• Mild to moderate ulcerative colitis or as adjunctive therapy in severe ulcerative colitis.
• Rheumatoid arthritis unresponsive or intolerant to salicylates and/or NSAIDs.

Contraindicated in:

• Hypersensitivity reactions to sulfonamides, salicylates, or sulfasalazine
• Cross-sensitivity with furosemide, sulfonylurea hypoglycemic agents, or carbonic anhydrase inhibitors may exist
• Glucose-6–phosphate dehydrogenase deficiency (↑ risk of hemolysis)
• Hypersensitivity to bisulfites (mesalamine enema only)
• Urinary tract or intestinal obstruction
• Porphyria.

Use Cautiously in:

• Severe hepatic impairment
• Severe renal impairment
• History of porphyria
• Blood dyscrasias
• OB: Neural tube defects have been reported; use during pregnancy only if potential maternal benefit justifies potential fetal risk
• Lactation: May compete with bilirubin for binding sites on plasma proteins in the newborn and cause kernicterus; bloody stools or diarrhea reported in breastfed infants
• Pedi: Children <2 yr (safety and effectiveness not established).

Derm: rash, ACUTE GENERALIZED EXANTHEMATOUS PUSTULOSIS, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), EXFOLIATIVE DERMATITIS, photosensitivity, STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN), yellow discoloration.

GI: anorexia, diarrhea, nausea, vomiting, drug-induced hepatitis.

GU: crystalluria, infertility, oligospermia, orange-yellow discoloration of urine, renal impairment.

Hemat: AGRANULOCYTOSIS, APLASTIC ANEMIA, blood dyscrasias, eosinophilia, hemolytic anemia, megaloblastic anemia, thrombocytopenia.

Neuro: headache, peripheral neuropathy.

Resp: pneumonitis.
Misc: fever, (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)HYPERSENSITIVITY REACTIONS .

Drug-Drug:

• May ↑ action/risk of toxicity from oral hypoglycemic agents, phenytoin, methotrexate, zidovudine, or warfarin.
• ↑risk of drug-induced hepatitis with other hepatotoxic agents.
• ↑risk of crystalluria with methenamine.
• May ↓ metabolism and ↑ effects/toxicity of mercaptopurine or thioguanine.

Drug-Food:

• May ↓ iron and folic acid absorption.

(Generic available)

• Tablets: 500 mg;
• Delayed-release (enteric-coated) tablets (Azulfidine EN-tabs): 500 mg;

Ulcerative Colitis

• PO (Adults): 1 g every 6–8 hr (may start with 500 mg every 6–12 hr), followed by maintenance dose of 500 mg every 6 hr.
• PO (Children >2 yr): Initial: 6.7–10 mg/kg every 4 hr or 10–15 mg/kg every 6 hr or 13.3–20 mg/kg every 8 hr. Maintenance: 7.5 mg/kg every 6 hr (not to exceed 2 g/day).

Rheumatoid Arthritis

• PO (Adults): 500 mg–1 g/day (as delayed-release tablets) for 1 wk, then ↑ by 500 mg/day every wk up to 2 g/day in 2 divided doses; if no benefit seen after 12 wk, ↑ to 3 g/day in 2 divided doses.
• PO (Children 6 yr): 30–50 mg/kg/day in 2 divided doses (as delayed-release tablets); initiate therapy at 25% of planned maintenance dose and ↑ every 7 days until maintenance dose is reached (not to exceed 2 g/day).

Azulfidine, Azulfidine EN-tabs

• Locally acting anti-inflammatory action in the colon, where activity is probably a result of inhibition of prostaglandin synthesis.

• Reduction in the symptoms of ulcerative colitis or rheumatoid arthritis.

Therapeutic Classification: antirheumatics (DMARD), gastrointestinal anti-inflammatories

Absorption: 10–15% absorbed after oral administration.

Distribution: Widely distributed; crosses the placenta and enters breast milk.

Protein Binding: 99%.

Metabolism/Excretion: Split by intestinal bacteria into sulfapyridine and 5-aminosalicylic acid. Some absorbed sulfasalazine is excreted by bile back into intestines; 15% excreted unchanged by the kidneys. Sulfapyridine also excreted mostly by the kidneys.

Half-life: 6 hr.

Salazopyrin

(plasma concentrations)

• Instruct patient on the correct method of administration. Advise patient to take medication as directed, even if feeling better. Take missed doses as soon as remembered unless almost time for next dose.
• May cause dizziness. Caution patient to avoid driving or other activities that require alertness until response to medication is known.
• Advise patient to notify health care professional if skin rash, sore throat, fever, mouth sores, unusual bleeding or bruising, wheezing, fever, or hives occur.
• Caution patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
• Inform patient that this medication may cause orange-yellow discoloration of urine and skin, which is not significant. May permanently stain contact lenses yellow.
• Instruct patient to notify health care professional if symptoms worsen or do not improve. If symptoms of acute intolerance (cramping, acute abdominal pain, bloody diarrhea, fever, headache, rash) occur, discontinue therapy and notify health care professional immediately.
• May cause fetal harm. Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, and to avoid breastfeeding during therapy. Neural tube defects have been reported in infants of women taking sulfasalazine during pregnancy. Monitor newborns for kernicterus if mother taking sulfasalazine; monitor breastfed infants for bloody stool or diarrhea. Inform male patient that sulfasalazine may cause infertility; usually reversible.
• Instruct patient to notify health care professional if symptoms do not improve after 1–2 mo of therapy.

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