INTESTINAL FATE OF 5‐AMINOSALICYLIC ACID: REGIONAL AND SYSTEMIC KINETIC STUDIES IN RELATION TO INFLAMMATORY BOWEL DISEASE

1997; Wiley; Volume: 81; Issue: s2 Linguagem: Inglês

10.1111/j.1600-0773.1997.tb01944.x

ISSN

1600-0773

Autores

S Bondesen,

Tópico(s)

Helicobacter pylori-related gastroenterology studies

Resumo

Pharmacology & ToxicologyVolume 81, Issue s2 p. 1-30 Free Access INTESTINAL FATE OF 5-AMINOSALICYLIC ACID: REGIONAL AND SYSTEMIC KINETIC STUDIES IN RELATION TO INFLAMMATORY BOWEL DISEASE Stig Bondesen, Stig BondesenSearch for more papers by this author Stig Bondesen, Stig BondesenSearch for more papers by this author First published: 25 March 2009 https://doi.org/10.1111/j.1600-0773.1997.tb01944.xCitations: 20AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinkedInRedditWechat References 1 Ahnfelt-Rønne, I., O. H. Nielsen, A. Christensen, E. Langholz, V Binder & P. Riis: Clinical evidence supporting the radical scavenger mechanism of 5-aminosalicylic acid. Gastroenterology 1990, 98, 1162– 1169. 2 Allgayer, H., N. O. Ahnfelt, W. Kruis, U. Klotz, K. Frank-Holmberg, H. N. Soderberg & G. Paumgartner: Colonic N-acetylation of 5-aminosalicylic acid in inflammatory bowel disease. Gastroenterology 1989, 97, 11– 38. 3 Allgayer, H., W. Kruis, J. Eisenburg & G. Paumgartner: Comparative pharmacokinetics of sulphasalazine and sulphapyridine after rectal and oral administration to patients with ulcer-ative colitis. Eur. J. Clin. Pharmacol. 1984, 26, 275– 277. 4 Allgayer, H., J. Sonnenbichler, W. Kruis & G. Paumgartner: Determination of the pK values of 5-aminosalicylic acid and N-acetylaminosalicylic acid and comparison of the pH dependent lipid-water partition coefficients of sulphasalazine and its metabolites. Arzneimittelforschung 1985, 35. 1457– 1459. 5 Almer, S., B. Norlander, M. Strøm & H. Osterwald: Steady-state pharmacokinetics of a new 4-gram 5-aminosalicylic acid retention enema in patients with ulcerative colitis in remission. Scand. J. Gastroenterology 1991, 26(3), 327– 335. 6 Astbury, C, A. J. Taggart, L. Juby, L. Zebouni & H. A. Bird: Comparison of the single-dose pharmacokinetics of sulphasalazine in theumatoid arthritis and inflammatory bowel disease. Ann. Rheum. Dis. 1990, 49, 587– 590. 7 Anthonisen, P., F. Barany, O. Folkenborg, et al.: The clinical effect of salazosulphapyridine in Crohn's disease. A controlled double-blind study. Scand. J. Gastroenterol. 1974, 9, 549– 554. 8 Azad Khan, A. K., J. Piris & S. C. Truelove: An experiment to determine the active therapeutic moiety of sulphasalazine. Lancet 1977, 29(2), 892– 895. 9 Azad Khan, A. K., G. Guthrie, J. H. Johnston, S. C. Truelove & D. H. Williamson: Tissue and bacterial splitting of sulphasalazine. Clin. Science 1983, 64, 349– 354. 10 Azad Khan, A. K. & D. T. Howes. J. Piris & S. C. Truelove: Optimum dose of sulphasalazine for maintenance treatment in ulcerative colitis. Gut 1980, 21, 232– 240. 11 Azad Khan, A. K. & S. C. Truelove & J. K. Aronson: The disposition and metabolism of sulphasalazine (salicylazosul-phapyridine) in man. Br. J. Clin. Pharmacol. 1982, 13, 523– 528. 12 Azad Khan, A. K. & S. C. Truelove: Circulating levels of sulphasalazine and its metabolites and their relation to the clinical efficacy of the drug in ulcerative colitis. Gut 1980, 21, 706– 710. 13 Back, D. J. & S. M. Rogers: Review: first pass metabolism by the gastrointestinal metabolism. Aliment Pharmacol. Therap. 1987, 1, 339– 357. 