Antazone , Anturan , Anturane, Apo-Sulfinpyrazone , Novopyrazone
Classifications: antigout agent; uricosuric; Therapeutic: antigout
Pregnancy Category: C
100 mg tablets; 200 mg capsules
Potent renal tubular blocking agent of uric acid in the kidney that lowers its serum blood level. Like all uricosurics, low
doses may inhibit tubular secretion of uric acid and cause urate retention. Inhibits release of adenosine diphosphate and
5-hydroxytryptophan, and thus decreases platelet adhesiveness and increases platelet survival time; has no effect on prothrombin
or blood clotting time.
Promotes urinary excretion of uric acid and reduces serum urate levels by competitively inhibiting tubular reabsorption
of uric acid in the kidney.
Maintenance therapy in chronic gouty arthritis and tophaceous gout.
Drug-induced hyperuricemia, to decrease platelet aggregation and increase their survival in prevention of TIAs and stroke.
Known hypersensitivity to phenylbutazone, or pyrazoline derivatives or salicylates; active peptic ulcer; concurrent administration
of salicylates; blood dyscrasias; patients with creatinine clearance <50 mg/min, treatment of hyperuricemia secondary to
neoplastic disease or cancer chemotherapy; bone marrow suppression; hematologic disease; nephrolithiasis.
NSAID hypersensitivity; impaired kidney function; severe hepatic disease; history of healed peptic ulcer; concurrent use
of anticoagulant therapy; thrombocytopenia; use in conjunction with sulfonamides and sulfonylureas; pregnancy (category
Route & Dosage
Adult: PO 100200 mg b.i.d. for 1 wk, then increase to 200400 mg b.i.d., may reduce to 200 mg/d after serum urate levels
are controlled (max: 800 mg/d)
Inhibition of Platelet Aggregation
Adult: PO 200 mg t.i.d. or q.i.d.
- Give with meals, milk, or antacid (prescribed) to prevent local drug irritant effect. Severity and frequency of symptoms
increase with dosage. Persistence of GI symptoms may require discontinuation of drug.
- Ensure fluid intake sufficient to support urinary output of at least 20003000 mL/d during early therapy (consult physician).
Also alkalinize urine (e.g., with large doses vitamin C) to increase solubility of uric acid and minimize risk of uric acid
Adverse Effects (≥1%)GI: Nausea,
vomiting, diarrhea, epigastric pain, blood loss, reactivation or aggravation of peptic ulcer, jaundice
Ataxia, dizziness, vertigo, convulsions, coma. Special Senses:
Tinnitus. Body as a Whole:
Edema, labored respirations, hypersensitivity, reactions (skin rashes, fever). Urogenital:
Precipitation of acute gout
, urolithiasis, renal
Diagnostic Test Interference
Sulfinpyrazone decreases urinary excretion of aminohippuric acid and phenolsulfonphthalein.
May decrease efficacy of nitrofurantoin
for UTI and increase its systemic toxicity. May displace sulfonylureas
from protein binding and increase risk of hypoglycemia; may augment prothrombin time increased by warfarin; cholestyramine
decreases absorption of sulfinpyrazone; aspirin
may inhibit uricosuric effects of sulfinpyrazone.
Readily absorbed from GI tract. Peak:
12 h. Duration:
46 h; may persist up to 10 h. Metabolism:
In liver to active and inactive metabolites. Elimination:
Slowly in urine; 5% in feces. Half-Life:
Assessment & Drug Effects
- Monitor therapy using serum urate levels (lower to about 6 mg/dL) to reduce joint changes, tophi formation, and frequency
of acute attacks and to improve kidney function.
- Lab tests: Obtain periodic blood cell counts during prolonged therapy. Also kidney function, particularly with renal impairment.
Monitor PT and INR with concurrent warfarin use.
- Frequency of acute gouty attacks may increase during first 612 mo of therapy, even when serum urate levels appear
to be controlled. Concurrent prophylactic doses of colchicine may be prescribed during first 36 mo of treatment to
prevent or lessen severity of attacks.
Patient & Family Education
- Remain under close medical supervision; therapy is continued indefinitely.
- Do not experiment with dosage; subtherapeutic doses may enhance urate retention and large doses may increase risk of toxicity.
- Continue medication without interruption even during acute gouty attack. Contact physician for concomitant treatment with
full therapeutic doses of colchicine or other antiinflammatory agent.
- Avoid aspirin-containing medications. If an analgesic is required (in patients with normal kidney function), acetaminophen
is generally recommended.