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‣ Treatment of postinfectious irritable bowel syndrome and noninfective irritable bowel syndrome with mesalazine

Bafutto,Mauro; Almeida,José Roberto de; Leite,Nayle Vilela; Oliveira,Enio Chaves; Gabriel-Neto,Salustiano; Rezende-Filho,Joffre
Fonte: Instituto Brasileiro de Estudos e Pesquisas de Gastroenterologia - IBEPEGE ; Colégio Brasileiro de Cirurgia Digestiva - CBCD ; Sociedade Brasileira de Motilidade Digestiva - SBMD ; Federação Brasileira de Gastroenterologia - FBG; Sociedade Brasileira de Hepatologia - SBH; Sociedade Brasileira de Endoscopia Digestiva - SOBED Publicador: Instituto Brasileiro de Estudos e Pesquisas de Gastroenterologia - IBEPEGE ; Colégio Brasileiro de Cirurgia Digestiva - CBCD ; Sociedade Brasileira de Motilidade Digestiva - SBMD ; Federação Brasileira de Gastroenterologia - FBG; Sociedade Brasileira de Hepatologia - SBH; Sociedade Brasileira de Endoscopia Digestiva - SOBED
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/03/2011 Português
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CONTEXT: Recent studies support the hypothesis that postinfectious irritable bowel syndrome and some irritable bowel syndrome patients display persistent signs of minor mucosal inflammation. Mesalazine has intestinal anti-inflammatory properties including cyclooxygenase and prostaglandin inhibition. The effects of mesalazine on postinfectious irritable bowel syndrome and noninfective irritable bowel syndrome patients are still unknown. OBJECTIVE: To observe the effects of mesalazine on postinfectious irritable bowel syndrome and noninfective irritable bowel syndrome with diarrhea patients. METHODS: Based on Rome III criteria, 61 irritable bowel syndrome with diarrhea patients (18 years old or more) were included in the evaluation. Patients were divided into two groups: postinfectious irritable bowel syndrome group, with 18 patients medicated with mesalazine 800 mg 3 times a day for 30 days; noninfective irritable bowel syndrome group, with 43 patients medicated with mesalazine 800 mg 3 times a day for 30 days. Symptom evaluations at baseline and after treatment were performed by means of a four-point Likert scale including stool frequency, stool form and consistency (Bristol Stool Scale), abdominal pain and distension (maximum score: 16; minimum score: 4). RESULTS: Postinfectious irritable bowel syndrome group presented a statistically significant reduction of the total symptom score (P<0.0001). The stool frequency was significantly reduced (P<0.0001)...

‣ TREATMENT OF DIARRHEA-PREDOMINANT IRRITABLE BOWEL SYNDROME WITH MESALAZINE AND/OR SACCHAROMYCES BOULARDII

BAFUTTO,Mauro; ALMEIDA,José Roberto de; LEITE,Nayle Vilela; COSTA,Michelle Bafutto Gomes; OLIVEIRA,Enio Chaves de; RESENDE-FILHO,Joffre
Fonte: Instituto Brasileiro de Estudos e Pesquisas de Gastroenterologia - IBEPEGE ; Colégio Brasileiro de Cirurgia Digestiva - CBCD ; Sociedade Brasileira de Motilidade Digestiva - SBMD ; Federação Brasileira de Gastroenterologia - FBG; Sociedade Brasileira de Hepatologia - SBH; Sociedade Brasileira de Endoscopia Digestiva - SOBED Publicador: Instituto Brasileiro de Estudos e Pesquisas de Gastroenterologia - IBEPEGE ; Colégio Brasileiro de Cirurgia Digestiva - CBCD ; Sociedade Brasileira de Motilidade Digestiva - SBMD ; Federação Brasileira de Gastroenterologia - FBG; Sociedade Brasileira de Hepatologia - SBH; Sociedade Brasileira de Endoscopia Digestiva - SOBED
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/12/2013 Português
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Context Irritable bowel syndrome (IBS) is a functional bowel disease characterized by abdominal pain and altered intestinal habits. The pathophysiology of IBS remains unclear. Recent studies have demonstrated that some IBS patients, especially in diarrhea-predominant IBS (IBS-D), display persistent signs of minor mucosal inflammation and a modified intestinal microflora. The mesalazine has known intestinal anti-inflammatory properties. Saccharomyces boulardii is a probiotic used for a long time in treatment of diarrhea, including infectious diarrhea. Objective Evaluate the effects of mesalazine alone, combined therapy of mesalazine with liophylised Saccharomyces boulardii or alone on symptoms of IBS-D patients. Methods Based on Rome III criteria, 53 IBS-D patients (18 year or more) were included. To exclude organic diseases all patients underwent colonoscopy, stool culture, serum anti-endomisium antibody, lactose tolerance test and ova and parasite exam. Patients were divided in three groups: mesalazine group (MG) - 20 patients received mesalazine 800 mg t.i.d. for 30 days; mesalazine and Saccharomyces boulardii group (MSbG) - 21 patients received mesalazine 800 mg t.i.d. and Saccharomyces boulardii 200 mg t.i.d. for 30 days and; Saccharomyces boulardii group (SbG) – 12 patients received Sb 200 mg t.i.d. for 30 days. Drugs that might have any effect on intestinal motility or secretion were not allowed. Symptom evaluations at baseline and after treatment were performed by means of a 4-point likert scale including: stool frequency...

