top of page
The Sound of Evolution
Bitolterol
Mechanism of action:
Bitolterol is a short-acting β₂-adrenergic agonist. Bitolterol is metabolized by esterases in the lungs or blood into its active form, colterol, which then binds to β₂ receptors on airway smooth muscle. This stimulates the Gₛ protein-adenylyl cyclase system, increases cAMP, activates protein kinase A (PKA), and thereby relaxes smooth muscle and reduces airway smooth muscle tone.
Reference(s):
1. Bierman CW et al. (1996). Efficacy and safety of inhaled bitolterol mesylate via metered-dose inhaler in children with asthma. Ann Allergy Asthma Immunol.
2. Friedel HA et al. (1988). Bitolterol: A preliminary review of its pharmacological properties and therapeutic efficacy in reversible obstructive airways disease. Drugs.
bottom of page