Safety and tolerability of β-blockers: importance of cardioselectivity

Cardioselective beta-blockade is generally well tolerated in practice and contraindications to this therapy are uncommon. beta-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 beta-blocker with the highest selectivity for blockade of beta(1)- vs. beta(2)-adrenoceptors, does not block beta(2)-adrenoceptors to an appreciable extent at doses in therapeutic use. Side-effects often attributed to beta-blockers, such as erectile dysfunction and adverse metabolic effects are uncommon with bisoprolol and other beta-blockers used at doses which only block beta(1)-adrenoceptors. Cautious use of a cardioselective beta-blocker is not contraindicated in people with chronic obstructive pulmonary disease or asthma and the outcomes benefits of beta-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 beta-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 beta-blocker, compared with up-titrating an existing monotherapy.