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Digestive Diseases (Basel, Switzerland) 2012Topical therapy with mesalazine and/or corticosteroids is the standard treatment for patients with distal ulcerative colitis. Rectal mesalazine is more effective than... (Review)
Review
Topical therapy with mesalazine and/or corticosteroids is the standard treatment for patients with distal ulcerative colitis. Rectal mesalazine is more effective than rectal systemically active corticosteroids or topically active corticosteroids like budesonide. In patients with mild to moderately active distal ulcerative colitis, topical mesalazine is therefore the treatment of choice. Doses of 1 g or higher are equally effective. The period of treatment is important (4 weeks are more effective than 2 weeks). In the case of nonresponse or nontolerability of rectal mesalazine, rectal budesonide is indicated. The standard dose of budesonide is 2 mg/day. This does not usually induce any corticosteroid-associated adverse events. Treatment with rectal mesalazine plus rectal topically active corticosteroids is even more effective than treatment with either substance alone. To overcome adherence problems with rectal therapy, rectal foam preparations have been developed which are usually better tolerated than enemas.
Topics: Administration, Topical; Adrenal Cortex Hormones; Budesonide; Colitis, Ulcerative; Humans; Mesalamine; Rectum
PubMed: 23295698
DOI: 10.1159/000342730 -
Gastroenterology Nov 1997The benefit of mesalamine for maintenance of remission in Crohn's disease is controversial. The aim of this study was to assess the effectiveness of mesalamine in... (Meta-Analysis)
Meta-Analysis
BACKGROUND & AIMS
The benefit of mesalamine for maintenance of remission in Crohn's disease is controversial. The aim of this study was to assess the effectiveness of mesalamine in maintaining remission of quiescent Crohn's disease.
METHODS
Pertinent randomized clinical trials were selected using MEDLINE (1986-1997) database, reference lists from published articles or reviews. Fifteen randomized, controlled trials of mesalamine maintenance therapy involving a total of 2097 patients were selected. The crude rates of patients with symptomatic relapse in treated and control groups were extracted according to the intention-to-treat method.
RESULTS
Therapy with mesalamine significantly reduced the risk of symptomatic relapse (pooled risk difference, -6.3%; 95% confidence interval, -10.4% to -2.1%). The pooled risk difference was significant in the postsurgical setting (-13.1%; 95% confidence interval, -21.8% to -4.5%) but not in the medical setting (-4.7%; 95% confidence interval, -9.6% to 2.8%). Multivariate model predicts that the probability of symptomatic relapse significantly decreases with mesalamine treatment, by increasing proportion of patients with ileal disease, with prolonged disease duration, and with surgically induced remission.
CONCLUSIONS
Mesalamine may be recommended for maintaining remission of quiescent Crohn's disease. The benefit is mainly observed in the postsurgical setting, in patients with ileitis and with prolonged disease duration.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Crohn Disease; Double-Blind Method; Humans; Mesalamine; Randomized Controlled Trials as Topic; Retrospective Studies
PubMed: 9352848
DOI: 10.1053/gast.1997.v113.pm9352848 -
Drugs in R&D Jun 2015Mesalamine (5-aminosalicylic acid; 5-ASA) is recommended first-line therapy for mild-to-moderate ulcerative colitis. Many mesalamine formulations employ a pH-dependent...
INTRODUCTION
Mesalamine (5-aminosalicylic acid; 5-ASA) is recommended first-line therapy for mild-to-moderate ulcerative colitis. Many mesalamine formulations employ a pH-dependent release mechanism designed to maximize drug release in the colon. This study compared the in vitro release of 5-ASA from six commercially available mesalamine formulations at pH levels similar to those typically encountered in the human gastrointestinal tract.
METHODS
The release of 5-ASA from six mesalamine formulations [Mesalazin-Kohlpharma (Kohlpharma, Germany), Mesalazin-Eurim (Eurimpharm, Germany), Mesalazina-Faes (Faes Farma, Spain), Mesalazine EC (Actavis B.V., Netherlands), Mesalazine EC 500 PCH (Pharmachemie B.V., Netherlands); multimatrix mesalamine (Shire US Inc., USA)] was monitored separately at three different pH levels [1.0 (2 h), 6.4 (1 h), and 7.2 (8 h)] using United States Pharmacopeia dissolution apparatus II. The dissolution percentage was calculated as a mean of 12 units for each formulation.
