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BMJ Case Reports Apr 2013The medical management of a patient with Crohn's disease should take into account the activity, site and behaviour of disease, and should be discussed with the patient,...
The medical management of a patient with Crohn's disease should take into account the activity, site and behaviour of disease, and should be discussed with the patient, and 5-aminosalicylates are a group of medications which have been commonly used. Sulfasalazine is a combination of 5-aminosalicylic acid and sulfapyridine which acts only as a carrier to the colonic site of action but can still cause systemic side-effects including lung disease. In mesalazine the specific sulfapyridine-related side-effects, especially pulmonary reactions, are avoided. However, we present a case of lung fibrosis which was associated with mesalazine in a Crohn's patient.
Topics: Aged, 80 and over; Anti-Inflammatory Agents, Non-Steroidal; Crohn Disease; Humans; Male; Mesalamine; Pulmonary Fibrosis; Tomography, X-Ray Computed
PubMed: 23576654
DOI: 10.1136/bcr-2013-008724 -
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 -
Toxins Dec 2021Colibactin is a genotoxin produced primarily by harboring the genomic island ( ). cause host cell DNA damage, leading to chromosomal instability and gene... (Review)
Review
Colibactin is a genotoxin produced primarily by harboring the genomic island ( ). cause host cell DNA damage, leading to chromosomal instability and gene mutations. The signature of colibactin-induced mutations has been described and found in human colorectal cancer (CRC) genomes. An inflamed intestinal environment drives the expansion of and promotes tumorigenesis. Mesalamine (i.e., 5-aminosalycilic acid), an effective anti-inflammatory drug, is an inhibitor of the bacterial polyphosphate kinase (PPK). This drug not only inhibits the production of intestinal inflammatory mediators and the proliferation of CRC cells, but also limits the abundance of in the gut microbiota and diminishes the production of colibactin. Here, we describe the link between intestinal inflammation and colorectal cancer induced by . We discuss the potential mechanisms of the pleiotropic role of mesalamine in treating both inflammatory bowel diseases and reducing the risk of CRC due to .
Topics: Anti-Inflammatory Agents, Non-Steroidal; Escherichia coli; Humans; Mesalamine; Neoplasms; Peptides; Polyketides
PubMed: 34941734
DOI: 10.3390/toxins13120897 -
Molecules (Basel, Switzerland) May 2021Co-crystals are one of the most popular ways to modify the physicochemical properties of active pharmaceutical ingredients (API) without changing pharmacological... (Review)
Review
Co-crystals are one of the most popular ways to modify the physicochemical properties of active pharmaceutical ingredients (API) without changing pharmacological activity through non-covalent interactions with one or more co-formers. A "green method" has recently prompted many researchers to develop solvent-free techniques or minimize solvents for arranging the eco-friendlier process of co-crystallization. Researchers have also been looking for less-risk co-formers that produce the desired API's physicochemical properties. This review purposed to collect the report studies of amino acids as the safe co-former and explored their advantages. Structurally, amino acids are promising co-former candidates as they have functional groups that can form hydrogen bonds and increase stability through zwitterionic moieties, which support strong interactions. The co-crystals and deep eutectic solvent yielded from this natural compound have been proven to improve pharmaceutical performance. For example, l-glutamine could reduce the side effects of mesalamine through an acid-base stabilizing effect in the gastrointestinal fluid. In addition, some amino acids, especially l-proline, enhances API's solubility and absorption in its natural deep eutectic solvent and co-crystals systems. Moreover, some ionic co-crystals of amino acids have also been designed to increase chiral resolution. Therefore, amino acids are safe potential co-formers, which are suitable for improving the physicochemical properties of API and prospective to be developed further in the dosage formula and solid-state syntheses.
