Jun 18, 2002

Beta-adrenoceptor agonists and asthma--100 years of development

European Journal of Pharmacology
Bertil Waldeck

Abstract

Inhaled beta(2)-adrenoceptor agonists are by far the most effective and safe bronchodilators currently available. They have not been surpassed by any other bronchodilating principle. The way to this position has been long and started with the first successful treatment of acute, severe asthma with s.c. injections of adrenaline 100 years ago. Over the years, synthetic congeners of adrenaline have been produced and tested for their pharmacological properties. During the first decades, little attention was given airway smooth muscle. The discovery of isoprenaline in 1940 was the first major step towards selective bronchodilation. This compound became a key tool for the classification of adrenoceptors into alpha and beta. Salbutamol and terbutaline were the first to show a significant attenuation of the cardiostimulant effect and confirmed the subdivision of beta-adrenoceptors into beta(1) and beta(2). Much effort was made to eliminate the next dose-limiting side effect, skeletal muscle tremor but in vain. Prolonged duration of action was achieved in three ways: with bambuterol, an orally active carbamate ester prodrug of terbutaline, salmeterol, an inhaled beta(2)-adrenoceptor agonist emerging from a purposeful research project, a...Continue Reading

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  • Citations68

Citations

Mentioned in this Paper

Bambuterol
Vaginal Intraepithelial Neoplasia
Formoterol
Smooth Muscle
Adrenergic beta-Agonists
Adverse Effects
Bronchodilator Agents
Carbamate esters
Salmeterol
Epinephrine Measurement

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