Sulfasalazine – Indications, Dosage, and Side Effects

Sulfasalazine (Azulfidine) is a rheumatic disease-modifying medication (DMARD). It can help alleviate arthritic pain and swelling, prevent joint degeneration and lower the chance of long-term impairment. Sulfasalazine is a sulfa medication. You should not use it if you are allergic to sulfa. Sulfasalazine is used to treat rheumatoid arthritis (RA), inflammatory bowel disease (IBD), and a few other autoimmune diseases. It acts as an anti-inflammatory agent in the body.

Sulfasalazine uses

Sulfasalazine is used to treat intestinal inflammation, diarrhea (frequent stools), rectal bleeding, and abdominal pain in people who have ulcerative colitis, an inflammatory disorder of the intestine.

Mechanism of action

The mechanism of action of Sulfasalazine or its metabolites, 5-aminosalicylic acid (5-ASA) and sulfapyridine (SP), is unknown, but may be related to the anti-inflammatory and/or immunomodulatory properties observed in animal and in vitro models, to its affinity for connective tissue, and/or to the relatively high concentrations found in serous fluids, the liver, and intestinal walls, as demonstrated in animal autoradiographic studies. Clinical investigations involving rectal administration of Sulfasalazine, SP, and 5-ASA have revealed that the 5-ASA moiety may exert the majority of the therapeutic effect in ulcerative colitis. It is unknown what role the parent drug and key metabolites play in rheumatoid arthritis.

Dosage of Sulfasalazine

Tablet:

500mg

enteric-coated tablet (delayed-release):

500mg

Ulcerative colitis

In mild to moderate cases, additional therapy is used, and remission is prolonged.

3-4 g/day PO split TID after meals; may begin with 1-2 g/day; dosages greater than 4 g/day may increase the risk of toxicity.

2 g daily in split doses at 8-hour intervals until endoscopic examination reveals improvement

Modifications to the dosage

Reduce dose by 50% and gradually increase to desired amount over several days; if GI intolerance persists, discontinue medication for 5-7 days and reintroduce at a lower daily dose.

Rheumatoid arthritis

Inadequate response to or sensitivity to salicylates or other nonsteroidal anti-inflammatory drugs

Delayed-release: 0.5-1 g/day PO divided BID; gradually increase to a maintenance dose of 2 g/day PO divided BID; if the response is insufficient, may be increased to 3 g/day after 12 weeks.

The Crohn’s Disease (Off-label)

3-6 g PO daily in split dosages for a maximum of 16 weeks

Administration

Consume immediately following meals. Distribute dosages evenly.

Sulfasalazine side effects

The most frequently reported adverse effects of sulfasalazine are as follows:

  1. Diarrhea
  2. Stomach ache
  3. Dizziness
  4. Headaches

These adverse events typically occur during the first three months of treatment and frequently resolve when the dose is reduced. After a period of time, you may be allowed to increase the dose again if your reaction to sulfasalazine improves and it helps your symptoms.

Interaction with other medications

Sulfasalazine oral tablet may interact with certain drugs, vitamins, or herbal supplements that you are currently using. When a chemical alters the way a drug functions, this is referred to as an interaction. This can be hazardous or impair the drug’s effectiveness.

Typically, these drugs are not taken concurrently. For additional information, consult your healthcare provider (e.g., doctor or pharmacist).

  1. Selected photosensitizing substances/tretinoin-mequinol
  2. Antimicrobials/vaccines for live typhoids
  3. Sulfonamides/methenamine

Interactions That Are Serious

These drugs may interact, resulting in extremely serious side effects. For additional information, consult your healthcare provider (e.g., doctor or pharmacist).

  1. Oral BCRP substrates/oral tedizolid selected
  2. BCRP substrates selected/darolutamide
  3. Immunomodulators/sodium iodide I 131 myelosuppressives
  4. Porfimers/photosensitizers selected
  5. Oral inhibitors of BCRP/talazoparib selected
  6. Aminolevulinic acid/selected photosensitizers
  7. Sulfasalazine/methotrexate sulfasalazine/methotrexate (oncology-injection)
  8. Myelosuppressive agents selected/clozapine
  9. Agents activated by iodide/radioactive iodide
  10. Myelosuppressive agents selected/deferiprone
  11. Sulfonamides/cyclosporine
  12. Sulfonamides/selected anticoagulants sulfonamides (vit k antagonists)

Precautions/ safety information

It is critical that your doctor monitors your or your child’s progress during routine visits. This enables your doctor to determine whether the medication is working appropriately. Blood and urine tests will be required to monitor for adverse reactions.

Call your doctor immediately if you get a persistent cough, weight loss, night sweats, fever, chills, runny or stuffy nose, headache, impaired vision, or an overall sense of being unwell. These symptoms may indicate that you have an infection.

Consult your physician immediately if you experience trouble breathing or swallowing, a rapid heartbeat, itching, rash, or redness of the skin, or swelling of the face, throat, or tongue. These symptoms could be the result of an allergic reaction to this medication.

This medication may result in significant skin reactions such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug response with eosinophilia and systemic symptoms (DRESS), and acute widespread exanthematous pustulosis (AGEP).

Storage

Keep at room temperature and out of direct sunlight and moisture. Keep out of the bathroom. Keep all medications out of the reach of youngsters.

Contraindications

Sulfasalazine is contraindicated in the following situations:

  1. Infants younger than two years of age.
  2. Patients are known to be allergic to sulfasalazine, its metabolites, or any of the excipients, as well as sulfonamides or salicylates.
  3. Porphyria patients.

Pregnancy or lactation

During pregnancy and breastfeeding, women who intend to become pregnant may continue to take sulfasalazine. Sulfasalazine has not been shown to raise the risk of pregnancy problems or birth abnormalities. Pregnant women who are on sulfasalazine should increase their daily folic acid intake to 2 mg. If you have inflammatory bowel disease, you should consult your physician.

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