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.