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Results for “AMINOSALICYLIC ACID”

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At least 253 records · Page 14Linked to original sources
PubMed1988

Delayed-release mesalazine (5-aminosalicylic acid): coat dissolution and excretion in ileostomy subjects.

1. Delayed-release mesalazine has been formulated to deliver 5-aminosalicylic acid to the colon. We have therefore studied the ileostomy excretion and coat dissolution of this preparation. 2. Following ingestion of a single tablet 88% (range 69-114%) of the 400 mg dose appeared unchanged in the ileosomy effluent over the subsequent 12 h. 3. Ileostomy effluent pH appeared to be a major determinant of 5-aminosalicylic acid release. 4. In vitro studies revealed rapid coat dissolution above pH 7.0, slow dissolution between pH 6.0 and 7.0 and non-dissolution at pH 2.0 and 4.0.

Adult↗
PubMed1981

Combined action of isoniazid and para-aminosalicylic acid in vivo on human chromosomes in lymphocyte cultures.

Two antitubercular drugs, viz., isoniazid (INH) and para-aminosalicylic acid (PAS), in combination, were evaluated for their in vivo clastogenic effects of human lymphocyte chromosomes. Lymphocyte cultures from tuberculosis patients taking a therapeutic dose of INH and PAS for a period of not less than 3 months and from two sets of controls were used: (1) newly diagnosed tuberculosis patients who were not yet under therapy and (2) healthy individuals from the general population. Chromosome aberration frequency was very significantly increased in the patients exposed to combined INH and PAS therapy as compared with controls. The most frequently observed aberrations were chromatid breaks and gaps. Isoniazid, the major antituberculosis drug, has been reported not to be clastogenic by itself. However, we observed that the INH--PAS combination commonly used in therapy was clastogenic. From this observation it may be concluded that INH and PAS act synergistically in producing chromosomal aberrations.

Aminosalicylic Acid↗
PubMed1987

Improved specificity of the PABA test with p-aminosalicylic acid (PAS).

Until now use of the PABA test together with [14C] PABA to calculate the PABA excretion index has probably been the best adaptation suggested to enhance the specificity of this non-invasive pancreatic function test. Drawbacks of the method are the application of radioactivity, the fact that children, pregnant women, and patients with renal insufficiency have to be excluded from the test, and the possible interference of drugs and isotopes. We propose simultaneous administration of p-aminosalicylic acid (PAS) in the PABA test and quantification of the urinary PABA and PAS excretion with liquid chromatography. Urinary PABA and PAS excretion in six hours are comparable (69.5 +/- 8.4% and 65.6 +/- 18.4% respectively in five healthy volunteers). Application of the PABA/PAS ratio was compared with the urinary PABA excretion in 21 normal controls, 38 patients with pancreatic disease, and 42 patients without pancreatic pathology. The PABA/PAS ratio and the per cent PABA excretion correlated very well in pancreatic patients: (PABA/PAS ratio) = 0.0149 (% PABA) + 0.052 (r = 0.902). Use of the PABA/PAS ratio enhanced the specificity of the test from 76 to 89%.

4-Aminobenzoic Acid↗
PubMed1988

In vitro susceptibility of diarrhoea producing gram negative enteric bacteria to sulfasalazine, 5-aminosalicylic acid, sulfapyridine and four quinolones. Brief report.

The in vitro susceptibility of diarrhoea producing Gram negative enteric bacteria to sulfasalazine, 5-aminosalicylic acid, sulfapyridine and four quinolones was investigated using an agar dilution method. All strains were resistant to 1600 micrograms/ml of sulfasalazine and 5-aminosalicylic acid. MIC range of sulfapyridine for Y. enterocolitica was 3.1-25 micrograms/ml (median:6.2) and for Salmonella 25-100 micrograms/ml (median: 100) Campylobacter jejuni/coli were less susceptible to sulfapyridine with MIC values ranging from 200 to 800 micrograms/ml. Shigella and three of five E. coli strains were resistant to 1600 micrograms/ml of sulfapyridine. Two strains of E. coli were inhibited by 25 micrograms/ml. All strains were fairly susceptible to enoxacin, ciprofloxacin, pefloxacin and ofloxacin. Cirpofloxacin was the most active drug on weight basis.

