Literature DB >> 2421751

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

T Hashimoto, A Shiina, T Toyo-Oka, S Hosoda, K Kondo.   

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.

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Year:  1986        PMID: 2421751      PMCID: PMC1400849          DOI: 10.1111/j.1365-2125.1986.tb05188.x

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


  6 in total

1.  Problems in echocardiographic volume determinations: echocardiographic-angiographic correlations in the presence of absence of asynergy.

Authors:  L E Teichholz; T Kreulen; M V Herman; R Gorlin
Journal:  Am J Cardiol       Date:  1976-01       Impact factor: 2.778

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Journal:  Circulation       Date:  1971-04       Impact factor: 29.690

3.  Tachycardia and bradycardia-dependent bundle branch block alternans: clinical observations.

Authors:  H C Cohen; I D'Cruz; E R Arbel; R Langendorf; A Pick
Journal:  Circulation       Date:  1977-02       Impact factor: 29.690

4.  Sources of variability in echocardiographic measurements.

Authors:  J M Felner; B A Blumenstein; R C Schlant; A D Carter; B N Alimurung; M J Johnson; S W Sherman; M W Klicpera; M H Kutner; L W Drucker
Journal:  Am J Cardiol       Date:  1980-05       Impact factor: 2.778

5.  The cardiovascular effects of ICI 118,587: A beta 1-adrenoceptor partial agonist.

Authors:  A Nuttall; H M Snow
Journal:  Br J Pharmacol       Date:  1982-10       Impact factor: 8.739

6.  Systolic time intervals in measurement of inotropic response to drugs.

Authors:  B F Johnson; M K Meeran; A Frank; S H Taylor
Journal:  Br Heart J       Date:  1981-11
  6 in total
  8 in total

Review 1.  Beta-adrenoceptor partial agonists: a renaissance in cardiovascular therapy?

Authors:  D G Waller
Journal:  Br J Clin Pharmacol       Date:  1990-08       Impact factor: 4.335

Review 2.  Xamoterol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use.

Authors:  R Furlong; R N Brogden
Journal:  Drugs       Date:  1988-10       Impact factor: 9.546

3.  Comparison of the effects of xamoterol and isoprenaline on rat cardiac beta-adrenoceptors: studies of function and regulation.

Authors:  M T Kowalski; D Haworth; X Lu; D S Thomson; D B Barnett
Journal:  Br J Pharmacol       Date:  1990-01       Impact factor: 8.739

Review 4.  Myocardial beta-adrenoceptor function and regulation in heart failure: implications for therapy.

Authors:  D B Barnett
Journal:  Br J Clin Pharmacol       Date:  1989-05       Impact factor: 4.335

5.  The pharmacokinetics of xamoterol in liver disease.

Authors:  D P Nicholls; A J Taggart; J P McCann; W Bastain; R G Shanks
Journal:  Br J Clin Pharmacol       Date:  1989-12       Impact factor: 4.335

6.  Beta-adrenoceptor antagonists increase sinus arrhythmia, a vagotonic effect.

Authors:  S B Bittiner; S E Smith
Journal:  Br J Clin Pharmacol       Date:  1986-12       Impact factor: 4.335

7.  Lack of pharmacodynamic interactions between acute dose flosequinan and xamoterol. A pilot study in healthy subjects.

Authors:  H W Ng; T J Walley; Y Tsao; A M Breckenridge
Journal:  Eur J Clin Pharmacol       Date:  1994       Impact factor: 2.953

8.  Placebo controlled trial of xamoterol versus digoxin in chronic atrial fibrillation.

Authors:  E L Ang; W L Chan; J G Cleland; D Moore; S J Krikler; N D Alexander; C M Oakley
Journal:  Br Heart J       Date:  1990-10
  8 in total

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