Abstract
5-ASA, the active moiety of sulfasalazine, offers the advantages of “targeted” delivery of a mucosal anti-inflammatory agent with equal or enhanced therapeutic potency and a markedly reduced side-effect profile in IBD. Although the mechanism(s) of action remain uncertain, the compound can be used as a model to study both anti-inflammatory mediators and intestinal delivery systems for alternative non-systemic therapies.
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References
Bachrach, W.H. (1988) ‘Sulfasalazine: I. An historical perspective’, Am J Gastroenterol 83, 487–496.
Svartz, N. (1988) ‘Sulfasalazine: II. Some notes on the discovery and development of salazopyrin’, Am J Gastroenterol 83, 497–503.
Peppercorn, M.A. (1984) ‘Sulfasalazine, pharmacology, clinical use, toxicity and new drug development’, Ann Intern Med 101, 377–386.
Hoult, J.R.S. (1986) ‘Pharmacological and biochemical actions of sulphasalazine’, Drugs 32, 18–26.
Margolin, M.L., Krumholz, M.P., Fochios, S.E., Korelitz, B.I. (1988) ‘Clinical trials in ulcerative colitis. II. Historical review’, Am J Gastroenterol, 83, 227–243.
Bondesen, S., Rasmussen, S.N., Rask-Madsen, J., Nielsen, O.H., Lauritsen, K., Binder, V., Hansen, S.H., Hvidberg, E.F. (1987) ‘5-aminosalicylic acid in the treatment of inflammatory bowel disease’, Acta Med Scand 221, 227–242.
Allgayer, H., Ahnfelt, N.O., Kruis, W., Klotz, U., Frank-Holmberg, K., Soderberg, H.N.A., Paumgartner, G. (1989) ‘Colonic N-acetylation of 5-aminosalicylic acid in inflammatory bowel disease’, Gastroenterology 97, 38–41.
American Hospital Formulary Service (1989), American Society of Hospital Pharmacists Drug Information Publishers.
Isselbacher, K.J. (1987) ‘The role of arachidonic acid metabolites in gastrointestinal homeostasis: biochemical, histological and clinical gastrointestinal effects. Drugs 33(Suppl 1), 38–46.
Donowitz, M. (1985) ‘Arachidonic acid metabolites and their role in inflammatory bowel disease: update requiring addition of a pathway’, Gastroenterology 88, 580–587.
Peskar, B.M., Dreyling, K.W., May, B., et al (1987) ‘Possible mode of action of 5-aminosalicylic acid’ Dig Dis Sci 32, 51–56S.
Grisham, M.B., Granger, D.N. (1988) ‘Neutrophil-mediated mucosal injury: role of reactive oxygen metabolites’, Dig Dis Sci 33, 6–15S.
Eliakim, R., Karmeli, F., Razin E., Rachmilewitz, D. (1988) ‘Role of platelet-activating factor in ulcerative colitis. Enhanced production during acute disease and inhibition by sulfasalazine and prednisolone’, Gastroenterology 95, 1167–1172.
MacDermott, R.P., Schloemann, S.R., Bertovich, M. J., Nash, G. S., Peters, M., Stenson, W.F. (1989) ‘Inhibition of antibody secretion by 5-aminosalicylic acid’, Gastroenterology 96, 442–448.
Williams, C.N., Haber, G., Aquino, J.A. (1987) ‘Double-blind, placebo-controlled evaluation of 5-ASA suppositories in active distal proctitis and measurement of extent of spread using 99mTc-labelled 5-ASA suppositories’, Dig Dis Sci 32, 71–75S.
Campieri, M., Lanfranchi, G.A., Brignola, C., Bazzocchi, G., Gionchetti, P., Minguzzi, M.R., Adami, F. (1985) ‘5-aminosalicylic acid for the treatment of inflammatory bowel disease’, Gastroenterology 89, 701–702.
Hanauer, S.B., (1989) ‘5-ASA enema therapy’ Netherlands J Med 35, 11–20S.
Norlander, B., Jotthard, R., Strom, M. (1989) ‘Comparative pharmacokinetic study of Claversal enteric-coated tablets and Claversal suppository versus sulfasalazine tablets’, (To be published Scand J Gastroenterol).
Sutherland, L.R., Martin, F., Greer, S., Robinson, M., Greenberger, N., Saibil, F., Martin, T., Sparr, J., Prokipchuk, E., Borgen, L. (1987) ‘5-aminosalicylic acid enema in the treatment of distal ulcerative colitis, proctosigmoiditis, and proctitis’ Gastroenterology 92, 1894–1898.
Truelove, S.C. (1988) ‘Evolution of olsalazine’, Scand J Gastroenterol 23 (Suppl 148), 3–6.
