Sulfinpyrazone
Indications
Sulphinpyrazone is indicated for the treatment of: Chronic gouty arthritis, Intermittent gouty arthritis
Description
Sulphinpyrazone helps to remove excess uric acid from the body. Too much uric acid can cause gout or gouty arthritis. Certain illness or medications can increase uric acid level. It can help to reduce the risk of complications (such as kidney stones) that can occur if uric acid levels in the blood are too high (hyperuricemia). It completely inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby facilitating urinary excretion of uric acid and decreasing plasma urate concentrations.
Pharmacology
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.
Dosage & Administration
Initial dose: 200-400 mg daily in two divided doses, with meals or milk, gradually increasing when necessary to full maintenance dosage in one week.
Maintenance dose: 400 mg daily, given in two divided doses, as above. This dosage may be increased to 800 mg daily, if necessary, and may sometimes be reduced to as low as 200 mg daily after the blood urate level has been controlled. Treatment should be continued without interruption even in the presence of acute exacerbations, which can be concomitantly treated with phenylbutazone or colchicine. Patients previously controlled with other uricosuric therapy may be transferred to Anturane (sulfinpyrazone) at full maintenance dosage.
Maintenance dose: 400 mg daily, given in two divided doses, as above. This dosage may be increased to 800 mg daily, if necessary, and may sometimes be reduced to as low as 200 mg daily after the blood urate level has been controlled. Treatment should be continued without interruption even in the presence of acute exacerbations, which can be concomitantly treated with phenylbutazone or colchicine. Patients previously controlled with other uricosuric therapy may be transferred to Anturane (sulfinpyrazone) at full maintenance dosage.
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Interaction
Decreased therapeutic effect when given with 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 with substances affecting homeostasis (e.g. non-steroidal antirheumatic drugs). Probenecid may inhibit renal tubular secretion of sulfinpyrazone.
Contraindications
Patients with an active peptic or symptoms of gastro-intestinal inflammation or ulceration should not receive the drug. The drug is contraindicated in patients with a history or the presence of hypersensitivity to phenylbutazone or other pyrazoles.
Side Effects
The symptoms are upset stomach, vomiting, loss of appetite and joint pain. If you experience any of the following symptoms like difficulty in breathing, tightness in the chest, skin rash, unusual bleeding, fever, sore throat and mouth sores, call your doctor immediately.
Pregnancy & Lactation
Pregnancy category C. This means that it is not known whether Sulphinpyrazone will harm an unborn baby. Don't take this without first talking to your doctor if you are pregnant.
It is also not known whether Sulphinpyrazone passess into breast milk. Do not take it without first talking to your doctor if you are breast-feeding a baby.
It is also not known whether Sulphinpyrazone passess into breast milk. Do not take it without first talking to your doctor if you are breast-feeding a baby.
Precautions & Warnings
Patients receiving Sulphinpyrazone should be kept under close medical supervision and periodic blood counts are recommended. It may be administered with care to patients with a history of healed peptic ulcer. It is suggested that Sulphinpyrazone should be used with caution in conjunction with sulfa drugs, the sulfonylurea hypoglycemic agents and insulin. Because Sulphinpyrazone is a potent uricosuric agent, it may precipitate urolithiasis and renal colic, especially in the initial stages of therapy. For this reason, an adequate fluid intake and alkalinization of the urine are recommended. Salicylates antagonize the uricosuric action of Sulphinpyrazone and for this reason, their concomitant uses are contraindicated in gouty arthritis.
Use in Special Populations
Renal Impairment: Mild to moderate: Reduce dose. Severe: Contraindicated.
Hepatic Impairment: Severe: Avoid.
Hepatic Impairment: Severe: Avoid.
Overdose Effects
Symptoms: Nausea, vomiting, diarrhea, epigastric pain, laboured respiration, convulsions and coma.
Treatment: No specific antidote. Induce emesis, gastric lavage, supportive treatment (intravenous glucose infusions).
Treatment: No specific antidote. Induce emesis, gastric lavage, supportive treatment (intravenous glucose infusions).
Therapeutic Class
Drugs used in Gout
Storage Conditions
Store between 15-30° C.