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At least 343 records · Page 19Linked to original sources
PubMed1985

Topical administration of 5-aminosalicylic acid enemas in patients with ulcerative colitis. Studies on rectal absorption and excretion.

5-aminosalicylic acid (5-ASA) is a new treatment for patients suffering from ulcerative colitis but only limited information is available about its rectal absorption. We therefore studied seven patients with ulcerative colitis in remission, and five with active disease to determine acetylated and free 5-ASA plasma concentrations and urinary acetyl 5-ASA after the administration of three different types of enemas: (2 g 5-ASA/100 ml, 4 g/100 ml, and 200 ml). In patients in remission urinary acetyl 5-ASA excretion was dose and volume dependent (p less than 0.01; p less than 0.05) but this correlation was absent in active disease. Because aminosalicylates are usually eliminated through the kidney, these low values (10% in active disease and 19% in those in remission) suggest that the beneficial action may be local. Urinary recovery was significantly lower in patients with active disease (p less than 0.01; p less than 0.02). No accumulation of 5-ASA was found in plasma after repeated daily administration.

Administration, Topical↗
PubMedDate not supplied

[Mechanism of specific chromogenic reaction by Klebsiella spp. on nutrient medium with 5-aminosalicylic acid].

The nature of the factor and the mechanism of color reaction with 5-aminosalicylic acid (5-ASA) inherent in bacteria of the genus Klebsiella were investigated. The color reaction was shown to proceed in two stages. During the first stage, occurring in aerobic and anaerobic conditions, the tested strains of Klebsiella decarboxylize 5-ASA yielding CO2 and p-aminophenol, which is a colorless product. During the next strictly aerobic stage which proceeds without participation of bacteria or their exoenzymes, p-aminophenol is oxidized by the air oxygen forming the dark-brown polymers. The color reaction shows high substrate specificity. It is suggested that the color reaction is realized by a previously unknown lyase-type enzyme 5-aminosalicylate decarboxylase (5-aminosalicylate-carboxy-lyase) localized inside the Klebsiella cells.

Aerobiosis↗
PubMed1987

Oral 5-aminosalicylic acid preparations in treatment of inflammatory bowel disease. An update.

Therapeutic efficacy of 5-aminosalicylic acid (5-ASA) preparations is reviewed. In the acute treatment of Crohn's disease, Pentasa and Salofalk seem to be more effective than placebo. When it is given in an equimolar 5-ASA regimen, Salofalk appears to be at least as effective as sulfasalazine (SAS) in the treatment of both Crohn's disease and ulcerative colitis. Asacol and SAS are equally effective in maintenance therapy of ulcerative colitis. Dipentum was more efficient than placebo. There was only a low incidence of side effects from oral 5-ASA preparations, but larger-scale trials may be needed for a more accurate profile of adverse reactions.

Administration, Oral↗
PubMed1999

[Clinical effects of 5-aminosalicylic acid preparations in Crohn disease].

The antiinflammatory drug 5-aminosalicylic acid is available either as mesalamine in various slightly different galenic preparations or as a prodrug with 5-ASA bound to a carrier molecule as inert as possible, which releases 5-ASA via bacterial degradation in the ileocolon. Data from therapeutic trials in patients with Crohn's disease are only available for mesalamine and sulfasalazine. In active Crohn's disease, high-dose (> 3 g per day) mesalamine only is more effective than placebo, but inferior to systemic steroids. They may be used in patients refusing treatment with classical steroids or not tolerating them if this does not make a case for budesonide. The therapeutic gain of mesalamine over placebo for the prevention recurrence in patients who have reached remission by drug treatment is marginal. Thus, its use in this clinical situation is not appealing. Results for the maintenance of a surgically induced remission appear slightly better so that the use of > 3 g of mesalamine per day may be still justified in this scenario. It is an unresolved question whether the clinical efficacy of different galenic mesalamine prepations in maintaining postoperative remission varies with the preoperative disease location. Present data are not sufficient to support differential drug treatment based on this parameter.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed2006

High-performance liquid-chromatographic determination of 5-aminosalicylic acid and its metabolites in blood plasma.

