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The first proof of concept in vivo for a new type of microbiota-sensitive film coatings allowing for colon targeting is presented. The efficacy of these polysaccharide barriers to optimize drug release for the treatment of inflammation is demonstrated in an experimental colitis model with Wister rats. 5-Aminosalicylic acid (5-ASA) pellets were prepared by extrusion-spheronization and coated with Nutriose:ethylcellulose (EC) 1:4 or peas starch:ethylcellulose 1:2 blends. The pellets were mixed with standard chow, and the daily drug dose was 150mg/kg. For reasons of comparison, also commercially available Pentasa pellets and placebo pellets were studied. At day 3 after the beginning of the treatment, colitis was induced by intrarectal administration of trinitrobenzene sulfonic acid (TNBS). Animals were sacrificed on day 6. Macroscopic and histological evaluations of colitis were performed blindly. In addition, inflammatory markers were evaluated using ELISA and real-time PCR. Rats receiving TNBS and placebo pellets developed a severe colitis in the distal half of the colon. 5-ASA administered in the form of Pentasa pellets reduced macroscopic inflammation by only 5%. In contrast, the colon lesions were much less severe upon treatment with Nutriose:EC- and peas starch:EC-coated pellets: The macroscopic score was reduced by 25 and 24%, respectively. Decreases of 37 and 38% of the histological lesions confirmed the efficacy of these new colon targeting systems. Also, inflammatory markers (MPO, IL-1β mRNA, TNF mRNA) were significantly decreased in rats receiving Nutriose:EC- and peas starch:EC-coated pellets compared to Pentasa pellets. Furthermore, real-time PCR analysis indicated increased activation of the target receptor PPAR-γ and the HMGCS2 gene in rats upon administration of 5-ASA loaded Nutriose:EC- and peas starch:EC pellets compared to the commercial product. Also, HPLC-MS/MS analysis of plasma samples demonstrated that the level of the main metabolite of the drug (N-acetyl-5-ASA) was much lower upon administration of Nutriose:EC or peas starch:EC coated pellets compared to Pentasa pellets, indicating that undesired premature drug release in the upper gastrointestinal tract was more effectively hindered. In addition to the rat study, in vivo imaging of transgenic mice expressing the luciferase gene evidenced much more pronounced PPAR-γ activation upon 5-ASA administration in the form of Nutriose:EC-coated pellets versus Pentasa pellets. All these results clearly demonstrate the superiority of these microbiota-sensitive polysaccharide-based film coatings for colon targeting in vivo.
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Users of 5-ASA have an increased risk of renal disease that may be partly attributable to the underlying disease. Although renal disease is a recognized adverse effect of 5-ASA, the incidence appears to be low and does not appear to be related to either the dose or type of 5-ASA used.
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Both 5-aminosalicylic acid hypersensitive subjects were successfully desensitized without complications and were able to tolerate therapeutic doses.
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1 Keratoconjunctivitis sicca (KCS) is an inflammatory eye condition, affecting the cornea and conjunctiva, caused by a deficiency in the aqueous fraction of tears. The condition is relatively common in the dog with a varied aetiology. A number of drugs have been implicated in the production of KCS in the dog including salicylazosulphapyridine (sulphasalazine). 2 This paper details clinically evident KCS in a 12-month oral toxicity study with 5-aminosalicylic acid (5-ASA), the therapeutically active metabolite of sulphasalazine. 3 The condition was first diagnosed at study week 22 and subsequently progressed both in incidence and severity. There was a distinct sex-difference in the response, with treated females being more affected than males. 4 There was a close correlation between the production of KCS and reduced lacrimation as assessed by the Schirmer tear test. 5 Although sulphasalazine causes KCS in dogs there have been no reports of ocular lesions of this type in man with this drug. It is highly probable that the dog is not a predictive model for man with regard to KCS induction by sulphasalazine or its metabolite 5-ASA.
