From the Guidelines
Alternatives to Sulfasalazine (Azulfidine) are Standard-Dose Mesalamine and Diazo-Bonded 5-ASA.
Alternatives to Sulfasalazine
- Standard-Dose Mesalamine (2–3 grams/day): This is a recommended alternative to sulfasalazine for patients with extensive mild-to-moderate ulcerative colitis, as it has been shown to be effective in inducing and maintaining remission 1.
- Diazo-Bonded 5-ASA: This class of medications, which includes balsalazide and olsalazine, is also a recommended alternative to sulfasalazine, as it has been shown to be effective in inducing and maintaining remission 1.
Rationale for Alternatives
The American Gastroenterological Association (AGA) recommends using standard-dose mesalamine or diazo-bonded 5-ASA instead of sulfasalazine due to its higher incidence of side effects and lower efficacy 2.
Comparison of Alternatives
A technical review by the AGA found that standard-dose mesalamine was superior to sulfasalazine in terms of inducing remission, with a relative risk of 1.27 (95% CI 0.94 to 1.73) 3.
Special Considerations
However, patients who are already on sulfasalazine and in remission, or those with prominent arthritic symptoms, may reasonably choose to continue sulfasalazine if alternatives are cost-prohibitive, despite its higher rate of intolerance 1.
The FDA Drug Labels for sulfasalazine (PO) do not address this question.
From the Research
Alternatives to Sulfasalazine
- A number of less toxic alternatives to sulphasalazine have been devised and are undergoing trial, as mentioned in the study 4
- These alternatives either convey 5-aminosalicylic acid in a coated tablet to the colon or, when conjugated to a non-toxic carrier, release 5-aminosalicylic acid by bacterial cleavage there, according to the study 4
- Mesalazine (mesalamine, 5-aminosalicylic acid) is a possible alternative, as it is the active therapeutic moiety of sulfasalazine, as stated in the studies 4, 5, 6
- Other disease-modifying antirheumatic drugs (DMARDs) such as methotrexate, penicillamine, hydroxychloroquine, or oral or parenteral gold may also be considered as alternatives, as mentioned in the studies 5, 7
Mechanism of Action
- Sulfasalazine is split by the action of bacterial azoreductases in the large intestine into sulfapyridine and mesalazine (mesalamine, 5-aminosalicylic acid), as explained in the studies 5, 6
- 5-Aminosalicylic acid may act locally and is not absorbed to any great extent, while sulphapyridine is mostly absorbed from the colon and may act both locally and systemically, according to the study 6
Side Effects and Toxicity
- Side effects of sulfasalazine are common but are mainly reversible and not serious, as stated in the study 4
- More serious, idiosyncratic side effects include skin rashes, leucopenia, and agranulocytosis, as mentioned in the study 4
- Renal complications, such as nephrolithiasis, may be an under-reported but potentially serious phenomenon in patients treated with sulfasalazine, as reported in the study 8