Role of olmesartan in combination therapy in blood pressure control and vascular function

Abstract

Angiotensin receptor blockers have emerged as a first-line therapy in the management of hypertension and hypertension-related comorbidities. Since national and international guidelines have stressed the need to control blood pressure to <140/90 mmHg in uncomplicated hypertension and <130/80 mmHg in those with associated comorbidities such as diabetes or chronic kidney disease, these goal blood pressures can only be achieved through combination therapy. Of several drugs that can be effectively combined to attain the recommended blood pressure goals, fixed-dose combinations of angiotensin receptor blockers and the calcium channel blocker amlodipine provide additive antihypertensive effects associated with a safe profile and increased adherence to therapy. In this article, we review the evidence regarding the beneficial effects of renin-angiotensin system blockade with olmesartan medoxomil and amlodipine in terms of blood pressure control and improvement of vascular function and target organ damage.

Keywords: amlodipine; angiotensin receptor blockers; angiotensin-converting enzyme 2; hypertension; renin–angiotensin system.

Figure 1

Comparative pharmacodynamic characteristics of five angiotensin receptor blockers in terms of their half maximal inhibitory concentration (IC₅₀) and dissociation constant (Ki). The active form of olmesartan shows high affinity for AT₁ receptors with an IC₅₀ equivalent to that of candesartan and much lower than the IC₅₀ for other angiotensin receptor blockers. Similarly, the lowest IC₅₀ for olmesartan is associated with the lowest dissociation constant from the receptor.

Figure 2

Bar graph denotes the average value of wall/media lumen ratio from small resistance arterioles obtained from normotensive subjects (normal) and patients with hypertension without diabetes assigned to either an atenolol-based or olmesartan-based therapy before and at week 52 after completion of the treatment regimen. Note: Values are means ± standard error of the mean. *P < 0.005 compared with normal. Drawn from data of Smith et al.