Does beta 1-selective agonistic activity interfere with the antihypertensive efficacy of beta 1-selective blocking agents?
In order to investigate whether addition of beta 1-selective agonism can interfere with the antihypertensive efficacy of beta 1-selective adrenoceptor blockers, two separate studies were carried out to evaluate the effects on blood pressure and heart rate of three beta 1-selective blockers with or without varying degree of beta 1-selective agonism. In hypertensive patients at rest, the greatest blood pressure reduction and bradycardia were found with atenolol, a beta 1-selective blocker without any agonistic activity; a consistently smaller effect on blood pressure and heart rate was observed with Visacor (ICI 141 292), a beta 1-selective blocker with moderate beta 1-selective agonism, whereas no clinically relevant decrease in blood pressure occurred with Corwin (ICI 118 587), the beta 1-selective blocker with high beta 1-selective agonism. In contrast, during exercise-induced sympathetic activation, all three compounds reduced systolic blood pressure and heart rate to a similar degree.
Leonetti
G
G
Istituto di Clinica Medica Generale e Terapia Medica di Milano, Ospedale Maggiore, Italy.
Sampieri
L
L
Cuspidi
C
C
Terzoli
L
L
Rupoli
L
L
Fruscio
M
M
Gradnik
R
R
Zanchetti
A
A
D000318:Adrenergic beta-Agonists / Q000494:pharmacology / Q000627:therapeutic use*; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology / Q000627:therapeutic use*; D000959:Antihypertensive Agents / Q000494:pharmacology / Q000627:therapeutic use*; D001262:Atenolol / Q000494:pharmacology / Q000627:therapeutic use; D044482:Benzeneacetamides; D004311:Double-Blind Method; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D011412:Propanolamines / Q000494:pharmacology / Q000627:therapeutic use; D017307:Xamoterol / Q000494:pharmacology / Q000627:therapeutic use
D000318:Adrenergic beta-Agonists; D000319:Adrenergic beta-Antagonists; D000959:Antihypertensive Agents; D044482:Benzeneacetamides; D011412:Propanolamines; D001262:Atenolol; D017307:Xamoterol; C038616:epanolol