Allopurinol

Indications
 Oral
Hyperuricaemia
Adult: Initially, 100 mg daily increased according to response until the plasma conc of urate is reduced to ≤6 mg/100 ml. Maintenance: 100-300 mg daily for mild to moderate gout; up to 600 mg daily for moderately severe tophaceous gout. Max: 800 mg daily. Up to 300 mg may be taken as a single dose; larger doses should be taken in divided doses to minimise gastric irritation.
Renal impairment: Max initial dose: 100 mg daily, increase only if the response is inadequate. Severe impairment: Doses should be <100 mg daily or 100 mg at intervals >1 day. Patients receiving dialysis 2-3 times/wk: 300-400 mg immediately after dialysis only. Adjust dose to maintain plasma-oxipurinol concentrations <15.2 mcg/ml.
Hepatic impairment: Dose reduction may be needed. Monitor liver function regularly.
Oral
Gout
Adult: Initially, 100 mg daily increased according to response until the plasma conc of urate is reduced to ≤6 mg/100 ml. Maintenance: 100-300 mg daily for mild to moderate gout; up to 600 mg daily for moderately severe tophaceous gout. Max: 800 mg daily. Up to 300 mg may be taken as a single dose; larger doses should be taken in divided doses to minimise gastric irritation.
Renal impairment: Max initial dose: 100 mg daily, increase only if the response is inadequate. Severe impairment: Doses should be <100 mg daily or 100 mg at intervals >1 day. Patients receiving dialysis 2-3 times/wk: 300-400 mg immediately after dialysis only. Adjust dose to maintain plasma-oxipurinol concentrations <15.2 mcg/ml.
Hepatic impairment: Dose reduction may be needed. Monitor liver function regularly.
Oral
Prophylaxis of uric acid nephropathy associated with cancer therapy
Adult: 600-800 mg/day in 2-3 divided doses for 2-3 days before starting cancer treatment. Ensure adequate fluid intake. Maintenance for patients with hyperuricaemia secondary to cancer or cancer therapy: 100-300 mg daily for mild to moderate gout; up to 600 mg daily for moderately severe tophaceous gout. Max: 800 mg daily. Dose is titrated based on response. Up to 300 mg may be taken as a single dose; larger doses should be taken in divided doses to minimise gastric irritation.
Child: <15 yr: 10-20 mg/kg daily. Max: 400 mg daily.
Renal impairment: Max initial dose: 100 mg daily, increase only if the response is inadequate. Severe impairment: Doses should be <100 mg daily or 100 mg at intervals >1 day. Patients receiving dialysis 2-3 times/wk: 300-400 mg immediately after dialysis only. Adjust dose to maintain plasma-oxipurinol concentrations <15.2 mcg/ml.
Hepatic impairment: Dose reduction may be needed. Monitor liver function regularly.
Oral
Recurrent calcium oxalate stones
Adult: 200-300 mg daily, may be given as a single dose or in divided doses. Dose is adjusted based on subsequent 24-hr urinary urate excretion.
Renal impairment: Max initial dose: 100 mg daily, increase only if the response is inadequate. Severe impairment: Doses should be <100 mg daily or 100 mg at intervals >1 day. Patients receiving dialysis 2-3 times/wk: 300-400 mg immediately after dialysis only. Adjust dose to maintain plasma-oxipurinol concentrations <15.2 mcg/ml.
Hepatic impairment: Dose reduction may be needed. Monitor liver function regularly.
Intravenous
Cancer therapy-induced hyperuricaemia
Adult: 200-400 mg/m2 daily given as a single dose or equally divided doses at 6-, 8- or 12-hr intervals; given as an infusion over 15-60 minutes. Max: 600 mg daily. Therapy should be started 24-48 hr before initiating the treatment. Ensure sufficient fluid intake to produce a daily urinary output of at least 2 L and maintenance of a neutral, or slightly alkaline urine.
Child: ≤10 yr: Start with 200 mg/m2 daily; >10 yr: 200-400 mg/m2 daily (max: 600 mg/day). Dose can be given as a single dose or equally divided doses at 6-, 8- or 12-hr intervals; infuse over 15-60 minutes. Therapy should be started 24-48 hr before initiating the chemotherapy treatment.
Renal impairment: Haemodialysis: Administer dose after session or administer 50% supplemental dose.
CrCl (ml/min)Dosage Recommendation
10-20200 mg daily.
<3100 mg daily at extended intervals.
3-10100 mg daily.
Hepatic impairment: Dose reduction may be needed. Monitor liver function regularly.

