Functional and Biochemical Rationales for the 24-Hour-Long Duration of Action of Olodaterol

  title={Functional and Biochemical Rationales for the 24-Hour-Long Duration of Action of Olodaterol},
  author={Paola Casarosa and Ines Kollak and Tobias Kiechle and Angela Ostermann and Andreas Schnapp and Ralf Kiesling and Michael Pieper and Peter Sieger and Florian Gantner},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={600 - 609}
β2-Adrenoceptor (β2-AR) agonists are powerful bronchodilators and play a pivotal role in the management of pulmonary obstructive diseases, such as asthma and chronic obstructive pulmonary disease. Although these agents first were used many years ago, progress in drug development has resulted in better tolerated, long-acting β2-AR agonists (LABAs), such as formoterol and salmeterol. Although LABAs have been on the market for several years, relatively little is known on the rationale(s) behind… 

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

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    European journal of pharmacology
  • 2002

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Evidence is presented supporting a unifying hypothesis that the duration of action both of formoterol and salmeterol is determined principally by their physicochemical interactions with membrane lipid bilayers (plasmalemma diffusion microkinetic model), rather than putative distinct exosite/exoceptor binding sites in or near the beta 2-adrenoceptor.

Formoterol fumarate, a new beta 2-adrenoceptor agonist. Acute studies of selectivity and duration of effect after inhaled and oral administration.

Four double-blind, double-dummy, randomized, crossover studies were performed in nine asthmatic patients to evaluate beta 2-adrenoceptor selectivity and the duration of effect of formoterol, concluding that inhaledformoterol is 5-15 times more potent than salbutamol.

β-Adrenoceptor Ligands: Characterization and Quantification of Drug Effects

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