Drug information of sulfinpyrazone


sulfinpyrazone

Drug group:

Sulfinpyrazone  is an uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties.

Mechanism of effect

Sulfinpyrazone is an oral uricosuric agent (pyrazolone derivative) used to treat chronic or intermittent gouty arthritis. Sulfinpyrazone competitively inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby facilitating urinary excretion of uric acid and decreasing plasma urate concentrations. This is likely done through inhibition of the urate anion transporter (hURAT1) as well as the human organic anion transporter 4 (hOAT4).

Sulfinpyrazone is not intended for the treatment of acute attacks because it lacks therapeutically useful analgesic and anti-inflammatory effects. Sulfinpyrazone and its sulfide metabolite possess COX inhibitory effects. Sulfinpyrazone has also been shown to be a UDP-glucuronsyltransferase inhibitor and a very potent CYP2C9 inhibitor. Sulfinpyrazone is also known to be a cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor as well as an inhibitor of several multridrug resistance proteins (MRPs).

Pharmacodynamic

Sulfinpyrazone's pharmacologic activity is the potentiation of the urinary excretion of uric acid. It is useful for reducing the blood urate levels in patients with chronic tophaceous gout and acute intermittent gout, and for promoting the resorption of tophi.

Pharmacokinetics

Protein binding: 98-99%

Metabolite: Sulfinpyrazone sulfide, Sulfinpyrazone sulfone

Half life: Approximately 4-6 hours

Dosage

Usual Adult Dose for Gouty Arthritis:

Initial: 200 to 400 mg orally given in 2 equally divided doses, with meals or milk, gradually increasing when necessary to full maintenance dosage in 1 week.

Maintenance: 400 mg daily in 2 equally divided doses; may increase to 800 mg daily or reduce to as low as 200 mg daily after the blood urate level has been controlled.

Side effects

stomach disorders , nausea

Alerts

Do not take aspirin, salsalate, magnesium salicylate or other aspirin-like products unless your doctor approves. These products decrease the effects of sulfinpyrazone. Taking one aspirin a day to reduce the risk of a heart attack is usually acceptable.

Stop taking sulfinpyrazone and seek emergency medical attention if you experience an allergic reaction (difficulty breathing; closing of your throat; swelling of your lips, tongue, or face; or hives).

Points of recommendation

Take each dose of sulfinpyrazone with a full glass of water. Also, to reduce the risk that kidney stones will form, drink at least 8 to 10 full glasses (8 ounces) of fluid every day, unless your doctor tells you not to.

Take sulfinpyrazone with food, milk, or an antacid to lessen stomach upset. If nausea, vomiting, or loss of appetite is severe or persistent, consult your doctor.

Pregnancy level

C

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