Control of Gout/Hyperuricemia
Adults: PO 100 to 800 mg/day. For amounts over 300 mg, give divided doses.
Secondary Hyperuricemia Associated with Malignancies
Children 6 to 10 yr of age: PO 300 mg/day.
Children under 6 yr of age: PO 150 mg/day.
Prevention of Uric Acid Nephropathy in Vigorous Chemotherapy of Neoplastic Disease
Adults: PO 600 to 800 mg/day for 2 to 3 days.
Reduction of Risk of Acute Gouty Attacks
Adults (initial dose): PO 100 mg/day, increased by 100 mg at weekly intervals until adequate response is achieved or max recommended dose (800 mg/day) is reached.
Leukemia, Lymphoma, Solid Tumor Malignancies
Adults: IV 200 to 400 mg/m2 /day (max 600 mg/day).
Children: IV Starting dose 200 mg/m2 /day.
Inhibits xanthine oxidase, the enzyme responsible for conversion of hypoxanthine to xanthine and then to uric acid.
Use Cautiously in:
CNS: Drowsiness; generalized seizure (injectable); headache; neuritis; paresthesias; peripheral neuropathy.
DERM: Allergic vasculitis; alopecia; ecchymosis; skin rash. Allergic reactions may be severe and sometimes fatal.
EENT: Epistaxis; myopathy; taste disturbance.
GI: Abdominal pain; diarrhea; dyspepsia; gastritis; granulomatous changes; nausea; vomiting.
GU: Renal failure; uremia.
HEMA: Bone marrow depression; eosinophilia; leukocytosis; leukopenia; thrombocytopenia.
HEPA: Cholestatic jaundice; elevated liver enzymes; hepatic necrosis; hepatitis; reversible hepatomegaly.
Acute gouty attacks; arthralgia; fever; myopathy; necrotizing angiitis.
Aluminum salts, uricosuric agents
May lessen effectiveness of allopurinol.
May increase incidence of ampicillin-induced skin rash.
May enhance bone marrow suppression.
Theophylline Cl may be decreased, leading to toxicity.
Thiopurines (eg, azathioprine, mercaptopurine)
Toxicity of these drugs may be increased.
Therapeutic Classification: antigout agents, antihyperuricemics
Pharmacologic Classification: xanthine oxidase inhibitors
Absorption: Well absorbed (80%) following oral administration.
Distribution: Widely distributed in tissue and breast milk.
Protein Binding: <1%.
Metabolism/Excretion: Metabolized to oxypurinol, an active compound with a long half-life. 12% excreted unchanged, 76% excreted as oxypurinol.
Half-life: 1–3 hr (oxypurinol 18–30 hr).
Duration after discontinuation of allopurinol
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