Overview of Gout
- Gout: A form of inflammatory
arthritis due to deposition of monosodium urate crystals.
- Cause: Hyperuricemia (serum
uric acid > 6.8 mg/dL)
- Management goals:
- Terminate acute attacks
- Prevent future attacks
- Lower serum uric acid
levels
Classification
of Anti-Gout Drugs
- Acute Attack Treatment:
- Colchicine
- NSAIDs
- Corticosteroids
- Chronic Management:
- Uricostatic agents (e.g.,
Allopurinol, Febuxostat)
- Uricosuric agents (e.g.,
Probenecid, Sulfinpyrazone)
- Class: Xanthine oxidase inhibitor
- Mechanism of Action:
- Inhibits xanthine oxidase
enzyme
- Decreases production of
uric acid
- Indications:
- Chronic gout
- Prevention of uric acid
nephropathy
- Tumor lysis syndrome
- Adverse Effects:
- Rash (can be severe - SJS)
- GI upset
- Hepatotoxicity
- Hypersensitivity syndrome
- Drug Interactions:
- Increases effect of
azathioprine and 6-mercaptopurine
- Requires dose reduction
with these drugs
Febuxostat
- Class: Selective xanthine oxidase
inhibitor
- Mechanism of Action:
- Non-purine selective
inhibitor of xanthine oxidase
- Reduces serum uric acid
- Indications:
- Chronic hyperuricemia in
gout
- Adverse Effects:
- Liver function
abnormalities
- Cardiovascular events
(boxed warning)
- Rash, nausea
- Drug Interactions:
- Same as allopurinol
(azathioprine, mercaptopurine)
Colchicine
- Class: Microtubule inhibitor
- Mechanism of Action:
- Binds tubulin, inhibits
neutrophil motility and activity
- Reduces inflammation in
gouty arthritis
- Indications:
- Acute gout attacks
- Gout prophylaxis
- Adverse Effects:
- GI upset (diarrhea, nausea,
vomiting)
- Myopathy and neuropathy
(especially with renal impairment)
- Bone marrow suppression
(rare)
- Drug Interactions:
- CYP3A4 and P-gp inhibitors
(e.g., clarithromycin, cyclosporine) increase toxicity
Probenecid
- Class: Uricosuric agent
- Mechanism of Action:
- Inhibits reabsorption of
uric acid in renal tubules
- Increases urinary excretion
of uric acid
- Indications:
- Chronic gout
(underexcreters of uric acid)
- Adverse Effects:
- Uric acid kidney stones
- GI irritation
- Rash
- Drug Interactions:
- Inhibits excretion of many
drugs (penicillin, NSAIDs)
- Increases risk of toxicity
Sulfinpyrazone
- Class: Uricosuric agent
- Mechanism of Action:
- Similar to probenecid
- Promotes renal excretion of
uric acid
- Indications:
- Chronic gout
- Adverse Effects:
- GI irritation
- Rash
- Agranulocytosis (rare)
- Drug Interactions:
- Displaces other drugs from
plasma proteins
- Inhibits metabolism of
warfarin
Presentation for Drugs for Gout
END OF THE CHAPTER
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