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At least 523 records · Page 29Linked to original sources
PubMed1994

5-Aminosalicylic acid inhibits leukotriene B4 omega-hydroxylase activity in human polymorphonuclear leukocytes.

omega-Oxidation is regarded as the major pathway for the metabolism and inactivation of leukotriene B4 (LTB4). To investigate the action of 5-aminosalicylic acid (5-ASA) on LTB4 omega-hydroxylase activity, we incubated human polymorphonuclear leukocytes (PMNLs) with 3H-labeled LTB4 after pre-incubation with various concentrations of 5-ASA. omega-oxidation metabolites were separated by high performance liquid chromatography and each radioactivity was measured by a liquid scintilation counter. LTB4 omega-hydroxylase activity was inhibited by 5-ASA in a concentration-dependent fashion. The 50% inhibitory dose was about 50 mumol/l, which is within the concentration range found in the colonic mucosa. Our findings may be valuable in elucidating the potentially critical aspect of 5-ASA treatment in ulcerative colitis (UC).

Aminosalicylic Acids↗
PubMed1991

Retrograde spread of mesalazine (5-aminosalicylic acid)-containing enema in patients with ulcerative colitis.

In order to investigate the retrograde spread in the colon and its relationship to the extent of the diseased area, the authors evaluated a 100ml enema of mesalazine (5-aminosalicylic acid, Pentasa') lg in a consecutive series of 30 patients with ulcerative colitis. The enema was labelled with 10 MBq 99mtechnetium-human serum albumin microcolloid. Sequential scintigraphic imaging was performed in all patients, and the results compared with the extension of the disease as found by colonoscopy. If the enema reached the entire affected area it was interpreted as 'topically adequate'. In 80% of the patients there was retrograde spread of the enema beyond the rectosigmoid, thus reaching the affected area in ulcerative colitis. No relationship was found between the extent of dispersion of the enema and the time of defecation prior to scintigraphy. The authors conclude that a 100ml 'Pentasa' enema may be adequate for treatment of ulcerative colitis extending up to the splenic flexure.

Adolescent↗
PubMed2005

5-Aminosalicylic acid reverses endosulfan-induced testicular toxicity in male rats.

Pre-treatment with 5-aminosalicylic acid (5-ASA) significantly reduced sperm-shape abnormalities in endosulfan-treated rats. The number of abnormal sperm in the epididymis was markedly increased by endosulfan treatment but pre-treatment with 5-ASA kept these values close to normal. Treatment with 5-ASA at a dose of 25 mg/kg bw was more effective in reducing sperm-shape abnormality and sperm count than at a dose of 50 mg/kg bw. Endosulfan significantly increased the level of lactate dehydrogenase (LDH) in rats but a marked decrease was observed upon pre-treatment with 25 mg/kg bw 5-ASA. Changes in plasma testosterone levels were not significantly correlated with 5-ASA pre-treatment but histopathological analysis of seminiferous tubules and Leydig cells showed significant protection from endosulfan-induced tissue damage such as necrosis. The population of Sertoli cells increased and the lumen of the seminiferous tubules contained a greater number of spermatids. There was a corresponding increase in the number of Leydig cells. A curative study with 5-ASA showed a similar protection from endosulfan-induced toxicity and cellular damage, but the extent of protection was significantly lower.

Animals↗
PubMed1990

Estimation of 5-aminosalicylic acid and its metabolite in human serum by front-face fluorometry: a simple and sensitive method.

Salicylazosulfapyridine (SASP), commonly used in the treatment of inflammatory bowel disease, breaks down in the colon into sulfapyridine and 5-aminosalicylic acid (5-ASA), the active moiety of SASP. We report a sensitive method to measure 5-ASA and its known major metabolite acetyl 5-ASA (Ac-5-ASA) directly from the serum without any extraction procedure. Using front-face fluorometry, 5-ASA and Ac-5-ASA were detected at the excitation wavelength of 310 nm with emission maxima at 475 nm and 440 nm, respectively. Standard curves were obtained by adding known amounts of 5-ASA and Ac-5-ASA to several individual and pooled human sera. Presence of sulfapyridine (0 to 20 micrograms/ml) and SASP (0 to 15 micrograms/ml) in the serum did not interfere with the assays. Five microliters of acetic anhydride was added to the serum to convert all 5-ASA to Ac-5-ASA. The difference in the spectrum before and after addition of acetic anhydride represented the concentration of free 5-ASA. The values thus estimated were within 1% of the expected readings from the standard curves. This assay was compared with the organic extraction method for the determination of free and acetylated 5-ASA in sera of patients given olsalazine (azodisalicylate). The results demonstrate that direct analysis of the sera by front-face fluorometry enables us to measure 5-ASA and Ac-5-ASA at levels as low as 0.1 micrograms/ml in serum, making this method at least 10-fold more sensitive than the current available extraction methods.

Aminosalicylic Acids↗
PubMed1990

Coated oral 5-aminosalicylic acid versus placebo in maintaining remission of inactive Crohn's disease. International Mesalazine Study Group.