14 Baron, J. H., A. M. Connell, J. E. Lennard-Jones & F. Avery Jones: Sulphasalazine and salicylazosulphadimidine in ulcerative colitis. Lancet 1962, ii, 1094– 1096. 15 Binder, V S. Halskov, E. Hvidberg, E. Kristensen, P. Riis, L. Tougaard, et al.: A controlled study of 5-acetaminosalicylic acid as enema in ulcerative colitis. Scand. J. Gastroenterol. 1981, 16, 1122. 16 Bondesen, S., S. N. Rasmussen, J. Rask-Madsen, O. H. Nielsen, K. Lauritsen, V. Binder, S. H. Hansen & E. F. Hvidberg: 5-aminosalicylic acid in the treatment of inflammatory bowel disease. Acta Med. Scand. 1987, 221, 227– 242. 17 Calder, I. C., C. C. Funder, C. R. Green, K. N. Ham & J. D. Tange: Nephrotoxic lesions from 5-amino-salicylic acid. BMJ 1972, 1, 152– 154. 18 Campieri, M., G. A. Lanfranchi, G. Bazzocchi, C. Brignola, F. Sarti, G. Franzin, A. Battocchia, G. Labo & P. R. DaiMonte: Treatment of ulcerative colitis with high-dose 5-aminosalicylic acid enemas. Lancet 1981, 2, 270– 271. 19 Campieri, M., G. A. Lanfranchi, S. Boschi, et al.: Topical administration of 5-aminosalicylic acid enemas in patients with ulcerative colitis. Studies on rectal absorption and excretion. Gut 1985, 26, 400– 405. 20 Campieri, M., G. A. Lanfranchi, C. Brignola, et al.: Retrograde spread of 5-aminosalicylic acid enemas in patients with active ulcerative colitis. Dis. Colon Rectum 1986, 29, 108– 110. 21 Christensen, L. A., J. Fallingborg, K. Abildgaard, B. A. Jacobsen, G. Sanchez, S. H. Hansen, S. Bondesen, E. F. Hvidberg & S. N. Rasmussen: Topical and systemic availability of 5-aminosalicylate: Comparisons of three controlled release preparations in man. Aliment Pharmacol. Ther. 1990, 4, 523– 533. 22 Christensen, L. A., O. Slot, G. Sanchez, J. Boserup, S. N. Rasmussen, S. Bondesen, S. H. Hansen & E. F. Hvidberg: Release of 5-aminosalicylic acid from Pentasa during normal and accelerated intestinal transit time. Br J Clin Pharmacol 1987, 23, 1062– 1070. 23 Corey, A. E., G. M. Rose & J. D. Conklin: Bioavailability of single and multiple doses of enteric coated mesalamine and sulphasalazine. J. Internal. Med. Res. 1990, 6, 441– 453. 24 Dale, K. Y., A. T. Elvin, B. Morrill, L. S. Eichmeier, R. C. Lanman, M. B. Lanman & D. H. Giesing: Effect of food coad-ministration on 5-aminosalicylic acid oral suspension bioavail-ability. Clin. Pharmacol. Ther. 1990, 48, 26– 33. 25 Danish 5-ASA group: Topical 5-aminosalicylic acid versus prednisolone in ulcerative proctosigmoiditis. A randomized, double-blind multicenter trial. Dig. Dis. Sci. 1987, 32, 598– 602. 26 Das, K. M.: Pharmacotherapy of inflammatory bowel disease. Part 1. Sulfasalazine. Postgrad. Med. 1983, 74(6), 141– 148, 150–151. 27 Das, K. M., M. A. Eastwood, J. P A. McManus & W. Sircus: The metabolism of salicylsazosulpha-pyridine in ulcerative colitis. Gut 1973, 14, 631– 5641. 28 Davis, S. S., J. G. Hardy & J. W. Fara: Transit of pharmaceutical dosage forms through the small intestine. Gut 1986, 27, 886– 892. 29 Day, J. M. & J. B. Houston: Saliva: plasma concentration relationships for sulphapyridine following sulphasalazine administration to normal volunteers and patients with inflammatory bowel disease. Br. J. Clin. Pharmacol. 1980, 9, 91– 94. 30 de Franchis, R., M. Vecchi, L. Carpinelli, G. Meucci & Torgano: Comparison of efficacy and safety of sulphasalazine and mesalazines in the maintenance treatment of ulcerative colitis: a metaanalysis. Eur. J. Gastroenterol. Hepatol. 1993, 5, 505– 510. 