‣ Development of mesalazine pellets coated with methacrylic-derived polymer

Déo,Simone Cristina; Andreazza,Itamar Francisco; Possamai,João Carlos
Fonte: Universidade de São Paulo, Faculdade de Ciências Farmacêuticas Publicador: Universidade de São Paulo, Faculdade de Ciências Farmacêuticas
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/03/2011 Português
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Mesalazine (5-ASA) is the standard drug for the treatment of inflammatory bowel disease (IBD) due to its local effect on intestinal and colonic mucosa. The effective and safe treatment of this disease requires more efficient delivery of the active substance to its site of action. The focus of this study was the use of multiparticulate systems, a modified release form in which the drug is divided into several functional subunits of release in the form of granules or pellets. When these forms are administered, they are rapidly disintegrated, distributing their content throughout the gastrointestinal tract. The aim of this study was to develop and evaluate a multiparticulate system consisting of pellets coated with polymer for pH-dependent release, derived from methacrylic acid and incorporated into the tablet dosage form of mesalazine as a model drug. The extrusion-spheronisation technique was used, resulting in smooth and spherical pellets with uniform size distribution, which were coated in fluidized bed using Opadry® Enteric 94K28327 containing Eudragit® S100 as the agent regulating drug release. The dissolution profile of coated pellets showed good control of drug release from the polymer at the two levels of coating evaluated (8% and 10%)...

‣ A randomised trial comparing mesalazine and prednisolone foam enemas in patients with acute distal ulcerative colitis.

Lee, F I; Jewell, D P; Mani, V; Keighley, M R; Kingston, R D; Record, C O; Grace, R H; Daniels, S; Patterson, J; Smith, K
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /02/1996 Português
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Distal ulcerative colitis can be treated with oral or rectal mesalazine, or both. A foam enema preparation has been developed and its efficacy investigated. The aim of this study was to evaluate the efficacy and safety of mesalazine foam enemas compared with prednisolone foam enemas in the treatment of patients with acute distal ulcerative colitis. Patients aged over 18 years presenting with a relapse of distal ulcerative colitis were randomly allocated treatment with mesalazine foam enema (n = 149 evaluable patients) and prednisolone foam enema (n = 146 evaluable patients) for four weeks. A randomised multicentre investigator blind parallel group trial was conducted. It was found that after four weeks of treatment, clinical remission was achieved by 52% of mesalazine treated patients and 31% of patients treated with prednisolone (p < 0.001). There was a trend in favour of more patients in the mesalazine group achieving sigmoidoscopic remission (40% v 31%, p = 0.10). Histological remission was achieved by 27% and 21% of patients receiving mesalazine and prednisolone respectively. Symptoms improved in both treatment groups. Significantly more mesalazine patients had no blood in their stools after four weeks of treatment (67% v 40%, p < 0.001). Prednisolone treated patients had significantly fewer days with liquid stools than mesalazine patients...

