Umeclidinium is a long-acting muscarinic antagonist (LAMA) bronchodilator, and vilanterol is a long-acting beta2-agonist (LABA) bronchodilator. The drug combo works because it relaxes and opens airways to the lungs, making breathing easier.
How does umeclidinium-vilanterol for COPD work?
The anticholinergic umeclidinium connects to the muscarinic receptors subtypes M1 to M5. The M3 receptor is located in the muscle of the bronchi and is responsible for bronchoconstriction. Umeclidinium inhibits the M3 receptor at the smooth muscle, leading to bronchodilation.
Vilanterol is a LABA, and its effects are due to the stimulation of an enzyme, called adenyl cyclase, in smooth muscle cells of the lungs. This enzyme helps convert adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). When the levels of cAMP increase, bronchial muscle cells relax and the release of mediators of immediate hypersensitivity, especially from mast cells, are effectively blocked.
Beta2-receptors are predominant in the muscle cells of the lungs, but they are also present in the heart, which means vilanterol may also have cardiac effects, such as irregular heartbeats.
Studies of umeclidinium-vilanterol
The safety and effectiveness of the umeclidinium-vilanterol combination were assessed in a clinical program that included 13 different trials.
In May 2016, GSK presented the results of a Phase 3 trial (NCT01899742) that aimed to compare the effectiveness of the umeclidinium-vilanterol combo powder (62.5/25 mcg) once daily with tiotropium (18 mcg) once daily for 12 weeks in people with COPD who were being treated with tiotropium but continued to have symptoms. Participants who were switched from tiotropium to umeclidinium-vilanterol combo showed a significant improvement in FEV1 (forced expiratory volume in one second, a measure of lung function) compared to those who stayed on tiotropium.
Indications and side effects
Long-acting beta2-adrenergic agonists such as vilanterol increase the risk of asthma-related death. A placebo-controlled study with another LABA (salmeterol) showed an increase in asthma-related deaths in subjects treated with salmeterol. This result is considered an effect of all LABAs, including vilanterol.
The umeclidinium-vilanterol combo in not indicated for the treatment of asthma.
It comes as a powder to inhale by mouth once daily. It should not be used as a rescue medication in a COPD attack.
The most common reported side effects are shaking of a part of the body without control, nervousness, runny nose and sore throat, constipation, diarrhea, pain in the arms or legs, muscle spasms, and neck pain.
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