Zopyrin

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

The mode of action of Zopyrin is still under investigation, but may be related to the anti inflammatory and/or immunomodulatory properties that have been observed in animal and in vitro models, to its affinity for connective tissue, and/or to the relatively high concentration it reaches in serous fluids, the liver and intestinal walls, as demonstrated in autoradiographic studies in animals. In ulcerative colitis, clinical studies utilizing rectal administration of Zopyrin, Sulfapyridine and 5-Aminosalyclic Acid have indicated that the major therapeutic action may reside in the 5-Aminosalyclic Acid moiety. The relative contribution of the parent drug and the major metabolites in rheumatoid arthritis is unknown.

Zopyrin is an anti-inflammatory indicated for the treatment of ulcerative colitis and rheumatoid arthritis.

Trade Name Zopyrin
Availability Prescription only
Generic Sulfasalazine
Sulfasalazine Other Names Azopyrin, Salazosulfapiridina, Salazosulfapyridine, Salazosulfapyridinum, Salicylazosulfapyridine, Sulfasalazin, Sulfasalazina, Sulfasalazine, Sulfasalazinum
Related Drugs Lialda, Pentasa, Apriso, Azulfidine, Asacol, Canasa, Delzicol, Asacol HD, Dipentum, Rowasa
Type
Formula C18H14N4O5S
Weight Average: 398.393
Monoisotopic: 398.068490268
Groups Approved
Therapeutic Class Drugs for Irritable Bowel Syndrome, Drugs used for Rheumatoid Arthritis, Ulcerative Colitis
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Zopyrin
Zopyrin

Uses

Zopyrin is used for:

  • Rheumatoid arthritis & Juvenile arthritis: In the treatment of patients with rheumatoid arthritis and pediatiric patients with polyarticular-course juvenile rheumatoid arthritis, who have responded inadequately to salicylates or other non-steroidal anti-inflammatory drugs (NSAIDs).
  • Ulcerative colitis and Crohn's Disease: As adjunct in the treatment of ulcerative colitis with the usual supportive and dietary measures. In the treatment of active Crohn's disease, especially in patients with colonic involvement.

Zopyrin is also used to associated treatment for these conditions: Crohn's Disease (CD), Polyarticular juvenile rheumatoid arthritis, chronic or unspecified, Proctitis, Rheumatoid Arthritis, Severe Ulcerative Colitis, Mild Ulcerative Colitis, Moderate Ulcerative colitis

How Zopyrin works

The mode of action of Zopyrin or its metabolites, 5-aminosalicylic acid (5-ASA) and sulfapyridine (SP), is still under investigation, but may be related to the anti-inflammatory and/or immunomodulatory properties that have been observed in animal and in vitro models, to its affinity for connective tissue, and/or to the relatively high concentration it reaches in serous fluids, the liver and intestinal walls, as demonstrated in autoradiographic studies in animals. In ulcerative colitis, clinical studies utilizing rectal administration of Zopyrin, SP and 5-ASA have indicated that the major therapeutic action may reside in the 5-ASA moiety. The relative contribution of the parent drug and the major metabolites in rheumatoid arthritis is unknown.

Dosage

Zopyrin dosage

The dosage of Zopyrin tablets should be individually adjusted according to the patient's tolerance and response to the treatment and taken in evenly divided doses preferably after meals.

Adult dose for crohn’s disease: 500 mg orally 2 to 4 times a day with food.

Pediatric use (6 years or older) for Ulcerative Colitis: The initial dose 40 to 60 mg/kg/day orally divided into 3 to 6 doses.

Adultdose for rheumatoid arthritis: 2 g daily in two evenly divided doses. It is advisable to initiate therapy with a lower dosage e.g. 0.5 to 1.0 g daily, to reduce possible gastrointestinal intolerance. A suggested dosing schedule is given bellow:

  • First week: One tablet in theevening
  • Secondweek: One tabletin the morning &One tabletin the evening
  • Thirdweek:One tabletin the morning & two tabletin the evening
  • Forthweek: Two tabletin the morning &two tabletin the evening

In case of rheumatoid arthritis 6 years or older: initial dose 10 mg/kg/day orally in 2 equally divided doses.

Juvenile rheumatoid arthritis-polyarticular course: Children 6 years of age and older: 30 to 50 mg/kg/day in two evenly divided doses. Typically the maximum dose is 2 g per day.

For other indications:

Initial therapy:

  • Adults: 3 to 4 g daily in divided doses with dosage intervals not exceeding eight hours. It may be advisable to initiate therapy with a lower dosage e.g. 1 to 2 g daily to reduce possible gastrointestinal intolerance.
  • Children 6 years of age and older: 40 to 60 mg/kg/day in to 3 to 6 divided doses.

Maintenance therapy:

  • Adults: 2 g daily.
  • Children 6 years of age and older: 30 mg/kg/day in 4 divided doses.

Side Effects

The common adverse reactions are anorexia, headache, nausea, vomiting, gastric distress, dyspepsia, abdominal pain, dizziness, apparently reversible oligospermia etc.

Precaution

Hepatic/renal impairment, G6PD deficiency, allergic bronchial asthma, lactation.

Interaction

Reduced absorption of folic acid and digoxin has been reported when those agents were administered concomitantly with sulfasalazine.

