Clinical Pharmacokinetics

, Volume 41, Issue 7, pp 505–516 | Cite as

β-Adrenergic Blockers in Systemic Hypertension

Pharmacokinetic Considerations Related to the Current Guidelines
  • William H. Frishman
  • Mamata Alwarshetty
Review Article Special Populations


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.


Propranolol Metoprolol Carvedilol Sotalol Plasma Drug Concentration 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.



No sources of funding were used to assist in the preparation of this manuscript. There are no potential conflicts of interest directly relevant to the contents of this manuscript.


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Copyright information

© Adis International Limited 2002

Authors and Affiliations

  • William H. Frishman
    • 1
  • Mamata Alwarshetty
    • 2
  1. 1.Department of MedicineNew York Medical College/Westchester Medical CenterValhallaUSA
  2. 2.Department of MedicineWeill Cornell Medical School/St. Barnabas Hospital CenterNew YorkUSA

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