The cardiovascular effects of xamoterol, a beta 1-adrenoceptor partial agonist, in healthy volunteers at rest

Br J Clin Pharmacol. 1986 Mar;21(3):259-65. doi: 10.1111/j.1365-2125.1986.tb05188.x.

Abstract

The cardiovascular effects of three single intravenous doses of a beta 1-adrenoceptor partial agonist, xamoterol (0.025, 0.05 and 0.1 mg kg-1) and placebo were studied in six healthy volunteers at rest using a single-blind design. In addition to heart rate and blood pressure measurements, cardiac contractility was measured by means of M-mode echocardiography and systolic time intervals. Ambulatory 24 h Holter-monitoring of the electrocardiogram was performed. Plasma concentrations of xamoterol were measured. Compared to baseline, xamoterol (0.025 mg kg-1) increased heart rate (61 +/- 3-68 +/- 3 beats min-1, means and SEM) and systolic blood pressure (119 +/- 3-138 +/- 5 mm Hg) but decreased pre-ejection period (100 +/- 4-76 +/- 5 msec). Stroke volume (88 +/- 6-104 +/- 10 ml), cardiac output (4.8 +/- 0.4-6.6 +/- 0.61 min-1), velocity of circumferential fibre shortening (1.15 +/- 0.06-1.50 +/- 0.06 circ s-1) were increased by xamoterol. No significant changes were produced by placebo. No dose-dependent effects were seen and maximum effects were produced by 0.025 mg kg-1 xamoterol. Significant effects were observed for 2 h. The areas under the plasma concentration curves (AUC0-12) showed a linear dose response. No adverse effects attributable to xamoterol were seen in haematological, biochemical, urinalysis or electrocardiographic tests. Four volunteers were aware of a more forceful heart beat after xamoterol, but this was mild and transient. It is concluded that xamoterol has a positive inotropic action.

Publication types

  • Clinical Trial
  • Controlled Clinical Trial

MeSH terms

  • Adrenergic beta-Agonists / pharmacology*
  • Adult
  • Blood Pressure / drug effects
  • Bundle-Branch Block / physiopathology
  • Cardiac Complexes, Premature / physiopathology
  • Cardiac Output / drug effects
  • Electroencephalography
  • Heart Rate / drug effects
  • Hemodynamics / drug effects*
  • Humans
  • Male
  • Myocardial Contraction / drug effects*
  • Propanolamines / adverse effects
  • Propanolamines / blood
  • Propanolamines / pharmacology*
  • Stroke Volume / drug effects
  • Xamoterol

Substances

  • Adrenergic beta-Agonists
  • Propanolamines
  • Xamoterol