Adult: Initially, 100-200 mg bid, increase gradually over 2-3 wk to 600 mg daily. Maintenance dose (after plasma-urate concentration is controlled): 200 mg daily in divided doses. Max: 800 mg daily.
Renal Impairment
Mild to moderate: Reduce dose. Severe: Contraindicated.
Hepatic Impairment
Severe: Avoid.
Administration
Should be taken with food.
Contraindications
Hypersensitivity to sulfinpyrazone and other pyrazolone derivatives. Patient in whom attacks of asthma, urticaria or acute rhinitis are precipitated by aspirin or other drugs w/ prostaglandin-synthetase inhibiting activity. Acute gout attack, blood coagulation disorders, uric acid renal calculi, porphyria, peptic ulceration, severe parenchymal lesions of liver or kidneys, blood dyscrasias. Severe hepatic and renal impairment. Concomitant use w/ salicylates.
Special Precautions
Patient w/ heart failure. Mild to moderate renal impairment. Pregnancy and lactation.
Adverse Reactions
Nausea, vomiting, diarrhoea, abdominal pain, GI bleeding, rashes, aplastic anaemia, agranulocytosis, leucopenia, thrombocytopenia, raised liver enzymes, jaundice, hepatitis, renal impairment, salt and water retention, acute renal failure.
Patient Counseling Information
Ensure adequate fluid intake (approx 2-3 L/day) and urine alkalinisation.
Monitoring Parameters
Monitor renal function, blood count.
Overdosage
Symptoms: Nausea, vomiting, diarrhoea, epigastric pain, ataxia, laboured breathing, seizures, coma. Anaemia, jaundice and ulceration may also occur. Management: Supportive treatment. Induce emesis or perform gastric lavage preferably w/ mild alkaline soln. May administer IV dextrose infusions and analeptics.
Drug Interactions
Decreased therapeutic effect when given w/ drugs that increase uric acid concentration (e.g. diuretics, pyrazinamide). May potentiate the action of coumarin anticoagulants (e.g. warfarin, acenocoumarol), hypoglycaemic agents and sulfonamides. May decrease plasma levels of theophylline. May increase plasma levels of penicillins and phenytoin. Increased risk of haemorrhage w/ substances affecting homeostasis (e.g. non-steroidal antirheumatic drugs). Probenecid may inhibit renal tubular secretion of sulfinpyrazone. Potentially Fatal: Salicylates may antagonise the effect of sulfinpyrazone.
Lab Interference
May interfere w/ renal function tests involving aminohippuric acid or phenolsulfonphthalein.
Action
Description: Mechanism of Action: Sulfinpyrazone increases urinary excretion of uric acid by competitively inhibiting tubular reabsorption of uric acid, thus lowering serum urate concentration and eventually reducing urate deposits in the tissues. Duration: 4-6 hr, or up to 10 hr. Pharmacokinetics: Absorption: Readily absorbed from the GI tract. Time to peak plasma concentration: 1-2 hr. Distribution: Plasma protein binding: Approx 98%. Metabolism: Undergoes partial hepatic metabolism by reduction to the sulfide and oxidation to the sulfone and to hydroxy-compounds. Excretion: Via urine (as unchanged drug and metabolites); via faeces (approx 5% of the drug). Plasma half-life: Approx 2-4 hr.
Chemical Structure
Sulfinpyrazone Source: National Center for Biotechnology Information. PubChem Database. Sulfinpyrazone, CID=5342, https://pubchem.ncbi.nlm.nih.gov/compound/Sulfinpyrazone (accessed on Jan. 23, 2020)
M04AB02 - sulfinpyrazone ; Belongs to the class of preparations increasing uric acid excretion. Used in the treatment of gout.
References
Buckingham R (ed). Sulfinpyrazone . Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. http://www.medicinescomplete.com. Accessed 23/06/2015.Joint Formulary Committee. Sulfinpyrazone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. http://www.medicinescomplete.com. Accessed 24/06/2015.McEvoy GK, Snow EK, Miller J et al (eds). Sulfinpyrazone. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). http://www.medicinescomplete.com. Accessed 23/06/2015.
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