Aminosalicylic Acids↗
PubMed1973

Poly(N-acryloyl-4- and -5-aminosalicylic acids. II. Antibacterial properties and uses for the preparation of active, insoluble antibiotics.

The antibacterial properties of poly(N-acryloyl-4- and -5-aminosalicylic acids) and their borate complexes were evaluated. Poly(N-acryloyl-4- and 5-aminosalicylic acids) were used to render the antibiotics streptomycin and gentamicin insoluble. The antibacterial properties of the resultant water-insoluble streptomycin and gentamicin derivatives were evaluated, and the results show that the polymers are suited to the preparation of active insoluble antibiotics. Potential antimicrobial applications of the polymers are discussed.

Acrylates↗
PubMed1980

The effect of topical N-acetyl-5-aminosalicylic acid in ulcerative colitis.

In a double-blind controlled therapeutic trial, retention enemas of N-acetyl-5-aminosalicylic acid (Ac-5-ASA) were compared with dummy enemas in the treatment of active ulcerative colitis. Forty patients were studied, each patient taking one test enema twice a day for 2 weeks. Seventeen of the patients had a mild clinical attack of the disease; the 23 others had sigmoidoscopic evidence of active inflammation although they were in clinical remission. Histological and sigmoidoscopic improvement were significantly commoner in the patients receiving the active treatment than in those taking the dummy preparation. Pronounced histological improvement was only seen in patients taking the Ac-5-ASA enemas. In those patients who had clinical attacks of ulcerative colitis at the start of the study, symptomatic improvement was commoner in the group treated with Ac-5-ASA enemas than in those who received placebo therapy. Ac-5-ASA resembles 5-aminosalicylic acid in its effect on the inflamed mucosa in ulcerative colitis. Further studies into other substituted salicylates may lead to the development of an effective oral agent that does not carry the side effects associated with the sulphapyridine moiety of sulphasalazine.

Aminosalicylic Acids↗
PubMed1994

Comparative bioavailability of 5-aminosalicylic acid from a controlled release preparation and an azo-bond preparation.

BACKGROUND: Knowledge of the bioavailability of 5-aminosalicylic acid (5-ASA, mesalazine) from the different 5-ASA-containing drugs is important for rational therapy of inflammatory bowel diseases. METHODS: The local and systemic bioavailability of 5-ASA from a controlled release 5-ASA preparation (Pentasa--2, 4 or 6 g/day) was investigated and compared with the azo-bond 5-ASA preparation olsalazine (Dipentum--2 g/day) in 13 healthy volunteers during steady state conditions. RESULTS: The therapeutically relevant parameter of 5-ASA at the rectal level, expressed as the mean concentration in faecal water, showed a significant trend towards higher concentrations with increasing Pentasa dose: 9.2 mmol/L, 19.0 mmol/L and 24.4 mmol/L, respectively. The concentration of olsalazine 2 g/day was 16.0 mmol/L. The concentration of the metabolite N-acetyl-5-aminosalicylic acid (Ac-5-ASA) did not rise with increasing Pentasa dose, indicating saturable presystemic acetylating capacity of 5-ASA. Total urinary excretion of 5-ASA and Ac-5-ASA, as a percentage of the daily ingested 5-ASA dose, remained constant on the three Pentasa doses, but there was a significant increase in the 5-ASA fraction. Mean steady state plasma concentrations of 5-ASA and Ac-5-ASA were significantly higher on Pentasa 4 g/day and 6 g/day than on 2 g/day. Values on Pentasa 2 g/day were comparable with those on olsalazine 2 g/day. CONCLUSIONS: The study confirmed that 5-ASA is released from Pentasa in a predictable manner, the amount released increasing with dose. Olsalazine is an excellent generator of 5-ASA in the colon.

Administration, Oral↗
PubMed1992

A case of diversion colitis treated with 5-aminosalicylic acid enemas.

An 85-yr-old female presented with diversion colitis after surgery with a resultant colostomy and excluded rectal segment. Treatment with 5-aminosalicylic acid (Rowasa) enemas resulted in both endoscopic and histological resolution. This is the first case of diversion colitis treated with 5-aminosalicylic acid enemas.

Aged↗
PubMed1987

Salazosulfapyridine and metabolites in fetal and maternal body fluids with special reference to 5-aminosalicylic acid.

