Selective beta-1 receptor blockade with oral practolol in man. A dose-related phenomenon

Juan J L Lertora; Allyn L Mark; U. James Johannsen; William R Wilson; Francois M Abboud

doi:10.1172/JCI108143

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Selective beta-1 receptor blockade with oral practolol in man. A dose-related phenomenon

Journal article

Open access

Peer reviewed

Selective beta-1 receptor blockade with oral practolol in man. A dose-related phenomenon

Juan J L Lertora, Allyn L Mark, U. James Johannsen, William R Wilson and Francois M Abboud

The Journal of clinical investigation, Vol.56(3), pp.719-724

09/1975

DOI: 10.1172/JCI108143

PMID: 239966

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Abstract

The purpose of this study was to test the hypothesis that oral administration of a low dose of practolol in man produces selective beta-1 receptor blockade, whereas oral administration of a high dose blocks both beta-1 and beta-2 receptors. Normal men were studied 2-4 h after a single oral dose of practolol (1.5 or 12 mg/kg) and after placebo. Effects on beta-1 receptors were studied by measuring heart rate responses to exercise. Effects on beta-2 receptors were tested by measuring forearm vascular responses to brachial arterial infusions of isoproterenol. Neither dose of practolol altered base-line heart rate, forearm vascular resistance, and arterial pressure, Both low and high doses significantly attenuated heart rate responses to exercise. Forearm vasodilator responses to isoproterenol were attenuated by the high dose, but not the low dose, of practolol. Serum concentrations of practolol 2 h after administration of the drug and at the time of the studies of forearm vascular responses averaged 0.5+/-0.1 (SE) and 5.9+/-1.0 mug/ml for low and high doses of practolol, respectively. The results indicate that the phenomenon of selective beta-1 receptor blockade in man is related to the dose and serum concentration of practolol selectively block beta-1 receptors; a high dose and serum concentrations block both beta-1 and beta-2 receptors.

Administration, Oral

Humans

Practolol - administration & dosage

Male

Practolol - blood

Practolol - pharmacology

Dose-Response Relationship, Drug

Adrenergic beta-Antagonists - pharmacology

Heart Rate - drug effects

Isoproterenol - pharmacology

Vascular Resistance - drug effects

Adult

Blood Pressure - drug effects

Details

Title: Subtitle: Selective beta-1 receptor blockade with oral practolol in man. A dose-related phenomenon
Creators: Juan J L Lertora
Allyn L Mark
U. James Johannsen
William R Wilson
Francois M Abboud
Resource Type: Journal article
Publication Details: The Journal of clinical investigation, Vol.56(3), pp.719-724
Publisher: American Society for Clinical Investigation
DOI: 10.1172/JCI108143
PMID: 239966
ISSN: 0021-9738
eISSN: 1558-8238
Language: English
Date published: 09/1975
Academic Unit: Molecular Physiology and Biophysics; Cardiovascular Medicine; Fraternal Order of Eagles Diabetes Research Center; Internal Medicine
Record Identifier: 9984025374302771

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