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Results for “AMINOSALICYLIC ACID”

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At least 559 records · Page 31Linked to original sources
PubMed1988

Treatment of ulcerative colitis with oral 5-aminosalicylic acid including patients with adverse reactions to sulfasalazine.

Sulfasalazine is an effective drug for maintaining remission in ulcerative colitis, but its use may be precluded by side effects. Eighty-five patients with active ulcerative colitis participated in a prospective open trial to examine the tolerance of the active constituent 5-aminosalicylic acid (5-ASA), coated with an acrylic resin, and its efficacy in inducing and subsequently maintaining a remission. Fifty-one of the patients had previously developed adverse reactions to sulfasalazine. After 4 wk of treatment with 3.2 g 5-ASA daily, a remission was achieved in 23 of 36 patients (64%) with mild or moderate disease, but in none of 43 patients with severe disease. Six patients were withdrawn because of side effects to 5-ASA, but only two of these patients had similar reactions on sulfasalazine. Supplementary corticosteroids for 6 wk or less induced a remission in 27 of the patients who had failed on 5-ASA alone. Fifty patients were therefore eligible for the maintenance phase of the trial, and 39 (78%) had a sustained clinical and endoscopic remission upon 1-yr follow-up. 5-ASA appears to be an effective drug for inducing remission in mild or moderate ulcerative colitis and for the maintenance of remission. It thus represents a valuable addition to the management of patients intolerant to sulfasalazine.

Administration, Oral↗
PubMed2005

Synthesis and properties of polysaccharide prodrugs of 5-aminosalicylic acid as potential colon-specific delivery systems.

The drug release of the polymer prodrugs of 5-aminosalicylic acid (5-ASA) was not only dependent on the property of the polymers but also dependent on the solubility of the prodrugs. We prepared several polysaccharide prodrugs of 5-ASA to examine the effect of solubility of prodrugs on the release characteristics of 5-ASA in the gastrointestinal contents of rats. The amide prodrug, chitosan-5-ASA (ChT-5-ASA), did not release the 5-ASA in the cecal and colonic contents. The ester prodrugs, hydroxypropyl cellulose-5-ASA (HPC-5-ASA), being poor solubility in 0.05mol/l acetic acid solution also did not release the 5-ASA in any of gastrointestinal contents of rats. Whereas the 5-ASA release from cyclodextrins-5-ASA (CyDs-5-ASA) in cecal and colonic contents was significantly higher than that in stomach and small intestine contents. And furthermore, with the decrease in the degree of substitution, the solubility of CyD-5-ASA increased, and the release of 5-ASA in the gastrointestinal contents was also higher at the same time interval of incubation. When the ratio of cyclodextrin (CyD) and 5-formylaminosalicylic acid (5-fASA), a precursor of 5-ASA prodrugs, was 1:10, CyD-5-ASA was very slightly soluble, and no release of 5-ASA was observed within 48h in gastrointestinal contents. The present results suggested that the ester prodrugs of 5-ASA with certain solubility could release 5-ASA in the cecal and colonic contents of rat.

Animals↗
PubMed1997

Controlled trial of oral 5-aminosalicylic acid for the prevention of early relapse in Crohn's disease.

BACKGROUND: Recent data indicate that 5-aminosalicylic acid (5-ASA) is most effective in preventing relapse of Crohn's disease in patients with a short duration of remission before enrollment. AIM: To evaluate the efficacy of oral 5-ASA treatment, started immediately after achieving steroid-induced remission, in preventing clinical relapses of Crohn's disease. METHODS: Patients with active Crohn's disease, achieving remission on steroids, were randomized to oral 5-ASA 3 g/day or placebo, while steroids were tapered over 6 weeks. The trial was terminated after interim analysis showed a slightly higher relapse rate in the 5-ASA group, and the calculated probability of seeing a statistically significant difference by completing the study was minimal. RESULTS: Final analysis included 117 patients (58 taking 5-ASA and 59 taking placebo; follow-up 9.2 +/- 6.5 months). Cumulative relapse rates at 6 and 12 months were 34% and 58% in 5-ASA patients and 31% and 52% in placebo patients, respectively (rate difference +0.095; 95% CI = -0.085 to +0.274). Subgroups analysis showed that 5-ASA was equally ineffective in patients with ileal, colonic or ileocolonic disease. CONCLUSIONS: Contrary to previous results, in our study early introduction of treatment with oral 5-ASA did not prevent relapse in Crohn's disease patients treated with steroids to induce remission.

Adolescent↗
PubMed1995

5-Aminosalicylic acid abrogates T-cell proliferation by blocking interleukin-2 production in peripheral blood mononuclear cells.