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Many oral 5-aminosalicylic acid (5-ASA) formulations are designed to maximize 5-ASA release in the colon where it acts topically on the colonic mucosa. Delayed-release formulations and azo-prodrugs minimize 5-ASA absorption in the upper gastrointestinal (GI) tract.
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Therapy with oral 5-aminosalicylic acid for inflammatory bowel disease has been reported as effective and safe. We report two cases of biochemically proven mild acute pancreatitis occurring 2 and 14 days, respectively, after oral 5-aminosalicylic acid therapy was instituted for inflammatory bowel disease. A hypersensitivity mechanism might be involved, owing to possible erratic systemic absorption of the drug. We suggest clinical and biochemical monitoring for patients undergoing oral 5-aminosalicylic acid therapy in order to confirm its possible association with acute pancreatitis and to assess the actual incidence of such an adverse reaction.
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Budesonide is more effective than placebo or mesalamine for induction of remission in Crohn's disease. Although short-term efficacy with budesonide is less than with conventional steroids, particularly in those with severe disease or more extensive colonic involvement, the likelihood of adverse events and adrenal suppression is lower.
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To compare the effects of alicaforsen enema to standard of care mesalazine (mesalamine) enema in subjects with mild to moderate active left-sided ulcerative colitis.
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We introduce an approach for detection of drug-protein interactions that combines a new yeast three-hybrid screening for identification of interactions with affinity chromatography for their unambiguous validation. We applied the methodology to the profiling of clinically approved drugs, resulting in the identification of previously known and unknown drug-protein interactions. In particular, we were able to identify off-targets for erlotinib and atorvastatin, as well as an enzyme target for the anti-inflammatory drug sulfasalazine. We demonstrate that sulfasalazine and its metabolites, sulfapyridine and mesalamine, are inhibitors of the enzyme catalyzing the final step in the biosynthesis of the cofactor tetrahydrobiopterin. The interference with tetrahydrobiopterin metabolism provides an explanation for some of the beneficial and deleterious properties of sulfasalazine and furthermore suggests new and improved therapies for the drug. This work thus establishes a powerful approach for drug profiling and provides new insights in the mechanism of action of clinically approved drugs.
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Patients with mildly to moderately active ulcerative colitis treated with A. paniculata extract (HMPL-004) at a dose of 1,800 mg daily were more likely to achieve clinical response than those receiving placebo.
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Ulcerative colitis is a lifelong disease causing inflammation and ulceration of the colon. Symptoms of ulcerative colitis include abdominal pain, bloody diarrhea, bloating, and fecal urgency. The current standard therapy for mild to moderate ulcerative colitis is the use of 5-aminosalicylates, with patients requiring continuous treatment to maintain remission. A substantial proportion of patients, however, are nonadherent to prescribed 5-aminosalicylate treatment regimens, resulting in a greater chance of disease relapse with severe associated symptoms. There are many reasons why a patient with ulcerative colitis may be nonadherent including the patient's perception of the condition or a lack of understanding about the disease or treatment. Multiple daily dosing or rectal administration of 5-aminosalicylate medications also can adversely affect adherence rates. Because gastrointestinal nurses often are the primary points of contact for patients with ulcerative colitis, they are in a unique position to take simple steps that will improve adherence rates and thus increase the efficacy of prescribed therapy. This article highlights important aspects of education and patient care for patients with ulcerative colitis.
In a randomized multicentre investigator-blind parallel group trial, 103 patients with mild to moderate left-sided colitis or proctosigmoiditis were randomly allocated to mesalazine 2 g gel enema (n = 50 evaluable patients) and mesalazine 2 g foam enema (n = 53 evaluable patients) for 4 weeks. Clinical symptoms, endoscopic and histological findings were assessed at entry, 2 and 4 weeks. Patients' evaluation of treatment tolerability and acceptability was assessed at 2 and 4 weeks.