‣ Comparison of delayed release 5 aminosalicylic acid (mesalazine) and sulphasalazine in the treatment of mild to moderate ulcerative colitis relapse.

Riley, S A; Mani, V; Goodman, M J; Herd, M E; Dutt, S; Turnberg, L A
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /05/1988 Português
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Oral formulations of 5-aminosalicylic acid (mesalazine) appear less toxic than sulphasalazine. We have therefore compared sulphasalazine, low dose mesalazine and high dose mesalazine in the treatment of mild to moderate relapse of ulcerative colitis. Sixty one patients (32 men, aged 20-78 years) were randomly allocated to sulphasalazine 2 g daily, mesalazine 800 mg daily, or mesalazine 2.4 g daily in a double blind, double dummy, four week trial. Groups were comparable for age, sex, extent of disease, and pretrial sulphasalazine intake. Four patients were unable to complete the study because of treatment failure (two taking sulphasalazine and two high dose mesalazine). A further two patients taking sulphasalazine developed side effects necessitating withdrawal. Within treatment comparisons revealed significant improvement of: sigmoidoscopic grade in the sulphasalazine group; rectal bleeding, sigmoidoscopic and histological grade in the low dose mesalazine group; stool frequency, rectal bleeding and sigmoidoscopic grade in the high dose mesalazine group. Greater improvement in rectal bleeding (p less than 0.05) and sigmoidoscopic appearances (p less than 0.05) occurred in patients taking high dose mesalazine than in those taking sulphasalazine. In two patients taking high dose mesalazine minor rises of plasma creatinine concentrations occurred...

‣ Use of mesalazine slow release suppositories 1 g three times per week to maintain remission of ulcerative proctitis: a randomised double blind placebo controlled multicentre study

Marteau, P; Crand, J; Foucault, M; Rambaud, J
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /02/1998 Português
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Background—Daily administration of rectal formulations of mesalazine is effective in preventing relapse of ulcerative proctitis. Maintenance of remission with lower doses would be an advantage. 
Aim—The efficacy of mesalazine suppositories (Pentasa) 1 g three times a week v placebo to maintain remission in patients with cryptogenetic proctitis was studied. 
Methods—Ninety five patients with cryptogenetic proctitis were randomised within two weeks of remission to receive for one year or until relapse three suppositories per week of either Pentasa (n=48) or placebo (n=47). In the case of a relapse, the patients received one suppository/day. 
Results—It was found that 25 of 48 subjects v 18 of 47 remained in remission in the mesalazine and placebo groups respectively. The relapse rate was lower in the mesalazine group for the following time intervals: 0-90 days (19% v 38%, p=0.035), 0-180 days (29% v 54%, p=0.017), 0-270 days (38% v 60%, p=0.031), and 0-365 days (48% v 62%, p=0.18). Treatment of relapse with one suppository/day induced remission in 11 of 18 and 2 of 26 patients in the mesalazine and placebo groups respectively (p=0.001). Overall, 61% v 28% patients remained in the protocol and were in remission at one year (p=0.001). Tolerance was good. 
Conclusion—Mesalazine suppositories 1 g three times a week are effective for preventing relapses of cryptogenetic proctitis. Increasing the dose to 1 g/day is effective in a high proportion of subjects who relapsed. 



‣ Low dose balsalazide (1.5 g twice daily) and mesalazine (0.5 g three times daily) maintained remission of ulcerative colitis but high dose balsalazide (3.0 g twice daily) was superior in preventing relapses

