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Expert Review of Clinical Pharmacology Mar 2012Ulcerative colitis (UC) is a chronic disease of the GI tract that is characterized by mucosal inflammation in the colon. Mesalamine (mesalazine) is a 5-aminosalicylic... (Review)
Review
Ulcerative colitis (UC) is a chronic disease of the GI tract that is characterized by mucosal inflammation in the colon. Mesalamine (mesalazine) is a 5-aminosalicylic acid compound that is the first-line treatment for patients with mild-to-moderate UC. There are multiple formulations of mesalamine available, primarily differentiated by their means of delivering active mesalamine to the colon. Mesalamine has been demonstrated in randomized controlled trials to induce both clinical response and remission, and maintain clinical remission, in these patients. It has few serious adverse effects and is generally well tolerated by patients. The main areas of uncertainty with use of mesalamine in patients with UC center on the optimal dose for induction of response, how to maintain patient adherence and the role of mesalamine in cancer chemoprophylaxis. Generic forms of mesalamine have yet to be approved by regulatory bodies in the USA.
Topics: Adolescent; Adult; Aged; Aged, 80 and over; Anti-Inflammatory Agents, Non-Steroidal; Child; Child, Preschool; Colitis, Ulcerative; Humans; Infant; Mesalamine; Middle Aged; Patient Compliance; Randomized Controlled Trials as Topic; Remission Induction; Severity of Illness Index; Therapeutic Equivalency; Treatment Outcome; Young Adult
PubMed: 22390554
DOI: 10.1586/ecp.12.2 -
Expert Review of Gastroenterology &... Jun 2008Mesalamine with MMX Multi Matrix System technology (hereafter referred to as MMX mesalamine) is an oral, high-strength (1.2 g/tablet), once-daily formulation of... (Review)
Review
Mesalamine with MMX Multi Matrix System technology (hereafter referred to as MMX mesalamine) is an oral, high-strength (1.2 g/tablet), once-daily formulation of 5-aminosalicylic acid used for the treatment of ulcerative colitis. This new formulation has been designed to provide delayed and prolonged 5-aminosalicylic acid release throughout the colon. In recent clinical studies, MMX mesalamine (taken as a once-daily dose of 2.4 or 4.8 g) effectively induced clinical remission and mucosal healing versus placebo in patients with active, mild-to-moderate ulcerative colitis. Once remission was achieved, MMX mesalamine effectively maintained disease remission in the majority of patients for at least 12 months. In this paper, we comprehensively review the results of studies exploring the clinical pharmacology, efficacy and safety of MMX mesalamine in patients with ulcerative colitis, and examine the implications of these findings on clinical practice.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Colitis, Ulcerative; Humans; Mesalamine; Remission Induction
PubMed: 19072380
DOI: 10.1586/17474124.2.3.299 -
Advanced Drug Delivery Reviews Jan 2005Sulfasalazine's role as the first-line of therapy in patients with inflammatory bowel disease has led to the development of other "designer" aminosalicylates, which... (Comparative Study)
Comparative Study Review
Sulfasalazine's role as the first-line of therapy in patients with inflammatory bowel disease has led to the development of other "designer" aminosalicylates, which eliminate the sulfa-moiety, and attempt to target the topically active mesalamine to the inflamed bowel. Olsalazine sodium and balsalazide disodium utilize the same azo-bond structure as sulfasalazine, requiring release of active mesalamine by colonic bacteria, and thus targeting these agents to the colon. Other mesalamine delivery systems use pH-dependant- or moisture-release to liberate the active mesalamine in both the large and small bowel. Direct application of mesalamine via enema or suppository is also effective in patients with distal colitis. The pharmacology and thus the undesirable drug absorption rates differ between drugs, although the clinical importance of these characteristics is debatable. Differences in release-systems, the impact of the fed and fasting state, and unique patient intolerances to individual agents demand an understanding of each of these products, and their application to patient therapy.
Topics: Animals; Drug Delivery Systems; Gastrointestinal Agents; Humans; Inflammatory Bowel Diseases; Mesalamine
PubMed: 15555743
DOI: 10.1016/j.addr.2004.08.008 -
Expert Opinion on Pharmacotherapy Apr 20085-Aminosalicylate (5-ASA) agents are the first-line therapy for ulcerative colitis (UC). A high-dose, once-daily formulation of 5-ASA known as MMX mesalamine has... (Review)
Review
BACKGROUND
5-Aminosalicylate (5-ASA) agents are the first-line therapy for ulcerative colitis (UC). A high-dose, once-daily formulation of 5-ASA known as MMX mesalamine has recently been approved for the treatment of UC.
OBJECTIVE
To summarize current data on MMX mesalamine and to discuss its impact on management of UC.
METHODS
A systematic review of published literature was performed on PubMed using the search terms 'MMX mesalamine' and 'Lialda'. Abstracts presented at US gastroenterology conferences between 2006 and 2007, were also reviewed.
