Metabolic and haemodynamic effects and pharmacokinetics of a new selective beta1-adrenoceptor agonist,prenalterol, in man |
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Authors: | O. Rönn E. Fellenius C. Graffner G. Johnsson P. Lundborg L. Svensson |
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Affiliation: | (1) Department of Medicine II, Sahlgrenska Sjukhuset Göteborg, Sweden;(2) Research Laboratories, AB Hässle, Mölndal, Sweden |
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Abstract: | Summary The metabolic and haemodynamic effects of three intravenous doses (0.5, 1.0 and 4.0 mg) of prenalterol, a selective 1-adrenoceptor agonist, were studied in 10 healthy male subjects. Plasma levels of prenalterol during the experiments were related to the haemodynamic effects. Prenalterol induced a dose-dependent increase in systolic blood pressure and heart rate. The maximal effects amounted to about 30 mm Hg and 15 beats/min, respectively, after the highest dose (4.0 mg). The diastolic blood pressure fell by a maximum of about 15 mm Hg. The effect of prenalterol on systolic blood pressure and heart rate persisted for about 3 h after the end of the last infusion, whereas that on diastolic blood pressure only lasted for 60 min. Compared with placebo, there was a moderate increase in plasma FFA and glycerol. A small rise in insulin level was also recorded, but no significant change was seen in other metabolic variables — triglycerides, glucose, lactate, pyruvate. Serum potassium tended to decrease and serum sodium was unchanged. The initial distribution of prenalterol was rapid (half-life 7 min) and the overall elimination rate corresponded to a plasma half-life of 2 h. A linear relationship was found between the plasma level of prenalterol and its effects on systolic blood pressure and heart rate. |
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Keywords: | prenalterol beta1-adrenoceptor agonist metabolic effects pharmacokinetics |
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