Pyrazone

Pyrazone Uses, Dosage, Side Effects, Food Interaction and all others data.

Pyrazone 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.

Pyrazone'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 Pyrazone
Availability Discontinued
Generic Sulfinpyrazone
Sulfinpyrazone Other Names Sulfinpyrazone, Sulfoxyphenylpyrazolidine, Sulphinpyrazone
Related Drugs prednisone, allopurinol, dexamethasone, triamcinolone, betamethasone, Decadron, febuxostat, cortisone, Zyloprim, probenecid
Weight 200mg
Type Tablet
Formula C23H20N2O3S
Weight Average: 404.482
Monoisotopic: 404.119463206
Protein binding

98-99%

Groups Approved
Therapeutic Class Drugs used in Gout
Manufacturer Incepta Pharmaceuticals Limited
Available Country Bangladesh
Last Updated: September 19, 2023 at 7:00 am
Pyrazone
Pyrazone

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

Pyrazone is also used to associated treatment for these conditions: Hyperuricemia, Platelet Aggregation

How Pyrazone works

Pyrazone is an oral uricosuric agent (pyrazolone derivative) used to treat chronic or intermittent gouty arthritis. Pyrazone 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). Pyrazone is not intended for the treatment of acute attacks because it lacks therapeutically useful analgesic and anti-inflammatory effects. Pyrazone and its sulfide metabolite possess COX inhibitory effects. Pyrazone has also been shown to be a UDP-glucuronsyltransferase inhibitor and a very potent CYP2C9 inhibitor. Pyrazone 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

Pyrazone 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.

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

You find simplified version here Pyrazone

FAQ

What is Pyrazone used for?

Pyrazone 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 Pyrazone?

Heartburn, nausea, and upset stomach are the most common side effects of Pyrazone  therapy.

How does Pyrazone work?

Pyrazone 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 Pyrazone safe during pregnancy?

Pyrazone has not been assigned to an FDA pregnancy category. There are no data from controlled human pregnancy studies. Pyrazone should be given during pregnancy only when benefit outweighs risk.

Is Pyrazone safe during breastfeeding?

There are no data on the excretion of Pyrazone into human milk.

Can I drink alcohol with Pyrazone?

Drinking too much alcohol may increase the amount of uric acid in the blood and lessen the effects of Pyrazone.

How is Pyrazone best taken?

Take Pyrazone  with food or milk.Keep taking Pyrazone 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 Pyrazone?

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 Pyrazone?

Seek emergency medical attention.Symptoms of a Pyrazone overdose include nausea, vomiting, diarrhea, stomach pain, poor coordination, difficulty breathing, seizures, and coma. An overdose of Pyrazone can result in death.

Who should not take Pyrazone?


Before taking this medication, tell your doctor if you

  • have ever had an allergic reaction to sulfinpyrazone,

  • have kidney disease or poorly functioning kidneys,

  • have kidney stones,

  • have an ulcer in your stomach,

  • have blood problems, or

  • are on high-dose aspirin or salicylate therapy.

What is the mechanism of action of Pyrazone?

Pyrazone 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 Pyrazone?

If you stop Pyrazone 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 Pyrazone stay in Pyrazone body?

This also explains why people can continue to have attacks of gout for up to two years after starting Pyrazone, because it takes up to two years for the crystals to dissolve completely.

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