Kruis, W; Schreiber, S; Theuer, D; Brandes, J; Schutz, E; Howaldt, S; Krakamp, B; Hamling, J; Monnikes, H; Koop, I; Stolte, M; Pallant, D; Ewald, U
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /12/2001 Português
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BACKGROUND—Balsalazide is a new 5-aminosalicylic acid (5-ASA) containing prodrug. Its efficacy in comparison with standard mesalazine therapy and the optimum dose for maintaining remission of ulcerative colitis are still unclear.
AIMS—To compare the relapse preventing effect and safety profile of two doses of balsalazide and a standard dose of Eudragit coated mesalazine.
METHODS—A total of 133 patients with ulcerative colitis in remission were recruited to participate in a double blind, multicentre, randomised trial: 49 patients received balsalazide 1.5 g twice daily, 40 received balsalazide 3.0 g twice daily, and 44 received mesalazine 0.5 g three times daily. Efficacy assessments were clinical activity index (CAI) and endoscopic score according to Rachmilewitz, and a histological score. In addition, laboratory tests were performed and urinary excretion of 5-ASA and its metabolite N-Ac-5-ASA was analysed. The study lasted for 26 weeks.
RESULTS—Balsalazide 3.0 g twice daily resulted in a significantly higher clinical remission rate (77.5%) than balsalazide 1.5 g twice daily (43.8%) and mesalazine 0.5 g three times daily (56.8%) (p=0.006). The respective times to relapse were 161 days, 131 days (p=0.003), and 144 days (NS). Accordingly...

‣ Coated mesalazine (5-aminosalicylic acid) versus sulphasalazine in the treatment of active ulcerative colitis: a randomised trial.

Rachmilewitz, D.
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em 14/01/1989 Português
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OBJECTIVE--To assess the safety and efficacy of a preparation of mesalazine (5-aminosalicylic acid) coated with a pH dependent resin (Eudragit L) as compared with sulphasalazine in patients with active mild to moderate ulcerative colitis. DESIGN--Eight week randomised double blind parallel group study. SETTING--Forty six gastroenterology outpatient clinics in seven countries. PATIENTS--Two hundred and twenty patients aged 18-70 who met the following criteria: clinical activity index greater than or equal to 6 and endoscopic index greater than or equal to 4; no concomitant treatment for ulcerative colitis; no hypersensitivity to salicylates or sulphonamides. Of the 164 patients eligible for efficacy analysis, 87 received the coated preparation of mesalazine and 77 sulphasalazine. Most of the remaining patients (28 in each group) were ineligible for the efficacy analysis because of treatment with steroid enemas. All pretrial characteristics were comparable in the two treatment groups. INTERVENTIONS--Coated mesalazine (Mesasal) 1.5 g daily or sulphasalazine 3.0 g daily for eight weeks. Compliance monitored by pill counts. END POINT--Clinical and endoscopic remission. MEASUREMENTS AND MAIN RESULTS--Clinical activity measured by daily diary cards...

‣ Acute Pancreatitis due to pH-Dependent Mesalazine That Occurred in the Course of Ulcerative Colitis

Arai, Yoshinori; Arihiro, Seiji; Ide, Daisuke; Odagi, Isao; Itagaki, Munenori; Komoike, Nobuhiko; Nakao, Yutaka; Takakura, Kazuki; Saruta, Masayuki; Matsuoka, Mika; Kato, Tomohiro; Tajiri, Hisao
Fonte: S. Karger AG Publicador: S. Karger AG
Tipo: Artigo de Revista Científica
Publicado em 07/10/2011 Português
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We report the case of a 26-year-old male who presented with acute pancreatitis during the course of treatment for pancolitic ulcerative colitis (UC) with a time-dependent mesalazine formulation, prednisolone and azathioprine (AZA). Despite a review of his clinical history and various tests, the cause of pancreatitis could not be determined. Since drug-induced pancreatitis was considered possible, administration of the time-dependent mesalazine preparation and AZA was discontinued, and conservative treatment for acute pancreatitis was performed. The pancreatitis promptly improved with these treatments, but drug lymphocyte stimulation test (DLST) for both the time-dependent mesalazine formulation and AZA was negative. A pH-dependent mesalazine formulation was given for maintenance therapy of UC. Subsequently, as the pancreatitis relapsed, drug-induced pancreatitis was strongly suspected. Administration of mesalazine was discontinued, and pancreatitis was smoothly in remission by conservative treatment. According to the positive DLST result for the pH-dependent mesalazine formulation and the clinical course, a diagnosis of pH-dependent mesalazine-induced pancreatitis due to this formulation was made. During the clinical course of UC, occurrence of drug-induced pancreatitis must always be considered.