RESULTS
At pH 1.0 and 6.4, <1 % of 5-ASA release was observed for each of the mesalamine formulations tested. At pH 7.2, complete release of 5-ASA occurred within 1 h for Mesalazine EC and Mesalazine EC 500 PCH, and within 2 h for Mesalazin-Kohlpharma, Mesalazin-Eurim, and Mesalazina-Faes; complete release of 5-ASA from multimatrix mesalamine occurred within 7 h. Little variability in rate of 5-ASA dissolution was observed between tablets of each formulation.
CONCLUSION
At pH 7.2, 5-ASA release profiles were variable among the commercially available mesalamine formulations that were tested.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Chemistry, Pharmaceutical; Gastrointestinal Tract; Humans; Hydrogen-Ion Concentration; Mesalamine; Solubility; Tablets
PubMed: 26115756
DOI: 10.1007/s40268-015-0097-5 -
Drug Metabolism Reviews Feb 2024Two aminosalicylate isomers have been found to possess useful pharmacological behavior: -aminosalicylate (PAS, 4AS) is an anti-tubercular agent that targets , and... (Review)
Review
Two aminosalicylate isomers have been found to possess useful pharmacological behavior: -aminosalicylate (PAS, 4AS) is an anti-tubercular agent that targets , and 5-aminosalicylate (5AS, mesalamine, mesalazine) is used in the treatment of ulcerative colitis (UC) and other inflammatory bowel diseases (IBD). PAS, a structural analog of pABA, is biosynthetically incorporated by bacterial dihydropteroate synthase (DHPS), ultimately yielding a dihydrofolate (DHF) analog containing an additional hydroxyl group in the pABA ring: 2'-hydroxy-7,8-dihydrofolate. It has been reported to perturb folate metabolism in , and to selectively target dihydrofolate reductase (mtDHFR). Studies of PAS metabolism are reviewed, and possible mechanisms for its mtDHFR inhibition are considered. Although 5AS is a more distant structural relative of pABA, multiple lines of evidence suggest a related role as a pABA antagonist that inhibits bacterial folate biosynthesis. Structural data support the likelihood that 5AS is recognized by the DHPS pABA binding site, and its effects probably range from blocking pABA binding to formation of a dead-end dihydropterin-5AS adduct. These studies suggest that mesalamine acts as a gut bacteria-directed antifolate, that selectively targets faster growing, more folate-dependent species.
Topics: Humans; Mesalamine; 4-Aminobenzoic Acid; Aminosalicylic Acid; Folic Acid; Mycobacterium tuberculosis; Tuberculosis
PubMed: 38230664
DOI: 10.1080/03602532.2024.2303507 -
Carbohydrate Polymers Dec 2020Xylan extracted from corn cobs was used to produce mesalamine-loaded xylan microparticles (XMP5-ASA) by cross-linking polymerization using a non-hazardous cross-linking...
Xylan extracted from corn cobs was used to produce mesalamine-loaded xylan microparticles (XMP5-ASA) by cross-linking polymerization using a non-hazardous cross-linking agent. The microparticles were characterized by thermal analysis (DSC/TG), X-ray diffraction (XRD), Infrared spectroscopy (FTIR-ATR) and scanning electron microscopy (SEM). A comparative study of the in vitro drug release from XMP5-ASA and from gastro-resistant capsules filled with XMP5-ASA (XMPCAP5-ASA) or 5-ASA was also performed. NMR, FTIR-ATR, XRD and DSC/TG studies indicated molecularly dispersed drug in the microparticles with increment on drug stability. The release studies showed that XMPCAP5-ASA allowed more efficient drug retention in the simulated gastric fluid and a prolonged drug release lasting up to 24 h. XMPCAP5-ASA retained approximately 48 % of its drug content after 6 h on the drug release assay. Thus, the encapsulation of 5-ASA into xylan microparticles together with gastro-resistant capsules allowed a better release control of the drug during different simulated gastrointestinal medium.