Mesalazine (5-aminosalicylic acid, 5-ASA), an anti-inflammatory agent for the treatment of inflammatory bowel diseases, is metabolized in organism to the principal biotransformation product, N-acetyl-5-ASA. Some other phase II metabolites (N-formyl-5-ASA, N-butyryl-5-ASA, N-beta-d-glucopyranosyl-5-ASA) have also been described. 5-ASA is a polar compound and besides it exhibits amphoteric properties. The extraction of this compound from biomatrices and its chromatographic analysis is complicated. In order to improve the reliability of the determination of parent 5-ASA, a derivatization of 5-ASA together with 4-ASA (added to samples as a precursor of I.S.-2) was involved into the method. More lipophilic N-propionyl-5-ASA and N-propionyl-4-ASA (I.S.-2) were obtained using propionic anhydride. These derivatives were well extractable together with N-acyl-5-ASAs (metabolites) and N-acetyl-4-ASA (I.S.-1). As the first internal standard (I.S.-1) was used for the evaluation of extracted N-acyl-metabolites, the second internal standard (I.S.-2) served for the evaluation of both derivatization and extraction steps of parent drug 5-ASA. Based on these reasonings, new HPLC bioanalytical method for the determination of 5-ASA and its metabolites in blood plasma was developed and validated. The sample preparation step consists of the deproteination of plasma by HClO(4) and the above-mentioned derivatization of ASAs followed by liquid-liquid extraction of all N-acyl-ASA-derivatives. Chromatographic analyses were performed on a 250-4 mm column containing Purospher RP-18 e, 5 microm (Merck, Darmstadt, Germany) with a precolumn (4-4 mm). The column effluent was monitored using both UV photodiode-array (lambda = 313 nm) and fluorescence detectors (lambda(exc.) = 300 nm/lambda(emiss.) = 406 nm) in tandem. The identity of individual N-acyl-ASAs in the extracts from biomatrices was verified by characteristic UV-spectra and by HPLC/MS experiments. The whole analysis lasted 23 min at the flow rate of 1 ml min(-1). LLOQ (LOD) was estimated 126 (20) pmol ml(-1) of plasma for N-acetyl-5-ASA and 318 (50) pmol ml(-1) of plasma for N-propionyl-5-ASA. The validated HPLC method was applied to pharmacokinetic studies of mesalazine in humans and animals.

Chromatography, High Pressure Liquid↗
PubMed2003

Birth outcome in women exposed to 5-aminosalicylic acid during pregnancy: a Danish cohort study.

BACKGROUND: 5-Aminosalicylic acid (5-ASA) preparations are the firstline drugs in the treatment of inflammatory bowel disease. Data on the safety of these drugs in pregnancy are sparse. AIMS: To examine the risk of adverse birth outcome in women who were prescribed 5-ASA drugs during pregnancy. PATIENTS: Women were included in the study if they were prescribed 5-ASA drugs immediately before or during pregnancy. To examine the risk of malformations, we included 60 pregnancies exposed to 5-ASA drugs 30 days before pregnancy or in the first trimester. To examine stillbirths, preterm births, and low birth weight, we included 88 pregnancies exposed during the entire pregnancy. Outcomes were compared with those of 19 418 pregnancies in which no drugs were prescribed for mothers during the study period. METHODS: We conducted a Danish cohort study based on data from a population based prescription registry, the Danish Birth Registry, and the Hospital Discharge Registry in North Jutland County. RESULTS: Odds ratios for malformations, stillbirth, preterm birth, and low birth weight in women who received prescriptions for 5-ASA drugs were 1.9 (95% confidence interval 0.7-5.4), 6.4 (1.7-24.9), 1.9 (0.9-3.9), and 1.2 (0.4-3.3), respectively. The increased risk of stillbirth and preterm birth were found only in patients with ulcerative colitis. CONCLUSIONS: We found an increased risk of stillbirth and preterm birth in women who had been prescribed 5-ASA drugs during pregnancy but no substantial increased risk of malformations. It was difficult to distinguish the specific effects of disease activity and 5-ASA drugs.