‣ Recurrent Mesalazine-Induced Myopericarditis in a Patient with Ulcerative Colitis

Park, Eun Hye; Kim, Byung Jin; Huh, Jung Kwon; Jeong, Eun Haeng; Lee, Sang Hyuk; Bang, Ki Bae; Seol, Ji Soo; Sung, Joo Wook; Kim, Bum Soo; Kang, Jin Ho
Fonte: Korean Society of Echocardiography Publicador: Korean Society of Echocardiography
Tipo: Artigo de Revista Científica
Português
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Inflammatory bowel disease (IBD) is considered as a dysregulated immune mediated disease. Pericarditis in IBD is a very rare disease both as an extra-intestinal manifestation of IBD and an adverse reaction of therapeutic drug for IBD such as mesalazine or sulfasalazine. A 26-year-old IBD male patient who had been taking mesalazine regularly for about 1 month was referred to our hospital because of fever, chest discomfort, and abnormal electrocardiographic findings. The patients was diagnosed as acute myopericarditis, and recovered after cessation of mesalazine using steroid and aspirin. When mesalazine was re-medicated some days after discharge, he suffered from myopericarditis again. Subsequently, myopericarditis was resolved just after cessation of mesalazine again. These findings suggest that the development of myopericarditis is caused by mesalazine.

‣ Gastroenterology case report of mesalazine-induced cardiopulmonary hypersensitivity

Ferrusquía, José; Pérez-Martínez, Isabel; Gómez de la Torre, Ricardo; Fernández-Almira, María Luisa; de Francisco, Ruth; Rodrigo, Luis; Riestra, Sabino
Fonte: Baishideng Publishing Group Inc Publicador: Baishideng Publishing Group Inc
Tipo: Artigo de Revista Científica
Português
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Mesalazine is a 5-aminosalicylic acid derivative that has been widely used to treat patients with inflammatory bowel disease. Accumulating evidence indicates that mesalazine has a very low rate of adverse drug reactions and is well tolerated by patients. However, a few cases of pulmonary and cardiac disease related to mesalazine have been reported in the past, though infrequently, preventing clinicians from diagnosing the conditions early. We describe the case of a 32-year-old man with ulcerative colitis who was admitted with a two-month history of persistent fever following mesalazine treatment initiated 14 mo earlier. At the time of admission, mesalazine dose was increased from 1.5 to 3.0 g/d, and antibiotic therapy was started with no improvement. Three weeks after admission, the patient developed dyspnea, non-productive cough, and chest pain. Severe eosinophilia was detected in laboratory tests, and a computed tomography scan revealed interstitial infiltrates in both lungs, as well as a large pericardial effusion. The bronchoalveolar lavage reported a CD4/CD8 ratio of 0.5, and an increased eosinophil count. Transbronchial biopsy examination showed a severe eosinophilic infiltrate of the lung tissue. Mesalazine-induced cardiopulmonary hypersensitivity was suspected after excluding other possible etiologies. Consequently...

‣ Estudo comparativo das expressões de TNF-alfa, IL1-beta e IL-8 na mucosa ileal de portadores da Doença de Crohn em uso de mesalazina ou azatioprina; TNF-alfa, IL1-beta and IL-8 expressions in ileal mucosa of Crohn's disease patients using mesalazine or azathioprine

Ana Paula Paiva Moreira
Fonte: Biblioteca Digital da Unicamp Publicador: Biblioteca Digital da Unicamp
Tipo: Dissertação de Mestrado Formato: application/pdf
Publicado em 29/07/2009 Português
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A doença de Crohn apresenta aspectos controversos e pouco compreendidos em relação a sua etiopatogenia e à sua evolução; o que torna difícil o manejo terapêutico desta doença. Nos últimos anos os avanços da biologia molecular têm possibilitado novas descobertas, no entanto, ainda existem muitas dúvidas em relação à sua etiopatogenia e à ação de diversos mediadores inflamatórios. Objetivo: Avaliar a expressão das citocinas pró-inflamatórias TNF-a, IL-1ß e IL-8 em fragmentos de íleo terminal de pacientes portadores de doença de Crohn em uso de mesalazina e azatioprina e compará-los aos indivíduos normais. Casuística e Métodos: Foram selecionados 25 pacientes acompanhados no Ambulatório de Doença Inflamatória Intestinal do HC-UNICAMP, portadores de doença de Crohn com acometimento de íleo terminal, e que foram, de acordo com protocolos vigentes, submetidos à colonoscopia de controle para avaliação da doença ou procedimento cirúrgico para ressecção ou plastia do segmento doente. Foi obtida amostra de íleo terminal para avaliação dos mediadores inflamatórios acima citados, por meio de técnica de imunoblot. Foram estudados sete pacientes que estavam em uso de mesalazina, nove que estavam em uso de azatioprina...

