Pharmacokinetic optimisation of therapy with beta-adrenergic blocking agents.
beta-Adrenergic blockade has provided one of the major pharmacotherapeutic advances of this century. The drugs in this class have the common property of blocking the binding of catecholamines to beta-adrenergic receptor sites; however, there are pharmacodynamic and pharmacokinetic differences between the individual agents which are of clinical importance. Among these differences are the completeness of gastrointestinal absorption, degree of hepatic first-pass metabolism, lipid solubility, protein binding, brain penetration, concentration within 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 ultrashort-acting agents are also available. The pharmacokinetics of beta-blocking drugs can also be influenced by race, age, cigarette smoking and concomitant drug therapy. The wide interpatient variability in plasma drug concentration observed with beta-blockers makes this parameter unreliable in routine patient management. Despite the pharmacokinetic differences among the beta-blockers, these drugs should always be titrated in the individual patient to achieve the desired clinical response.
Department of Medicine Division, Albert Einstein College of Medicine, Bronx, New York.
W H
WH
Frishman
E J
EJ
Lazar
G
G
Gorodokin
D000319:Adrenergic beta-Antagonists / Q000493:pharmacokinetics* / Q000627:therapeutic use; D000375:Aging / Q000378:metabolism; D004347:Drug Interactions; D006801:Humans; D044469:Racial Groups; D012907:Smoking / Q000378:metabolism
D000319:Adrenergic beta-Antagonists