Abnormalities, Drug-Induced↗
PubMed1995

[Acute pancreatitis--induced by 5-aminosalicylic acid or an extraintestinal manifestation of ulcerative colitis?].

5-aminosalicylic acid has been reported to cause acute pancreatitis. We report the first Scandinavian case. A 27 year-old woman with a three month history of ulcerative colitis treated with Mesalazine developed acute abdominal pain. Serum and urine amylase were raised, and ultrasonographic and computed tomography scan showed oedema of the pancreas. Immediately following withdrawal of the drug, serum and urine amylase returned to normal. We discuss the possibility of acute pancreatitis as an extraintestinal manifestation of ulcerative colitis.

Acute Disease↗
PubMedDate not supplied

[Acute pancreatitis induced by drugs derived from 5-aminosalicylic acid: case report and review of the literature].

The pancreatic toxicity of oral 5-aminosalicylic acid (5ASA) derivatives used for the treatment of inflammatory bowel diseases remains controversial. A new case of mesalazine-induced acute pancreatitis (AP), with positive rechallenge, and an analysis of the previous published cases are presented. Twenty-nine patients (17 women, 12 men), aged 26.4 +/- 9.9 (12-43) years, were involved, receiving sulfasalazine (n = 11), mesalazine (n = 16), olsalazine (n = 1) or 5ASA without further informations (n = 1), for ulcerative colitis (n = 15), Crohn's disease (n = 13) or another indication (n = 1). The AP occurred in the first month of treatment in 71.4 per cent of the cases (n = 28). The clinical course was essentially benign in most of the cases. Recurrence of AP after rechallenge was observed in 17 of the 19 cases, even if the molecule, the dose or the form were modified. These results show that all 5ASA derivatives are potentially pancreatotoxic. An AP must be considered when an occurrence or increase of abdominal pain occurs during such therapy and warrants serum amylase assay and discontinuation of the drug.

Acute Disease↗
PubMed1993

Oral 5-aminosalicylic acid for inflammatory bowel disease in pregnancy: safety and clinical course.

BACKGROUND: Oral 5-aminosalicylic acid (5-ASA) has proven an effective maintenance therapy of ulcerative colitis and may also be useful in Crohn's disease, but its safety in pregnancy has not been established. The present study therefore examined the course and outcome of pregnancies in patients with inflammatory bowel disease who continued to take oral 5-ASA. METHODS: Ten patients with ulcerative colitis and 7 patients with Crohn's disease with a total of 19 pregnancies were studied while they were receiving 5-ASA. All patients were previously in remission on 5-ASA, at a mean dose of 1.7 g/day (range, 0.8-2.4 g/day). They continued taking the drug without a change in dose and were followed up throughout their pregnancies and postpartum. RESULTS: Eighteen pregnancies resulted in full-term delivery. No fetal abnormalities were found at delivery, and there were no clinical or biochemical abnormalities in the neonatal period. Four patients had a relapse. One patient required a colectomy but carried on to a full-term pregnancy. One patient had a miscarriage, but she had miscarried on four previous occasions before taking 5-ASA. She subsequently had a successful pregnancy on 5-ASA. CONCLUSIONS: Oral 5-ASA appears to be safe for the management of inflammatory bowel disease during pregnancy.

Administration, Oral↗
PubMed2006

Oral 5-aminosalicylic acid for maintenance of remission in ulcerative colitis.

