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

Abstract

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.

Once daily vs multiple daily mesalamine therapy for mild to moderate ulcerative colitis: a meta‐analysis

“… stated that OD mesalamine can achieve a better efficacy than MD dosing in inducing remission than in maintaining remission (RR 0.80, 95% CI 0.64–0.99). As is well known several factors influence drug efficacy including total doses, formulation of the drug, different routes of administration, disease course and duration of therapy. In the present study subgroup analyses were performed to increase the statistical power of the meta‐analyses and there were in addition two other advantages over previous studies.…”

Does the 5-Aminosalicylate Concentration Correlate with the Efficacy of Oral 5-Aminosalicylate and Predict Response in Patients with Inflammatory Bowel Disease? A Systematic Review

“…Table, see www.karger.com/ doi/10.1159/000499331). Since 5-ASA acts topically, all formulations aim to optimise drug delivery to the colonic mucosa with as little systemic absorption as possible [15]. To this end, prodrugs, pH-dependent release and time-dependent release formulations have been developed.…”

Mesalazine – gold standard in the treatment of ulcerative colitis

“…Szacuje się jednak, że około 20-30% pacjentów wykazuje objawy nietolerancji tego preparatu. Według obecnego stanu wiedzy to właśnie mesalazyna jest uznawana za jedyny aktywny jego metabolit, salazopirydyna natomiast jest odpowiedzialna za większość obserwowanych działań niepożądanych [2][3][4].…”

“…Wydaje się, że decydującą rolę odgrywa miejscowe działanie leku bezpośrednio na komórki błony śluzowej jelita grubego, co prowadzi do zahamowania reakcji indukujących przewlekłe zapalenie. Właściwości przeciwzapalne mesalazyna zawdzięcza prawdopodobnie zdolności hamowania syntezy prostaglandyn i leukotrienów, odpowiednio przez blokowanie szlaków cyklooksygenazy i lipooksygenazy [3,5,6]. Wykazano również, że stanowi ona ligand, a tym samym oddziałuje agonistycznie na typ γ receptora aktywowanego przez proliferatory peroksysomów (ang.…”