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. 2001 Dec;49(6):783–789. doi: 10.1136/gut.49.6.783

Low dose balsalazide (1.5 g twice daily) and mesalazine (0.5 g three times daily) maintained remission of ulcerative colitis but high dose balsalazide (3.0 g twice daily) was superior in preventing relapses

W Kruis 1, S Schreiber 1, D Theuer 1, J Brandes 1, E Schutz 1, S Howaldt 1, B Krakamp 1, J Hamling 1, H Monnikes 1, I Koop 1, M Stolte 1, D Pallant 1, U Ewald 1
PMCID: PMC1728533  PMID: 11709512

Abstract

BACKGROUND—Balsalazide is a new 5-aminosalicylic acid (5-ASA) containing prodrug. Its efficacy in comparison with standard mesalazine therapy and the optimum dose for maintaining remission of ulcerative colitis are still unclear.
AIMS—To compare the relapse preventing effect and safety profile of two doses of balsalazide and a standard dose of Eudragit coated mesalazine.
METHODS—A total of 133 patients with ulcerative colitis in remission were recruited to participate in a double blind, multicentre, randomised trial: 49 patients received balsalazide 1.5 g twice daily, 40 received balsalazide 3.0 g twice daily, and 44 received mesalazine 0.5 g three times daily. Efficacy assessments were clinical activity index (CAI) and endoscopic score according to Rachmilewitz, and a histological score. In addition, laboratory tests were performed and urinary excretion of 5-ASA and its metabolite N-Ac-5-ASA was analysed. The study lasted for 26 weeks.
RESULTS—Balsalazide 3.0 g twice daily resulted in a significantly higher clinical remission rate (77.5%) than balsalazide 1.5 g twice daily (43.8%) and mesalazine 0.5 g three times daily (56.8%) (p=0.006). The respective times to relapse were 161 days, 131 days (p=0.003), and 144 days (NS). Accordingly, pairwise contrasts of the final endoscopic score demonstrated a significant difference (p=0.005) between the two balsalazide treatment groups while differences between either of these two groups and mesalazine were not statistically significant. Patients treated with balsalazide excreted less 5-ASA and N-Ac-5-ASA than patients receiving mesalazine but these differences were not statistically significant. Discontinuation of the trial because of adverse effects occurred in nine patients: three in the balsalazide 1.5 g twice daily group, two in the balsalazide 3.0 g twice daily group, and four in the mesalazine 0.5 g three times daily group. No clinically important new drug safety related findings were identified in this study.
CONCLUSIONS—High dose balsalazide (3.0 g twice daily) was superior in maintaining remission in patients with ulcerative colitis compared with a low dose (1.5 g twice daily) or a standard dose of mesalazine (0.5 g three times daily). All three treatments were safe and well tolerated.


Keywords: balsalazide; mesalazine; aminosalicylic acid; ulcerative colitis

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Figure 1  .

Figure 1  

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Disposition of the patients enrolled in the study.

Figure 2  .

Figure 2  

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Percentage of patients still in remission after 26 weeks of treatment with balsalazide twice daily (bid) or mesalazine three times daily (tid) (χ2 tests).

Figure 3  .

Figure 3  

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Kaplan-Meier estimates for time in remission for patients treated with balsalazide twice daily (bid) or mesalazine three times daily (tid).

Figure 4  .

Figure 4  

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Estimated treatment effects and 95% confidence intervals for equivalent dose of mesalazine with respect to balsalazide, using a clinical activity index.

Figure 5  .

Figure 5  

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Adverse events by system organ class (SOC): number of adverse events per 1000 treatment days after balsalazide twice daily (bid) or mesalazine three times daily (tid). RES, reticuloendothelial system.

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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