Urapidil – an antihypertensive drug with a dual action mechanism

Czech version

Authors: Souček M.; Novák J.
Authors‘ workplace: II. interní klinika LF MU a FN U sv. Anny v Brně
Published in: Kardiol Rev Int Med 2020, 22(2): 69-71

Overview

We provide a comprehensive overview of the mechanisms of actions and indications of urapidil in the treatment of hypertension. The antihypertensive effect of most centrally-acting antihypertensive drugs is mediated by the activation of the central alpha-2 adrenergic receptors and/or imidazol receptors located in the cardiovascular regulatory centres in the medulla oblongata. Urapidil is unique in having both a central agonistic effect on the 5-HT1A receptors (and according to primary studies, also a mild agonistic effect on the central alpha-2 receptors) and a peripheral antagonistic effect on postsynaptic alfa-1 receptors. These unique properties make urapidil a well-tolerated drug in the treatment of patients with resistant hypertension.

Keywords:

hypertension – imidazoline receptors – alpha receptors – urapidil

Sources

1. Widimský J, Filipovský J, Ceral J et al. Doporučení pro diagnostiku a léčbu arteriální hypertenze ČSH 2017. Hypertenze a kardiovaskulární prevence 2018; 7 (Suppl): 1–17.

2. Fariello R, Boni E, Corda L et al. Influence of new multifactorial antihypertensive on blood pressure and metabolic profile in essential hypertension associated with non-insulin-dependent diabetes mellitus. Eur Heart J 1992; 13 (Suppl A): 65–69. doi: 10.1093/ eurheartj/ 13.suppl_a.65.

3. Sechser T, Suchopár J, Uhlíř J. Urapidilum. Remedia 1992; 2: 224–229.

4. Widimský a kol. Hypertenze. 5. vyd. Praha: Triton 2019: 546.

5. Itner KP, Bucher M, Zimmermann M et al. Effect of three different doses of urapidil on blood glucose concentration in the streptozocin diabetic rat. Eur J Anaesthesiol 2002; 19(7): 504–509. doi: 10.1017/ S0265021502000820.

6. Švejda J. Dnešní pohled na perorální urapidil v léčbě arteriální hypertenze. Cor Vasa 2009; 51(2): 138–141.

7. Janota T, Zelinka T. Urapidil, lék první volby pro těžké hypertenzní stavy. Interv Akut Kardiol 2013; 12(3): 150–152.