NSAIDs 2 - Gout Flashcards
(27 cards)
What is gout?
Acute arhtiritis due to deposits of urate crystals in joints and cartilage
Crystals activate cytokine response
High serum uric acid levels occur due to increased production or decreased excretion
What acute therapy options do we have for gout?
Colchicine NSAIDs (Indomethacin, Ibuprofen, Naproxen)
What is colchicine?
Anti-inflammatory used only in gout
Works by reducing motility leukocytes, binds tubulin
Adverse effects of colchicine?
Nausea, vomiting, diarrhea
Cramps
All of these are signs of toxicity
D/c drug if they occur
Toxicity of colchicine can lead to what?
Bone marrow suppression
Renal toxicity
What NSAIDs are used for acute treatment of gout?
Indomethacin
Ibuprofen
Naproxen
NOT aspirin - because acetylsalicylic acid inhibits uric acid secretion
These have replaced colchicine as first line agents
What is first line treatment for acute gout attacks?
NSAIDs
Indomethacin
Ibuprofen
Naproxen
How is chronic gout treated?
By decreasing production of uric acid or Increasing excretion of uric acid or Increasing metabolism of uric acid to allantoin for excretion (Rasburicase! but this is for hyperuricemia caused by leukemia)
What is allopurinol?
Xanthine oxidase inhibitor
This enzyme converts purines to hypoxanthine, which is converted to xanthine and uric acid
Pharmacokinetics of allopurinol?
Rapidly absorped
Active metabolite oxypurinol has a 20 hour half life
Toxicities of allopurinol?
Nausea
vomiting
hepatitis
Skin rashes
25% of patients cant tolerate the side effects
Cautions with allopurinol?
Avoid in kidney, liver, or heart problems
What is Febuxostat?
Non-purine, noncompetitive selective inhibitor of xanthine oxidase
(More selective than allopurinol!)
How is Febuxostat administered?
Orally absorbed (so I assume PO)
Toxicities with Febuxostat?
Nausea, vomiting, diarrhea
Abnormal liver function tests
Hypersensitivity
Gout flair ups (lol…)
INCREASED INCIDENCE OF MI AND STROKE in trials
Cautions with Febuxostat?
Avoid in cardiac, renal, hepatic disease
Counsel on shortness of breath and chest pain
2012 FDA warning on hepatic problems
What agents decrease production of uric acid?
Allopurinol
Febuxostat
Which agents increase excretion of uric acid?
Probenecid
Sulfinpyrazone
Rasburicase
What is probenecid?
Drug combined with colchicine to increase excretion of uric acid by preventing re-absorption in the kidney
It competes with uric acid in the transporters in the proximal tubule to prevent uric acid from being re-absorbed
How is probenecid administered?
Orally
MUST be taken with water to prevent urate stones in the kidney
Start low and increase dose to therapeutic effect
Adverse effects of probenecid?
Skin rashes
What is Sulfinpyrazone?
Analog of phenylbutazone, a strong acid that prevents uric acid re-absorption in the renal tubule
How is Sulfinpyrazone administered?
Oral administration
Stay hydrated to prevent urate stones in the kidney
Adverse effects of Sulfinpyrazone?
Gi irritation in 10-15% of patients
Hematological problems
Nausea, vomiting
Urate stones in kidney - stay hydrated
