The effects of formoterol, a long-acting beta 2-adrenoceptor agonist, on mucociliary activity.
The effect on mucociliary function of formoterol, a beta 2-adrenoceptor agonist bronchodilator with a prolonged duration of action (as compared with salbutamol or terbutaline), was investigated both in vitro and in vivo with a photoelectric technique. Formoterol, and its (R,R)-enantiomer, increased ciliary beat frequency in vitro in guinea pig trachea preparations (peak increase 17.2 +/- 2.0% at a concentration of 10(-7) M) and in vivo in the rabbit maxillary sinus (peak increase 23.0 +/- 4.0% at a dosage of 1 nmol/kg). Formoterol was approximately 100 times more potent than terbutaline in vitro, as judged from the dose-response curve. The main difference between their effect in vivo was the 2-fold longer duration of the mucociliary acceleration after formoterol at 1 nmol/kg than after terbutaline at the equi-effective dosage of 10 nmol/kg terbutaline (20 vs. 10 min, respectively). The findings indicate formoterol to be a powerful, long-acting ciliostimulant, a property which may be of clinical advantage in the treatment of airway disease.
Lindberg
S
S
Department of Oto-Rhino-Laryngology, Head and Neck Surgery, University Hospital, Lund, Sweden.
Khan
R
R
Runer
T
T
D058666:Adrenergic beta-2 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000494:pharmacology*; D000818:Animals; D001993:Bronchodilator Agents / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004983:Ethanolamines / Q000494:pharmacology*; D005260:Female; D000068759:Formoterol Fumarate; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009079:Mucociliary Clearance / Q000187:drug effects*; D011817:Rabbits; D013237:Stereoisomerism; D013268:Stimulation, Chemical; D013726:Terbutaline / Q000494:pharmacology; D014132:Trachea / Q000187:drug effects
D058666:Adrenergic beta-2 Receptor Agonists; D000318:Adrenergic beta-Agonists; D001993:Bronchodilator Agents; D004983:Ethanolamines; D013726:Terbutaline; D000068759:Formoterol Fumarate