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Mesalazine or Beclomethasone dipropionate (BDP) enema have been shown effective in treatment of distal active ulcerative colitis (UC). This study was aimed to determine whether the combination of topical mesalazine and BDP is superior to topical mesalazine or BDP used alone in patients with distal active UC. PATIENTS AND METHODS: One-hundred and twenty patients with clinical, endoscopic and histological diagnosis of distal active UC were randomly assigned to a regimen with mesalazine tablets 2.4 g/day associated to either mesalazine enema 4 g/day (group A, n=40), BDP 3 mg/60 ml every day (group B, n=40) or the combination treatment with the two compounds in a single administration (group C, n=40) for eight weeks. After four weeks of treatment all patients underwent clinical controls but only 109 patients returned back for clinical, endoscopic and histological controls at the end of the treatment period.
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As a new colon-specific prodrug of 5-aminosalicylic acid (5-ASA), 5-aminosalicyl-glycine (5-ASA-Gly) was prepared by a simple synthetic route in good yield. Apparent partition coefficients of 5-ASA-Gly were lower than those of 5-ASA, which determined in CHCl3/pH 6.8 buffer or n-octanol/pH 6.8 buffer system. Stability of 5-ASA-Gly by peptidases was investigated by incubation of 5-ASA-Gly with the homogenates of tissue and contents of stomach, proximal small intestine or distal small intestine of rats at 37 degrees C. 5-ASA was not detected, indicating that the prodrug was stable in the upper intestine. The amount of 5-ASA liberated from incubation of the prodrug in cecal or colonic contents of rats was about 65% or 27% in 8 hrs, respectively, which indicated that the prodrug activation took place more readily in the rat cecum whose bacterial counts are high like human colon. Results from in vitro experiments suggested 5-ASA-Gly as a promising candidate of a colon-specific prodrug of 5-ASA.
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Butyrate is effective in experimental colitis by increasing transglutaminase activity. Because ulcerative colitis increases the risk of colonic neoplasia, the aim of this study was to investigate whether butyrate treatment reduces mucosal sensitivity to colon cancer development in rats with experimental colitis.
Patients with inflammatory bowel disease (IBD) are at risk for hepatobiliary disease and toxicity, and the diagnosis of drug-induced liver disease in patients being treated for IBD can represent a clinical challenge. There are a number of disease states associated with IBD, which are primary sclerosing cholangitis, cholangiocarcinoma and autoimmune hepatitis. There is a wide spectrum of hepatic injury that can occur from the agents used to treat IBD, such as acute or chronic hepatic injury directly attributable to the drugs used to treat IBD (e.g. sulfasalazine, mesalamine, thiopurines, methotrexate, TNF antagonists, quinolone antibiotics); liver toxicity from drugs used to treat complications of immunomodulators and TNF antagonists (e.g. isoniazid for treatment of reactivation tuberculosis), and exacerbation of underlying chronic viral hepatitis with infliximab and other TNF antagonists. Thiopurines are also associated with the development of hepatic vascular lesions, such as nodular regenerative hyperplasia and peliosis hepatic. In addition, biologics can be associated with the reactivation of underlying chronic viral hepatitis, mandating universal screening prior to initiation of TNF-alpha antagonist therapy.
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To summarize current data on MMX mesalamine and to discuss its impact on management of UC.
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We report a patient with uncontrolled Crohn's disease who presented with progressive weakness of proximal muscles and a marked elevation of serum creatine kinase. Muscle biopsy from the left deltoid exhibited myositic changes with inflammatory infiltrates in the perimysium, endomysium, and perivascular locations. Most were stained as CD68-positive macrophages, whereas some were CD4- and CD8-positive T lymphocytes. Due to uncontrolled bowel inflammation, several fistulae were found in the descending colon, and partial colectomy was performed. An examination of the resected colon exhibited inflammation of the bowel structure surrounded mainly by CD68-positive macrophages. The histopathological findings of the descending colon were analogous to those of the muscle. After an increased dose of mesalazine and partial colectomy, her muscle symptoms improved. These findings suggest that the myositis in Crohn's disease is immune-mediated and that treatment of bowel inflammation should be emphasized as opposed to steroid or other immunosuppressive therapy.
