Anti Gout Drugs

Anti Gout Drugs
ANTI GOUT DRUGS

Gout is a metabolic disorder characterized
by high levels of uric acid in the blood
(hyperuricemia).
● It can lead to deposition of sodium

urate crystals in tissues, especially
the joints and kidneys.
Hyperuricemia does not always lead to

gout, but gout is always preceded by
hyperuricemia.
● Normal urate level 1-4mg/dL.

● The aim of therapy is to lower uric
acid level below 6mg/dL
(saturation point)
DRUGS USED IN GOUT
ACUTE GOUT
NSAIDs
Colchicine
Corticosteroids
CHRONIC GOUT / HYPERURICAEMIA
Uricosurics:
Probenecid
Sulfinpyrazone
Synthesis inhibitor:
Allopurinol
Febuxostat
SAMSON’S MEDLIN 9747 987 000 1

Anti Gout Drugs
ACUTE GOUT
Acute gout manifests as sudden onset of severe inflammation in a small joint (commonest is
metatarso-phalangeal joint of great toe) due to precipitation of urate crystals in the joint
space.
The joint becomes red, swollen and extremely painful and requires immediate treatment.
NSAIDs:
● Indomethacin, Naproxen, Piroxicam, Diclofenac and Etoricoxib

● Indomethacin is the NSAID of choice
● They decrease the movement of granulocytes into the affected area.
● Decrease pain and inflammation.
Aspirin is contraindicated, because it competes with uric acid for the organic acid secretion
in the proximal tubule of the kidney.
CORTICOSTEROIDS:
Intraarticular administration of glucocorticoids (when only one or two joints are affected) is
also appropriate in the acute settings. Prednisolone 40–60 mg may be given in one day,
followed by tapering doses over few weeks.
COLCHICINE:
● It is an alkaloid from Colchicum autumnale.

● Colchicine is neither analgesic nor anti-inflammatory, but it specifically suppresses
gouty inflammation. It does not inhibit the synthesis or promote the excretion of uric
acid. Thus, it has no effect on blood uric acid levels.
● Colchicine binds to tubulin and cause its depolymerization leading to disruption of
cellular functions.
● Decreases the migration of granulocytes into the affected area.
● It blocks cell division
● It also inhibits the synthesis and release of the leukotrienes.
Pharmacokinetics
Colchicine is rapidly absorbed orally, partly metabolized in liver and excreted in

bile—undergoes enterohepatic circulation; ultimate disposal occurs in urine and
faeces over many days.
● Orally administered
● Should not be used in pregnancy
● Should be avoided if creatinine clearance is less than 10 ml/min

Anti Gout Drugs
Adverse effects: Nausea, Vomiting, Abdominal pain, Diarrhoea.
Chronic administration may lead to: Myopathy, Neutropenia, Aplastic anaemia, Alopecia
Other uses:
● Antimitotic: causes metaphase arrest (It was tried for cancer chemotherapy but
abandoned due to toxicity).
● To induce polyploidy in plants
CHRONIC GOUT:
The pain and stiffness are persisting in the joints between attacks. There will be
hyperuricaemia, tophi (chalk-like stones under the skin in pinna, eyelids, nose, around joints
and other places) and urate stones in the kidney.
URICOSURIC DRUGS:
PROBENCID
● It is a highly lipid-soluble organic acid.

● At therapeutic dose, blocks proximal tubular reabsorption of uric acid. At low dosage,
these agents block proximal tubular secretion of uric acid.
● It inhibits renal tubular secretion of penicillin thus the duration of action of penicillin
can be prolonged.
Interactions:
1. In addition to Penicillins, Probenecid inhibits the urinary excretion of Cephalosporins,

Sulfonamides, Methotrexate and Indomethacin.
2. It inhibits biliary excretion of rifampicin. Pyrazinamide and ethambutol may interfere with
uricosuric action of probenecid.
3. Probenecid inhibits tubular secretion of nitrofurantoin which may not attain antibacterial
concentration in urine.
4. Salicylates block uricosuric action of probenecid.
Pharmacokinetics
Probenecid is completely absorbed orally; 90% plasma protein bound: partly conjugated in
liver and excreted by the kidney; plasma t½ is 8–10 hours.
Adverse effects
Dispepsia is the most common side effect.
Toxic doses cause convulsions and respiratory failure.