‣ DECISION TREE CONSTRUCTION AND COST-EFFECTIVENESS ANALYSIS OF TREATMENT OF ULCERATIVE COLITIS WITH PENTASA®MESALAZINE 2 G SACHET

NISHIKAWA,Alvaro Mitsunori; PALADINI,Luciano; DELFINI,Régis; KOTZE,Paulo Gustavo; CLARK,Otavio
Fonte: Instituto Brasileiro de Estudos e Pesquisas de Gastroenterologia - IBEPEGE ; Colégio Brasileiro de Cirurgia Digestiva - CBCD ; Sociedade Brasileira de Motilidade Digestiva - SBMD ; Federação Brasileira de Gastroenterologia - FBG; Sociedade Brasileira de Hepatologia - SBH; Sociedade Brasileira de Endoscopia Digestiva - SOBED Publicador: Instituto Brasileiro de Estudos e Pesquisas de Gastroenterologia - IBEPEGE ; Colégio Brasileiro de Cirurgia Digestiva - CBCD ; Sociedade Brasileira de Motilidade Digestiva - SBMD ; Federação Brasileira de Gastroenterologia - FBG; Sociedade Brasileira de Hepatologia - SBH; Sociedade Brasileira de Endoscopia Digestiva - SOBED
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/12/2013 Português
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ContextUnspecified Ulcerative Rectocolitis is a chronic disease that affects between 0.5 and 24.5/105 inhabitants in the world. National and international clinical guidelines recommend the use of aminosalicylates (including mesalazine) as first-line therapy for induction of remission of unspecified ulcerative rectocolitis, and recommend the maintenance of these agents after remission is achieved. However, multiple daily doses required for the maintenance of disease remission compromise compliance with treatment, which is very low (between 45% and 65%). Use of mesalazina in granules (2 g sachet) once daily - Pentasa® sachets 2 g - can enhance treatment adherence, reflecting in an improvement in patients' outcomes.ObjectiveTo evaluate the evidence on the use of mesalazine for the maintenance of remission in patients with unspecified ulcerative rectocolitis and its effectiveness when taken once versus more than once a day. From an economic standpoint, to analyze the impact of the adoption of this dosage in Brazil's public health system, considering patients' adherence to treatment.MethodsA decision tree was developed based on the Clinical Protocol and Therapeutic Guidelines for Ulcerative Colitis, published by the Ministry of Health in the lobby SAS/MS n° 861 of November 4 th...

‣ Mesalazine preparations for the treatment of ulcerative colitis: Are all created equal?

Ye, Bei; van Langenberg, Daniel R
Fonte: Baishideng Publishing Group Inc Publicador: Baishideng Publishing Group Inc
Tipo: Artigo de Revista Científica
Português
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Oral mesalazine (also known as mesalamine) is a 5-aminosalicylic acid compound used in the treatment of mild to moderate ulcerative colitis, with high rates of efficacy in induction and maintenance of remission. The therapeutic effect of mesalazine occurs topically at the site of diseased colonic mucosa. A myriad of oral mesalazine preparations have been formulated with various drug delivery methods to minimize systemic absorption and maximise drug availability at the inflamed colonic epithelium. It remains unclear whether different oral mesalazine formulations are bioequivalent. This review aims to evaluate the differences between mesalazine formulations based on the currently available literature and explore factors which may influence the selection of one agent above another.