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In the clinical setting, adherence to aminosalicylate therapy has been less than optimal. Topical formulations are associated with poor retention, abdominal bloating, and discomfort during administration. Although oral formulations are more convenient than topical formulations, many require multiple-daily-dosing regimens and have a high pill burden, which make patient adherence poor. A number of oral aminosalicylate formulations use colonic bacteria to release the active drug. Although these oral formulations are effective for the treatment of active UC, therapy is not optimal with regard to clinical outcome. Because of the short half-life, the vast majority of current therapies require multiple daily dosing. In addition, the dose strength of these formulations ranges from 250 to 500 mg, which requires patients to take several tablets at a time. Some patients may also require additional topical aminosalicylate to maintain treatment efficacy. However, many patients dislike topical formulations, and refill rates have been shown to be much lower than with oral formulations. New aminosalicylate formulations are now being designed to improve dosing schedules and increase patient adherence, potentially improving clinical and economic outcomes. High-dose, oral mesalamine formulations have been designed to reduce pill burden.
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Combined mesalazine oral/enema treatment achieved a significantly higher rate of improvement in abbreviated ulcerative colitis disease activity index (score decrease ≥ 2) within 2 weeks, compared with oral-only treatment (p = 0.032). Bleeding ceased significantly more quickly with combination vs. oral therapy (p = 0.003). More patients showed mucosal healing (disease activity index endoscopic mucosal appearance score 0/1) with combination vs. oral therapy, which was significantly different between groups at week 4 (p = 0.052). Both groups showed quality of life improvements, with a significant benefit for combination vs. oral therapy at week 4 in multiple domains. Most patients reported finding the treatment acceptable.
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A case of mesalazine-induced acute interstitial nephritis (AIN) in a 41-year-old patient with ulcerative colitis (UC) is reported here. Clinical symptoms such as fever and arthralgia, and laboratory findings such as eosinophilia and renal failure suggested AIN, which was confirmed by biopsy. With withdrawal of mesalazine and intravenous methylprednisolone the patient's renal function was recovered. It is observed that early discontinuation of mesalazine is associated with amelioration of interstitial nephritis in most patients, so the recommendation is that patients receiving mesalazine should undergo routine monitoring of renal function. Delayed diagnosis may lead to permanent renal function impairment.
In electrophysiological experiments, we identified the natural phenols, caffeic acid (EC50 1.3 µM) and resveratrol (EC50 10 µM) as KCa3.1 inhibitors with moderate potency. The phenols, vanillic acid, gallic acid, and hydroxytyrosol had weak or no blocking effects. Out of the NSAIDs, flufenamic acid was moderately potent (EC50 1.6 µM), followed by mesalamine (EC50≥10 µM). The synthetic fluoro-trivanillic ester, 13b ([3,5-bis[(3-fluoro-4-hydroxy-benzoyl)oxymethyl]phenyl]methyl 3-fluoro-4-hydroxy-benzoate), was identified as a potent mixed KCa2/3 channel inhibitor with an EC50 of 19 nM for KCa3.1 and 360 pM for KCa2.3, which affected KCa1.1 and Kv channels only at micromolar concentrations. The KCa3.1/KCa2-activator SKA-31 antagonized the 13b-blockade. In proliferation assays, 13b was not cytotoxic and reduced proliferation of 3T3 fibroblasts as well as caffeic acid. In isometric vessel myography, 13b increased contractions of porcine coronary arteries to serotonin and antagonized endothelium-derived hyperpolarization-mediated vasorelaxation to pharmacological KCa3.1/KCa2.3 activation.