Objective: To review the pharmacology, pharmacokinetics, and pharmacodynamic properties of commonly used β-blockers (atenolol, carvedilol, metoprolol succinate, metoprolol tartrate, and nebivolol).
Data sources: A MEDLINE literature search (1966-May 2013) was performed using the following key terms: hypertension, β-blockers, atenolol, carvedilol, metoprolol tartrate, metoprolol succinate, nebivolol, pharmacology, pharmacodynamics, pharmacokinetics, blood pressure, metabolic, lipid, central aortic pressure, diabetes, and insulin resistance. References from publications reviewed were included.
Study selection and data extraction: English-language articles identified were reviewed. Animal studies and studies in patients for a primary diagnosis of coronary artery disease were excluded.
Data synthesis: β-Blockers are no longer recommended first-line therapy for primary hypertension, based on data showing that β-blockers are inferior to other antihypertensives and no better than placebo, in spite of provision of blood pressure reduction. Because atenolol is the β-blocker used in 75% of these studies, uncertainty about widespread application to all β-blockers exists. Different pharmacological and physiological properties, both within β-blockers and compared with other antihypertensives, may explain divergent effects. Evidence shows that β-blockers have a truncated effect on central aortic pressure, an independent predictor of cardiovascular events, compared with other antihypertensive classes; differences within the class may exist, but the evidence is inconclusive. Metabolic effects differ within the β-blocker class, with evidence that carvedilol causes less metabolic dysregulation.
Conclusion: Emerging evidence reveals physiological differences within the β-blocker class and in comparison to other antihypertensives. These differences provide insight into the diverse clinical effects β-blockers provide in cardiovascular disease.
Keywords: central aortic pressure; hypertension; metabolic; pharmacodynamics; pharmacology; β-blockers.