Sulphinpyrazone
Sulphinpyrazone Uses, Dosage, Side Effects, Food Interaction and all others data.
Sulphinpyrazone 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.
Sulphinpyrazone'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.
Trade Name | Sulphinpyrazone |
Availability | Discontinued |
Generic | Sulfinpyrazone |
Sulfinpyrazone Other Names | Sulfinpyrazone, Sulfoxyphenylpyrazolidine, Sulphinpyrazone |
Related Drugs | prednisone, allopurinol, dexamethasone, triamcinolone, betamethasone, Decadron, febuxostat, cortisone, Zyloprim, probenecid |
Type | |
Formula | C23H20N2O3S |
Weight | Average: 404.482 Monoisotopic: 404.119463206 |
Protein binding | 98-99% |
Groups | Approved |
Therapeutic Class | Drugs used in Gout |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
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.
Sulphinpyrazone is used for the treatment of: Chronic gouty arthritis, Intermittent gouty arthritis
Sulphinpyrazone is also used to associated treatment for these conditions: Hyperuricemia, Platelet Aggregation
How Sulphinpyrazone works
Sulphinpyrazone is an oral uricosuric agent (pyrazolone derivative) used to treat chronic or intermittent gouty arthritis. Sulphinpyrazone 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). Sulphinpyrazone is not intended for the treatment of acute attacks because it lacks therapeutically useful analgesic and anti-inflammatory effects. Sulphinpyrazone and its sulfide metabolite possess COX inhibitory effects. Sulphinpyrazone has also been shown to be a UDP-glucuronsyltransferase inhibitor and a very potent CYP2C9 inhibitor. Sulphinpyrazone is also known to be a cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor as well as an inhibitor of several multridrug resistance proteins (MRPs).
Dosage
Sulphinpyrazone dosage
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 theblooduratelevel has been controlled. Treatment should be continued without interruption even in the presence ofacuteexacerbations, which can be concomitantly treated with phenylbutazone orcolchicine. Patients previously controlled with other uricosuric therapy may be transferred to Anturane (sulfinpyrazone) at full maintenance dosage.
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.
Toxicity
Symptoms of overdose include nausea, vomiting, diarrhea, epigastric pain, ataxia, labored respiration, convulsions, coma. Possible symptoms, seen after overdosage with other pyrazolone derivatives: anemia, jaundice, and ulceration.
Precaution
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.
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.
Food Interaction
- Take with food.
Sulphinpyrazone Drug Interaction
Moderate: acetaminophen, oxycodone, acetaminophen / tramadolMinor: niacinUnknown: ubiquinone, heparin, sodium iodide, carbonyl iron, ferrous sulfate, thiamine, cyanocobalamin, pyridoxine, ascorbic acid, cholecalciferol, phytonadione
Sulphinpyrazone Disease Interaction
Major: blood dyscrasias, upper GI irritationModerate: dehydration, renal dysfunction
Half Life
Approximately 4-6 hours
Pregnancy & Breastfeeding use
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.
Contraindication
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.
Special Warning
Renal Impairment: Mild to moderate: Reduce dose.
Severe: Contraindicated.Hepatic Impairment: Severe: Avoid.
Acute Overdose
Symptoms: Nausea, vomiting, diarrhea, epigastric pain, laboured respiration, convulsions and coma.
Treatment: No specific antidote. Induce emesis, gastric lavage, supportive treatment (intravenous glucose infusions).
Storage Condition
Store between 15-30° C.
Innovators Monograph
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FAQ
What is Sulphinpyrazone used for?
Sulphinpyrazone is used in the treatment of chronic gout, which is caused by too much uric acid in the blood.
What are the common side effects of Sulphinpyrazone?
Heartburn, nausea, and upset stomach are the most common side effects of Sulphinpyrazone therapy.
How does Sulphinpyrazone work?
Sulphinpyrazone works by lowering the amount of uric acid in your blood, preventing gout attacks. The drug helps prevent attacks but will not treat an attack once it has started.
Is Sulphinpyrazone safe during pregnancy?
Sulphinpyrazone has not been assigned to an FDA pregnancy category. There are no data from controlled human pregnancy studies. Sulphinpyrazone should be given during pregnancy only when benefit outweighs risk.
Is Sulphinpyrazone safe during breastfeeding?
There are no data on the excretion of Sulphinpyrazone into human milk.
Can I drink alcohol with Sulphinpyrazone?
Drinking too much alcohol may increase the amount of uric acid in the blood and lessen the effects of Sulphinpyrazone.
How is Sulphinpyrazone best taken?
Take Sulphinpyrazone with food or milk.Keep taking Sulphinpyrazone as you have been told by your doctor or other health care provider, even if you feel well.
What happens if I miss a dose of Sulphinpyrazone?
Take the missed dose as soon as you remember. However, if it is almost time for your next dose, skip the dose you missed and take only your next regularly scheduled dose. Do not take a double dose of this medication.
What happens if I overdose of Sulphinpyrazone?
Seek emergency medical attention.Symptoms of a Sulphinpyrazone overdose include nausea, vomiting, diarrhea, stomach pain, poor coordination, difficulty breathing, seizures, and coma. An overdose of Sulphinpyrazone can result in death.
Who should not take Sulphinpyrazone?
Before taking this medication, tell your doctor if you
- have ever had an allergic reaction to sulfinpyrazone,
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- have kidney disease or poorly functioning kidneys,
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- have kidney stones,
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- have an ulcer in your stomach,
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- have blood problems, or
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- are on high-dose aspirin or salicylate therapy.
What is the mechanism of action of Sulphinpyrazone?
Sulphinpyrazone and lesinurad competitively inhibit the urate anion transporter responsible for reabsorption of uric acid in the proximal tubule. They increase urate excretion in urine and reduce the concentration in plasma.
What happen If I suddenly stop taking Sulphinpyrazone?
If you stop Sulphinpyrazone treatment suddenly, there is a high risk that gout may get worse or you will get serious side effects. Only stop taking if a doctor tells you to.
How long does Sulphinpyrazone stay in Sulphinpyrazone body?
This also explains why people can continue to have attacks of gout for up to two years after starting Sulphinpyrazone, because it takes up to two years for the crystals to dissolve completely.