Editor-in-Chief Hatice Kübra Elçioğlu Vice Editors Levent Kabasakal Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy 2022 , Vol 26 , Issue 1
Evaluation of anti-inflammatory, immunomodulatory effects and celiac-like side effect of olmesartan medoxomil as a vitamin D receptor agonist and angiotensin II receptor blocker
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Altınbaş University, Bakırköy 34147, İstanbul Turkey
2Department of Pharmaceutical Technology, Faculty of Pharmacy, Ege University, Bornova, 35040, Izmir, Turkey
3Center for Drug R&D and Pharmacokinetic Applications (ARGEFAR), Ege University, 35040, Izmir, Turkey
DOI : 10.29228/jrp.104 Prodrug Olmesartan Medoxomil (OM) is an angiotensin II receptor blocker (ARB) and a vitamin D Receptor (VDR) agonist. Reducing the inflammation and improving the immune system OM prevents organ damage. Angiotensin II receptor blockers (ARBs) can raise serum and tissue levels of the membrane-bound form of monocarboxypeptidase angiotensin converting enzyme 2 (ACE2). Increased ACE2 activity causes the balance in the RAAS to shift towards the positive ACE2-Ang-(1-7). Therefore It can be useful with anti-inflammatory, anti-fibrotic and anti-oxidative stress signals in the treatment of immune system diseases. OM is also known to have adverse effects, such as celiac-like enteropathy which was accepted by the FDA. The mechanism of OM's intestinal injury is thought to be the excessive consumption of the enzymes POX1 and carboxymethylenebutenolidase, which are also responsible for the the digestion of gliadin during the hydrolysis of the drug. Cell-mediated immune response and genetic predisposition are the other factors. Our histopathological findings of olmesartan-induced celiac-like enteropathy in rat intestines were increased mononuclear cell infiltration and villous atrophy. In this study these various action mechanisms of OM and its possible immun system booster effects were discussed. The findings of our rat intestines after exposure to OM-Suspension supported and correlated clinical findings of OM. In conclusion, by making extensive evaluations, OM can be a promising immunomodulator agent in immune system diseases. Keywords : ARB; vitamin-D; VDR-agonist; ACE2; Ang-(1-7); PON1; celiac-like-enteropathy; immunotherapeutic
Marmara University