The combination of glycopyrrolate and indacaterol (brand name, Utibron Neohaler; Novartis) is a long-term maintenance treatment of airflow obstruction or to prevent bronchospasm in people with COPD. It is not a rescue medication, and will not work fast enough to treat a sudden bronchospasm attack or acute COPD symptoms.
Glycopyrrolate is a LAMA (long-acting muscarinic antagonist) bronchodilator, and indacaterol is a LABA (long-acting beta2-agonist) bronchodilator.
How does glycopyrrolate-indacaterol for COPD work?
Glycopyrrolate and indacaterol work by relaxing the muscles in the airways to improve breathing.
Glycopyrrolate is a long-acting muscarinic antagonist, also known as anticholinergic. It connects to the muscarinic receptors subtypes M1 to M5. The M3 receptors are located in the muscle of the bronchi, and are responsible for bronchoconstriction. As glycopyrrolate has affinity to the M3 receptors, it works by inhibiting them on the muscle of the bronchi, leading to bronchodilation.
Indacaterol is a long-acting beta2-agonist (LABA), and its effects are due to the stimulation of an enzyme, called adenyl cyclase, that is in the interior of the lung muscle cells. This enzyme helps convert adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). When the levels of cAMP increase, bronchial muscle cells relax, and inhibit release of mediators of immediate hypersensitivity, especially from mast cells.
Beta2-receptors are predominant in the muscle cells of the lungs, but they are also present in the heart, which means indacaterol may have cardiac effects, such as irregular heartbeats.
Studies of glycopyrrolate-indacaterol
The U.S. Food and Drug Administration (FDA) approved Utibron Neohaler (glycopyrrolate-indacaterol) in 2015 based on the results of the Phase 3 EXPEDITION trial program, which included more than 2,500 COPD patients and consisted of two 12-week efficacy studies, FLIGHT1 (NCT01727141) and FLIGHT2 (NCT01712516), and one 52-week safety study, FLIGHT3, (NCT01682863). All participants were current or former smokers and had moderate-to-severe airflow limitation (post-bronchodilator FEV1 ≥ 30% and <80% of the predicted normal).
Twice daily glycopyrrolate-indacaterol treatment during the 12-week studies showed superior and sustained improvement in lung function at the study’s end, compared to either drug individually or to placebo. Treated patients also needed less rescue medication (albuterol) than those given placebo.
At 52 weeks, Utibron Neohaler treatment showed “significant treatment effect,” as seen by improvements in FEV1, a measure of lung function, Novartis reported.
Indications and side effects
Indacaterol, part of this combination, is not to be used by people with asthma, because it is a LABA medicine and a study in another LABA drug (salmeterol) found an increased risk of asthma-related death. In COPD patients, the combination is not indicated for relief of acute bronchospasms, or breathing problems; it is not a short-acting bronchodilator.
Glycopyrrolate-indacaterol comes as a powder inhaled by mouth using a special device, and is usually used twice daily. Typically, the dose is one Utibron capsule used with the inhaler device.
The most common glycopyrrolate-indacaterol side effects can include a stuffy nose and sore throat, and increased blood pressure that can cause headache, pounding in the neck or ears, and nosebleeds.
There is no generic available.
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