Kinetics of pamatolol, a cardioselective beta adrenoreceptor blocker

Clinical Pharmacology and Therapeutics
S G CarruthersD L Azarnoff

Abstract

The systemic bioavailability, elimination half-life (t1/2), and plasma concentration--response relationships of pamatolol, a relatively cardioselective beta adrenoceptor blocker, have been measured in healthy subjects. Pamatolol is rapidly and completely absorbed after oral dosing. Elimination t1/2 ranged from 2.9 to 4.6 hr after oral doses and from 2.2 to 5.6 hr after intravenous doses. There was a clear relationship between log plasma pamatolol concentration and sympathetic blockade assessed by reduction of exercise heart rate. Concentration-response curves were essentially identical after oral and intravenous doses. There is no evidence of a first-pass effect, nor is there any evidence of metabolite activity.

Related Concepts

Positive Regulation of Secondary Metabolite Biosynthetic Process
Intravenous
Intravenous Injections
Propanolamines
Beta Adrenoceptor Activity
Teens
Adrenergic Receptor
Plasma
Heart
Biological Availability

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