A randomized, double-blind, placebo-controlled multicentre study was undertaken to evaluate the safety and efficacy of coated, oral 5-aminosalicylic acid (Mesasal/Claversal; 5-ASA) in maintaining remission of inactive Crohn's disease for up to 12 months. A total of 248 patients were entered from eight countries, of which 206 adhered to the protocol and were included in the analysis. The patients had Crohn's disease for an average of 5 years, with their disease clinically inactive for at least 1 month prior to entry into the study, and for an average of over 12 months previously. Thirty per cent of patients had had a previous resection, 16% of patients had been treated with sulphasalazine, while none of those analysed received glucocorticosteroids. Treatment consisted of 500 mg 5-ASA t.d.s. or placebo. 'Relapse' was defined as the first occurrence of Best's Crohn's Disease Activity Index greater than 150, which had increased 60 points from the pre-trial index. The cumulative life-table relapse estimate was lower in 5-ASA patients compared to placebo (22.4% vs 36.2%, respectively, Log rank test P = 0.0395). The 12-month relapse estimate in the 5-ASA group was also lower in patients with ileal disease (8.3% for 5-ASA and 31.0% for placebo, P = 0.0535) and in patients with previous bowel resections (14.2% vs 47.0%, P = 0.0436). The incidence of side-effects was similar in both treatment groups. It is concluded that 5-ASA was significantly superior to placebo in preventing relapse of Crohn's disease; this effect was most apparent in patients with disease restricted to the ileum and in patients with previous bowel resection. 5-ASA was well-tolerated, as demonstrated by a low incidence of adverse events.

Adolescent↗
PubMed1990

5-Aminosalicylic acid suppositories in the maintenance of remission in idiopathic proctitis or proctosigmoiditis: a double-blind placebo-controlled clinical trial.

Thirty patients with distal ulcerative colitis in remission (17 proctitis, 13 proctosigmoiditis) were randomly given either 5-aminosalicylic acid (5-ASA) or placebo suppositories, 400 mg bid. During the 1-yr follow-up, patients were assessed clinically every month, and flexible sigmoidoscopy with a rectal pinch biopsy specimen and laboratory data were carried out every 3 months. Two patients in the 5-ASA group chose to withdraw from the study, one relapsed, and 12 remained in remission. In the placebo group, one patient chose to withdraw, 11 relapsed, and three remained in remission. The cumulative remission rate at the 12th month was 92% in the 5-ASA group and 21% in the placebo group. Log rank test showed a significant difference in the relapse rate between the two groups (chi 2 = 14.26, p less than 0.001). No side effects were observed. We conclude that 5-ASA in suppository form (800 mg/day), administered for 1 yr, is safe and effective in maintaining remission of distal ulcerative colitis.

Administration, Rectal↗
PubMed1988

Comparison of 5-aminosalicylic acid (3 g) and prednisolone phosphate sodium enemas (30 mg) in the treatment of distal ulcerative colitis. A prospective, randomized, double-blind trial.

Twenty-nine patients with attacks of distal ulcerative colitis were treated randomly with 3 g 5-aminosalicylic acid (5-ASA) or 30 mg of prednisolone phosphate sodium (PP) enemas (40 ml). Endoscopic, clinical, and histologic improvement were comparable in the two treatment groups. Our study showed that topical treatment with 5-ASA is as efficacious as PP in improving distal ulcerative colitis.

Adult↗
PubMed1984

The prophylactic effect of 5-aminosalicylic acid and salazosulphapyridine on degraded-carrageenan-induced colitis in guinea pigs.

Experimental colitis was induced in guinea pigs by administration of 5% degraded carrageenan for 5 days. The prophylactic effect of a slow-release preparation of 5-aminosalicylic acid (5-ASA; 13 mg/100 g/day) was compared with approximately equimolar amounts of salazosulphapyridine (SASP; 26 mg/100 g/day) and placebo. Treatment was started 2 days before initiation of carrageenan administration. The drugs were administered through a chronic gastric fistula. At the end of the study concentrations of 5-ASA and acetylated 5-ASA (Ac-5-ASA) in cecal contents and in plasma were determined. In the placebo group, all guinea pigs developed many small punctiform ulcerations in the cecum (median, 30/cm2). In the 5-ASA group no protective effect was demonstrated, since the number of ulcerations was 37/cm2. The difference is not statistically significant. However, the SASP group presented significantly fewer ulcerations (4/cm2). The concentrations of 5-ASA and/or its acetylated metabolite were several times higher in the cecum content and twice as high in plasma in the SASP group, indicating a difference in the absorption patterns of 5-ASA and the two drugs. These results and the etiological difference between the human ulcerative colitis and the carrageenan model may account for the lack of prophylactic effect of the slow-release 5-ASA in this experiment.

Aminosalicylic Acids↗
PubMed1986

[Drug therapy of chronic inflammatory intestinal diseases--current status of 5-aminosalicylic acid].

Assessment of the nature, location and extent of the disease, disease activity and the intestinal and extraintestinal complications and manifestations is an essential prerequisite in the treatment of inflammatory bowel disease. Corticosteroids, sulfasalazine (SASP) and rectal administration of 5-aminosalicylic acid (5-ASA) are effective in the treatment of ulcerative colitis. Oral 5-ASA in the form of a slow-release preparation is probably also effective. Rectal SASP or 5-ASA in addition to corticosteroids is indicated in distal colitis. In severe pancolitis oral or intravenous corticosteroids are required, whilst in less severe forms SASP or 5-ASA can be used. However, the safety of 5-ASA over longer treatment periods has yet to be verified. Surgery is indicated in colitis refractory to maximal treatment over several months. Apart from parenteral or enteral nutrition, treatment with prednisolone is effective in acute exacerbations of Crohn's disease. SASP is possibly effective in colonic disease. The role of 5-ASA has yet to be defined. A prednisolone-induced remission can be maintained by means of low doses of prednisolone. SASP is probably not effective, whilst with 5-ASA conclusive data are missing. Metronidazole and azathioprin are considered to be reserve drugs and can be used in the treatment of fistulae or in order to cut down the dosage of prednisolone during remission. Substitution with vitamins and trace elements is necessary in a large number of patients with Crohn's disease.

Adrenal Cortex Hormones↗