Abstract
Objective: This review covers the pharmacokinetics and pharmacodynamic of β-blockers, the rationale for their use, some recent controversies in its use for managing hypertension, as well as, the beneficial properties of the third-generation β-blockers beyond hypertension.
Background: The efficacy and safety of β-blockers in the treatment of hypertension and other cardiovascular diseases have been established during more than 50 years of clinical experience. Recent updates of clinical guidelines have downgraded the use of β-blockers for the treatment of uncomplicated hypertension to second and third line therapy. It is a well-known fact that β-blockers exhibit heterogeneous pharmacokinetic and pharmacodynamic properties that clearly influence their clinical efficacy and tolerability in the management of essential hypertension. Conventional nonvasodilating β-blockers (atenolol and metoprolol) are inferior to first-line antihypertensive agents in terms of cardioprotection due to lower ability to reduce central blood pressure and its variability and the adverse effects on glycemic and lipid metabolism.
Conclusion: New vasodilating β-blockers, mainly carvedilol and nebivolol, show enhanced hemodynamic and metabolic properties, which probably result in a higher prevention of major cardiovascular events in hypertensive patients. Despite head-to-head clinical trials comparing the effects of vasodilating vs. nonvasodilating β-blockers on hard clinical endpoints are lacking, the current evidence suggests that third-generation β-blockers are superior to conventional β-blockers for the prevention of cardiovascular events in patients with essential hypertension. Moreover, beyond their antihypertensive properties, third-generation β-blockers also have pleiotropic, antioxidant and antiinflammatory effects that warrant a “promissory new era” of this newly group.
Keywords: β-blockers, essential hypertension, central blood pressure, pharmacokinetics, pharmacodynamics, target organ damage, glycemia, lipids.
Current Pharmaceutical Design
Title:What is the Real Efficacy of Beta-Blockers for the Treatment of Essential Hypertension?
Volume: 23 Issue: 31
Author(s): Christian Hocht*, Facundo M. Bertera, Julieta S. Del Mauro, Yanina Santander Plantamura, Carlos A. Taira and Ariel H Polizio
Affiliation:
- Universidad de Buenos Aires, Facultad de Farmacia y Bioquimica, Departamento de Farmacologia. Buenos Aires,Argentina
Keywords: β-blockers, essential hypertension, central blood pressure, pharmacokinetics, pharmacodynamics, target organ damage, glycemia, lipids.
Abstract: Objective: This review covers the pharmacokinetics and pharmacodynamic of β-blockers, the rationale for their use, some recent controversies in its use for managing hypertension, as well as, the beneficial properties of the third-generation β-blockers beyond hypertension.
Background: The efficacy and safety of β-blockers in the treatment of hypertension and other cardiovascular diseases have been established during more than 50 years of clinical experience. Recent updates of clinical guidelines have downgraded the use of β-blockers for the treatment of uncomplicated hypertension to second and third line therapy. It is a well-known fact that β-blockers exhibit heterogeneous pharmacokinetic and pharmacodynamic properties that clearly influence their clinical efficacy and tolerability in the management of essential hypertension. Conventional nonvasodilating β-blockers (atenolol and metoprolol) are inferior to first-line antihypertensive agents in terms of cardioprotection due to lower ability to reduce central blood pressure and its variability and the adverse effects on glycemic and lipid metabolism.
Conclusion: New vasodilating β-blockers, mainly carvedilol and nebivolol, show enhanced hemodynamic and metabolic properties, which probably result in a higher prevention of major cardiovascular events in hypertensive patients. Despite head-to-head clinical trials comparing the effects of vasodilating vs. nonvasodilating β-blockers on hard clinical endpoints are lacking, the current evidence suggests that third-generation β-blockers are superior to conventional β-blockers for the prevention of cardiovascular events in patients with essential hypertension. Moreover, beyond their antihypertensive properties, third-generation β-blockers also have pleiotropic, antioxidant and antiinflammatory effects that warrant a “promissory new era” of this newly group.
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Cite this article as:
Hocht Christian *, Bertera M. Facundo , Del Mauro S. Julieta , Santander Plantamura Yanina , Taira A. Carlos and Polizio H Ariel, What is the Real Efficacy of Beta-Blockers for the Treatment of Essential Hypertension?, Current Pharmaceutical Design 2017; 23 (31) . https://dx.doi.org/10.2174/1381612823666170608085109
DOI https://dx.doi.org/10.2174/1381612823666170608085109 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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