31 De Mey, C. & I. Meineke: Prandial and diurnal effects on the absorption of orally administered enteric coated 5-aminosalicylic acid (5-ASA). Br. J. Clin. Pharmacol. 1992, 33(2): 179– 182. 32 De Vos, M., H. Verdievel, R. Schoonjans, M. Praet, M. Bogaert & F. Barbier: Concentrations of 5-ASA and Ac-5-ASA in human ileocolonic biopsy homogenates after oral 5-ASA preparations. Gut 1992, 33, 1338– 1342. 33 Dew, M. J., P. Ebden, N. S. Kidwai, G. Lee, B. K. Evans & J. Rhodes: Comparison of the absorption and metabolism of sulphasalazine and acrylic-coated 5-amino salicylic acid in normal subjects and patients with colitis. Br. J. clin. Pharmacol. 1984, 17, 474– 476. 34 Dick, A. P., M. J. Grayson, R. G. Carpenter & A. Petrie: Controlled trial of sulphasalazine in the treatment of ulcerative colitis. Gut 1964, i: 437– 42. 35 Dissanayake, A. S. & S. C. Truelove: A controlled long-term maintenance treatment of ulcerative colitis with sulphasalazine. Gut 1973, 14, 923– 926. 36 Dull, B. I., K. Salata, A. van Langenhove & Å P. Goldman: 5-aminosalicylate: Oxidation by activated leukocytes and protection of cultured cells from oxidative damage. Biochem. Pharmacol. 1987, 36, 2467– 2472. 37 Ewe, K. Herfarth, Malchow & H. J. Jesdinsky: Postoperative recurrence of Crohn's disease in relation to radicality of operation and sulfasalazine prophylaxis: a multicenter trial. Digestion 1989, 42, 224– 232. 38 Fischer, C., K. Maier, E. Stumpf, U. Von-Gaisberg & U. Klotz: Disposition of 5-aminosalicylic acid, the active metabolite of sulphasalazine, in man. Eur. J. Clin. Pharmacol. 1983, 25, 511– 515. 39 Friedman, L. S., J. M. Richter, S. E. Kirkham, H. J. DeMonaco & R. J. May: 5-aminosalicylic acid enemas in refractory distal ulcerative colitis: a randomized, controlled trial. Am. J. Gastroenterol. 1986, 81, 412– 418. 40 Giaffer, M. H., C. J. O'Brien & C. D. Holdsworth: Clinical tolerance to three 5-aminosalicylic acid releasing preparations in patients with inflammatory bowel disease intolerant or allergic to sulphasalazine. Aliment Pharmacol. Ther. 1992, 6(1), 51– 59. 41 Goebell, H., U. Klotz, B. Nehlsen & P. Layer: Oroileal transit of slow release 5-aminosalicylic acid. Gut 1993, 34, 669– 675. 42 Goldman, P.: Will there be a next generation of sulfasalazine? Gastroenterology 1982, 83, 1138– 1141. 43 Greenfield, S. M., N. A. Punchard, J. P. Teare & R. P. Thompson: Review article: the mode of action of the aminosalicylates in inflammatory bowel disease. Aliment Pharmacol. Ther. 1993, 7(4), 369– 383. 44 Grisham, M. B. & D. N. Granger: 5-aminosalicylic acid concentration in mucosal interstitium of cat small and large intestine. Dig. Dis. Sci. 1989, 34, 573– 578. 45 Grisham, M. B., K. Ware, S. Marshall, T. Yamada & I. S. Sandhu: Prooxidant properties of 5-aminosalicylic acid. Possible mechanism for its adverse side effects. Dig. Dis. Sci. 1992, 37, 1383– 1389. 46 Hanauer, S., J. Schwartz, M. Robinson, W. Roufail, S. Arora, J. Cello & M. Safdi: Mesalamine capsules for treatment of active ulcerative colitis: results of a controlled trial. Pentasa Study Group. Am, J, Gastroenterol, 1993, 88(8), 1188– 1197. 47 Hanauer, S. B. & G. Stathopoulos: Risk-benefit assessment of drugs used in the treatment of inflammatory bowel disease. Drug Safety 1991, 6(3), 192– 219. 48 Hansen, S. H.: assay of 5-aminosalicylic and its acetylated metabolite in biological fluids by hiigh-performance liquid chromatography on dynamically modified silica. J. Chromatogr. 1981, 162, 237– 243. 