Comparison of angiotensin II type 1 receptor antagonists in the treatment of essential hypertension
Related Experiment Video
Updated: Jun 29, 2026

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors
Published on: June 7, 2016
1Integrium, Tustin, California 92780, USA. dsmith@integrium.com
Insights
Angiotensin receptor blockers (ARBs) effectively lower blood pressure, but direct comparisons show limited evidence of significant efficacy or tolerability differences between agents. Newer ARBs may offer some advantages in blood pressure reduction.
Area of Science:
- Pharmacology
- Cardiovascular Medicine
- Nephrology
Background:
- Hypertension is a global health issue, often under-diagnosed and undertreated.
- Angiotensin II type 1 receptor antagonists (ARBs) are effective antihypertensives with good tolerability and renoprotective benefits.
- Clinical differences in efficacy and tolerability among ARBs remain unclear.
Purpose of the Study:
- To compare the efficacy of various Angiotensin II type 1 receptor antagonists (ARBs) based on published randomized clinical trial data.
- To assess differences in blood pressure lowering efficacy and 24-hour blood pressure control among ARBs.
- To evaluate attainment rates for guideline-recommended blood pressure goals.
Main Methods:
- Systematic review of published randomized, comparative clinical trials involving Angiotensin II type 1 receptor antagonists (ARBs).
- Analysis of blood pressure (BP) lowering efficacy, including systolic BP (SBP) and diastolic BP (DBP) control.
- Examination of tolerability data and assessment of adherence to treatment guidelines.
Main Results:
- Evidence suggests potential differences in BP-lowering efficacy and 24-hour BP control among ARBs, but tolerability differences appear minimal.
- Few studies have assessed combined SBP/DBP goal attainment or directly compared more than two ARBs.
- Newer ARBs like olmesartan medoxomil and telmisartan show promise in reducing DBP and/or SBP compared to older agents in some trials.
Conclusions:
- Insufficient evidence exists to definitively conclude comparative efficacy among all available ARBs.
- Further head-to-head trials are needed to clarify comparative efficacy, particularly for SBP control and guideline goal attainment.
- Olmesartan medoxomil demonstrates high BP control rates in some studies, warranting further comparative investigation.
Abstract:
Hypertension is a major health problem worldwide, yet remains under-diagnosed and under-treated. Angiotensin II type 1 receptor antagonists (angiotensin receptor blockers [ARBs]) are highly effective at reducing blood pressure (BP), exhibit renoprotective properties and have placebo-like tolerability. However, it is unclear whether there are clinical differences in efficacy and tolerability between the available ARBs. A review of published, randomized, comparative clinical trials suggests that differences in BP-lowering efficacy and 24-hour BP control may exist between ARBs, although it appears that there is no evidence for important differences in tolerability between ARBs. Few studies have assessed attainment rates for important combined systolic BP (SBP)/diastolic BP (DBP) goals recommended in treatment guidelines. Likewise, few studies have directly compared more than two agents or ARB/hydrochlorothiazide fixed-dose combinations, and most ARBs have not been compared across their full recommended dosage ranges. Overall, there is insufficient weight of evidence to allow definitive conclusions to be drawn regarding the comparative efficacy of the available ARBs. However, newer ARBs (e.g. olmesartan medoxomil and telmisartan) appear to be more effective than older ARBs (e.g. losartan and valsartan) in reducing DBP and/or SBP in some trials. In addition, olmesartan medoxomil treatment regimens resulted in high BP control rates in several trials, but head-to-head trials with other ARBs are required to put these control rates into perspective, especially for SBP control with various agents. The purpose of this review is to present published data from ARB efficacy trials for a comparison of various efficacy parameters among the agents within this drug class.
Related Concept Videos
Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally, α1-blockers effectively address urinary obstruction...
Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors
Antihypertensive Drugs: Angiotensin II Receptor Blockers
Antihypertensive Drugs: Direct Renin Inhibitors
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System
Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme (ECE). Of...