Special Populations: Reduce dose in patients with renal impairment.

Reconstitution: Recommended to further dilute the reconstituted solution to ≤6 mg/ml with normal saline or 5% dextrose solution.
Incompatibility: Y-site incompatibility: Amikacin sulfate, amphotericin B, carmustine, cefotaxime sodium, chlormethine hydrochloride, chlorpromazine hydrochloride, cimetidine hydrochloride, clindamycin phosphate, cytarabine, dacarbazine, daunorubicin hydrochloride, diphenhydramine hydrochloride, doxorubicin hydrochloride, doxycycline hyclate, droperidol, floxuridine, gentamicin sulfate, haloperidol lactate, hydroxyzine hydrochloride, idarubicin hydrochloride, imipenem with cilastatin sodium, methylprednisolone sodium succinate, metoclopramide hydrochloride, minocycline hydrochloride, nalbuphine hydrochloride, netilmicin sulfate, ondansetron hydrochloride, pethidine hydrochloride, prochlorperazine edisilate, promethazine hydrochloride, sodium bicarbonate, streptozocin, tobramycin sulfate and vinorelbine tartrate.
Contraindications
 Hypersensitivity; acute attack of gout.
Warnings / Precautions
 Ensure adequate fluid intake. Prophylactically with an anti-inflammatory or colchicine for at least 1 mth. Withdraw immediately when sensitivity (skin rash, etc) appears. Pregnancy, lactation. Hepatic and renal impairment.
Adverse Reactions
 Rash; alopoecia; GI disorders, taste disturbances, nausea, vomiting, abdominal pain, diarrhoea; paraesthesia, peripheral neuropathy, vertigo, headache, hepatic necrosis, drowsiness, neuritis, arthralgia; hypertension.
Potentially Fatal: Stevens-Jonhson and/or Lyell's Syndrome (urticaria, fever, lymphadenopathy, arthralgia). Occasionally, thrombocytopaenia, agranulocytosis and aplastic anaemia.
Drug Interactions
 Increased risk of skin rash when used with ampicillin or amoxicillin. May prolong half-life of chlorpropamide and dicumarol. May increase serum levels of ciclosporin. May increase bone marrow depression when used with cyclophosphamide
Potentially Fatal: Increased haematological effects of azathioprine and mercaptopurine when co-administered with allopurinol.
See Below for More allopurinol Drug Interactions
Mechanism of Actions
 Allopurinol is an inhibitor of the enzyme xanthine oxidase which converts hypoxanthine to xanthine then uric acid. The reduced production of uric acid relieves all symptoms associated with hyperuricaemia and gout. Inhibition of xanthine oxidase leads to accumulation of its substrates hypoxanthine and xanthine but since their renal clearance is more than 10 times that of uric acid, there is no risk of nephrolithiasis.
Absorption: 90% of the dose is absorbed from the GI tract (oral); peak plasma concentrations after 1-2 hrs.
Distribution: Enters breast milk. Protein-binding: None.
Metabolism: Converted to oxipurinol (alloxanthine).
Excretion: Urine (as unchanged drug and metabolite), faeces. Elimination half-life: 1-2 hr (allopurinol), 15 hr (oxipurinol).
Administration
 Should be taken with food. (Take immediately after meals.)
Storage Conditions
 Intravenous: Powder for inj: Store at 15-30°C. After reconstitution: Store at 20-25°C. Solution should be used within 10 hr of preparation. Oral: Store below 25°C.
ATC Classification
 M04AA01 - allopurinol ; Belongs to the class of preparations inhibiting uric acid production. Used in the treatment of gout.
Storage
 Intravenous: Powder for inj: Store at 15-30°C. After reconstitution: Store at 20-25°C. Solution should be used within 10 hr of preparation. Oral: Store below 25°C.
Available As
  • Allopurinol 100 mg
  • Allopurinol 200 mg
  • Allopurinol 250 mg
  • Allopurinol 300 mg

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