Studies of two novel sulfasalazine analogs, ipsalazide and balsalazide.
Sulfasalazine appears to exert its beneficial effect in colitis by releasing 5-aminosalicylic acid in the colon, but its use can be limited by side effects. Ipsalazide and balsalazide are novel sulfasalazine analogs designed to release 5-aminosalicylic acid and a nontoxic carrier molecule in the gastrointestinal tract. They have a low oral toxicity following single or repeat administration to mouse, rat, and ferret, and balsalazide is not mutagenic in the Ames test. Ipsalazide and balsalazide are split in rat and man, and the urinary and fecal excretion pattern of the 5-aminosalicylic acid released is similar to that of sulfasalazine; the carrier molecules are absorbed to a lesser extent than the sulfapyridine derived from sulfasalazine. These two analogs deserve therapeutic trial.
19 references, click to expand
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Sulphasalazine and male infertility: reversibility and possible mechanism.Gut. 1981 Jun;22(6):445-51 PMID: 6114897
-
The metabolism of salicylazosulphapyridine in ulcerative colitis. I. The relationship between metabolites and the response to treatment in inpatients.Gut. 1973 Aug;14(8):631-41 PMID: 4147555
-
Determination of sulphapyridine and its metabolites in biological materials after administration of salicylazosulphapyridine.Acta Pharm Suec. 1973 Mar;10(1):87-92 PMID: 4145285
-
Therapeutic efficacy of sulfasalazine and its metabolites in patients with ulcerative colitis and Crohn's disease.N Engl J Med. 1980 Dec 25;303(26):1499-502 PMID: 6107853
-
Disodium azodisalicylate in ulcerative colitis.Lancet. 1981 Nov 21;2(8256):1168-9 PMID: 6118605
-
Salicylazosulfapyridine in clinical practice.Gastroenterology. 1973 Jul;65(1):166-9 PMID: 4146457
-
Sulphasalazine and salicylazosulphadimidine in ulcerative colitis.Lancet. 1962 May 26;1(7239):1094-6 PMID: 13865153
-
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 Jul;21(7):632-5 PMID: 6107263
-
Effect of sulphasalazine in patients with active Crohn's disease: a controlled double-blind study.Gut. 1981 May;22(5):404-9 PMID: 6114023
-
Methods for detecting carcinogens and mutagens with the Salmonella/mammalian-microsome mutagenicity test.Mutat Res. 1975 Dec;31(6):347-64 PMID: 768755
-
Incidence of sulphasalazine-induced male infertility.Gut. 1981 Jun;22(6):452-5 PMID: 6114898
-
Influence of intestinal transit time on azo-reduction of salicylazosulphapyridine (Salazopyrin).Gut. 1979 Apr;20(4):300-4 PMID: 36332
-
The role of intestinal bacteria in the metabolism of salicylazosulfapyridine.J Pharmacol Exp Ther. 1972 Jun;181(3):555-62 PMID: 4402374
-
Determination of salicylazosulphapyridine in biological materials.Acta Pharm Suec. 1973 May;10(2):107-10 PMID: 4146996
-
Colorimetric determination of 5-aminosalicylic acid and its N-acetylated metabolite on urine and feces.Res Commun Chem Pathol Pharmacol. 1975 Nov;12(3):571-81 PMID: 747
-
Absorption, metabolism, and excretion of salicylazosulfapyridine in man.Clin Pharmacol Ther. 1972 Jul-Aug;13(4):539-51 PMID: 4402886
-
National Cooperative Crohn's Disease Study: results of drug treatment.Gastroenterology. 1979 Oct;77(4 Pt 2):847-69 PMID: 38176
-
Determination of free and acetylated 5-aminosalicylic acid in serum and urine after administration of salicylazosulphapyridine.Acta Pharm Suec. 1973 May;10(2):153-5 PMID: 4146997
-
An experiment to determine the active therapeutic moiety of sulphasalazine.Lancet. 1977 Oct 29;2(8044):892-5 PMID: 72239
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