β-Adrenergic blockade has provided one of the major pharmacotherapeutic advances of the 20th century. β-Blockers are first-line drugs for the management of systemic hypertension, used alone and in combination with other antihypertensive agents. Drugs in the β-blocking class have the common property of blocking the binding of catecholamines to β-adrenergic receptor sites; however, there are significant pharmacodynamic and pharmacokinetic differences between the individual agents that are of clinical importance. Among these differences are the completeness of gastrointestinal absorption, the degree of hepatic first-pass metabolism, lipid solubility, protein binding, brain penetration, concentration within the cardiac tissue, rate of hepatic biotransformation, and renal clearance of drug and/or metabolites. Long-acting formulations of existing β-blockers are currently in use, and ultra-short-acting agents are also available.Age, race, cigarette smoking and concomitant drug therapy can also influence the pharmacokinetics of β-blocking drugs. The wide interpatient variability in plasma drug concentrations observed with β-blockers makes this parameter unreliable in routine patient management. Despite the pharmacokinetic differences among β-blockers, these drugs should always be titrated to achieve the desired individual patient response.