49 Hansson, K. A.: Determination of free and acetylated 5-aminosalicylic acid in serum and urine after administration of salicylazosulphapyridine. Acta Pharm. Suec. 1973, 10, 153– 155. 50 Hardy, J. D., J. N. C. Healey, S. W. Lee & J. R. Reynolds: Gastrointestinal transit of an enteric-coated delayed-release 5-aminosalicylic acid tablet. Aliment Pharmacol. Therap. 1987, 1, 209– 217. 51 Hardy, J. G., W. J. Harvey, R. A. Sparrow, G. B. Marshall, K. P. Steed, M. Macarios & I. R. Wilding: Localization of drug release sites from an oral sustained-release formulation of 5-ASA (Pentasa) in the gastrointestinal tract using gamma scintigraphy. J Clin. Pharmacol. 1993, 33(8), 712– 718. 52 Houston, J. B., J. Day & J. Walker: Azo reduction of sulphasalazine in healthy volunteers. Br. J. Clin. Pharmacol. 1982, 14, 395– 398. 53 Houston J. B. & M. K. Cassidy: Rate-limiting steps in metabolite kinetics: formation of 5-acetyl-aminosalicylate after administration of 5-aminosalicylate. J Pharm. Pharmacol. 1982, 34, 536– 538. 54 Ireland, A., J. D. Priddle & D. P. Jewell: Acetylation of 5-aminosalicylic acid by isolated human colonic epithelial cells. Clin. Sci. 1990, 78, 105– 111. 55 Ireland, A., J. D. Priddle & D. P. Jewell: Comparison of 5-aminosalicylic acid and N-acetylaminosalicylic acid uptake by the isolated human colonic epithelial cell. Gut 1992, 33(10), 1343– 1347. 56 Jacobsen, B. A., K. Abildgaard, H. H. Rasmussen, L. A. Christensen, J. Fallingborg, S. H. Hansen & S. N. Rasmussen: Availability of mesalazine (5-aminosalicylic acid) from enemas and suppositories during steady-state conditions. Scand. J. Gastroenterology 1991, 26(4), 374– 378. 57 Jarnerot, G.: Newer 5-aminosalicylic acid based drugs in chronic inflammatory bowel disease. Drugs 1989, 37, 73– 86. 58 Jensen, J., C. Cornett, C. E. Olsen, S. Bondesen, J. Christensen, L. A. Christensen, J. Tjornelund & S. H. Hansen: Identification of oxidation products of 5-aminosalicylic acid in faeces and the study of their formation in vitro. Biochem. Pharmacol. 1993, 45(6), 1201– 1209. 59 Kellow, J. E., T. J. Borody, S. F. Phillips, A. C. Haddad & M. L. Brown: Sulfapyridine appearance in plasma after salicyla-zosulfapyridine. Gastroenterology 1989, 91, 396– 400. 60 Kiilerich, S., K. Ladefoged, T. Rannem, P. J. Ranløv and the Danish Olsalazine study group: Prophylactic effects of sulfasalazine during 12 months naintenance treatment of ulcerative colitis. Gut 1992, 33, 252– 255. 61 Kirsner, J. B.: Inflammatory bowel disease. Part I: Nature and pathogenesis. Dis. Mon. 1991, 37, 605– 666. 62 Kirsner, J. B.: Inflammatory bowel disease. Part II: Clinical and therapeutic aspects. Dis. Mon. 1991, 37, 669– 746. 63 Kjeldsen, J. & O. B. Schaffalitzky de Muckadell: Assessment of disease Severity and activity in inflammatory bowel disease. Review. Scand. J. Gastroenterol. 1993, 28, 1– 9. 64 Klotz, U.: Clinical pharmacokinetics of sulphasalazine, its metabolites, and other products of 5-aminosalicylic acid. Clin. Pharmacokinet. 1985, 10, 285– 302. 65 Larouche, J., J. Morais, M. Picard, C. Lambert, J. Spenard, H. Landriault, G. Kennedy & P. Poitras: Release of 5-aSa from Pentasa in patients with Crohn's disease of the small intestine. Aliment Pharmacol. Ther. 1995, 9(3), 315– 320. 66 Lauritsen, K., J. Hansen, M. Ryde & J. Rask-Madsen: Co-Ionic azodisalicylate metabolism determined by in vivo dialysis in healthy volunteers and patients with ulcerative colitis. Gastroenterology 1984, 86, 1496– 1500. 