Maintaining remission in ulcerative colitis &amp;ndash; role of once daily extended-release mesalamine

Oliveira, Lilliana; Cohen, Russell D.

doi:10.2147/dddt.s5392

Cited by 5 publications

(1 citation statement)

References 32 publications

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“…In addition, it is widely used to maintain remission in UC [ 29 ]. The mechanism of 5-ASA’s anti-inflammatory effect is not fully explained; however, existing data indicate that 5-ASA antagonizes pro-inflammatory mediators such as interferon-γ, IL-8, nuclear factor-κB, and tumor necrosis factor-α [ 29 , 30 , 31 , 32 , 33 ]. Mesalazine also inhibits the cyclooxygenase (COX) and lipoxygenase (LOX) pathways, contributing to the inhibition of prostaglandin E2 and leukotriene release [ 34 ], which are strongly associated with inflammation.…”

Section: Mesalazine—an Old Drug New Possibilitiesmentioning

confidence: 99%

Molecular Mechanisms of the Antitumor Effects of Mesalazine and Its Preventive Potential in Colorectal Cancer

2023

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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.

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Section: Mesalazine—an Old Drug New Possibilitiesmentioning

confidence: 99%

Molecular Mechanisms of the Antitumor Effects of Mesalazine and Its Preventive Potential in Colorectal Cancer

2023

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Tacrolimus Effects and Side Effects After Liver Transplantation: Is There a Difference Between Immediate and Extended Release?

Weiler

Thrun

Eberlin

et al. 2013

Transplantation Proceedings

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Pharmacokinetics in Wistar Rats of 5-[(4-Carboxybutanoyl)Amino]-2-Hydroxybenzoic Acid: A Novel Synthetic Derivative of 5-Aminosalicylic Acid (5-ASA) with Possible Anti-Inflammatory Activity

et al. 2016

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5-[(4-carboxybutanoyl)amino]-2-hydroxybenzoic acid (C2) is a novel synthetic derivative of 5-aminosalicylic acid (5-ASA), which is currently being evaluated ex vivo as an anti-inflammatory agent and has shown satisfactory results. This study aimed to obtain the pharmacokinetic profiles, tissue distribution and plasma protein binding of C2 in Wistar Rats. Additionally, an HPLC method was developed and validated to quantify C2 in rat plasma. The pharmacokinetic profiles of intragastric, intravenous and intraperitoneal administration routes at singles doses of 100, 50, and 100 mg/kg, respectively, were studied in Wistar rats. The elimination half-life of intravenously administered C2 was approximately 33 min. The maximum plasma level of C2 was reached approximately 24 min after intragastric administration, with a Cmax value of 2.5 g/mL and an AUCtot value of 157 μg min-1/mL; the oral bioavailability was approximately 13%. Following a single intragastric or oral dose (100 mg/kg), C2 was distributed and detected in all examined tissues (including the brain and colon). The results showed that C2 accumulates over time. The plasma protein binding results indicated that the unbound fraction of C2 at concentrations of 1 to 20 μg/mL ranged from 89.8% to 92.5%, meaning that this fraction of C2 is available to cross tissues. Finally, the blood-plasma partitioning (BP ratio) of C2 in rat plasma was 0.71 and 0.6 at concentrations of 5 and 10 μg/mL, respectively, which indicates that C2 is free in the plasmatic phase and not inside blood cells. The results of this study suggest that a fraction of the administered C2 dose is absorbed in the stomach, and the fraction that is not absorbed reaches the small intestine and colon. This distribution constitutes the main advantage of C2 compared with 5-ASA for the treatment of ulcerative colitis (UC) and Crohn's disease (CD).

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Maintaining remission in ulcerative colitis – role of once daily extended-release mesalamine

Cited by 5 publications

References 32 publications

Molecular Mechanisms of the Antitumor Effects of Mesalazine and Its Preventive Potential in Colorectal Cancer

Molecular Mechanisms of the Antitumor Effects of Mesalazine and Its Preventive Potential in Colorectal Cancer

Tacrolimus Effects and Side Effects After Liver Transplantation: Is There a Difference Between Immediate and Extended Release?

Pharmacokinetics in Wistar Rats of 5-[(4-Carboxybutanoyl)Amino]-2-Hydroxybenzoic Acid: A Novel Synthetic Derivative of 5-Aminosalicylic Acid (5-ASA) with Possible Anti-Inflammatory Activity

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