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Uses

Gout

Reduction of serum and urinary uric acid concentrations in primary and secondary gout. In early uncomplicated gout, preferred over uricosurics in patients with urinary uric acid excretion >900 mg daily and in those with gouty nephropathy, urinary tract stones or obstruction, or azotemia.

Management of gout when uricosuric agents cannot be used because of adverse effects, allergy, or inadequate response; when there are visible tophi or radiographic evidence of uric acid deposits and stones; or when serum urate concentrations exceed 8.5–9 mg/dL and patient has family history of tophi and low urate excretion.

Management of primary or secondary gouty nephropathy with or without secondary oliguria.

Not recommended for management of asymptomatic hyperuricemia; however, some clinicians have suggested that therapy be initiated when serum urate concentrations exceed 9 mg/dL (by colorimetric method) because these concentrations often are associated with increased joint changes and renal complications.

Of no value in the treatment of acute gout attacks (due to lack of analgesic or anti-inflammatory activity).

Chemotherapy-induced Hyperuricemia

A component of therapy (with urinary alkalinization and IV hydration) in patients with leukemia, lymphoma, and solid tumor malignancies who are undergoing cancer therapy expected to result in tumor lysis and subsequent elevations of serum and urinary uric acid concentrations.

Oral allopurinol may be slower and less effective in decreasing plasma uric acid concentrations than IV rasburicase.

Recurrent Renal Calculi

Management of recurrent calcium oxalate renal calculi in males and females whose urinary urate excretion exceeds 800 and 750 mg daily, respectively.

Prevention of uric acid renal calculi in patients with history of recurrent stone formation.

Other Uses

Has been used to reduce hyperuricemia secondary to glucose-6-phosphate dehydrogenase deficiency†, Lesch-Nyhan syndrome†, polycythemia vera†, or sarcoidosis† or secondary to administration of thiazides† or ethambutol†.

Dosage and Administration

General

• Maintain fluid intake to yield daily urine output of ≥2 L. Maintain neutral or, preferably, alkaline urine.

Gout

• Transition period of several months may be required when allopurinol is added to regimen of colchicine, uricosuric agents, and/or anti-inflammatory agents. During transition period, administer drugs concomitantly, adjusting allopurinol dosage to achieve normal serum urate concentrations and freedom from acute gouty attacks for several months. Withdraw uricosuric agent gradually over several weeks.

Chemotherapy-induced Hyperuricemia

• For prevention of acute uric acid nephropathy in patients undergoing chemotherapy, begin allopurinol treatment 24–48 hours before initiating chemotherapy.

Administration

Administer orally or by IV infusion.

Oral Administration

Usually administered orally once daily, preferably after meals. If oral dose >300 mg, administer in divided doses.

IV Infusion

For solution and drug compatibility information, see Stability under Compatibility.

Reconstitution

Reconstitute vial containing allopurinol sodium equivalent to 500 mg of allopurinol with 25 mL of sterile water for injection to provide a solution containing 20 mg/mL of allopurinol. Should be diluted further before IV administration.

Dilution

Dilute concentrate containing allopurinol 20 mg/mL with a compatible IV solution (see Solution Compatibility under Stability) to a final concentration of ≤6 mg/mL. Do not use diluent containing sodium bicarbonate.

Rate of Administration

Administer daily dosage by continuous infusion or in equally divided intermittent IV infusions at 6-, 8-, or 12-hour intervals. Infusion rate depends on volume of infusate.

Dosage

Available as allopurinol (oral) or allopurinol sodium (for IV use); dosage is expressed in terms of allopurinol.

Pediatric Patients

Chemotherapy-induced Hyperuricemia

Oral

Children <6 years of age: Initially, 150 mg daily.

Children 6–10 years of age: Initially, 300 mg daily.

Adjust dosage after about 48 hours according to patient response.

IV

Children ≤10 years of age: Initial dosage of 200 mg/m² daily.

Children >10 years of age: 200–400 mg/m² daily.

Adults

Gout

Oral

Initially, 100 mg daily. May increase dosage by 100 mg weekly until serum urate concentration falls to ≤6 mg/dL or until maximum recommended dosage of 800 mg daily is reached. Usual dosage is 200–300 mg daily in patients with mild gout and 400–600 mg daily in those with moderately severe tophaceous gout.

After serum urate concentrations are controlled, dosage reduction may be possible; average maintenance dosage is 300 mg daily, and minimum effective dosage is 100–200 mg daily.

Chemotherapy-induced Hyperuricemia

Oral

600–800 mg daily for 2–3 days.

IV

200–400 mg/m² daily.

Recurrent Calcium Oxalate Renal Calculi

Oral

Initially, 200–300 mg daily. Titrate dosage based on 24-hour urinary urate determinations.

Prescribing Limits

Pediatric Patients

IV

Children >10 years of age: Maximum 600 mg daily.

Adults

Oral

Maximum 800 mg daily.

IV

Maximum 600 mg daily.

Special Populations

Dosage in Renal Impairment

Oral

IV