67 Lauritsen, K., L. S. Laursen, K. Bukhave & J. Rask-Madsen: Effects of topical 5-aminosalicylic acid and prednisolone on prostaglandin E2 and leukotriene B4 levels determined by equilibrium in vivo dialysis of rectum in relapsing ulcerative colitis. Gastroenterology 1986, 91, 837– 844. 68 Laursen, L. S., K. Stokholm, K. Bukhave, J. Rask-Madsen & K. Lauritsen: Disposition of 5-aminosalicylic acid by olsalazine and three mesalazine preparations in patients with ulcerative colitis: Comparisons of intraluminal colonic concentrations, serum values and urinary excretions. Gut 1990, 31, 1271– 1276. 69 Layer, P. H., H. Goebell, J. Keller, A. Dignass & U. Klotz: Delivery and fate of oral mesalamine microgranules within the human small intestine. Gastroenterology 1995, 108(5), 1427– 1433. 70 Malchow, H., K. Ewe, J. W. Brandes, H. Goebell, H. Ehms, H. Sommer & H. Jesdinsky: European cooperative Crohn's disease study (ECCDS): Results of drug treatment. Gastroenterology 1984, 86, 249– 266. 71 Mardini, H. Al, D. C. Lindsay, C. M. Deighton & C. O. Record: Effect of polymer coating on faecal recovery of ingested. 5-aminosalicylic acid in patients with ulcerative colitis. Gut 1987, 28, 1084– 1089. 72 Marshall J. K. & E. J. Irvine: Rectal aminosalicylate therapy for distal ulcerative colitis: a meta-analysis. Aliment Pharmacol. Ther. 1995, 9(3), 293– 300. 73 McLeod, R. S., Z. Coehn, B. J. Vari, J. E. Blair & G. R. Greenberg: The release profile of a controlled release preparation of 5-aminosalicylic acid (Rowasa) in humans. Dis. Col. Rect. 1990, 33, 21– 25. 74 Meese, C. O. C. Fischer & U Klotz: Is N-acetylation of 5-aminosalicylic acid reversible in man? Br. J. Clin. Pharmacol. 1984, 18, 612– 615. 75 Messori, A., C. Brignola, G. Trallori, R. Rampazzo, G. Bardazzi, C. Belloli, G. D'albasio, G. De Simone & N. Martini: Effectiveness of 5-aminosalicylic acid for maintaining remission in patients with Crohn's disease: a meta-analysis. Am. J. Gastroenterol. 1994, 89(5), 692– 698. 76 Meyers, S. & H. D. Janowitz: Natural history of Crohn's disease: An analytical review of the placebo lesson. Gaslroenterology 1984, 87, 1189– 1192. 77 Misiewicz, J. J., J. E. Lennard-Jones, A. M. Connell, J. H. Baron & F. Avery Jones: Controlled trial of sulphaslazine in maintenance therapy for ulcerative colitis. Lancet 1965, i, 185– 188. 78 Mulder, C. J., G. N. Tytgat, I. T. Weterman. W. Dekker, P. Blok, M. Schrijver & H. van der Heide: Double-blind comparison of slow-release 5-aminosalicylate and sulfasalazine in remission maintenance in ulcerative colitis. Gastroenlerology 1988, 95, 1449– 1453. 79 Myers, B., D. N. W. Evans, J. Rhodes, B. R. Hughes, M. G. Lee, A. Richens & D. Richards: Metabolism and urinary excretion of 5-amino-salicylic acid in healthy volunteers when given intravenously or released for absorption at different sites in the gastrointestinal tract. Gut 1987, 28, 196– 200. 80 Norlander, B., R. Gotthard & M. Strøm: Steady-state pharm-acokinetics of enteric coated 5-amino-salicylic acid tablets in healthy volunteers and in patients with Crohn's diasese or ulcerative colitis. Alimentary Pharmacology & Therapeutics 1991, 5(3), 291– 300. 81 Orholm, M., L. Iselius, A. Sørensen, P. Munkholm, E. Langholz & V Binder: Investigation of chronic inflammatory bowel diseases bycomplex segregational analysis. BMJ 1993, 306, 20– 24. 82 Peppercorn, M. A. & P. Goldman: Distribution studies of salicylazosulfapyridine and its metabolites. Gastroenterology 1973, 64, 240– 245. 83 Peppercorn, M. A. & R Goldman: The role of intestinal bacteria in the metabolism of salicylazosulfapyridine. J Pharmacol. Exp. Therap. 