‣ Mesalazine (5-aminosalicylic acid) induced chronic hepatitis

Deltenre, P; Berson, A; Marcellin, P; Degott, C; Biour, M; Pessayre, D
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /06/1999 Português
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BACKGROUND—Treatment of ulcerative colitis or Crohn's disease with sulphasalazine causes several adverse effects, including hepatitis. Sulphasalazine is cleaved by colonic bacteria into 5-aminosalicylic acid and sulphapyridine. Received wisdom was that 5-aminosalicylic acid was topically active, whereas sulphapyridine was absorbed and caused immunoallergic side effects. Mesalazine, a slow release formulation of 5-aminosalicylic acid, was expected to be a safe alternative. However, several cases of acute hepatitis have been reported.
CASE REPORT—A 65 year old man had increased liver enzymes, anti-nuclear and anti-smooth muscle autoantibodies and IgG levels, and lesions of chronic hepatitis after 21 months of mesalazine treatment. Although liver dysfunction had been identified eight months earlier, simvastatin rather than mesalazine had been withdrawn, without any improvement. In contrast, liver enzyme and IgG levels became normal and autoantibodies disappeared after discontinuation of mesalazine administration.
CONCLUSION—Contrary to initial expectations, mesalazine can cause most of the sulphasalazine induced adverse effects, and hepatic side effects may be almost as frequent. When liver dysfunction occurs, mesalazine administration should be discontinued to avoid the development of chronic hepatitis and liver fibrosis.


Keywords: mesalazine; 5-aminosalicylic acid; adverse drug reaction; hepatotoxicity; chronic hepatitis; liver

‣ Drug therapy: dose-response relationship of oral mesalazine in inflammatory bowel disease.

Mulder, C J; van den Hazel, S J
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em //1998 Português
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Mesalazine is widely used in the treatment of inflammatory bowel disease. Little is known about the dose-response relationship and about possible dose related side effects. In ulcerative colitis higher dosages of mesalazine (3 g) are more effective in maintaining a remission than lower dosages (1.5 g). In mild to moderately active ulcerative colitis, studies also indicate that higher dosages might be more effective in inducing remission. Dose-comparing studies in Crohn's disease are even more sparse, but the available results indicate higher efficacy at higher dose levels. None of the known side effects of mesalazine are clearly dose-related. A pH-dependent release system, however, can cause a sudden release of high doses of mesalazine. Consequent peak levels in serum have been implicated in mesalazine induced nephrotoxicity. In conclusion, despite the current practice of using increasing dosages of mesalazine in inflammatory bowel disease, both efficacy and safety have been established tentatively.

‣ Aligning oral mesalazine treatment to health service priorities: guidance for nurses

Kemp, Karen; Sephton, Mark
Fonte: BMJ Publishing Group Publicador: BMJ Publishing Group
Tipo: Artigo de Revista Científica
Português
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Oral mesalazine represents a crucial front-line agent for the treatment of active ulcerative colitis (UC) and the maintenance of remission. Clinical aspects of mesalazine therapy are guided by robust evidence-based guidelines, although there is a relative paucity of guidance examining the specific administrative and professional issues faced by inflammatory bowel disease (IBD) nurses. As IBD nurses frequently influence treatment decisions in UC, this article was written to provide a practical review of the key evidence and issues affecting mesalazine treatment. Therefore, it may act as an additional resource for IBD nurses, to enhance prescribing decisions. Using the UK's Quality, Innovation, Productivity and Prevention (QIPP) agenda as a framework, it considers clinical and health service priorities affecting treatment decisions. The quality of care perspective naturally focuses on efficacy; recent interest in specific aspects of efficacy, such as the speed of symptom resolution allows targeting of mesalazine treatment to individual needs. Furthermore, innovative adherence programmes build on the latest evidence to develop robust, integrated patient support approaches. In terms of productivity, nurse-led activities and more sophisticated management strategies may offer the best routes towards reducing the costs of care. Key opportunities for preventing ill health include improving adherence to maintenance therapy and achieving mucosal healing. The principles and approaches highlighted by the QIPP agenda emphasise that prescribing decisions for mesalazine in UC must take account of the full spectrum of clinical and health service needs...

