Alternatives to Sulfasalazine

• Four 5-aminosalicylic acid derivatives are currently available for use in the US:
• balsalazide, mesalamine, olsalazine, and sulfasalazine.
• The 5-ASA derivatives are available in oral and topical formulations and are indicated in the treatment and/or maintenance of remission of ulcerative colitis.
• The 5-ASA derivatives are the core of drug therapy for ulcerative colitis.
• Current ulcerative colitis practice guidelines recommend oral 5-ASA agents for achieving and maintaining remission.
• Sulfasalazine is still recognized as the preferred first-line agent and balsalazide, mesalamine, and olsalazine are listed as effective alternatives.

Adverse Drug Reactions

• The most common adverse events reported with the agents are headache and gastrointestinal upset.
• Adverse events are reported more frequently in patients taking sulfasalazine.
• Sulfasalazine is an arylamine sulfonamide with antibiotic activity. It therefore may exhibit cross-reactivity with other arylamine sulfonamide antibiotics
• Adverse effects are reported in up to 45% of patients taking sulfasalazine and are thought to be related primarily to the sulfa moiety
• Adverse events reported with sulfasalazine treatment can be dose related, including headache, nausea, and fatigue, and may be minimized by taking the medicine with food or by reducing the dose
• Allergic reactions can occur with sulfasalazine treatment and may include rash, including Stevens-Johnson syndrome, or other serious reactions like hepatitis,
• pneumonitis, and hemolytic anemia.
• In addition, sulfasalazine inhibits intestinal folate absorption and patient’s receiving treatment with sulfasalazine may require folate supplementation

Alternatives

• newer 5-ASA are associated with lower rates of adverse effects compared to sulfasalazine treatment
• Approximately 90% of those with intolerance to sulfasalazine can tolerate mesalamine. 
• Mesalamine does not contain the sulfa group
• There are several mesalamine-based oral 5-ASA agents including, Asacol®HD, Pentasa®, Lialda®, Apriso™, Delzicol™. These agents all use the same mesalamine, but differ in terms of the medication coating.
• Nephrotoxicity is a rare but serious concern associated with 5-ASA treatment and renal function should be monitored in all patients receiving these agents

References:

1. CCFA Fact Sheet, January 2015
2. 5-Aminosalicylic Acid Derivatives Drug Class Review, University of Utah College of Pharmacy, October 2013.