1972, 181. 555– 562. 84 Pieniaszek, H. J. Jr. & T. R. Bates: Colorimetric determination of 5-aminosalicylic acid and its N-acetylated metabolite on urine and feces. Res. Commun. Chem. Pathol. Pharmacol. 1975, 12, 571– 581. 85 Pieniaszek, H. J. Jr. & T. R. Bates: Capacity-limited gut wall metabolism of 5-aminosalicylic acid, a therapeutically active metabolite of sulfasalazine, in rats. J. Pharm. Sci. 1979, 68, 1323– 1325. 86 Pieniaszek, H. J. D. E. Resetarits, W. W. Wilferth, D. E. Blumenthal & T. E. Bates: Relative systemic availability of sulfapyridine from commercial enteric-coated and uncoated sulfasalazine tablets. J. Clin. Pharmacol. 1979, 1, 39– 45. 87 Prantera, C., F. Pallone, G. Brunetti, M. Cottone & M. Miglioli: Oral 5-aminosalicylic acid (Asacol) in the maintenance treatment of Crohn's disease. The Italian IBD Study Group Gastroenterology 1992, 103, 363– 368. 88 Rachmilewitz, D.: Coated mesalazine (5-aminosalicylic acid) versus sulphasalazine in the treatment of actived ulcerative colitis: a randomized trial. BMJ 1989, 298, 82– 86. 89 Rasmussen, S. N., V Binder, K. Maier, S. Bondesen, C. Fischer, U. Klotz, S. H. Hansen & E. F. Hvidberg: Treatment of Crohn's disease with peroral 5-aminosalicylic acid. Gastroenterology 1983, 85, 1350– 1353. 90 Rasmussen, S. N., S. Bondesen & E. F. Hvidberg: 5-amino-salicylic acid in a slow-release preparation: bioavailability, plasma level, and excretion in humans. Gastroenterology 1982, 83, 1062– 1070. 91 Rasmussen, S. N., K. Lauritsen, U. Tage-Jensen, et al.: 5-aminosalicylic acid in the treatment of Crohn's disease. A 16-week double-blind, placebo-controlled, multicentre study with Pentasa. Scand. J. Gastroenterol. 1987, 22, 877– 883. 92 Rijk, M. C., R. A. van Hogezand, H. J. J. van Lier & J. H. M. van Tongeren: Sulphasalazine and prednisone compared with sulphasalazine for treating active Crohn disease. Ann. Int. Med. 1991, 114, 445– 450. 93 Rijk, M. C., R. A. van Hogezand, A. van Schaik & J. H. van Tongeren: Disposition of 5-aminosalicylic acid from 5-aminosalicylic acid-delivering drugs during accelerated intestinal transit in healthy volunteers. Scand. J. Gastroenterol. 1989, 24, 1179– 1185. 94 Rijk, M. C., A. van Schaik & J. H. van Tongeren: Disposition of 5-aminosalicylic acid by 5-aminosalicylic acid-delivering compounds. Scand. J. Gastroenterol. 1988, 23, 107– 112. 95 Rijk, M. C., A. van Schaik & J. H. D. van Tongeren: Disposition of mesalazine from mesalazine-delivering drugs in patients with inflammatory bowel disease, with and without diarrhoea. Scand. J. Gastroenterol. 1992, 27(10), 863– 868. 96 Riley, S. A., V. Mani. M. J. Goodman, M. E. Herd, S. Dutt & L. A. Turnberg: Comparison of delayed-release 5-aminosalicylic acid (mesalazine) and sulphasalazine in the treatment of mild to moderate ulcerative colitis relapse. Gut 1988, 29, 669– 674. 97 Riley, S. A., I. A. Tavares, A. Bennett & V. Mani: Delayed-release mesalazine (5-aminosalicylic acid): coat dissolution and excretion in ileostomy subjects. Br. J. Clin. Pharmacol. 1988, 26, 173– 177. 98 Roediger, W., G. Schapel, M. Lawson, B. Radcliffe & S. Nance: Effect of 5-aminosalicylic acid (5-ASA) and other salicylates on short-chain fat metabolism in the colonic mucosa. Pharmacolo gical implications for ulcerative colitis. Biochem. Pharmacol. 1986, 35, 221– 225. 99 Salomon, P., A. Kornbluth, J. Aisenberg & H. D. Janowitz: How effective are current drugs for Crohn's disease. a meta-analysis. J. Clin. Gastroenterol. 