Effects of dilevalol, a beta-adrenoceptor antagonist with intrinsic sympathetic activity in asthmatic patients.
The effects on baseline ventilation as well as beta 2-receptor stimulant-induced bronchodilation and tremor of atenolol and dilevalol, a beta-blocking agent with non-selective beta-antagonistic properties and intrinsic activity on the beta 2-receptor were evaluated in 8 patients with stable asthma. Both atenolol and dilevalol were found to significantly decrease both forced expiratory volume during 1 s (FEV1) and forced vital capacity (FVC). This decrease was significantly more pronounced after atenolol. Both agents decreased systolic and diastolic blood pressure as well as heart rate to a similar degree. Increased activation of beta 2-adrenoceptors by terbutaline infusion resulted in increased FEV1 and FVC as well as beta 2-adrenoceptor mediated reflex tachycardia and skeletal muscle tremor. The dose response curves for all these parameters were significantly shifted to the right and a decrease of the maximum relative response was seen after atenolol pretreatment. This effect was more pronounced after treatment with dilevalol with a further shift to the right of the response curve and a decrease of the maximum relative response. The haemodynamic and ventilatory effects of dilevalol are consistent with a non-selective beta-adrenoceptor blockade combined with intrinsic activity on the beta 2-receptors.
Hedner
J
J
Department of Clinical Pharmacology, Sahlgrenska University Hospital, Gothenburg, Sweden.
Ullman
A
A
Lemne
C
C
Svedmyr
N
N
D000319:Adrenergic beta-Antagonists / Q000009:adverse effects* / Q000493:pharmacokinetics; D000328:Adult; D000368:Aged; D001249:Asthma / Q000150:complications / Q000503:physiopathology*; D001262:Atenolol / Q000009:adverse effects / Q000493:pharmacokinetics; D004311:Double-Blind Method; D005260:Female; D005541:Forced Expiratory Volume; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D007741:Labetalol / Q000009:adverse effects* / Q000493:pharmacokinetics; D008297:Male; D008875:Middle Aged; D013726:Terbutaline / Q000493:pharmacokinetics / Q000627:therapeutic use; D014202:Tremor / Q000139:chemically induced / Q000503:physiopathology; D014797:Vital Capacity
D000319:Adrenergic beta-Antagonists; D001262:Atenolol; D013726:Terbutaline; D007741:Labetalol