Balsalazide ulcerative colitis

Ulcerative colitis Take three 750 mg capsules 3 times a day for a total daily dose of 6.75 g for a duration of 8 weeks. Some patients in clinical trials required treatment for up to 12 weeks. Safety and efficacy of balsalazide disodium beyond 12 weeks have not been established. 

Olsalazine sodium (Dipentum) links two 5-ASA molecules with an azo linkage. Following cleavage of the azo linkage in the colon, two 5-ASA molecules are released. Olsalazine is approved for maintenance of remission of ulcerative colitis, but a commonly reported side effect is a paradoxical increase in diarrhea. The U. S. Food and Drug Administration (FDA) has approved balsalazide disodium (Colazal) as a treatment of mild to moderately active ulcerative colitis. Balsalazide... 

In a randomized, double-blind study, balsalazide 3 g/day and mesalazine 1.2 g/day effectively maintained remission in 99 patients with ulcerative colitis (4). Adverse events were equally common in the two groups, the most common being headache, abdominal pain and diarrhea, respiratory infections, body pains, and flu-like symptoms. 

The relapse-preventing effects and safety profiles of balsalazide 1.5 g bd, balsalazide 3 g bd, and mesalazine 0.5 g tds have been studied in a multicenter, randomized, double-blind trial in 133 patients with ulcerative colitis in remission (7). High-dose balsalazide was significantly more effective in maintaining remission compared with the other two treatments. All three treatments were well tolerated. 

The use of oral enteric-coated mesalazine, which releases mesalazine in the terminal ileum and colon, has been reviewed (88,100). Dose-related improvements in clinical and endoscopic parameters have been reported with prolonged-release mesalazine 1-A g/day in trials in patients with mild to moderately active ulcerative colitis. About 74% of patients with mild to moderate ulcerative colitis improve with enteric-coated mesalazine 2.4. 8 g/ day. There is a trend toward a better response with higher doses. Oral enteric-coated mesalazine 0.8-4.4 g/day appears to be as effective as sulfasalazine 2-4 g/day, modified-release mesalazine 1.5 g/day, and balsalazide 3 g/day in maintaining remission in ulcerative colitis. 

Green JR, Gibson JA, Kerr GD, Swarbrick ET, Lobo AJ, Holdsworth CD, Crowe JP, Schofield KJ, Taylor MD. Maintenance of remission of ulcerative colitis a comparison between balsalazide 3 g daily and mesalazine 1.2 g daily over 12 months. ABACUS Investigator group. Aliment Pharmacol Ther 1998 12(12) 1207-16. 

Azo Prodrugs Amines have been incorporated into an azo linkage to form prodrugs that can be activated through azo reduction. In fact, sulfa dmgs were discovered because of prontosil (93), an inactive azo dye that was converted in vivo to the active sulfanilamide (95) (Scheme 15). Clinically useful balsalazide (23), olsalazine (25), and sulfasalazine (26) are azo prodrugs of mesalazine (27). They are converted in vivo by bacterial azo reductases in the gut to the active 5-aminosalicylic acid (5-ASA or mesalazine, 27), which is responsible for their anti-inflammatory activity in the treatment of ulcerative colitis, as discussed earlier. 

Pruitt R, Hanson J, Safdi M, et al. Balsalazide is superior to mesalamine in the time to improvement of signs and symptoms of acute mild-to-moderate ulcerative colitis. Am J Gastroenterol 2002 97 3078-3086. 

McGrane J, Paravasthu M, Candlish W, Gravil J. Unilateral balsalazide-induced eosinophilic pneumonia in an ulcerative colitis patient. J R Coll Physicians Edinb 2010 40 216-8. 

A 38-year-old man with ulcerative colitis who had taken mesalazine for many years was switched to balsalazide 2.25 g tds and prednisolone 15 mg/day. However, 14 days later, while his bowel symptoms were improving, he developed intermittent chest pain (not typical of ischemia or pericarditis). Cardiac troponin I and C reactive protein were raised and there was widespread T wave inversion. Echocardiography showed apical and posterior segment wall motion abnormality with no effusion. A diagnosis of myocarditis was made, and balsalazide was withdrawn. His cardiac symptoms resolved within 48 hours. 

Quiros JA, Heyman MB, Pohl JF, Attard TM, Pieniaszek HJ, Bortey E, Walker K, Forbes WP. Safety, efficacy, and pharmacokinetics of balsalazide in pediatric patients with mild-to-moderate active ulcerative colitis results of a randomized, double-blind study. J Pediatr Gastroenterol Nutr 2009 49 571-9. 

Kang SM, Jang YR, Yoon HH, Kim S, Kim EY, Ha SY, et al. A case of balsalazide-induced limited form of granulomatosis with polyangiitis with bronchiolitis obhterans organizing pneumonia-Kke variant in ulcerative colitis. Tuberc Respir EHs Seoul 2012 72 323-7. 

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