In 7 pregnant women, treated prophylactically with salazosulfapyridine (SASP) 3 g/day, amniotic fluid (16th week, n = 4, maternal and cord plasma (n = 5) and breast milk (n = 3) were analysed for SASP and the metabolites sulfapyridine (SP), acetyl sulfapyridine (Ac-SP), 5-aminosalicylic acid (5-ASA) and acetyl 5-aminosalicylic acid (Ac-5-ASA). Amniotic fluid contained concentrations of SASP, SP and Ac-SP and partly also Ac-5-ASA comparable to those previously found by others, whereas 5-ASA concentrations were very low. The ratios of maternal to cord plasma for all SASP metabolites were about 1:1-1:2, except for 5-ASA, cord plasma being extremely low. In breast milk, only traces of 5-ASA were detected, while Ac-5-ASA was above the plasma level. Only negligible amounts of 5-ASA are thus transferred to the fetus/newborn, which is of significance for the future use of the new non-sulfa-containing 5-ASA preparations during and after pregnancy.

Adult↗
PubMed2002

Intrarectal administration of 5-aminosalicylic acid to rabbits and dogs.

Intrarectal administration of 5-aminosalicylic acid (5-ASA) to rabbits and dogs was performed to obtain safety data. Groups of rabbits and dogs received twice daily intrarectal doses of 250, 500 or 1000 mg 5-ASA for 14 consecutive days. Treatment had no adverse effect on the behaviour or performance of the animals and microscopic examination revealed no evidence of systemic or local toxicity.

Administration, Rectal↗
PubMed1989

5-Aminosalicylic acid suppositories in the management of ulcerative colitis.

5-aminosalicylic acid (5-ASA) suppositories have been used in the author's out-patient clinic in Bologna for the treatment of distal ulcerative colitis (UC). One hundred fifty-six patients with mild or moderate attacks of UC were treated using different protocols for controlling active disease. Improvement was observed in 88.5 percent of the therapeutic cycles after one month. A small preliminary maintenance study using only 400-mg suppositories of 5-ASA twice a day for 6 or 12 months showed a remission percentage similar to salicylazosulfapyridine (SASP).

Adult↗
PubMed2003

Aminosalicylic acid reduces the antiproliferative effect of hyperglycaemia, advanced glycation endproducts and glycated basic fibroblast growth factor in cultured bovine aortic endothelial cells: comparison with aminoguanidine.

Hyperglycaemia reduces proliferation of bovine aortic endothelial cells in vitro. A similar effect in vivo may contribute to long-term complications of diabetes such as impaired wound-healing and retinopathy. We report the effect of increased glucose concentrations, glycated basic fibroblast growth factor (FGF-2) and bovine serum albumin-derived advanced glycation endproducts (BSA-AGE) on the proliferation of bovine aortic endothelial cells. Glucose (30 and 50 mmol/l) had an antiproliferative effect on endothelial cells. This effect may be mediated through reduced mitogenic activity of FGF-2. The glycation of FGF-2 with 250 mmol/l glucose-6-phosphate led to reduced mitogenic activity compared to native FGF-2. BSA-AGE at concentrations of 10, 50 and 250 microg/ml had an antiproliferative effect on cultured endothelial cells. Aminosalicylic acid at a concentration of 200 micromol/l proved to be more effective than equimolar concentrations of aminoguanidine in protecting endothelial cells against the antiproliferative effects of both high (30 mmol/l) glucose and 50 microg/ml BSA-AGE. FGF-2 glycated in the presence of 4 mmol/l aminosalicylic acid or aminoguanidine retained mitogenic activity compared to that glycated in their absence. Compounds like aminoguanidine and, in particular, aminosalicylic acid protect endothelial cells against glucose-mediated toxicity and may therefore have therapeutic potential.

Aminosalicylic Acids↗
PubMed1993

Successful treatment of pyoderma gangrenosum with topical 5-aminosalicylic acid.

Pyoderma gangrenosum in a twenty-nine-year-old woman with associated long-standing Crohn's disease was treated with topical 5-aminosalicylic acid cream. Significant improvement in the ulceration occurred despite progressive deterioration of the inflammatory bowel disease. The possible mode of action is reviewed. The efficacy, together with the lack of side effects, warrants further study into the therapeutic role of topical 5-aminosalicylic acid.

Administration, Cutaneous↗