Background:

Olmesartan medoxomil, the medoxomil ester of olmesartan, is novel and oral antagonist of angiotensin II TYPE-1 receptor (AT₁receptor) with an inhibition constant IC₅₀of 33 nmol/L. Through oral administration, olmesartan medoxomil is rapidly absorbed by the gastrointestinal tract converting to its active metabolite olmesartan, whose inhibition constant IC₅₀towards AT₁receptor is 8 nmol/L. The esterification of olmesartan with medoxomil moiety is just to improve its water solubility (from 4.5% to 28.6%). Olmesartan medoxomil is used for the treatment of hypertension, in which olmesartan dose-dependently reduces the blood pressure through arterial vasodilation and reducing sodium retention.

Reference

[1].HR Brunner. The new oral angiotensin II antagonist olmesartan medoxomil: a concise overview. Journal of Human Hypertension (2002) 16 (Suppl 2), S13-S16
[2].Shailesh T. Prajapati, Hitesh H. Bulchandani, Dashrath M. Patel, Suresh K. Dumaniya and Chhaganbhai N. Patel. Formulation and evaluation of liquisolid compacts for olmesartan medoxomil. Journal of Drug Delivery 2013.