1992, 14, 211– 215. 100 Sandberg-Gertzen, H., M. Ryde & G. Jarnerot: absorption and excretion of a single 1-g dose of azodisal sodium in subjects with ileostomy. Scand. J. Gastroenterol. 1983, 18, 107– 111. 101 Schninsky, C. A., D. H. Cort, F. Shanahan, B. J. Powers, J. T. Sessions, R. E. Pruit, et al.: Oral mesalamine (asacol) for mildly to moderately active ulcerative colitis. Ann, Int. Med. 1991, 115, 350– 355. 102 Schroder, H. & D. E. S. Campbell: Absorption, metabolism and excretion of salicylazosulfapyridine in man. Clin. Pharmacol. Ther. 1972, 13, 539– 551. 103 Schöder, H. & B. E. Gustafsson: Azo reduction of salicyl-azo-sulphapyridine in germ free and concentional rats. Xenobiotica 1973, 4, 225– 231. 104 Schröder, H. & A. K. Johansson: Redox potential in caecal contents of the rat and azo reduction of salicyl-azo-sulpha-pyridine. Xenobiotica 1973, 3, 233– 246. 105 Schroeder, K. W., W. J. Tremaine & D. M. Ilstrup: Coated oral 5-aminosalicylic acid therapy for mildly to moderately active ulcerative colitis. A randomized study. N. Engl. J. Med. 1987, 317, 1625– 1629. 106 Shafii, A., J. R. Chowdhury & K. M. Das: Absorption, enterohepatic circulation, and excretion of 5-aminosalicylic acid in rats. Am. J. Gastroenterol. 1982, 77, 297– 299. 107 Shah, S. A. & M. A. Peppercorn: Inflammatory bowel disease therapy: an update. Compr-Ther. 1995, 21, 296– 302. 108 Shanahan, F. & S. Targan: Medical treatment of inflammatory bowel disease. Annu. Rev. Med. 1992, 43, 125– 133. 109 Singleton, J. W., S. B. Hanauer, G. L. Gitnick, M. A. Peppercorn, M. G. Robinson, L. D. Wruble & E. L. Krawitt: Mesalamine capsules for the treatment of active Crohn's disease: results of a 16-week trial. Pentasa Crohn's Disease Study Group. Gastroenterology 1993, 104(5), 1293– 1301. 110 Spiller, R. C.: Where do all the tablets go? Gut 1986, 27, 879– 885. 111 Steinhart, A. H., D. Hemphill & G. R. Greenberg: Sulfasalazine and mesalazine for the maintenance therapy of Crohn's disease: A meta-analysis. Am. J. Gastroenterol. 1994, 89, 2116– 2124. 112 Stolz, A., Nortemann & H.-J. Knackmuss: Bacterial metabolism of 5-aminosalicylic acid. Biochem. J. 1992, 282, 675– 680. 113 Summers, R. W., D. M. Switz, J. T. Sessions, J. M. Bectel, W. R. Best, F. Kern & J. W. Singleton: National cooperative Crohn's disease study: result of drug treatment. Gastroenterology 1979, 77, 847– 869. 114 Sutherland, L. R., F. Martin, S. Greer, M. Robinson, N. Greenberger, F. Saibil, T. Martin, J. Sparr, Prokipchuk & L. Boregn: 5-aminosalicylic acid enema in the treatment of distal ulcerative colitis, proctosigmoiditis, and proctitis. Gastroenterology 1987, 92, 1894– 1898. 115 Sutherland, L. R., G. R. May & E. A. Shaffer: Sulfasalazine revisited: A meta-analysis of 5-aminosalicylic acid in the treatment of ulcerative colitis. Ann. Intern. Med. 1993, 118, 540– 549. 116 Svartz, N.: Salazopyrin, a new sulfanilamide preparation. Acta Med. Scand. 1942, 110, 577– 598. 117 Swift, G. L., C. M. Mills, J. Rhodes, B. K. Evans, A. Bennett & I. A. Tavares: A pharmacokinetic study of sulphasalazine and two new formulations of mesalazine. Aiment Pharmacol. Ther. 1992, 6, 259– 266. 118 Tiel van Buul, M. M., C. J. Mulder, E. A. van Royen, E. H. Wiltink & G. N. Tytgat: Retrograde spread of mesalazine (5-aminosalicylic acid)-containing enema in patients with ulcerative colitis. Clinical Pharmacokinetics 1991, 20(3), 247– 251. 