Balsalazide

C3H7NO2 107-95-9) see Balsalazide sodium Calcium pantothenate Pamidronic acid L-alanine benzyl ester... 

CnHijNjO, 80573-04-2) see Balsalazide sodium DL-(l-carboxyethyl)oxamic acid diethyl ester (C7H15NO5 23460-73-3) see Pyridoxine... 

C7H4N2O2 619-24-9) see Tazanolast A -(4-nitrobenzoyl)-p-alanine (CJ0H10N2O3 59642-21-6) see Balsalazide sodium /7-nitrobenzoyl chloride... 

C7Hft03 69-72-7) see Acetylsalicylic acid Balsalazide sodium Flavoxate Hydroxyethyl salicylate Mesalazine Salazosulfapyridine Salsalate salicylic acid sodium salt... 

Newer mesalamine products utilize non-sulfapyridine methods for drug delivery. Olsalazine uses two mesalamine molecules linked together, while balsalazide uses the inert carrier molecule 4-aminobenzoyl-P-alanine. Both drugs use a diazo bond similar to sulfasalazine. Other mesalamine formulations are pH-dependent formulations that release mesalamine at various points throughout the GI tract. 

RP Chan, DJ Pope, AP Gilbert, PJ Sacra, JH Buron, JE Lennard-Jones. Studies of two novel sulfasalazine analogs, ipsalazide and balsalazide. Digest Dis Sci 28 609-716, 1983. 

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. 

Pharmacology Balsalazide 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 4-aminobenzoyl- -alanine. The recommended dose of 6.75 g/day for the treatment of active disease provides 2.4 g of free 5-aminosalicylic acid (5-ASA) to the colon. 

Distribution - The binding of balsalazide to human plasma proteins was at least 99%. 

Hypersensitivity to salicylates or any of the components of balsalazide capsules or balsalazide metabolites. 

Renal function impairment There have been no reported incidents of renal impairment in patients taking balsalazide. Renal toxicity has been observed in patients given other mesalamine products. Therefore, exercise caution when administering balsalazide to patients with known renal dysfunction or a history of renal disease. 

Lactation It is not known whether balsalazide is excreted in breast milk. Exercise caution when administering to a nursing woman. 

Children Safety and efficacy of balsalazide in pediatric patients have not been established. 

Pyloric stenosis Patients with pyloric stenosis may have prolonged gastric retention of balsalazide capsules. 

Alosetron (Lotronex) Budoneside, oral (Entocort EC) Balsalazide (Colazal) Dexpanthenol (Ilopan-Choline Oral, Ilopan) Dibucaine (NupCTcainal) Dicyclomine (Bentyl) Hydrocortisone, Rectal (Anusol-HC Suppository, Cortifoam Rectal, Proctocort, oth s) Hyoscyamine (Anaspaz, Cystospaz, Levsin, othCTs)... 

There are oral formulations that deliver drug to the lower intestine. In mesalazine 5-amino-salicylic acid is formulated in a polymer-coated oral preparation. Olsalazine is a dimer of 5-aminosalicylate linked by an azo bond. Balsalazide is delivered to the colon where it is cleaved by bacterial azoreduction to release equimolar quantities of mesalazine and 4-aminobenzoyl-/i-alanine. The newer 5-ASA preparations were shown to be superior to placebo and tended towards therapeutic benefit over sulfasalazine. However, considering their relative costs, a clinical advantage to using the newer 5-ASA preparations in place of sulfasalazine appears unlikely. 

Balsalazide (5ASA azo-bonded to para-aminobenzoic acid) 2.25 ... 

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... 

Drugs that contain 5-aminosalicylic acid (5-ASA) have been used successfully for decades in the treatment of inflammatory bowel diseases (Figure 62-8). 5-ASA differs from salicylic acid only by the addition of an amino group at the 5 (meta) position. Aminosalicylates are believed to work topically (not systemically) in areas of diseased gastrointestinal mucosa. Up to 80% of unformulated, aqueous 5-ASA is absorbed from the small intestine and does not reach the distal small bowel or colon in appreciable quantities. To overcome the rapid absorption of 5-ASA from the proximal small intestine, a number of formulations have been designed to deliver 5-ASA to various distal segments of the small bowel or the colon. These include sulfasalazine, olsalazine, balsalazide, and various forms of mesalamine. 

Sulfasalazine, balsalazide, and olsalazine contain 5-ASA bound by an azo (N=N) bond to an inert compound or to another 5-ASA molecule (Figure 62-8). In sulfasalazine, 5-ASA is bound to sulfapyridine in balsalazide, 5-ASA is bound to 4-aminobenzoyl-B-alanine and in olsalazine, two 5-ASA molecules are bound together. The azo structure markedly reduces absorption of the parent drug from the small intestine. In the terminal ileum and colon, resident bacteria cleave the azo bond by means of an azoreductase enzyme, releasing the active 5-ASA. Consequently, high concentrations of active drug are made available in the terminal ileum or colon. 

Of the azo compounds, 10% of sulfasalazine and less than 1% of balsalazide are absorbed as native compounds. After azoreductase breakdown of sulfasalazine, over 85% of the carrier molecule sulfapyridine is absorbed from the colon. Sulfapyridine undergoes hepatic metabolism (including acetylation) followed by renal excretion. By contrast, after azoreductase breakdown of balsalazide, over 70% of the carrier peptide is recovered intact in the feces and only a small amount of systemic absorption occurs. 

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