Safety and tolerability of β-blockers: importance of cardioselectivity

Cardioselective β-blockade is generally well tolerated in practice and contraindications to this therapy are uncommon. β-blockers are a diverse therapeutic class, and their individual tolerability profiles are influenced strongly by their pharmacodynamic effects across different adrenergic receptors. Bisoprolol, probably the β-blocker with the highest selectivity for blockade of β₁- vs. β₂-adrenoceptors, does not block β₂-adrenoceptors to an appreciable extent at doses in therapeutic use. Side-effects often attributed to β-blockers, such as erectile dysfunction and adverse metabolic effects are uncommon with bisoprolol and other β-blockers used at doses which only block β₁-adrenoceptors. Cautious use of a cardioselective β-blocker is not contraindicated in people with chronic obstructive pulmonary disease or asthma and the outcomes benefits of β-blockers in patients with coronary heart disease or heart failure are also apparent in patients with concurrent COPD. Starting with a low dose and titrating upwards carefully is important for optimising the tolerability of a β-blocker. Most people with hypertension will receive combination antihypertensive therapy in practice, and the low-dose combination therapy approach provides a useful strategy for optimising the efficacy and tolerability of a regimen that includes a β-blocker, compared with up-titrating an existing monotherapy.