2 inhibitor in peripheral tissues; lacks anti-inflammatory properties.
Acetaminophen
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
Colchicine
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.
Uricosuric agents
(Probenecid and sulfinpyrazone)
Used between acute episodes by inhibiting xanthine oxidase, thereby decreasing the plasma urate level and the size of the urate pool.
Allopurinol
Nonpurine inhibitor of xanthine oxidase; extensively metabolized in the liver; SE: liver function abnormalities.
Febuxostat