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Sulfasalazine information from DrugsUpdate  

See Available Brands of Sulfasalazine in India

P - Contraindicated in pregnancy
L - Caution when used during lactation

Sulfasalazine (brand name Azulfidine in the U.S., Salazopyrin in Europe) is a sulfa drug, a derivative of Mesalazine (5-aminosalicylic acid abbreviated as 5-ASA), used primarily as an anti-inflammatory agent in the treatment of inflammatory bowel disease as well as for rheumatoid arthritis. It may be abbreviated SSZ. It is not a pain killer.

Pharmacodynamics

The mode of action of Sulfasalazine (SSZ) 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 SSZ, SP, and 5-ASA have indicated that the major therapeutic action may reside in the 5-ASA moiety.

Pharmacokinetics

Actual mechanism not determined. Sulphasalazine may have direct anti-inflammatory action in the colon. It also systemically interferes with secretion by prostaglandin synthesis inhibition.

Absorption
15% of the dose is absorbed from small intestine, the rest reaches the colon where the azo bond is cleaved by the intestinal flora, producing sulfapyridine and 5-aminosalicylic acid (mesalazine). 60% of the sulfapyridine and 10-30% of the 5-aminosalicylic acid is absorbed from the colon.

Distribution
Following IV admin, vol of distribution is 7.5 L. Sulfasalazine and sulfapyridine crosses the placenta and found in breast milk. Sulfasalazine is extensively protein bound while sulfapyridine is distributed to most body tissues.

Metabolism
Absorbed sulfapyridine undergoes extensive metabolism by acetylation, hydroxylation, and glucuronidation. Slow acetylators are 2-3 times more likely to experience adverse effects from sulfapyridine compared to fast acetylators. Absorbed 5-aminosalicylic acid undergoes acetylation.

Excretion
Via urine,as unchanged sulfasalazine (15%), sulfapyridine and its metabolites (60%), and 5-aminosalicylic acid and its metabolites (20-33%).

Sulfasalazine Indications / Sulfasalazine Uses

Information Not Available

Sulfasalazine Adverse Reactions / Sulfasalazine Side Effects

Headache, anorexia, nausea, vomiting, diarrhoea, abdominal discomfort, photosensitivity, crystalluria, reversible oligospermia, yellow-orange staining of contact lens, skin, urine and other body fluids, alopoecia.

Potentially Fatal: Severe hypersensitivity reactions, blood dyscrasias, renal and hepatic toxicity, fibrosing alveolitis.

Precautions

Sulfasalazine tablets should be given with caution to patients with severe allergy or bronchial asthma. Adequate fluid intake must be maintained in order to prevent crystalluria and stone formation. Patients with glucose-6 phosphate dehydrogenase deficiency should be observed closely for signs of hemolytic anemia. This reaction is frequently dose related. If toxic or hypersensitivity reactions occur, the drug should be discontinued immediately.

Overdosage
Nausea, vomiting, gastric distress, abdominal pains, drowsiness, convulsions. Gastric lavage or emesis plus catharsis as required. Alkalinize urine. If kidney function is normal, increase fluids. If anuria is present, restrict fluids and salt, and treat accordingly. Catheterization of the ureters may be needed for complete renal blockage by crystals. Hemodialysis may facilitate removal of sulfasalazine and its metabolites. Concentrations of serum sulfapyridine may be used to monitor the progress of recovery.

Special Precautions

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

Other Drug Interactions

Plasma levels reduced by rifampicin and ethambutol. Interferes with absorption of folic acid. Additive leucopaenia with gold therapy for rheumatoid arthritis. Increased haematological toxicity with azathioprine. Reduced serum levels of digoxin.

Other Interactions

Information Not Available

Dosage

Oral
Inflammatory bowel disease
Adult: Initially, 1-2 g 4 times daily until remission occurs. Maintenance: 2 g/day in divided doses.
Child: ≥2 years: 40-60 mg/kg/day in divided doses. Maintenance: 20-30 mg/kg/day in divided doses.
CrCl (ml/min)    Dosage Recommendation
10-30ml/min     Admin twice daily.
<10ml/min       Admin once daily.
Hepatic impairment: Avoid use.

Oral
Rheumatoid arthritis
Adult: As enteric-coated tablet: Initially, 500 mg daily for the 1st weeks increased by 500 mg every weeks. Max: 3 g daily in 2-4 divided doses.
Child: For polyarticular juvenile rheumatoid arthritis: ≥6 years: As enteric-coated tablet: 30-50 mg/kg/day in 2 divided doses. Begin treatment with 1/4 to 2/3 of expected maintenance dose and increase wkly to reach maintenance dose in 1 month. Max: 2 g daily.
CrCl (ml/min)    Dosage Recommendation
10-30 mL/min   Admin twice daily.
<10ml/min       Admin once daily.
Hepatic impairment: Avoid use.

Rectal
Inflammatory bowel disease
Adult: As suppository: 0.5-1 g in the morning and night, either alone or as an adjunct to oral treatment. As enema: 3 g at night, retained for at least 1 hour.
Child: As suppository (may be given as divided doses): 5-8 years: 500 mg bid; 8-12 years: 500 mg in the morning and 1 g at night; 12-18 years: 1 g bid. As enema (to be retained for at least 1 hour): 2-7 years: 1-1.5 g; 7-12 years: 1.5-2.25 g; 12-18 years: 3 g, dose to be given at night.

Food(before/after)

Should be taken with food. (Take after meals. Ensure adequate fluid intake.)

List of Contraindications

Sulfasalazine and Pregnancy

Contraindicated in pregnancy

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

If administered near term.

Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Sulfasalazine and Lactation

Caution when used during lactation

Sulfasalazine and Children

Safety and efficacy not established for children younger than 2 yr of age with ulcerative colitis. Safety and efficacy of delayed-release tablets not established for children younger than 6 years of age with rheumatoid arthritis.

Sulfasalazine and Geriatic

Information Not Available

Sulfasalazine and Other Contraindications

Hypersensitivity to sulphonamides or salicylates, porphyria, <2 years of age, intestinal or urinary obstruction, blood dycrasias, history of leucopenia with gold therapy.

Storage

Oral
Store below 25°C.

Lab interference

Oral
Store below 25°C.

Sulfasalazine brands in India:

Iwata Saaz Saaz-DS Salazar Salazar-DS Salazopyrin Sazo Sazo-EN

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