Willoughby, C.P., Aronson, J.R., Agback, H., Bodin, N.O., Truelove, S.C. (1982) ‘Distribution and metabolism in healthy volunteers of disodium azodisalicylate, a potential therapeutic agent for ulcerative colitis’, Gut 23, 1081–1087.
Van Hogezand, R.A., Van Hees, P.A.M., Zwanenberg, B., Van Rossum, J.M., Tongeren, J.H.M. (1985) ‘Disposition of disodium azodisalicylate in healthy subjects. A possible new drug for inflammatory bowel disease’, Gastroenterology 88, 717–722.
Pamukcu, R., Hanauer, S.B., Chang, E.B. (1988) ‘Effect of disodium azodisalicylate on electrolyte transport in rabbit ileum and colon in vitro’, Gastroenterology 95, 975–981.
Hanauer, S.B. (1988) ‘5-ASA agents’, in M. Peppercorn (ed.), The Management of Inflammatory Bowel Disease, Marcek Dekker Publishers, 65–91.
Dew, M.J., Ebden, P., Kidwai, N.S., Lee, G.I., Evans, B.K., Rhodes, J. (1984) ‘Comparison of the absorption and metabolism of sulphasalazine and acrylic-coated 5-aminosalicylic acid in normal subjects and patients with ulcerative colitis’, Br J Clin Pharmacol 17, 474–476.
Rijk, M.C.M., Van Schaik, A., Van Tongeren, J.H.M. (1988) ‘Disposition of 5-aminosalicylic acid by 5-aminosalicylic acid-delivering compounds’, Scand J Gastroenterol 23, 107–112.
Klotz, U., Maier, K.E., Fischer, C., Bauer, K.H. (1985) ‘A new slow-release form of 5-aminosalicylic acid for the oral treatment of inflammatory bowel disease: biopharmaceutic and clinical pharmacokinetic characteristics’, Arzneim.-Forsch./Drug Res 35(1), 636–639.
Hardy, J.G., Healey, J.N.C., Lee, S.W., Reynolds, J.R. (1987) ‘Gastrointestinal transit of an enteric-coated delayed-release 5-aminosalicylate acid tablet’, Alimentary Pharmacol Ther 1(3), 209–216.
Rasmussen, S.N., Bondesen, S., Hvidberg, E.F., Hansen, S.B., Binder, V., Halskov, S., Flachs, H. (1982) ‘5-aminosalicylic acid in a slow release preparation: bioavailability, plasma level, and excretion in humans’, Gastroenterology 83, 1062–1070.
Khan, A.K.A., Piris, J., Truelove, S.C. (1977) ‘An experiment to determine the active therapeutic moiety of sulphasalazine’, Lancet 2, 892–895.
Klotz, U., Maier, K., Fischer C., Heinkel, K. (1980) ‘Therapeutic efficacy of sulfasalazine and its metabolites in patients with ulcerative colitis and Crohn’s disease’, New Engl J Med 303, 1499–1502.
Van Hees, P.A., Bakker, J.H., Van Tongeren, J.H.M. (1980) ‘Effect of sulphapyridine, 5-aminosalicylic acid, and placebo in patients with idiopathic proctitis: A study to determine the active therapeutic moiety of sulphasalazine’, Gut 21, 632.
Borgen, L.A., Hanauer, S.B., Good, L., Williams, C.N., Haber, G. (1988) ‘Mesalamine suppository efficacy in ulcerative proctitis: A multicenter placebo-controlled trial’, Gastroenterology 94(5), A42.
Hanauer, S.B., Kane, S.V., Guernsey, B., O’Connor, T., Robinson, M., Peppercorn, M., Rosenberg, F.B., Weinberg, D., Rogers, A.I., Singleton, J. (1989) ‘Randomized clinical trial of mesalamine (5-ASA) enemas in distal ulcerative colitis: A dose-ranging placebo controlled study’, Gastroenterology 96(5), A247
Campieri, M., Lanfranchi, G.A., Bazzocchi, G., Brignola, A., Sarti, F., Franzin, G., Battochia, A., Labo, G., Dal Monte, P.R. (1981) ‘Treatment of ulcerative colitis with high-dose 5-aminosalicylic acid enemas’, Lancet 2, 270–271.
Ginsberg, A.L., Beck, L.S., McIntosh, T.M., Nochomovitz, L.E. (1988) ‘Treatment of left-sided ulcerative colitis with 4-aminosalicylic acid enemas: A double-blind, placebo-controlled trial’, Ann Intern Med 108, 195–199.
Gandolfo, J., Farthing, F., Powers, G., Eagen, K., Goldberg, M., Berman, P., Kaplan, M. (1987) ‘4-aminosalicylic acid retention enemas in treatment of distal colitis’, Dig Dis Sci 32(7), 700–704.
Sandberg-Gertzen, H., Ryde, M., Janerot, G. (1983) ‘Absorption, metabolism and excretion of a single 1 gm dose of azodisal sodium in subjects with ileostomy’, Scand J Gastroenterol 18, 107–111.
