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Renin Angiotensin Blockers and Cardiac Protection: From Basis to Clinical Trials
Bernard I Lévy1, Jean Jacques Mourad2
1Inserm U970, PARRC, Hôpital Lariboisière, Paris, France.
Insights
Angiotensin-converting enzyme inhibitors (ACEIs) show better cardiovascular protection than angiotensin II type 1 receptor blockers (ARBs). Pharmacological differences explain why ACEIs are preferred over ARBs for cardiac protection.
Area of Science:
- Pharmacology
- Cardiovascular Medicine
- Nephrology
Background:
- Angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin II type 1 receptor blockers (ARBs) similarly lower blood pressure.
- Clinical trials indicate ARBs may increase cardiovascular mortality and reduce myocardial infarction protection compared to ACEIs.
- European guidelines recommend ARBs for patients intolerant to ACEIs.
Purpose of the Study:
- To review pharmacological differences between ACEIs and ARBs.
- To elucidate how these differences impact cardiac protection.
- To provide insights into the distinct cardiovascular effects of ACEIs and ARBs.
Main Methods:
- Review of existing clinical trials and meta-analyses comparing ACEIs and ARBs.
- Analysis of pharmacological mechanisms of action for both drug classes.
- Examination of effects on bradykinin, nitric oxide, and angiotensin II receptor signaling.
Main Results:
- ACEIs uniquely affect bradykinin levels and nitric oxide bioavailability, influencing endothelial function, atherogenesis, and fibrinolysis.
- ARBs cause a sustained increase in plasma angiotensin II, potentially overstimulating available receptors.
- Animal models suggest AT4 and AT2 receptor activation by angiotensin II may have deleterious effects in certain conditions.
Conclusions:
- Pharmacological distinctions, particularly ACEIs' effects on bradykinin and nitric oxide, may explain differing cardiovascular outcomes.
- The chronic increase in angiotensin II and potential AT2 receptor overstimulation with ARBs warrant consideration.
- Reserve ARBs for patients with ACEI intolerance due to potential adverse cardiovascular effects.
Abstract:
Despite a similar beneficial effect on blood pressure lowering observed with angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin II type 1 receptor (AT1R) blocker (ARBs), several clinical trials and meta-analyses have reported higher cardiovascular mortality and lower protection against myocardial infarction with ARBs when compared with ACEIs. The European guidelines for the management of coronary syndromes and European guidelines on diabetes recommend using ARBs in patients who are intolerant to ACEIs. We reviewed the main pharmacological differences between ACEIs and ARBs, which could provide insights into the differences in the cardiac protection offered by these 2 drug classes. The effect of ACEIs on the tissue and plasma levels of bradykinin and on nitric oxide production and bioavailability is specific to the mechanism of action of ACEIs; it could account for the different effects of ACEIs and ARBs on endothelial function, atherogenesis, and fibrinolysis. Moreover, chronic blockade of AT1 receptors by ARBs induces a significant and permanent increase in plasma angiotensin II and an overstimulation of its still available receptors. In animal models, AT4 receptors have vasoconstrictive, proliferative, and inflammatory effects. Moreover, in models with kidney damage, atherosclerosis, and/or senescence, activation of AT2 receptors could have deleterious fibrotic, vasoconstrictive, and hypertrophic effects and seems prudent and reasonable to reserve the use of ARBs for patients who have presented intolerance to ACE inhibitors.
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