Azulfidine (sulfasalazine) represents a cornerstone therapy in the management of chronic inflammatory conditions, particularly rheumatoid arthritis and inflammatory bowel diseases. As a disease-modifying antirheumatic drug (DMARD) with both anti-inflammatory and immunomodulatory properties, it offers clinicians a well-established option for long-term disease control. This sulfonamide antibiotic derivative requires careful patient management but provides significant benefits for appropriate candidates. The following comprehensive product card details its pharmacological profile, clinical applications, and essential safety information.

Features

• Active ingredient: Sulfasalazine 500 mg enteric-coated tablets
• Mechanism: Combines 5-aminosalicylic acid (5-ASA) and sulfapyridine moieties
• Formulation: Delayed-release to minimize gastric irritation
• Pharmacokinetics: Split metabolism—sulfapyridine component absorbed systemically, 5-ASA acts locally in colon
• Half-life: 5-10 hours (sulfapyridine component)
• Excretion: Primarily renal, with enterohepatic recirculation
• Pregnancy category: Category B (adequate human data supporting safety)

Benefits

• Modifies disease progression in rheumatoid arthritis by reducing joint damage and preserving function
• Induces and maintains remission in ulcerative colitis through localized anti-inflammatory action in the colon
• Demonstrates steroid-sparing effects, reducing dependence on corticosteroids and their associated adverse effects
• Offers cost-effective long-term management compared to biologic alternatives
• Provides dual mechanism: antibacterial (sulfapyridine) and anti-inflammatory (5-ASA) actions
• Established safety profile with decades of clinical use and extensive post-marketing surveillance

Common use

Azulfidine is primarily indicated for the management of moderately to severely active rheumatoid arthritis in patients who have responded inadequately to salicylates or other non-steroidal anti-inflammatory drugs (NSAIDs). It is equally fundamental in the treatment of ulcerative colitis, particularly for inducing remission in mild to moderate disease and maintaining remission in chronic cases. Off-label uses include Crohn’s disease, ankylosing spondylitis, and psoriatic arthritis, though evidence supporting these applications varies. The medication is typically incorporated into treatment regimens when conventional first-line therapies provide insufficient control or when disease-modifying effects are specifically sought.

Dosage and direction

For rheumatoid arthritis: Initiate with 500 mg daily, increasing by 500 mg weekly to a maintenance dose of 2-3 grams daily in divided doses. Maximum recommended dose is 3 grams daily. For ulcerative colitis: Adults typically start with 1-2 grams daily in divided doses, increasing to 3-4 grams daily in divided doses for active disease. Maintenance therapy generally ranges from 2 grams daily. Tablets should be swallowed whole with ample water, preferably after meals to minimize gastrointestinal discomfort. Regular blood monitoring (complete blood count, liver function tests) is mandatory during initial months and periodically thereafter.

Precautions

Patients require comprehensive education about potential adverse effects, particularly the need to report any fever, sore throat, mouth ulcers, or rash immediately. Regular laboratory monitoring is essential—complete blood counts should be performed every two weeks during the first three months, then monthly for the remainder of the first year, and quarterly thereafter. Liver function tests and renal function assessments should accompany hematological monitoring. Adequate hydration (2-3 liters daily) is crucial to prevent crystalluria and renal complications. Patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency require heightened vigilance due to increased hemolysis risk.

Contraindications

Absolute contraindications include hypersensitivity to sulfonamides, salicylates, or any component of the formulation; intestinal or urinary obstruction; porphyria; and children under 2 years of age. Additional contraindications include severe renal impairment (creatinine clearance <30 mL/min), severe hepatic impairment, and pregnancy at term. Relative contraindications require careful risk-benefit assessment and include mild to moderate renal or hepatic impairment, bronchial asthma, and history of allergic reactions to other medications.

Possible side effect

Common reactions (≥1%) include nausea (20%), headache (15%), anorexia (10%), and gastrointestinal distress (8%). Oligospermia (reversible upon discontinuation) affects approximately 60% of male patients. Orange-yellow discoloration of skin and urine occurs frequently but is harmless. Serious adverse effects requiring immediate medical attention include Stevens-Johnson syndrome, toxic epidermal necrolysis, agranulocytosis, aplastic anemia, hepatitis, and pneumonitis. Approximately 20% of patients discontinue therapy due to adverse effects, primarily gastrointestinal intolerance.

Drug interaction

Significant interactions occur with warfarin (increased anticoagulant effect), methotrexate (increased hematologic toxicity), and digoxin (reduced absorption). Concurrent use with hepatotoxic drugs increases liver injury risk. Sulfasalazine may reduce cyclosporine levels. Antibiotics may alter intestinal flora and affect sulfasalazine metabolism. Urinary alkalinizers increase sulfapyridine excretion, while urinary acidifiers may promote crystalluria. Patients taking oral diabetes medications may experience enhanced hypoglycemic effects.

Missed dose

If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. Patients should never double the dose to make up for a missed administration. Consistent dosing is important for maintaining therapeutic drug levels, particularly in inflammatory bowel disease management. If multiple doses are missed, patients should contact their healthcare provider for guidance on resumption, as dose retitration may be necessary.

Overdose

Sulfasalazine overdose primarily manifests as nausea, vomiting, gastric distress, and drowsiness. Severe overdose may cause hematologic disturbances, jaundice, crystalluria, hematuria, and neurological symptoms including seizures. Management involves immediate gastric lavage if presentation is early, followed by supportive care including forced diuresis and urinary alkalinization to enhance elimination. Hemodialysis may be beneficial in severe cases. Specific antidotes are unavailable, so treatment remains symptomatic and supportive.

Storage

Store at controlled room temperature (20-25°C/68-77°F) in the original container, protected from light and moisture. Keep tightly closed and away from excessive heat or humidity. Do not transfer tablets to other containers as moisture protection may be compromised. Keep out of reach of children and pets. Properly discard any medication that has expired or is no longer needed through medication take-back programs.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions must be made by qualified healthcare professionals based on individual patient circumstances. Patients should not alter their medication regimen without consulting their prescribing physician. The manufacturer is not liable for any consequences arising from the use or misuse of this information.

Reviews

Clinical studies demonstrate that approximately 60-70% of rheumatoid arthritis patients achieve significant improvement with sulfasalazine therapy, with effects typically apparent within 4-8 weeks. In ulcerative colitis, remission rates of 50-60% are observed in mild to moderate cases. Long-term extension studies show sustained efficacy over years of treatment. Patient-reported outcomes indicate improved quality of life measures, particularly regarding physical function and pain reduction. Gastroenterologists and rheumatologists consistently rate sulfasalazine as a valuable first-line or second-line option in appropriate patient populations.