119 Tjornelund, J., S. H. Hansen & C. Cornett: New metabolites of the drug 5-aminosalicylic acid. I. N-β-D-glucopyranosyl-5-aminosalicylic acid. Xenobiotica 1989, 19, 891– 899. 120 Tjørnelund, J., S. H. Hansen & C. Cornett: New metabolites of the drug 5-aminosalicylic acid. II. N-formyl-5-aminosalicylic acid. Xenobiotica 1991, 21, 605– 612. 121 Travis, S. P. L. & D. P. Jewell: Salicylates for ulcerative colitis -their mode of action. Pharmacol. Ther. 1994, 63, 135– 161. 122 Travis, S. P. L., C. Tysk, H. J. de Silva, H. Sandberg-Gertzén, D. P. Jewell & C. Järnerot: Optimum dose of olsalazine for maintaining remission in ulcerative colitis. Gut 1994, 35, 1282– 1286. 123 Ursing, B., T. Alm, F. Barany, Bergelin, K. G. Norlin, J. Hoevels, B. Huitfeldt, G. Järnerot, U. Krause, A. Krook, N. Lindström, Ö. Nordle & A. Rosen: Metronidazole and sulfasalazine for active Crohn's disease: The cooperative Crohn's disease study in Sweden. Gastroenterology 1982, 83, 550– 562. 124 van Hees, P. A. M., J. H. Bakker & J. H. Van-Tongeren: Effect of sulphapyridine, 5-aminosalicylic acid, and placebo in patients with idiopathic proctitis: a study to determine the active therapeutic moiety of sulphasalazine. Gut 1980, 21, 632– 635. 125 van Hees, P. A. M., J. H. Tuinte, J. M. Van-Rossum & J. H. Van-Tongeren: Influence of intestinal transit time on azo-reduction of salicylazosulphapyridine (Salazopyrin). Gut 1979, 20, 300– 304. 126 van Hees, P. A. M. & H. J. J. van Lier, P. H. van Elteren, W. M. M. Driessen, R. A. van Hogezand, G. P. M. Ten Velde, J. H. Bakker & J. H. M. van Tongeren: Effect of sulphasalazine in patients with active Crohn's disease: controlled double-blind study. Gut 1981, 22, 404– 409. 127 van Hees, P. A. M. & J. H. M. van Tongeren: Compliance to therapy in patients on a maintenance dose of sulfasalazine. J. Clin. Gastroenterol. 1982, 4, 333– 336. 128 van Hogezand, R. A., H. M. Kennis, A. van Schaik, J. P. Koopman & P. A. M. van Hees: Bacterial acetylation of 5-aminosalicylic acid in faecal suspensions under aerobic and anaerobic conditions. Eur. J. Clin. Pharmacol. 1992, 43, 189– 192. 129 van Hogezand, R. A., P. A. M. van Hees, J. P. W. M. van Gorp, H. J. J. van Lier, P. Wesseling, et al.: Double blind comparison of 5-aminosalicylic acid and acetyl 5-aminosalicylic acid suppositories in patients with idiopathic proctitis. Aliment Pharmacol. Therap. 1988, 2, 33– 40. 130 Vitti, R. A., F. Meyers, L. C. Knight, J. A. Siegel, L. S. Maimud & R. S. Fisher: Quantitative distribution of radiolabelled 5-aminosalicylic acid enemas in patients with left-sided ulcerative colitis. Dig. Dis. Sci. 1989, 34, 1792– 1797. 131 Wenckert, A., M. Kristensen, A. E. Eklund, et al.: The long-term prophylactic effect of salazosulphapyridine in primarily resected patients with Crohn's disease. A double-blind trial. Scand. J. Gastroenterol. 1978, 13, 161– 167. 132 Willoughby, C. P., J. Piris & S. C. Truelove: The effect of topical N-acetyl-5-aminosalicylic acid in ulcerative colitis. Scand. J. Gastroenterol. 1980, 15, 715– 719. 133 Wright, J. P., E. A. O'Keefe, L. Cuming & K. Jaskiewicz: Olsalazine in maintenance of clinical remission in patients with ulcerative colitis. Dig. Dis. Sci. 1993, 38(10), 1837– 1842. 134 Yashuara, M., Y. Kurosaki, T. Kimura & H. Sezaki: Drug elimination function of rat small intestine: metabolism and intraluminal excretion. Biochemical Pharmacology 1984, 33, 3131– 3136. Citing Literature Volume81, Issues2October 1997Pages 1-30 ReferencesRelatedInformation

Referência(s)