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Chapter 74. Drug Therapy of Gout. Gout. Recurrent inflammatory disorder Seen mainly in men Hyperuricemia Uric acid level greater than 7 mg/dL in men or greater than 6 mg/dL in women Uric acid crystals deposited in joints Episodes of severe joint pain (typically in large toe) Causes

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chapter 74

Chapter 74

Drug Therapy of Gout

slide2
Gout
  • Recurrent inflammatory disorder
    • Seen mainly in men
  • Hyperuricemia
    • Uric acid level greater than 7 mg/dL in men or greater than 6 mg/dL in women
    • Uric acid crystals deposited in joints
  • Episodes of severe joint pain (typically in large toe)
  • Causes
    • Excessive production of uric acid
    • Impaired renal excretion of uric acid
overview of drug therapy
Overview of Drug Therapy
  • Short-term to relieve symptoms of attack
    • Infrequent flare-ups (fewer than 3 times/yr)
    • NSAIDs: first-line agents
    • Glucocorticoids also used
  • Long-term to lower blood levels of uric acid
    • 3 or more times per year
    • Uricosuric drugs
nsaids
NSAIDs
  • Agents of first choice for gouty arthritis
    • Better tolerated and more predictable than colchicine
    • Relief should be within 24 hours; swelling subsides over the next few days
  • Adverse effects
    • GI ulceration, decreased renal function, fluid retention, increased risk of cardiovascular events
nsaids1
NSAIDs
  • Indomethacin (Indocin)
  • Naproxen (Naprosyn)
  • Diclofenac (Voltaren)
glucocorticoids
Glucocorticoids
  • Highly effective in relieving pain
  • Useful for patients who are hypersensitive to, are unresponsive to, or have medical conditions that contraindicate the use of NSAIDs
  • Avoid in patients prone to hyperglycemia
colchicine
Colchicine
  • Anti-inflammatory agent
    • No longer the first-line drug
    • Now reserved for patients who are unresponsive/intolerant to safer agents
  • Uses
    • Treats acute gouty attack
    • Reduces incidences of attack
    • Aborts an impending attack
colchicine1
Colchicine
  • Mechanism of action
  • Pharmacokinetics
  • Adverse effects
    • Gastrointestinal
    • Myelosuppression
    • Myopathy
  • Drug interaction
drug therapy for hyperuricemia
Drug Therapy for Hyperuricemia
  • Goals of therapy
    • Promote dissolution of urate crystals
    • Prevent new crystal formation
    • Prevent disease progression
    • Reduce the frequency of acute attacks
    • Improve quality of life
  • Note: Because these drugs have no analgesic or anti-inflammatory actions, they are not useful in an acute gouty attack
drug therapy for hyperuricemia1
Drug Therapy for Hyperuricemia
  • Allopurinol (Zyloprim)
    • Inhibits uric acid formation
  • Febuxostat (Uloric)
    • Inhibits uric acid formation
  • Probenecid (Benemid)
    • Increases uric acid excretion
  • Sulfinpyrazone (Anturane)
    • Increases uric acid excretion
allopurinol zyloprim
Allopurinol (Zyloprim)
  • Reduces blood levels of uric acid
  • Uses
    • Chronic tophaceous gout
    • Hyperuricemia due to chemotherapy
  • Adverse effects (generally well tolerated)
    • Hypersensitivity syndrome
    • Gastrointestinal effects
    • Neurologic effects
febuxostat uloric
Febuxostat (Uloric)
  • Reduces blood levels of uric acid
  • Uses
    • Chronic tophaceous gout
  • Adverse effects (uncommon)
    • Liver function abnormalities
    • Nausea
    • Arthralgia
    • Rash
probenecid generic only
Probenecid (Generic Only)
  • Acts on renal tubules to inhibit reabsorption of uric acid
    • Prevents formation of new tophi and helps existing tophi decrease
  • May exacerbate acute episodes of gout
    • Add indomethacin for relief
  • Adverse effects
    • Usually well tolerated, but mild GI effects occasionally occur; take with food
  • Drug interactions