Mechanism of action

The active ingredients in SPIOLTO® RESPIMAT® are tiotropium, a long acting muscarinic receptor antagonist (LAMA) and olodaterol, a long acting beta2-adrenergic agonist (LABA) delivered via RESPIMAT®. Together the LAMA/LABA combination provide additive bronchodilation due to their different modes of action and different locations of the target receptors in the lungs.1

In the airways tiotropium binds to the muscarinic receptors in the bronchial smooth muscle cells, antagonising the cholinergic (bronchoconstrictive) effects of acetylcholine, resulting in bronchial smooth muscle relaxation, that can last longer than 24 hours.1

Olodaterol binds and activates the beta2-adrenoreceptor after administration by inhalation. The activation of these receptors in the airways results in a stimulation of an enzyme that mediates the synthesis of cyclic-3',5' adenosine monophosphate (cAMP). Elevated levels of cAMP induce bronchodilation by relaxation of airway smooth muscle cells.1

Since muscarinic receptors appear to be more prominent in the central airways while beta2-adrenoceptors have a higher expression in the peripheral airways, a combination of tiotropium and olodaterol should provide optimal bronchodilation in all regions of the lungs.1

Onset of action

SPIOLTO® RESPIMAT® (tiotropium/olodaterol) has a fast onset of action, providing lung function improvements within 5 minutes, and a long-lasting duration of action of at least 24 hours.1

 

References

  1. SPIOLTO® RESPIMAT® Summary of Product Characteristics February 2017.