RESULTS
MMX mesalamine uses a novel multi-matrix delivery system to achieve a sustained release of 5-ASA throughout the colon. Clinical trials have demonstrated MMX mesalamine 2.4 g/day or 4.8 g/day to be superior to placebo in inducing remission in active mild to moderate UC. The drug is well tolerated with a safety profile comparable to other oral 5-ASA agents. With a high-dose formulation of 1.2 g 5-ASA per tablet, MMX mesalamine can be administered conveniently at two to four pills once a day.
CONCLUSION
MMX mesalamine is the first and only approved once-daily 5-ASA treatment option for patients with UC. It is efficacious for the induction of remission in mild to moderate UC and has a favorable safety profile. With the advantage of low pill burden and easy dosing schedule, it may potentially improve patient compliance and treatment success.
Topics: Clinical Trials as Topic; Colitis, Ulcerative; Delayed-Action Preparations; Gastrointestinal Agents; Humans; Mesalamine; Patient Compliance
PubMed: 18377346
DOI: 10.1517/14656566.9.6.1049 -
Expert Opinion on Biological Therapy Apr 2020: For 30 years, 5-aminosalicylic acid (5-ASA) has been the backbone of therapeutic management in patients with ulcerative colitis (UC). In the biologic era, it still... (Review)
Review
: For 30 years, 5-aminosalicylic acid (5-ASA) has been the backbone of therapeutic management in patients with ulcerative colitis (UC). In the biologic era, it still remains the treatment of choice in mild-to-moderate UC. Positioning of this therapeutic class in moderate-to-severe UC is less clear.: Several studies demonstrated the ability of 5-ASA to induce endoscopic remission to a similar extent as anti-TNF therapy on the moderate segment of UC. Histologic remission is achieved after induction in up to 45% of patients treated with topical 5-ASA and 30% with oral formulations. Aminosalicylates offer a favorable safety profile compared to that of immunomodulators and biologics. High-dose 5-ASA therapy may be a valuable option for patients with moderately active disease, and physicians should weigh the pros and cons of this strategy in selected patients. Whether aminosalicylates should be continued in combination with thiopurines or biologic therapy remains under debate.: In the era of biologics, aminosalicylates remain the first-line therapy in patients with mild UC, and have to be considered in case of moderate UC, given their favorable risk-benefit profile. We suggest that 5-ASA should be used in moderate patients without poor prognostic factors, while biologics should be preferred otherwise.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Antibodies, Monoclonal; Colitis, Ulcerative; Gastrointestinal Diseases; Humans; Intestinal Mucosa; Mesalamine; Remission Induction; Severity of Illness Index; Tumor Necrosis Factor-alpha
PubMed: 31498003
DOI: 10.1080/14712598.2019.1666101 -
Drug Design, Development and Therapy Feb 2011The aminosalicylates (5-ASA; also referred to as mesalamine-based agents) are considered as first-line in the maintenance of remission of mild to moderate ulcerative... (Review)
Review
The aminosalicylates (5-ASA; also referred to as mesalamine-based agents) are considered as first-line in the maintenance of remission of mild to moderate ulcerative colitis (UC). Traditionally these agents have required a large pill burden and multiple daily dosing regimens which may account for the low adherence rates, especially in patients in remission. Extended-release mesalamine is the first once daily mesalamine product approved by the Food and Drug Administration for the maintenance of UC remission. This review will examine the pharmacokinetics, dosing, efficacy, and safety data of extended-release mesalamine, and discuss the potential role of improving medication compliance and decreasing costs in UC maintenance.
Topics: Colitis, Ulcerative; Delayed-Action Preparations; Humans; Medication Adherence; Mesalamine; Remission Induction
PubMed: 21448448
DOI: 10.2147/DDDT.S5392 -
Alimentary Pharmacology & Therapeutics Jun 2015Budesonide and mesalazine (mesalamine) are commonly used in the medical management of patients with mild to moderate Crohn's disease. (Comparative Study)
Comparative Study Meta-Analysis Review
BACKGROUND
Budesonide and mesalazine (mesalamine) are commonly used in the medical management of patients with mild to moderate Crohn's disease.
AIM
To assess their comparative efficacy and harm using the methodology of network meta-analysis.
METHODS
A comprehensive search of Medline, Embase, the Cochrane Library and ClinicalTrials.gov, through October 2014, was performed to identify randomised controlled trials (RCTs) that recruited adult patients with active or quiescent Crohn's disease, and compared budesonide or mesalazine with placebo, or against each other, or different dosing strategies of one drug.
RESULTS
Twenty-five RCTs were combined using Bayesian network meta-analysis. Budesonide 9 mg/day, or at higher doses (15 or 18 mg/day), was shown superior to placebo for induction of remission [odds ratio (OR), 2.93; 95% credible interval (CrI), 1.52-5.39, and OR, 3.28; CrI, 1.46-7.55 respectively] and ranks at the top of the hierarchy of the competing treatments. For maintenance of remission, budesonide 6 mg/day demonstrated superiority over placebo (OR, 1.69; CrI, 1.05-2.75), being also at the best ranking position among all compared treatment strategies. No other comparisons (i.e. different doses of mesalazine vs. placebo or budesonide, for induction or maintenance of remission) reached significance. The occurrence of withdrawals due to adverse events was not shown different between budesonide, mesalazine and placebo, in both the induction and maintenance phases.
