SPIOLTO RESPIMAT Inhalation solution Ref.[51419] Active ingredients: Olodaterol Olodaterol and Tiotropium bromide Tiotropium

Olodaterol has a high affinity and high selectivity to the human beta₂-adrenoceptor. The compound exerts its pharmacological effects by binding and activation of beta₂-adrenoceptors after topical administration by inhalation. Activation of these receptors in the airways results in a stimulation of intracellular adenyl cyclase, 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.

Fixed dose combination containing a long acting muscarinic receptor antagonist, tiotropium and a long acting beta₂-adrenergic agonist, olodaterol (LAMA/LABA). The two active ingredients provide additive bronchodilation due to their different mode of action. Since muscarinic receptors appear to be more prominent in the central airways while β₂ adrenoceptors have a higher expression level in the peripheral airways, a combination of tiotropium and olodaterol should provide optimal bronchodilatation in all regions of the lungs.

Tiotropium is a long-acting, specific, muscarinic receptor antagonist, in clinical medicine often called an anticholinergic. By binding to the muscarinic receptors in the bronchial smooth musculature, tiotropium inhibits the cholinergic (bronchoconstrictive) effects of acetylcholine, released from parasympathetic nerve endings.