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26 Cards in this Set
- Front
- Back
Gout what is it
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characterized biochemically by hyperuricemia and clinically by episodes of severe, acute arthritis due to deposits of monosodium urate in joints and cartilage.
i.e., IMBALANCE OF URIC ACID -- OVERPRODUCTION & UNDERSECRETION |
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The untreated disease may develop through four stages.
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1. Asymptomatic hyperuricemia: 90% due to undersecretion of uric acid.
2. Acute gouty arthritis - - PAINFUL; inflammation • Urate deposits in synovial space • First metatarsophalangeal joint--“Hot Toe” 3.Asymptomatic intercritical period 4.Chronic tophaceous gout • Tophi: Chalky aggregates of monosodium urate monohydrate in joints, cartilage, tendon, bursae. • Destructive arthropathy; ulceration URATE STONES IN KIDNEY |
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Principal objectives of treatment are:
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1. Terminate the inflammatory process of an acute attack.
2. Reduce hyperuricemia: Prevent formation of urate deposits and recurrent attacks; resolution of tophi. |
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DRUGS USED FOR ACUTE ATTACKS OF GOUTY ARTHRITIS
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1. Nonsteroidal anti-inflammatory drug(NSAID’s)--DOC
- Indomethacin (Indocin) - naproxen (Naprosyn; Anaprox) - ibuprofen (Motrin) 2. Colchicine 3. Adrenal corticosteroids and corticotropin (ACTH): “Last resort” |
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Colchicine
MOA |
INHIBITS PHAGOCYTOSIS BY & release of chemotactic factors by NEUTROPHILS
Binds tubulin and inhibits mictotubule formation |
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Colchicine: route
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IV or oral
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Colchicine: Clinical Use
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ACUTE gouty arthritis if you can't use NSAIDS. Will relieve pain 12-24 hrs
Chronic gout to prevent acute flair up when using allopurinol or probenecid |
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Colchicine
Adverse reactions: |
NV, Diarrhea, abdominal cramping (80%)
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Colchicine
Overdose toxicity: |
NV, bloody diarrhea,vascular damage, shock, kidney damage, blood dyscrasias, CNS toxicity,etc.
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Colchicine
Contraindications: |
Serious GI, renal, hepatic or cardiac disease; bone marrow depression.
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Indomethacin (Indocin)
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most common NSAID used for ACUTE gout-- short term relief of pain, inflammation.
watch for GI upset. Contridicted in renal failure or CHF. |
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DRUG USED FOR THE CHRONIC TREATMENT OF GOUT:
Uricosuric Agents: |
Probenecid
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Probenecid:
route and excretion |
PO, kidney
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Uricosuric Agent:Probenecid
MOA: effects: |
BLOCKS REABSOPTION OF URIC ACIDS
effects: •increased excretion of uric acid •decreased total body pool of uric acid •tophaceous deposits of urate are reabsorbed •decreased plasma uric acid levels |
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Probenecid enhances the blood levels of penicillins when administered together)
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T/F
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Probenecid
clinical uses |
chronic gout
Less effective if creatinine clearance is < 50 ml/min; maintain adequate hydration |
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Probenecid
Adverse reactions: |
GI irritation - - especially
Intrarenal precipitation of uric acid Hypersensitivity reactions: -Erythema, pruritus May precipitate an attack of acute gouty arthritis - - avoided by simultaneously giving colchicine. |
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Probenecid
Contraindications, cautions, drug interactions: |
• History of peptic ulcer or renal calculi
• Blood dyscrasias; leukopenia • Plenty of fluids; alkalinize urine • Do NOT initiate therapy during acute attack |
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Probenecid
drug interactions: |
salicylates
sulfonamides indomethacin oral hypoglycemic agents rifampin. |
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Allopurinol (Zyloprim; Lopurin)
Route |
PO
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Allopurinol (Zyloprim; Lopurin)
MOA |
INHIBITS XO & URATE SYNTHESIS
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Allopurinol (Zyloprim; Lopurin)
Effects: |
• Plasma uric acid level decreases
• Total body pool of uric acid is decreased • Tophi are reabsorbed and formation inhibited • Urinary excretion of uric acid is decreased • Uric acid stone formation is decreased |
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Allopurinol (Zyloprim; Lopurin)
Clinical use: |
Chronic tophaceous gout and in patients with renal urate stones - - preferred
Treatment of hyperuricemia associated with excessive production of uric acid. |
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Allopurinol (Zyloprim; Lopurin)
Adverse reactions: |
Attacks of acute gouty arthritis may occur when therapy initiated; start with low dose and use with colchicine.
Occasionally - - headache, drowsiness, GI effects Hypersensitivity reactions: rash, pruritus (1-3%) • Exfoliative dermatitis; urticaria; blood dyscrasias; peripheral neuritis; liver toxicity – rare. |
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Allopurinol (Zyloprim; Lopurin)
Contraindications, cautions, and drug interactions |
Do not use if a severe reaction has previously occurred
Do not initiate therapy during acue attack • Plenty of fluids; alkalinize urine • Renal insufficiency; liver disease; blood dyscrasias |
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Allopurinol (Zyloprim; Lopurin)
and drug interactions |
-- probenecid
-- mercaptopurine and azathioprine -- oral anticoagulants -- ampicillin - - rash |