Anti Gout Drugs
SULFINPYRAZONE
● It is a pyrazolone derivative related to phenylbutazone with uricosuric action.

● At therapeutic doses, it inhibits tubular reabsorption of uric acid, but smaller doses
can decrease urate excretion as do small doses of probenecid.
● Its uricosuric action is additive with probenecid but antagonised by salicylates.
● It inhibits platelet aggregation.
Adverse effects
Gastric irritation is the most common side effect—contraindicated in patients with peptic
ulcer.
URIC ACID SYNTHESIS INHIBITOR:
ALLOPURINOL
● It is a purine analogue.
● It reduces the production of uric acid by competitively inhibiting the enzyme
xanthine oxidase.
Pharmacokinetics:
● Completely absorbed after oral administration

● The t1/2 of allopurinol is 2 hours. Major metabolite is alloxanthine (oxypurinol) which
is also a xanthine oxidase inhibitor property with a half-life of 15 to 18 hours. Thus it
is suitable for once daily dosage.
Adverse drug reaction:
● Hypersensitivity reactions- especially skin rashes.

● GI side effects -nausea and diarrhoea.
FEBUXOSTAT
● Non purine xanthine oxidase inhibitor.

● The most important adverse effect is liver damage; liver function needs to be
monitored during febuxostat therapy
Drug interactions: Both Allopurinol and Febuxostat interferes with the metabolism of 6
mercaptopurine, Azathioprine and Theophylline requiring a reduction in dosage of these
drugs.
RASBURICASE
● It is a new recombinant xanthine oxidase enzyme that oxidizes uric acid to soluble
and easily excreted allantoin.
● indicated only for preventing chemotherapy associated hyperuricaemia

Anti Gout Drugs
PEGLOTICASE
● A recombinant form of the enzyme urate oxidase or uricase.

● Converts uric acid to allantoin.
● It is indicated for patients with gout who fail treatment with standard therapies such
as xanthine oxidase inhibitors.
● It is administered as IV infusion every 2 weeks.

Anti Gout Drugs

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Anti Gout Drugs

ANTI GOUT DRUGS

● It can lead to deposition of sodium

Hyperuricemia does not always lead to

● Normal urate level 1-4mg/dL.

DRUGS USED IN GOUT

SAMSON’S MEDLIN 9747 987 000 1

● Indomethacin, Naproxen, Piroxicam, Diclofenac and Etoricoxib

● It is an alkaloid from Colchicum autumnale.

Colchicine is rapidly absorbed orally, partly metabolized in liver and excreted in

SAMSON’S MEDLIN 9747 987 000 2

Adverse effects: Nausea, Vomiting, Abdominal pain, Diarrhoea.

● It is a highly lipid-soluble organic acid.

1. In addition to Penicillins, Probenecid inhibits the urinary excretion of Cephalosporins,

4. Salicylates block uricosuric action of probenecid.

Dispepsia is the most common side effect.

Toxic doses cause convulsions and respiratory failure.

SAMSON’S MEDLIN 9747 987 000 3

● It is a pyrazolone derivative related to phenylbutazone with uricosuric action.

URIC ACID SYNTHESIS INHIBITOR:

● Completely absorbed after oral administration

Adverse drug reaction:

● Hypersensitivity reactions- especially skin rashes.

● Non purine xanthine oxidase inhibitor.

SAMSON’S MEDLIN 9747 987 000 4

● A recombinant form of the enzyme urate oxidase or uricase.

SAMSON’S MEDLIN 9747 987 000 5

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