Topics: Amino Acids; Animals; Chemistry, Pharmaceutical; Crystallization; Drug Evaluation, Preclinical; Humans; Hydrogen Bonding; Hydrogen-Ion Concentration; Mesalamine; Pharmaceutical Preparations; Proline; Solubility; Solvents; Temperature
PubMed: 34071731
DOI: 10.3390/molecules26113279 -
Alimentary Pharmacology & Therapeutics Oct 2004This review aims to provide an insight into some of the common pathways involved in the development of colorectal cancer--so-called chromosomal instability and... (Review)
Review
This review aims to provide an insight into some of the common pathways involved in the development of colorectal cancer--so-called chromosomal instability and microsatellite instability. There is both clinical and molecular evidence to show that colorectal cancer development occurs over an extended period of time. Together with a knowledge of the molecular pathogenesis of colorectal cancer, this time window allows physicians to counteract cancer development, a strategy known as chemoprevention. In familial and sporadic colorectal cancer, aspirin, other nonsteroidal anti-inflammatory drugs and cyclo-oxygenase-2 inhibitors have been tested for their ability to reduce polyp and cancer development in clinical studies. In inflammatory bowel disease-related colorectal cancer, evidence from retrospective case-control studies shows that mesalazine (mesalamine) can reduce the development of dysplastic lesions or cancer. Although the mechanisms behind this are incompletely understood, general anti-inflammatory, oxygen scavenger and some pro-apoptotic and cyclo-oxygenase inhibitory activities of mesalazine are thought to be involved. New molecular evidence points to a direct DNA stabilizing effect of mesalazine, resulting in a significant reduction of spontaneous microsatellite mutations.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Antineoplastic Agents; Aspirin; Chemoprevention; Chromosomal Instability; Colitis; Colorectal Neoplasms; Humans; Mesalamine; Microsatellite Repeats; Precancerous Conditions
PubMed: 15352891
DOI: 10.1111/j.1365-2036.2004.02045.x -
Gastroenterology Aug 2023
Topics: Humans; Colitis, Ulcerative; Interleukin-2; Mesalamine; Anti-Inflammatory Agents, Non-Steroidal
PubMed: 37030335
DOI: 10.1053/j.gastro.2023.03.230 -
Gut May 2003
Topics: Aminosalicylic Acids; Anti-Inflammatory Agents, Non-Steroidal; Colonic Diseases, Functional; Humans; Mesalamine; Sulfasalazine
PubMed: 12692073
DOI: 10.1136/gut.52.5.771 -
Clinical Pharmacokinetics Jan 2019Ulcerative colitis (UC) is an inflammatory bowel disease (IBD) of unknown etiology, probably caused by a combination of genetic and environmental factors. The treatment... (Review)
Review
Ulcerative colitis (UC) is an inflammatory bowel disease (IBD) of unknown etiology, probably caused by a combination of genetic and environmental factors. The treatment of patients with active UC depends on the severity, localization and history of IBD medication. According to the classic step-up approach, treatment with 5-aminosalicylic acid compounds is the first step in the treatment of mild to moderately active UC. Corticosteroids, such as prednisolone are used in UC patients with moderate to severe disease activity, but only for remission induction therapy because of side effects associated with long-term use. Thiopurines are the next step in the treatment of active UC but monotherapy during induction therapy in UC patients is not preferred because of their slow onset. Therapeutic drug monitoring (TDM) of the pharmacologically active metabolites of thiopurines, 6-thioguanine nucleotide (6-TGN), has proven to be beneficial. Thiopurine S-methyltransferase (TMPT) plays a role in the metabolic conversion pathway of thiopurines and exhibits genetic polymorphism; however, the clinical benefit and relevance of TPMT genotyping is not well established. In patients with severely active UC refractory to corticosteroids, calcineurin inhibitors such as ciclosporin A (CsA) and tacrolimus are potential therapeutic options. These agents usually have a rather rapid onset of action. Monoclonal antibodies (anti-tumor necrosis factor [TNF] agents, vedolizumab) are the last pharmacotherapeutic option for UC patients before surgery becomes inevitable. Body weight, albumin status and antidrug antibodies contribute to the variability in the pharmacokinetics of anti-TNF agents. Additionally, the use of concomitant immunomodulators (thiopurines/methotrexate) lowers the rate of immunogenicity, and therefore the concomitant use of anti-TNF therapy with an immunomodulator may confer some advantage compared with monotherapy in certain patients. TDM of anti-TNF agents could be beneficial in patients with primary nonresponse and secondary loss of response. The potential benefit of applying TDM during vedolizumab treatment has yet to be determined.
