β-blockers: a review of their pharmacological and physiological diversity in hypertension.

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.