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sulfasalazine (SSZ, Azulfidine, SAS)

Tradename: Azulfidine. Indications: - rheumatoid arthritis - spondyloarthritis [6] - psoriatic arthritis [5] - inflammatory bowel disease & enteropathic arthritis - scleroderma [5] - microsopic colitis [5] Contraindications: Cautions: 1) renal or hepatic impairment 2) blood dyscrasias 3) slow acetylators 4) bronchial asthma 5) glucose-6-phosphate dehydrogenase (G6PD) deficiency Pregnancy category: B Dosage: 1) mild to moderate inflammatory bowel disease: a) 500-1000 mg PO QID b) do not exceed 8 hours between night time & morning dose 2) maintenance 1-2 g/day in divided doses 3) take plenty of water 4) avoid direct sunlight 5) pediatrics: 20-60 mg/kg/day Tabs: 500 mg. Liquid: 250 mg/5 mL. Pharmacokinetics: 1) different with different formulations 2) primary site of action is the colon Monitor: - CBC, LFTs, serum creatinine baseline & every 3-6 months thereafter [6] Adverse effects: 1) common (> 10%) - fever, itching, rash, photosensitivity, dizziness, headache, anorexia, nausea/vomiting, diarrhea, reversible oligospermia 2) less common (1-10%) - granulocytopenia, leukopenia, thrombocytopenia, aplastic anemia, hemolytic anemia, hepatitis, Lyell's syndrome, Stevens-Johnson syndrome - megaloblastic anemia due to folate deficiency manifesting as fatigue [7] 3) uncommon (< 1%) - crystalluria, hematuria, thyroid dysturbance, interstitial nephritis, serum sickness-like reaction, jaundice, acute nephropathy 4) other - abdominal pain - hypersensitivity reactions - skin rash - fever - hepatotoxicity - agranulocytosis - aplastic anemia - fatigue - paradoxical exacerbations of colitis - may cause orange & yellow discoloration of the skin & urine - may precipitate porphyria Drug interactions: 1) folic acid: reduced absorption of folic acid; consider folate replacement with long-term therapy 2) digoxin: reduced absorption of digoxin Mechanism of action: 1) converted to sulfapyridine & mesalamine - mesalamine is active component in GI tract - sulfapyridine component exerts systemic effects

Interactions

drug interactions drug adverse effects of NSAIDs monitor with non steroidal anti-inflammatory agents (NSIADs)

Related

mesalamine (Asacol, Rowasa, Pentasa, Pentasacaps, Lialda, Apriso, Canasa, Delzicol) sulfapyridine

General

5-aminosalicylate (5-ASA) disease-modifying antirheumatic agent (DMARD)

Properties

INHIBITS: cyclooxygenase MISC-INFO: elimination route KIDNEY pregnancy-category B safety in lactation ?

Database Correlations

PUBCHEM cid=5339

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 356
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Deprecated Reference
  6. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
  7. NEJM Knowledge+ Gastroenterology