The authors have evaluated the effectiveness of the protection of a new beta 2-adrenergic compound, reproterol, against broncho-constriction induced by physical exercise in a group of individuals of paediatric age sensitive to broncho-stimulation. This study has been carried out comparing reproterol with salbutamol, using placebo as a control, following a randomized single-blind crossover trial. The provocation test has been performed following the instructions of the Italian Society of Paediatrics. The drugs have been administered in the oral liquid form at the dose of 0.28 mg/kg and 0.1 mg/kg of reproterol and salbutamol, respectively. The two substances have shown a similar preventive effectiveness in controlling exercise-induced asthma up to 2 hours from administration with reproterol having a stronger action at the beginning of the observation.
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http://dx.doi.org/10.1177/030006058501300103 | DOI Listing |
Arzneimittelforschung
April 2006
Gustav Embden Center of Biological Chemistry, University of Frankfurt/Main, Germany.
Electron paramagnetic resonance (EPR) spectroscopy with spin labels 5- and 16-doxyl-stearic acid (DSA) was used to differentiate between actions of beta-agonists on human mononuclear cell membrane. Reproterol (CAS 13055-82-8), salbutamol (CAS 51022-70-9) and fenoterol (CAS 1944-12-3) compared to cromoglycate (CAS 15826-37-6) were used at concentrations of 10-100 nmol/l per 10(7) cells. With reproterol, order and polarity was not much changed, whereas salbutamol and fenoterol significantly destabilized the membrane to similar extent.
View Article and Find Full Text PDFEur J Med Res
July 2004
Department of Pneumology, Allergology and Sleep Medicine, Medical Outpatient Clinic, Bonn University Hospital, Germany.
Background: Beta2-adrenergic receptor agonists have several effects on airway function, most of which are mediated in a variety of cell types resulting in increased c-AMP-production and inhibition of inflammatory mediator production. However, their stimulating effects on cAMP-production became known to be inversed by increasing phosphodiesterase (PDE) activity and degradation of cAMP. Therefore, in this study we have evaluated the efficacy of reproterol, a dual acting beta2-adrenoceptor agonist and PDE-inhibitor, as compared to salbutamol and fenoterol with respect to production of cAMP and LTB4 in cultured monocytes.
View Article and Find Full Text PDFPulm Pharmacol Ther
November 2004
INSERM U400, School of Medicine, 8 rue du Général Sarrail, 94010, Créteil Cédex, France.
In vitro studies in rat mastocytes and human monocytes suggested that reproterol (a selective beta(2)-adrenoceptor agonist with a theophylline moiety) exerts anti-inflammatory actions through inhibition of cyclic AMP (cAMP) PDE activity. Thus, reproterol was tested for its ability to inhibit cAMP PDE in cultured mouse mastocytoma P-815 cells. cAMP PDE activity was measured in intact cells by spectrofluorometry using the fluorescent substrate 2'-O-anthraniloyl cAMP.
View Article and Find Full Text PDFJ Pharm Biomed Anal
October 2001
Chemistry Department, Faculty of Science, Cairo University, Cairo, Egypt.
A simple and sensitive conductimetric method for the determination of salbutamol sulphate and reproterol and pipazethate hydrochlorides is presented based on their ion associates with phosphotungstic and phosphomolybdic acids. The effect of solvent, molar ratio, reagent concentration and temperature were studied, and the solubility products of the formed ion associates were calculated. The method was applied to the determination of the drugs in their pure state or pharmaceutical preparations with mean recovery values of 99.
View Article and Find Full Text PDFCochrane Database Syst Rev
August 2001
Department of Respiratory Medicine, Alfred Hospital, Commercial Road, Prahan, Victoria, Australia.
Background: Inhaled beta2-adrenergic agonists delivered by inhalation are very widely used in asthma. There has been much controversy of the use and possible consequences of the use of these agents for regular, as opposed as-needed use in asthma.
Objectives: This review to assessed the clinical trial evidence to test whether using regular use of short-acting beta2-agonists reduced asthma control and pulmonary function; worsened symptoms, airway reactivity and quality of life; and increased the rate of exacerbations.
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