Beta-adrenergic blockers in systemic hypertension: pharmacokinetic considerations related to the current guidelines.
Beta-adrenergic blockade has provided one of the major pharmacotherapeutic advances of the 20th century. Beta-blockers are first-line drugs for the management of systemic hypertension, used alone and in combination with other antihypertensive agents. Drugs in the beta-blocking class have the common property of blocking the binding of catecholamines to beta-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 beta-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 beta-blocking drugs. The wide interpatient variability in plasma drug concentrations observed with beta-blockers makes this parameter unreliable in routine patient management. Despite the pharmacokinetic differences among beta-blockers, these drugs should always be titrated to achieve the desired individual patient response.
Frishman
William H
WH
Department of Medicine, New York Medical College/Westchester Medical Center, Room 263 Munger Pavilion, Valhalla, NY 10595, USA.
Alwarshetty
Mamata
M
D000319:Adrenergic beta-Antagonists / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D000368:Aged; D001682:Biological Availability; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D006207:Half-Life; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000378:metabolism; D007408:Intestinal Absorption; D011485:Protein Binding; D013329:Structure-Activity Relationship
D000319:Adrenergic beta-Antagonists