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Drugs used in Gout
•Gout is a form of arthritis caused by excess
uric acid in the bloodstream. The symptoms
of gout are due to the formation of
monosodium urate crystals in the joints and
the body's response to them. Gout most
classically affects the joint in the base of the
big toe
Classification
Acute Arthritis Drugs Chronic Gout
(Urate Lowering Drugs)
Colchicine Allopurinol
NSAID’s Probenecid
Steroids Sulfinpyrazone
Urate Lowering drugs
Decreases synthesis Increases excretion
(uricose uric)
Allopurinol Probenecid
Sulfinpyrazone
Colchicine
Mechanism of action
•Binds to tubulin (microtubular protein ) disrupt
cellular function , such as migration of granulocytes to
affected area
•Inhibits the synthesis and release of leukotrienes &
TNF-α (strong inflammatory mediators)
•Blocks cell division by binding to mitotic spindles
•In Acute gout colchicine 1mg maybe given
orally followed by 0.5-1mg after every 2
hours
•Not an analgesic
Adverse effects
• Diarrhea is a common adverse effect.
• Nausea.
• vomiting
• abdominal cramps.
Chronic use may cause:
• alopecia
• peripheral neuritis
• myopathy.
• Bone marrow depression
Allopurinol
Purine catabolism
Hypoxanthine
Xanthine
xanthine
oxidase
allopurinol inhibits xanthine
oxidase
Uric acid
Adverse effects
• Hypersensitivity
• Hepatotoxicity,
• Bone marrow suppression
• Vasculitis
• Teratogenic
• Steven jhonson syndrome(serious disorder of your skin and mucous membranes. It's usually
a reaction to a medication or an infection. Often, it begins with flu-like symptoms, followed
by a painful red or purplish rash that spreads and blisters).
• Nausea, upper stomach pain, itching, loss of appetite, weight loss, dark urine, clay-colored
stools, jaundice
• Pain or bleeding when urinating
• Joint pain
Probenecid
•Mechanism of action:
weak acid that causes inhibition of a renal
tubular transporter, thereby facilitating the
excretion of the disease causative uric acid by
blocking reuptake.
•Commonly used for prophylaxis of gout and
hyperuricemia.
• t1/2 is 6-12 hours.
•Rapidly absorbed after oral administration.
•Peak plasma level attain within 2-4 hours.
•85-90% bound to plasma protein.
Adverse effects
• Nausea
• Vomiting
• Headache
• Skin rashes
• Hepatic necrosis
• Aplastic anemia
Sulfinpyrazone
•Mechanism of action:
competitively inhibits the reabsorption of uric
acid at the proximal convoluted tubule, thereby
facilitating urinary excretion of uric acid and
decreasing plasma urate concentrations.
Adverse effects
•Nausea.
•heartburn.
•Dizziness.
• ringing in the ears.

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Drugs used in gout

  • 2. •Gout is a form of arthritis caused by excess uric acid in the bloodstream. The symptoms of gout are due to the formation of monosodium urate crystals in the joints and the body's response to them. Gout most classically affects the joint in the base of the big toe
  • 3. Classification Acute Arthritis Drugs Chronic Gout (Urate Lowering Drugs) Colchicine Allopurinol NSAID’s Probenecid Steroids Sulfinpyrazone
  • 4. Urate Lowering drugs Decreases synthesis Increases excretion (uricose uric) Allopurinol Probenecid Sulfinpyrazone
  • 6. Mechanism of action •Binds to tubulin (microtubular protein ) disrupt cellular function , such as migration of granulocytes to affected area •Inhibits the synthesis and release of leukotrienes & TNF-α (strong inflammatory mediators) •Blocks cell division by binding to mitotic spindles
  • 7. •In Acute gout colchicine 1mg maybe given orally followed by 0.5-1mg after every 2 hours •Not an analgesic
  • 8. Adverse effects • Diarrhea is a common adverse effect. • Nausea. • vomiting • abdominal cramps. Chronic use may cause: • alopecia • peripheral neuritis • myopathy. • Bone marrow depression
  • 10. Adverse effects • Hypersensitivity • Hepatotoxicity, • Bone marrow suppression • Vasculitis • Teratogenic • Steven jhonson syndrome(serious disorder of your skin and mucous membranes. It's usually a reaction to a medication or an infection. Often, it begins with flu-like symptoms, followed by a painful red or purplish rash that spreads and blisters). • Nausea, upper stomach pain, itching, loss of appetite, weight loss, dark urine, clay-colored stools, jaundice • Pain or bleeding when urinating • Joint pain
  • 11. Probenecid •Mechanism of action: weak acid that causes inhibition of a renal tubular transporter, thereby facilitating the excretion of the disease causative uric acid by blocking reuptake.
  • 12. •Commonly used for prophylaxis of gout and hyperuricemia. • t1/2 is 6-12 hours. •Rapidly absorbed after oral administration. •Peak plasma level attain within 2-4 hours. •85-90% bound to plasma protein.
  • 13. Adverse effects • Nausea • Vomiting • Headache • Skin rashes • Hepatic necrosis • Aplastic anemia
  • 14. Sulfinpyrazone •Mechanism of action: competitively inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby facilitating urinary excretion of uric acid and decreasing plasma urate concentrations.