CONCLUSIONS
Budesonide, at the doses of 9 mg/day, or higher, for induction of remission in active mild or moderate Crohn's disease, and at 6 mg/day for maintenance of remission, appears to be the best treatment choice.
Topics: Adult; Bayes Theorem; Budesonide; Crohn Disease; Humans; Mesalamine; Odds Ratio; Randomized Controlled Trials as Topic
PubMed: 25864873
DOI: 10.1111/apt.13190 -
Journal of Crohn's & Colitis Jul 20215-Aminosalicylates [5-ASAs] are the mainstay of treatment for ulcerative colitis [UC]. The optimum preparation, dose, and route of administration for UC remain unclear.... (Meta-Analysis)
Meta-Analysis
BACKGROUND
5-Aminosalicylates [5-ASAs] are the mainstay of treatment for ulcerative colitis [UC]. The optimum preparation, dose, and route of administration for UC remain unclear. We conducted a network meta-analysis to examine this issue.
METHODS
We searched MEDLINE, EMBASE, EMBASE Classic, and the Cochrane central register of controlled trials from inception to December 2020. We included randomised controlled trials [RCTs] comparing oral, topical, or combined oral and topical 5-ASAs, with each other or placebo for induction of remission or prevention of relapse of UC. Results were reported as pooled relative risks [RRs] with 95% confidence intervals [CIs] to summarise effect of each comparison tested, with treatments ranked according to P-score.
RESULTS
We identified 40 RCTs for induction of remission and 23 for prevention of relapse. Topical mesalazine [P-score 0.99], or oral and topical mesalazine combined [P-score 0.87] ranked first and second for clinical and endoscopic remission combined. Combined therapy ranked first in trials where ≥50% of patients had left-sided/extensive disease, and topical mesalazine first in trials where ≥50% of patients had proctitis/proctosigmoiditis. High-dose [≥3.3 g/day] oral mesalazine ranked third in most analyses, with the most trials and most patients. For relapse of disease activity, combined therapy and high-dose oral mesalazine ranked first and second, with topical mesalazine third. 5-ASAs were safe and well tolerated, regardless of regimen.
CONCLUSIONS
Our results support previous evidence; however, higher doses of oral mesalazine had more evidence for induction of remission than combined therapy and were significantly more efficacious than lower doses. Future RCTs should better establish the role of combined therapy for induction of remission, as well as optimal doses of oral 5-ASAs to prevent relapse.
Topics: Administration, Oral; Administration, Topical; Anti-Inflammatory Agents, Non-Steroidal; Colitis, Ulcerative; Humans; Mesalamine; Network Meta-Analysis
PubMed: 33433562
DOI: 10.1093/ecco-jcc/jjab010 -
Nihon Shokakibyo Gakkai Zasshi = the... 2020A 30-year-old man presented with constipation and abdominal pain. He was suspected of having ulcerative colitis, and administration of 2400mg/day of oral mesalazine was...
A 30-year-old man presented with constipation and abdominal pain. He was suspected of having ulcerative colitis, and administration of 2400mg/day of oral mesalazine was initiated. After 10 days of treatment, he experienced fever and chest pain. Blood examination, electrocardiography, and cardiac ultrasonography revealed elevated cardiac enzymes, ST-segment elevation, and diffuse hypokinesis, respectively. Mesalazine-induced acute myocarditis was diagnosed based on a positive drug-induced lymphocyte stimulation test and the absence of other myocarditis-causing conditions. Prompt cessation of mesalazine quickly improved his heart function and test results. Although rare, clinicians should consider the possibility of cardiac adverse events caused by mesalazine.
Topics: Adult; Anti-Inflammatory Agents, Non-Steroidal; Colitis, Ulcerative; Fever; Humans; Male; Mesalamine; Myocarditis
PubMed: 33298675
DOI: 10.11405/nisshoshi.117.1093 -
Der Chirurg; Zeitschrift Fur Alle... Mar 2022The treatment spectrum for ulcerative colitis has greatly increased in recent years. Mesalazine is still the standard drug treatment for uncomplicated ulcerative colitis... (Review)
Review
The treatment spectrum for ulcerative colitis has greatly increased in recent years. Mesalazine is still the standard drug treatment for uncomplicated ulcerative colitis in various forms of administration. Glucocorticoids are highly effective in the acute treatment of ulcerative colitis but should only be used on a short-term basis due to the pronounced side effects. For forms with a complicated course of ulcerative colitis, immunosuppressive and immunomodulating substances, such as azothioprine as well as various biologicals, Janus kinase inhibitors (JAKi), sphingosine-1-phosphate receptor agonists (S1PR agonists) and calcineurin inhibitors are available after failure of conventional treatment. A proctocolectomy should be considered in cases of a treatment-refractive course or with detection of carcinomas and high-grade epithelial dysplasia.
Topics: Colitis, Ulcerative; Glucocorticoids; Humans; Immunosuppressive Agents; Mesalamine; Proctocolectomy, Restorative
PubMed: 35166864
DOI: 10.1007/s00104-022-01594-y