Topics: Adrenal Cortex Hormones; Animals; Antibodies, Monoclonal; Biological Factors; Calcineurin Inhibitors; Colitis, Ulcerative; Humans; Mesalamine; Purines
PubMed: 29752633
DOI: 10.1007/s40262-018-0676-z -
Acta Gastro-enterologica Belgica 2015Diverticulosis of the colon is a common disease with an increasing incidence in Western countries. Recent literature has shown some changes in the traditional approach... (Review)
Review
Diverticulosis of the colon is a common disease with an increasing incidence in Western countries. Recent literature has shown some changes in the traditional approach of this disease. The theory that diverticulosis is caused by a reduced intake of dietary fibre, is doubtful. There might be some chemical and histological overlap between diverticulitis, inflammatory bowel disease and irritable bowel disease. High quality clinical study found no effect for antibiotics in acute, uncomplicated diverticulitis. Cyclic administration of mesalazine and rifaximin result in reduced symptoms of diverticular disease. For the treatment of diverticular abscesses, percutaneous drainage shows promising results. Recurrence of acute diverticulitis is rare and most serious complications are linked to the first episode. Recent evidence does not support the traditional recommendation for elective surgery after two episodes of acute diverticulitis any more. This review summarizes the last evidence in diverticular disease and diverticulitis.
Topics: Abscess; Anti-Bacterial Agents; Anti-Inflammatory Agents, Non-Steroidal; Dietary Fiber; Diverticulitis; Drainage; Gastrointestinal Agents; Humans; Inflammatory Bowel Diseases; Irritable Bowel Syndrome; Mesalamine; Rifamycins; Rifaximin
PubMed: 26118576
DOI: No ID Found -
The New England Journal of Medicine Aug 1998Crohn's disease is often treated with glucocorticoids or mesalamine. We compared the efficacy and safety of controlled-ileal-release budesonide capsules and slow-release... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
BACKGROUND
Crohn's disease is often treated with glucocorticoids or mesalamine. We compared the efficacy and safety of controlled-ileal-release budesonide capsules and slow-release mesalamine tablets in patients with active Crohn's disease affecting the ileum, the ascending colon, or both.
METHODS
In a double-blind, multicenter trial, we enrolled 182 patients with scores of 200 to 400 on the Crohn's Disease Activity Index (with higher scores indicating greater disease activity) and randomly assigned 93 to receive 9 mg of budesonide once daily and 89 to receive 2 g of mesalamine twice daily for 16 weeks. The primary efficacy variable was clinical remission, defined as a score of 150 or less on the Crohn's Disease Activity Index.
RESULTS
In the analysis of all patients who received at least one dose of study drug, the rates of remission after 8 weeks of treatment were 69 percent in the budesonide group and 45 percent in the mesalamine group (P=0.001); the respective rates after 16 weeks of treatment were 62 percent and 36 percent (P<0.001). Seventy-seven patients in the budesonide group completed the 16 weeks of treatment, as compared with 50 patients in the mesalamine group (P<0.001). The numbers of patients with adverse events were similar in the two groups, but those assigned to budesonide had fewer severe adverse events. Among patients who completed 16 weeks of treatment, the morning plasma cortisol value was normal in 67 percent of budesonide-treated patients and 83 percent of mesalamine-treated patients (P=0.06); 90 percent and 100 percent, respectively, had normal increases in cortisol in response to cosyntropin (P=0.02).
CONCLUSIONS
In patients with active Crohn's disease affecting the ileum, the ascending colon, or both, a controlled-ileal-release formulation of budesonide was more effective in inducing remission than a slow-release formulation of mesalamine.
Topics: Administration, Topical; Adolescent; Adult; Aged; Anti-Inflammatory Agents; Anti-Inflammatory Agents, Non-Steroidal; Budesonide; Crohn Disease; Delayed-Action Preparations; Double-Blind Method; Female; Humans; Hydrocortisone; Male; Mesalamine; Middle Aged; Remission Induction
PubMed: 9691103
DOI: 10.1056/NEJM199808063390603