Update on Newer Antihypertensive Medicines

Article information

J Korean Med Assoc. 2010;53(8):717-722
Publication date (electronic) : 2010 July 30
doi : https://doi.org/10.5124/jkma.2010.53.8.717
Department of Cardiology, Cardiovascular Center, Korea University Guro Hospital, Seoul, Korea.
Corresponding author: Chang Gyu Park. packcg@kumc.or.kr
Received 2010 July 13; Accepted 2010 July 26.

Abstract

The majority of hypertensive patients do not achieve target blood pressure for a variety of reasons, including insufficient medication, drug resistance, and noncompliance. There remains a significant need to develop new agents to better control hypertension. Nebivolol is a third-generation β-adrenergic receptor blocker which is very highly cardioselective and has direct vasodilator properties via stimulation of endothelial nitric oxide synthase activity. Aliskiren is the first orally active inhibitor of renin as an antihypertensive agent. It is associated with dose-related falls in blood pressure comparable to other major classes of antihypertensive drugs with a placebo level of side effects. Endothelin is a powerful vasoconstrictor peptide. An endothelin-receptor antagonist such as bosentan significantly lowered blood pressure in patients with essential hypertension. Vasopeptidase inhibitors inhibit neutral endopeptidase and angiotensin converting enzymes, but side-effects such as angio-oedema and cough remain to be overcome. AngQb vaccine in hypertensive patients showed a marked reduction in early morning blood pressure without serious adverse events.

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Figure 1

The renin_angiotensin system and the sites of inhibition by renin-inhibitors, angiotensin-converting enzyme inhibitors (ACEIs),angiotensin receptor blockers (ARBs), aldosterone-receptor blockers, and neutral endopeptidase (NEP) inhibitors. This figure was adapted from the reference 7.

Figure 2

The opposing effects of endothelin on endothelial and vascular smooth muscle cells are shown and are mediated by differential response to endothelin-receptor (ETA and ETB) stimulations. Endothelin-converting enzyme (ECE) is found on endothelial cells and is responsible for conversion of big endothelin-1 to endothelin-1, the predominant form of endothelin. This figure was adapted from the reference 7.