Jewell, D.P., Ireland, A. (1988) ‘Controlled trial comparing olsalazine and sulphasalazine for maintenance treatment of ulcerative colitis’, Scand J Gastroenterol 23 (Suppl 148), 45–47.
Meyers, S., Sachar, D.B., Present, D.H., Janowitz, H.D. (1987) ‘Olsalazine sodium in the treatment of ulcerative colitis among patients intolerant of sulfasalazine’, Gastroenterology 93, 1255–1262.
Riley, S.A., Mani, V., Goodman, M.J., Herd, M.E., Dutt, S., Turnberg, L.A. (1988) ‘Comparison of delayed release 5-aminosalicylic acid (mesalazine) and sulphasalazine in the treatment of mild to moderate ulcerative colitis relapse’, Gut 29, 669–674.
Schroeder, K.W., Tremaine, W.J., Ilstrup, D.M. (1987) ‘Coated oral 5-aminosalicylic acid therapy for mildly to moderately active ulcerative colitis’, New Engl J Med 317, 1625–1629.
Dew, M.J., Harries, A.D., Evans, N., Evans, B.K., Rhodes, J. (1984) ‘Maintenance of remission in ulcerative colitis with 5-aminosalicylic acid in high doses by mouth’, Brit Med J 287, 23–24.
Riley, S.A., Mani, V., Goodman, M.J., Herd, M.E., Dutt, S., Turnberg, L.A. (1988) ‘Comparison of delayed-release 5-aminosalicylic acid (Mesalazine) and sulfasalazine as maintenance treatment for patients with ulcerative colitis’, Gastroenterology 94, 1383–1389.
Rachmilewitz, D., et al. (1989) ‘Coated mesalazine (5-aminosalicylic acid) versus sulphasalazine in the treatment of active ulcerative colitis: a randomized trial’, Brit Med J 298, 82–86.
Rutgeerts, P. (1989) ‘Efficacy and safety of mesalazine (Claversal) in maintenance treatment of ulcerative colitis: a report of a double-blind, randomized comparison with sulfasalazine’, (To be published Scand J Gastroenterol).
Thomson, A.B.R. (1989) ‘Preliminary data of a clinical trial. Claversal presents relapses and maintains remission of inactive Crohn’s disease’, (To be published Scand J Gastroenterol).
Mulder, C.J.J., Tytgat, G.N.J., Weterman, I.T., Dekker, W., Blok, P., Schrijver M., V.D. Heide, H. (1988) ‘Double-blind comparison of slow-release 5-aminosalicylate and sulfasalazine in remission maintenance in ulcerative colitis’, Gastroenterology 95, 1449–1453.
Hanauer, S.B., Schwartz, J., Roufail, W., Robinson, M., Cello, J., Safdi, M., Guernsey, B., Beshears, L. (1989) ‘Dose-ranging study of oral mesalamine capsule (PentasaR) for active ulcerative colitis’, Gastroenterology 96, A195.
Rasmussen, S.N., Lauritsen, K., Tage-Jensen, U., Nielsen, O.H., Bytzer, P., Jacobsen, O., Ladefoged, K., Vilien, M., Binder, V., Rask-Madsen, J., Bondesen, S., Honore Hansen, S., Hvidberg, E.F. (1987) ‘5-aminosalicylic acid in the treatment of Crohn’s disease: A 16-week double-blind, placebo-controlled, multicentre study with Pentasa’, Scand J Gastroenterol 22, 877–883.
Rao, S.S., Cann, P.A., Holdsworth, C.D. (1987) ‘Clinical experience of the tolerance of mesalazine and olsalazine in patients intolerant of sulphasalazine’, Scand J Gastroenterol 22, 332–336.
Riley, S.A. Lecarpentier, J., Mani, V., Goodman, M.J., Mandal, B.K., Turnberg, L.A. (1987) ‘Sulphasalazine induced seminal abnormalities in ulcerative colitis: Results of mesalazine substitution’, Gut 28, 1008–1012.
Poldermans, D., Van Blankenstein, M. (1988) ‘Pancreatitis induced by disodium azodisalicylate’, Am J Gastroenterol 83, 578–590.
Clementz, G.L., Dolin, B.J. (1988) ‘Sulfasalazine-induced lupus erythematosus’, Am J Med 84, 535–538.
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Hanauer, S.B. (1990). 5-ASA in Ulcerative Colitis. In: Rachmilewitz, D., Zimmerman, J. (eds) Inflammatory Bowel Diseases 1990. Developments in Gastroenterology, vol 11. Springer, Dordrecht. https://doi.org/10.1007/978-94-009-1980-8_20
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DOI: https://doi.org/10.1007/978-94-009-1980-8_20
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