Clinical and pathogenetic rationale for the use of ursodeoxycholic acid in the treatment of cholelithiasis
Shul'pekova Yu.O.¹, Shul'pekova N.V.¹, Semenistaya M.Ch.¹, Usanova A.A.², Pavlov Ch.S.¹, Kardasheva S.S.<sup>1

1</sup> First Moscow State Medical University named after I.M. Sechenov
² National Research Mordovian State University named after N.P. Ogarev, Saransk

Stones, mainly consisting of cholesterol (CS), are the most common (75-90% of cases of CLS). Almost 50 years ago the gallstones were successfully dissolved with the use of chenodeoxycholic acid (CDCA), but its application was associated with the adverse effects. Hydrophilic UDCA is a spatial stereoisomer (or more accurately an epimer) of CDCA, which does not have cytotoxicity, showed higher efficacy and significantly better tolerability and safety. The biological effect of UDCA is multifaceted: the effect on saturation of bile cholesterol - increases the dispersion of cholesterol with the formation of the liquid crystal phase, reduces the viscosity of bile and improves its outflow; anti-inflammatory effect and the effect on the contractile activity of the gallbladder - suppresses the expression of Class I HLA antigens on hepatocytes and the production of pro-inflammatory cytokines, phagocytosis, peroxidation reactions; effect on liver cells - UDCA activates cellular anti-apoptotic mechanisms; role in the regulation of metabolism - the effects of UDCA are mediated by interaction with nuclear farnesoid receptors of the X cells of the small intestine and liver, and their activity affects lipid and glucose metabolism; influence on the functional state of the intestine - it has a laxative effect, stimulating intestinal secretion and peristalsis. UDCA is used to dissolve small and medium cholesterol stones under the condition of preserved contractile function of the gallbladder and patency of the biliary tract.

Key words: ursodeoxycholic acid, cholelithiasis, biological action, nuclear farnesoid receptor X (farnesoid X receptor, FXR), dissolution of stones, dose, efficacy and safety, Urdoxa®.
For citation: Shul'pekova Yu.O., Shul'pekova N.V., Semenistaya M.Ch. et al. Clinical and pathogenetic rationale for the use of ursodeoxycholic acid in the treatment of cholelithiasis // RMJ. 2017. № 10. P. 745–749.