The antiinflammatory agent sulfasalazine (SS) is prescribed to treat Crohn's disease, ulcerative colitis and rheumatoid arthritis. Activated T cells are present within diseased mucosal and synovial sites. We tested whether SS or its metabolites 5-aminosalicylic acid (5-ASA) and sulfapyridine (SP) inhibited the T-cell activation products interleukin 2 (IL-2) and interleukin 2 receptor alpha-chain (IL-2R alpha). Experiments were performed in phytohemaglutinin- and phorbol ester-stimulated peripheral blood mononuclear cells. Radioactive thymidine and leucine incorporation assayed DNA and protein synthesis, respectively. Enzyme-linked immunosorbent assay and Northern blot analysis measured IL-2 and IL-2R alpha. Lactate dehydrogenase release determined cell viability, and intracellular free calcium was measured by an indole fluorescent indicator. SS and 5-ASA, but not SP, inhibited T-cell proliferation and protein synthesis in phytohemaglutinin- and phorbol ester-stimulated peripheral blood monomuclear cells. 5-ASA (625 microM) markedly reduced culture supernatant IL-2 protein levels by 92% and steady-state IL-2 messenger RNA levels 4.4-fold at 24 and 18 hr, respectively. The supplementation of IL-2 restored T-cell proliferation only in 5-ASA-treated cultures. SS, 5-ASA and SP did not alter intracellular calcium accumulation after mitogenic stimulation. SS and 5-ASA (625 microM) caused 71% and 37% cytotoxicity, respectively, in 72-hr cultures. 5-ASA inhibits T-cell proliferation in part by blocking IL-2 messenger RNA accumulation and protein production downstream of the rise in cytosolic calcium. Inhibition of IL-2 production is an additional mechanism of action for 5-ASA.

Aminosalicylic Acids↗
PubMed1988

Influence of salazosulphapyridine and 5-aminosalicylic acid on seminal qualities and male sex hormones.

Seminal abnormalities are a common side effect of salazosulphapyridine (SASP) treatment. We evaluated semen qualities and sex hormone concentrations in 11 patients with inflammatory bowel disease (IBD) during SASP treatment and 4 months after replacing SASP with an oral slow-release preparation of 5-aminosalicylic acid (5-ASA). Significant improvement in sperm count (p less than 0.01), morphology (p less than 0.02), and motility (p less than 0.02) could be observed during 5-ASA therapy, in comparison with SASP treatment. Three pregnancies occurred during the study period. The serum concentrations of gonadotrophins, prolactin, and sex hormone-binding globulin were normal in all patients and not significantly different in the two treatment periods. The mean total testosterone concentration decreased significantly (p less than 0.02) after 5-ASA substitution, together with serum albumin (p less than 0.005), although all values remained within normal limits. The apparent free testosterone concentration was not significantly different in the two treatment periods. It is concluded that a significant improvement in semen quality can be obtained in male patients with IBD after replacing SASP with 5-ASA.

Adult↗
PubMed1993

Slow-release 5-aminosalicylic acid therapy in children with small intestinal Crohn's disease.

Pharmacologic agents effective in the treatment of Crohn's disease confined to the small intestine are limited. The therapeutic efficacy of oral mesalazine in small bowel inflammation, although theoretically promising, remains unproven. In an open-labeled initial trial, timed-release 5-aminosalicylic acid (5-ASA), administered at a daily dosage of 30.6 +/- 9.0 mg/kg (mean +/- SEM) to children with active Crohn's disease involving the small intestine, was associated with improvement on the Harvey index in six of 12 patients treated for 8.1 +/- 3.9 weeks. In a subsequent prospective, double-blind study 14 children, ages 9.3 to 16.1 years, with active Crohn's disease limited radiologically in the small intestine were randomized to receive either timed-release 5-ASA [50 mg/kg/day (maximum 3 g/day)] or placebo for 8 weeks. Following a 4-week washout period, patients crossed over to receive the other study drug for a further 8 weeks. Six children completed the entire 20-week trial. The van Hees index improved among patients receiving 5-ASA for 8 weeks (delta = -18 +/- 6.4) but deteriorated among patients given placebo (delta = +14 +/- 4.1) (p < 0.05). Mean Crohn's Disease Activity Index (CDAI) decreased marginally after 8 weeks of 5-ASA treatment (delta = -48 +/- 38.2) but not with placebo (delta = -3.0 +/- 7.9) (p = 0.31). Of the eight noncompleters, more patients dropped out of the study because of lack of therapeutic response to placebo (n = 5) than to 5-ASA (n = 2).(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