Sulfinpyrazone

Trade Names:Anturane- Capsules 200 mg- Tablets 100 mg

Pharmacology

Potent uricosuric agent that inhibits renal tubular reabsorption of uric acid and reduces renal tubular secretion of other organic anions; possesses antithrombotic and platelet-inhibiting effects.

Pharmacokinetics

Absorption

Sulfinpyrazone is well absorbed after oral administration.

Distribution

98% to 99% of sulfinpyrazone is bound to plasma proteins.

Elimination

Around 50% of an orally administered dose appears in urine after 24 h, 90% as unchanged drug and 10% as its active metabolite, N ¹ -p-hydroxyphenol.

Indications and Usage

Treatment of chronic and intermittent gouty arthritis. Not intended for relief of acute attack of gout.

Unlabeled Uses

Post MI treatment (within 1 to 6 mo of acute MI) to decrease incidence of sudden cardiac death. May also be used to reduce frequency of systemic embolism in rheumatic mitral stenosis.

Contraindications

Active peptic ulcer or symptoms of GI inflammation or ulceration; hypersensitivity to phenylbutazone or other pyrazoles; blood dyscrasias.

Dosage and Administration

PO Initial: 200 to 400 mg daily in 2 divided doses with meals or milk, gradually increasing to full maintenance dosage in 1 wk. Maintenance: 200 to 800 mg daily, given in 2 divided doses; may increase or decrease after serum urate level is controlled. In case of acute exacerbations, administer concomitant treatment with indomethacin (or another NSAID) or colchicine.

Drug Interactions

Increased hepatotoxicity and reduced efficacy of acetaminophen may occur.

Blood levels and toxicity of these agents may increase.

Uricosuric action of sulfinpyrazone may be reduced.

Reduced efficacy of verapamil may occur.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Dermatologic

Rash.

GI

Nausea; vomiting; epigastric distress.

Hematologic

Blood dyscrasias, including anemia; leukopenia; agranulocytosis; thrombocytopenia; aplastic anemia.

Respiratory

Bronchoconstriction (in aspirin-sensitive patients).

Precautions

Pregnancy

Use only when clearly needed.

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

Periodically assess renal function.

Alkalinization of urine

Sulfinpyrazone use may precipitate acute gouty arthritis, urolithiasis and renal colic. Adequate fluid intake (10 to 12 eight oz glasses of fluid) and alkalinization of urine are recommended to reduce potential for renal complications.

Healed peptic ulcer

Administer with care to these patients.

Overdosage

Symptoms

Nausea, vomiting, diarrhea, epigastric pain, ataxia, labored respiration, convulsions, coma.

Patient Information

• Tell patient that medication is taken on daily basis to provide long-term protection from attacks of gout.
• Point out that gout attacks may worsen during initial treatment but continue the drug.
• Explain that other medications may be needed to control attacks of gout.
• Explain that drug may cause GI distress and to take with food or milk and antacid if needed.
• Instruct patient to report these symptoms to health care provider: rash, difficulty breathing, unusual bleeding or bruising, sore throat, fatigue, or fever.
• Explain importance of adequate hydration and instruct patient to drink 10 to 12 full glasses of fluid each day.
• Advise patient to consult health care provider before using aspirin or other salicylates, acetaminophen, or drinking alcohol.
• Tell patient to notify health care provider if GI distress continues.