Topics: Chitosan; Computer Simulation; Delayed-Action Preparations; Drug Delivery Systems; Drug Liberation; Gastrointestinal Tract; Humans; Mesalamine; Models, Biological; Particle Size; Xylans
PubMed: 33049843
DOI: 10.1016/j.carbpol.2020.116929 -
Lancet (London, England) Jan 1998
Topics: Anti-Inflammatory Agents, Non-Steroidal; Humans; Inflammatory Bowel Diseases; Mesalamine
PubMed: 9433450
DOI: 10.1016/s0140-6736(05)78050-8 -
Molecules (Basel, Switzerland) Jun 2023Chemoprevention is one of the ways to fight colorectal cancer, which is a huge challenge in oncology. Numerous pieces of evidence indicate that chronic inflammation in... (Review)
Review
Chemoprevention is one of the ways to fight colorectal cancer, which is a huge challenge in oncology. Numerous pieces of evidence indicate that chronic inflammation in the course of Crohn's disease or ulcerative colitis (UC) is a significant cancer risk factor. Epidemiologic studies suggest that long-term use of non-steroidal anti-inflammatory drugs (NSAIDs), including mesalazine, has beneficial effects on colitis-associated colorectal cancer. Mesalazine is a first-line therapy for UC and is also widely used for maintaining remission in UC. Data showed that mesalazine has antiproliferative properties associated with cyclooxygenase (COX) inhibition but can also act through COX-independent pathways. This review summarizes knowledge about mesalazine's molecular mechanisms of action and chemopreventive effect by which it could interfere with colorectal cancer cell proliferation and survival.
Topics: Humans; Mesalamine; Anti-Inflammatory Agents, Non-Steroidal; Colitis, Ulcerative; Crohn Disease; Colorectal Neoplasms
PubMed: 37446747
DOI: 10.3390/molecules28135081 -
Revue Du Rhumatisme (English Ed.) Oct 1997We report a case of lupus induced by mesalazine therapy taken for over a year for Crohn's disease. The patient had polyarthritis, alopecia, lymphoneutropenia,...
We report a case of lupus induced by mesalazine therapy taken for over a year for Crohn's disease. The patient had polyarthritis, alopecia, lymphoneutropenia, antinuclear factors, anti-histone antibodies, anti-Sm and anti-RNP. Discontinuation of mesalazine was followed by rapid resolution of the joint manifestations, alopecia and lymphoneutropenia; the anti-histone antibodies fell to undetectable levels and the titers of the other auto-antibodies decreased gradually.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Crohn Disease; Diagnosis, Differential; Female; Follow-Up Studies; Glucocorticoids; Humans; Lupus Vulgaris; Mesalamine; Middle Aged
PubMed: 9385697
DOI: No ID Found -
Deutsche Medizinische Wochenschrift... Jan 1996
Topics: Alopecia; Aminosalicylic Acids; Anti-Inflammatory Agents, Non-Steroidal; Crohn Disease; Humans; Mesalamine
PubMed: 8565806
DOI: No ID Found -
Digestive Diseases (Basel, Switzerland) 2016Aminosalicylates (5-ASAs) are foundational therapies for patients with mild-moderate active ulcerative colitis (UC) and to maintain remissions. A variety of oral and... (Review)
Review
Aminosalicylates (5-ASAs) are foundational therapies for patients with mild-moderate active ulcerative colitis (UC) and to maintain remissions. A variety of oral and topical formulations have been evaluated in both active and quiescent disease in both extensive and distal UC. This review summarizes data on pharmacokinetics and applications of oral and topical 5-ASA therapies in active and quiescent, extensive colitis and distal disease, both as monotherapies and in combination and reviews dosing and dosing intervals for oral 5-ASA in both active disease and to maintain remissions.
Topics: Administration, Oral; Administration, Topical; Clinical Trials as Topic; Colitis, Ulcerative; Humans; Mesalamine; Treatment Outcome
PubMed: 26982709
DOI: 10.1159/000443026