Balsalazide

Balsalazide disodium capsules are indicated for the treatment of mildly to moderately active ulcerative colitis in patients 5 years of age and older. Limitations of Use Safety and effectiveness of balsalazide disodium capsules beyond 8 weeks in pediatric patients 5 years to 17 years of age and 12 weeks in adults have not been established. Balsalazide disodium capsules are an aminosalicylate indicated for the treatment of mildly to moderately active ulcerative colitis in patients 5 years of age and older. Limitations of Use: Safety and effectiveness of balsalazide disodium capsules beyond 8 weeks in children (ages 5 years to 17 years) and 12 weeks in adults have not been established.

Balsalazide disodium is delivered intact to the colon where it is cleaved by bacterial azoreduction to release equimolar quantities of mesalamine, which is the therapeutically active portion of the molecule, and the 4-aminobenzoyl-β-alanine carrier moiety. The carrier moiety released when balsalazide disodium is cleaved is only minimally absorbed and is largely inert. The mechanism of action of 5-ASA is not fully understood, but appears to be a local anti-inflammatory effect on colonic epithelial cells. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with ulcerative colitis, and it is possible that 5-ASA diminishes inflammation by blocking production of arachidonic acid metabolites in the colon.

Administration Instructions Evaluate renal function before initiating therapy with balsalazide disodium capsules. Swallow capsules whole. Do not cut, break, crush or chew. For patients who cannot swallow intact capsules, the capsules may be opened and sprinkled on applesauce, then chewed and swallowed immediately. Teeth and/or tongue staining may occur when administered sprinkled on applesauce. Drink an adequate amount of fluids. Take balsalazide disodium capsules with or without food. Dosage Adults: The recommended dosage is 2.25 g (three 750 mg capsules) three times daily for 8 weeks. Some adult patients required treatment for up to 12 weeks in clinical trials. Pediatric Patients 5 Years to 17 Years of Age: The recommended dosage is either: 2.25 g (three 750 mg capsules) three times for up to 8 weeks. OR: 750 mg (one capsule) three times daily for up to 8 weeks.

Balsalazide disodium capsules are contraindicated in patients with known or suspected hypersensitivity to salicylates, aminosalicylates, or to any of the components of balsalazide disodium capsules or balsalazide metabolites. Known or suspected hypersensitivity to salicylates, aminosalicylates, or any of the components of balsalazide disodium capsules or balsalazide metabolites.

Renal Impairment: Assess renal function at the beginning of treatment and periodically during treatment. Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs, monitor renal function. Discontinue if renal function deteriorates. Mesalamine-Induced Acute Intolerance Syndrome: Symptoms may be difficult to distinguish from an exacerbation of ulcerative colitis, monitor for worsening symptoms, discontinue treatment if acute intolerance syndrome is suspected. Hypersensitivity Reactions, including Myocarditis and Pericarditis: Evaluate patients immediately and discontinue if a hypersensitivity reaction is suspected. Hepatic Failure: Evaluate the risks and benefits in patients with known liver impairment.

The following clinically significant adverse reactions are described elsewhere in labeling: Renal Impairment Mesalamine-Induced Acute Intolerance Syndrome Hypersensitivity Reactions Hepatic Failure Severe Cutaneous Adverse Reactions Upper Gastrointestinal Tract Obstruction Photosensitivity Nephrolithiasis Most common adverse reactions (≥3%) are: headache, abdominal pain, diarrhea, nausea, vomiting, respiratory infection, and arthralgia. Adverse reactions in pediatric patients were similar.

Nephrotoxic Agents including NSAIDs: Increased risk of nephrotoxicity, monitor for changes in renal function and mesalamine-related adverse reactions. Azathioprine or 6-Mercaptopurine: Increased risk of blood disorders, monitor complete blood cell counts and platelet counts.

Storage Store at 20° to 25°C (68° to 77°F), excursions permitted between 15° and 30°C (59° and 86°F).