Dec 1, 1975

Plasma concentrations and the time-course of beta blockade due to propranolol

Clinical Pharmacology and Therapeutics
D G McDevitt, D G Shand

Abstract

The effectiveness of intravenously administered propranolol in antagonizing the chronotropic effect of isoproterenol and exercise has been investigated, and has been found at all times to be a predictable function of its plasma concentrations according to the classical drug-receptor theory for competitive antagonism. The data show further that the relationship between effectiveness and time depends on the way in which antagonism is measured. If the dose ratio to isoproterenol (DR) is measured, then (DR-1) declines with time in parallel with drug concentration. On the other hand, if propranolol's effects are measured as percentage reduction in a given response, then this declines linearly with time, even though plasma concentrations decline exponentially. This fact explains why confusion has in the past arisen concerning the relationship of the duration of beta blockade and pharmacokinetic half-life.

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Mentioned in this Paper

Novodrin
Norepinephrine Receptors
Propranolol
Isoproterenol
HLA-DRB1
Blockade
Rexigen
Half-Life
Pulse Rate
Adrenergic beta-Antagonists

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