BACKGROUND: The newer 5-ASA preparations were intended to avoid the adverse effects of SASP while maintaining its therapeutic benefits. The efficacy and safety of 5-ASA preparations have been evaluated in numerous clinical trials that have often lacked sufficient statistical power to arrive at definitive conclusions. Previously, it was found that newer 5-ASA drugs were more effective than placebo but no more effective than SASP in inducing remission in ulcerative colitis. This updated review includes more recent studies and evaluates the effectiveness, dose-responsiveness, and safety of 5-ASA preparations in terms of more precise outcome measures. OBJECTIVES: To assess the efficacy, dose-responsiveness and safety of the newer release formulations of 5-aminosalicylic acid (5-ASA) compared to placebo or sulfasalazine (SASP) in the maintenance of remission in ulcerative colitis. SEARCH STRATEGY: A computer-assisted literature search for relevant studies (1981-2005) was performed using MEDLINE, BIOS, the Cochrane Controlled Trials Register, the Cochrane IBD/FBD Group Specialized Trials Register, and the Science Citation Index, followed by a manual search of reference lists from previously retrieved articles, review articles, symposia proceedings, and abstracts from major gastrointestinal conferences. SELECTION CRITERIA: Studies were accepted for analysis if they were prospective, randomized, double-blinded, and placebo- or SASP-controlled clinical trials of parallel design with treatment duration of at least six months. DATA COLLECTION AND ANALYSIS: Based on an intention to treat principle, the primary outcome was the failure to maintain clinical or endoscopic remission. Secondary outcomes were the number of patients experiencing adverse events, the number of patients withdrawn due to adverse events, and exclusions or withdrawals after entry into the study (not due to relapse). All data were analyzed using the Peto odds ratio and corresponding 95% confidence intervals (CI). MAIN RESULTS: The Peto odds ratio for the failure to maintain clinical or endoscopic remission (withdrawals and relapses) for 5-ASA versus placebo was 0.47 (95% CI, 0.36 to 0.62) with an NNT of 6. These values were also calculated for the trials in which SASP and 5-ASA were compared, revealing an odds ratio of 1.29 (95% CI, 1.05 to 1.57), with a negative NNT value (-19), suggesting a higher degree of therapeutic effectiveness for SASP.SASP and 5-ASA had similar adverse event profiles, with odds ratios of 1.16(0.62 to 2.16), and 1.31(0.86 to 1.99), respectively. The NNH values were determined to be 171 and 78 respectively. AUTHORS' CONCLUSIONS: The newer 5-ASA preparations were superior to placebo in maintenance therapy. However, the newer preparations had a statistically significant therapeutic inferiority relative to SASP. This review updates the existing review of oral 5-aminosalicylic acid for maintenance of remission in ulcerative colitis which was published in the Cochrane Library (Issue 1, 2006).

Administration, Oral↗
PubMed1996

Distribution and concentrations of 5-aminosalicylic acid in rectosigmoid biopsy specimens after rectal administration.

PURPOSE: Using the autofluorescent properties of 5-aminosalicylic acid (5-ASA), we studied the penetration and distribution of this molecule in human colonic biopsies at different time intervals after administration of 5-ASA enemas. METHODS: Fluorescence scores of rectosigmoidal biopsy specimens were compared with 5-ASA and acetyl-5-aminosalicylic (Ac-5-ASA) concentrations, determined by high-performance liquid chromatography, in adjacent biopsies and in serum samples. RESULTS: 5-ASA penetrates into the rectal mucosa and into the epithelial cells after local application by means of an enema. We found a characteristic 5-ASA staining of two intramucosal structures that need further identification: intraepithelial triangular configurations and "5-ASA scavengers" in the lamina propria. Fluorescence scores correlate well with 5-ASA concentrations in adjacent biopsies (r = 0.67; P < 0.005) and correlate even better with serum concentrations of 5-ASA (r = 0.84; P < 0.005) and Ac-5-ASA (r = 0.80; P < 0.005), hence reflecting the amount of systemically absorbed and metabolized 5-ASA. CONCLUSION: 5-ASA penetrates into the rectal mucosa after local application. Local availability, assessed by means of fluorescence microscopy, correlates well with serum concentrations.

Administration, Rectal↗