Food Interaction

  • Drink plenty of fluids. Inadequate fluid intake is associated with crystalluria and stone formation.
  • Take with food.

Volume of Distribution

  • 7.5 ± 1.6 L

Half Life

5-10 hours

Clearance

  • 1 L/h [IV administration]

Elimination Route

The majority of 5-ASA stays within the colonic lumen and is excreted as 5-ASA and acetyl-5-ASA with the feces.

Pregnancy & Breastfeeding use

Use in pregnancy: Pregnancy category B. This drug should be used during pregnancy only if clearly needed.

Use in lactation: Caution should be exercised when sulfasalazine is administered to a nursing mother.

Contraindication

Hypersensitivity to Zopyrin, its metabolites, sulfonamides or salicylates, patients with intestinal or urinary obstruction and porphyria.

Storage Condition

Store in a cool and dry place, protected from light.

Innovators Monograph

You find simplified version here Zopyrin

Zopyrin contains Sulfasalazine see full prescribing information from innovator Zopyrin Monograph, Zopyrin MSDS, Zopyrin FDA label

FAQ

What is Zopyrin used for?

Zopyrin is used to treat bowel inflammation, diarrhea, rectal bleeding, and abdominal pain in patients with ulcerative colitis, a condition in which the bowel is inflamed.

How safe is Zopyrin?

Zopyrin may cause reversible male infertility, but it is entirely safe for use during pregnancy and lactation. Overall, Zopyrin has a long and impressive safety record, provided the drug is used with an awareness and appreciation of its potential pitfalls.

How does Zopyrin work?

Zopyrin is an anti-inflammatory drug.Zopyrin believed that it affects your immune system and decreases inflammation. Zopyrin work by locally in the colon to decrease inflammation. It also works throughout the body by inhibiting the formation of a chemical known as prostaglandins.

What are the common side effects of Zopyrin?

The more common side effects of Zopyrin are include:

  • decreased appetite
  • headache
  • nausea
  • vomiting
  • stomach upset and pain
  • rash
  • itching
  • decreased sperm count (only while taking the medication)
  • dizziness

Is Zopyrin safe during pregnancy?

Zopyrin does not increase the risk of any complications of pregnancy or the risk of birth defects.

Is Zopyrin safe during breastfeeding?

Zopyrin is considered safe to use while you are breastfeeding, unless the baby is premature or at risk of jaundice.

Can I drink alcohol with Zopyrin?

There's no particular reason to avoid alcohol while on Zopyrin. However, it's recommended that people try to keep well within the recommended limits for alcohol. This limit is 14 units a week for women and men.

How quickly does Zopyrin work?

Zopyrin start to work could be at least 12 weeks before you notice any effects. You shouldn't take Zopyrin if you're known to have an allergy to salicylates.

When is the best time to take Zopyrin?

It is best to take Zopyrin right after meals, at evenly spaced times throughout the day and night. Try not to let more than 8 hours go by between doses, even at night.

Does Zopyrin cause weight gain?

Zopyrin can causes weight gain also with other side effects.

Is Zopyrin a steroid?

No, Zopyrin is not a steroid and is actually considered a "steroid-sparing" medication.

How long can I stay on Zopyrin?

Zopyrin takes time to work. Most patients start to feel the positive effects of at 4-8 weeks, with maximum benefit at 3-6 months.

Who should not take Zopyrin?

If you have or have ever had asthma, kidney or liver disease, porphyria, blood problems, or blockage in your intestine or urinary tract you should not use Zopyrin.

Does Zopyrin cause hair loss?

Zopyrin may not causes hair loss.

Does Zopyrin reduce inflammation?

Zopyrin works inside the bowels by helping to reduce the inflammation and other symptoms of the disease.

Is Zopyrin bad for my liver?

Zopyrin has been linked to cases of acute liver failure, particularly with hepatocellular patterns of injury.

Can Zopyrin affect my eyes?

Zopyrin is generally considered safe and well tolerated. There has been a report of peripheral facial nerve palsy and blurred near vision in association with Zopyrin treatme.

How does Zopyrin affect sperm?

Zopyrin can decrease sperm counts and sperm motility.

How bad is Zopyrin for you?

Zopyrin may cause blood problems. These problems may result in a greater chance of certain infections, slow healing, and bleeding of the gums.

Can Zopyrin cause high blood pressure?

found no effect of Zopyrin on blood pressure, hyperemic response, or arterial diameter.

Can Zopyrin make me infertile?

These studies confirmed the preliminary report and suggest that prolonged treatment with Zopyrin may universally depress semen quality and cause reversible infertility.

What happens if I miss a dose?

If you forget to take a dose of Zopyrin, take Zopyrin as soon as you remember. If it is almost time for your next scheduled dose, take only your next dose. Do not take two doses of Zopyrin at once.

What happens if I overdose of Zopyrin?

Overdose symptoms may include vomiting, stomach pain, drowsiness, or seizure.

How long does it take for Zopyrin to leave my body?

Zopyrin is safe to just stop Zopyrin you do not need to slowly reduce the dose. However, keep in mind, if you were gaining any benefit, it will usually take at least 6 weeks to lose it.

*** Taking medicines without doctor's advice can cause long-term problems.
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