pharmacology test 4 gout & RA

  1. level indicating hyperuricemia
    > 7 mg/dl
  2. how effective is diet in lowering purine levels
    low, only reduces by 1mg/dl
  3. 2 groups who have problems with urate in the body and the prevelance
    • under-excretor - 90%
    • over-producer
  4. steps of metabolism of a purine
    hypoxanthine ->Xanthine oxidase -> xanthine  -> xanthine oxidase -> uric acid
  5. dosage effects of aspirin on gout
    • low dose (<2.6 g/day) blocks secretion
    • high dose increases excretion
  6. gout pathophysiology
    • urate crystals acted on by synoviocytes
    • producing PG and IL-1
    • macrophages take up the crystals and stimulate PG release
  7. 5 triggers of acute gouty arthritis
    • 1. joint trama
    • 2. starvation
    • 3. acidosis
    • 4. alcohol or purine ingestion
    • 5. medications
  8. first choice for gout
    does not lower uric acid levels
    severe diarrhea
    inhibits chemotaxis
    cochicine (colcrys)
  9. 3 uses of gout
    • acute gouty attack
    • prophylaxis of gouty attack
    • mobilization gout
  10. 2nd choice for gout
    efffective at any point during attack
    inhibits PG synthesis
    inhibits phagocytosis of urate crystals
    indomethacin (indocin)
  11. 3 NSAIDS not to be used for gout
    • aspirin
    • salicylates
    • tolmetin
  12. used for gout only when NSAIDS and colchiine are ineffective or contraindicated
  13. prophylaxis for gout
    promotes the excretion of uric acid
    do not use if CrCl < 50 ml/min
    never begin therapy during acute attack
    probenecid (benemid)
  14. what 4 groups would you use allopurinol in
    • overproducers
    • history of renal stones
    • impaired renal function
    • lymphoproliferative disorder
  15. MOA of allopurinol
    competitive antagonist of xanthine oxidase
  16. adverse effects of allopurinol
    • mobilization gout
    • allopurinol hypersensitivity syndrome
    • toxic epidermal necrolysis (TEN)
  17. xanthine oxidase inhibitor
    not a purine analog
    can be used without dose reduction in patients with mild to moderate renal impairment
    febuxostat - (urolic)
  18. indicated for hyperuricemia in children with leukemia, lymphoma and solid-tumor malignancies
    rasburicase (elitek)
  19. generally the first DMARD prescribed
    methotrexate - rheumatrex
  20. also preferred therapy for mild RA
    • hydroxychloroquine
    • sulfasalazine
  21. MOA of methotrexate
    inhibits dihydrofolate reductase that catalyzes the conversion of DHF to THF.
  22. leflunomide MOA
    • oral inhibitor of pyrimidine synthesis
    •       inhibits dihydroorotate dehydgrogenase
  23. DMARD
    oral inhibitor of pyrimidine synthesis
    AE - debilitating diarrhea
    leflunomide - arava
  24. DMARD
    inhibits IL-1 release
    used in combination with methotrexate and sulfasalazine
    AE - nausea
           hemolysis in G6PD deficient subjects
           immediate blurred vision
    hydroxychloroquine - plaquenil
  25. DMARD
    prevents joint erosion 
    inhibits cell proliferation
    ROS scavenger
    AE -lupus-like syndrome
          hemolysis in patients with G6PD   deficiency
    sulfaslazine - azulfidine
  26. DMARD
    AE - drug induced lupus
    C/I - young children and women during pregnancy and breast feeding
    minocycline - minocin
  27. RA agents reserved for moderate to severe disease
    tumor necrosis factor inhibitors
    act more quickly than DMARDs
    biological agents
  28. TNF inhibitor
    recombinant human fusion protein linked to human IgG1 Fc fragment
    etanercept - enbrel
  29. TNF inhibitor
    chimeric human/mouse anti-TNF monoclonal antibody
    given IV
    infliximab - remicade
  30. TNF inhibitor
    recombinant human monoclonal anti-TNF antibody
    adalimumab - humira
  31. TNF inhibitor
    monoclonal antibody approved as monotherapy or in combination with methotrexate
    golimumab - simponi
  32. TNF inhibitor
    humanized pegylated anti-TNF monoclonal antibody
    certolizumab pegol - cimzia
  33. adverse effects of this group of RA drugs are serious infections
    make sure the patient is current on immunizations
    TNF inhibitors
  34. non-tnf biologic
    chimeric monoclonal antibody against CD20
    given with DMARD
    IV infusion
    rituximab - rituxan
  35. non tnf biologic
    genetically engineered fusion protein that interferes with T-cell activation
    IV & SC
    abatacept - orencia
  36. non tnf biologic
    humanized monoclonal antibody that competively inhibits the binding of the pro-inflammatory cytokine interleukin 6 to its receptor
    tociliumab - actemra
  37. non - tnf biologics
    genetically engineered IL-1 receptor antagonist
    least effective biologic DMARD
    anakinra - kineret
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pharmacology test 4 gout & RA
pharmacology test 4 gout