‣ Bezoar by mesalazine tablets: cause of intestinal obstruction in Crohn's disease

Albuquerque,Idblan Carvalho de; Carvalho,Mariana Andrade; Batista,Rodrigo Rocha; Formiga,Galdino José Sitonio
Fonte: Sociedade Brasileira de Coloproctologia Publicador: Sociedade Brasileira de Coloproctologia
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/12/2012 Português
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The stricturing and fistulizing forms of Crohn's disease (CD) exhibit many different results to clinical treatment and good response to surgical therapy. The prevalence of strictures in CD ranges from 12 to 54% and they are more frequently in patients with longer disease duration, and the terminal ileum is the most commonly affected location. The pharmacobezoars can be formed in any part of the gastrointestinal tract and are often associated with factors predisposing anatomic, functional or other concomitant conditions. The pharmacological properties of drugs may contribute to the pathophysiology of bezoars. The objective of this case report is to alert for the importance of the quality of prescribed medications that are used by patients with CD, through the finding of more than 350 tablets of mesalazine during the surgical treatment of a patient with the fibrostenotic pattern.

‣ Development of mesalazine pellets coated with methacrylic-derived polymer

Déo, Simone Cristina; Andreazza, Itamar Francisco; Possamai, João Carlos
Fonte: Universidade de São Paulo. Faculdade de Ciências Farmacêuticas Publicador: Universidade de São Paulo. Faculdade de Ciências Farmacêuticas
Tipo: info:eu-repo/semantics/article; info:eu-repo/semantics/publishedVersion; ; ; ; ; ; Formato: application/pdf
Publicado em 01/03/2011 Português
Relevância na Pesquisa
37.60929%
A mesalazina (5-ASA) tem se apresentado como fármaco padrão para o tratamento da doença inflamatória intestinal (DII) devido ao seu efeito local na mucosa intestinal e colônica. A terapia efetiva e segura desta doença requer a chegada da substância ativa ao seu local de ação com maior eficiência. Nessa busca, tem se destacado o uso de Sistemas Multiparticulados, forma farmacêutica de liberação modificada, em que o fármaco está dividido em várias subunidades funcionais de liberação, sob a forma de grânulos ou péletes, que quando administrados, são rapidamente desintegrados distribuindo seu conteúdo por todo trato gastrintestinal. Este trabalho teve como objetivo desenvolver e avaliar péletes revestidos com polímero de liberação pH-dependente, derivado do ácido metacrílico, tendo como fármaco modelo a mesalazina. A técnica de extrusão-esferonização foi utilizada obtendo-se péletes lisos e esféricos com distribuição granulométrica uniforme, que foram revestidos em leito fluidizado utilizando Opadry® Enteric 94K28327 contendo Eudragit® S100 como agente regulador da liberação do fármaco. O perfil de dissolução dos péletes revestidos demonstrou bom controle na liberação do fármaco por parte do polímero nos dois níveis de revestimento avaliados (8 e 10%)...

‣ Mesalazine induced tubulointersticial nephritis

Campos,Andreia; Santos,Sofia; Santos,Josefina; Malheiro,Jorge; Rodrigues,Anabela; Lobato,Luísa; Viscaíno,J. Ramón; Cabrita,António
Fonte: Sociedade Portuguesa de Nefrologia Publicador: Sociedade Portuguesa de Nefrologia
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/06/2015 Português
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37.735544%
Inflammatory bowel disease and its various treatments may affect the kidney in several ways. Tubulointersticial nephritis is a rare but serious complication of longer-term mesalazine use. There are few cases reported in the literature. We report the first two cases of mesalazine-induced tubulointersticial nephritis, recently diagnosed in our department. The first one refers to a patient with ulcerous colitis and the second one to a patient with Crohn’s disease. Then the authors present a review of literature about the renal involvement in the inflammatory bowel disease. New cases of mesalazine nephrotoxicity should be reported to allow more accurate incidence estimation of this serious adverse effect. Routine monitoring of renal function is simple, inexpensive and allows an early diagnosis of this complication