Glycopyrrolate-formoterol (brand name Bevespi Aerosphere; Astra Zeneca) is a LAMA/LABA combination to maximize bronchodilation as a long-term maintenance treatment for COPD. Glycopyrrolate is a LAMA (long-acting muscarinic antagonist) bronchodilator, and formoterol is a LABA (long-acting beta2-agonist) bronchodilator.

How does glycopyrrolate-formoterol for COPD work?

Bevespi Aerosphere uses a co-suspension technology, which enables the stable administration of one or more medicines in a single inhaler.

Glycopyrrolate is a long-acting muscarinic antagonist, also known as anticholinergic, that connects to the muscarinic receptor 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 these receptors on the smooth muscle of the bronchi, leading to bronchodilation.

Formoterol is a selective 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 lung muscle cells but they are also present in the heart, which means salmeterol may have cardiac effects like an irregular heartbeat.

Studies of glycopyrrolate-formoterol

The U.S. Food and Drug Administration (FDA) approved the glycopyrrolate-formoterol combination known as Bevespi Aerosphere in April 2016 based the PINNACLE clinical trial program. The program included two Phase 3 studies in some 3,700 patients with moderate to very severe COPD — NCT01854645 and NCT01854658 — and a safety extension study (NCT01970878).

In these trials, Bevespi Aerosphere taken twice daily (glycopyrrolate 18 mcg/formoterol 9.6 mcg,) demonstrated statistically significant improvements in FEV1 (a measure of lung health) in treated patients compared to either medication as a monotherapy or to placebo. Patients given the combination also showed a significant improvement ing peak FEV1 two hours after treatment administration and a less need for rescue medication.

The most common adverse reactions in trial patients using Bevespi Aerosphere, compared to placebo, were urinary tract infections (2.6% vs 2.3%, respectively ) and cough (4.0% vs 2.7%).

Indications and side effects

The combination of glycopyrrolate-formoterol comes as an aerosol to inhale by mouth using a special inhaler, and is usually used twice a day. As a maintenance COPD therapy, it is intended to treat sudden breathing problems or acute bronchospasm, and is not a short-acting or rescue bronchodilator.

The most common side effects of glycopyrrolate-formoterol include cough and urinary tract infections.

There is no generic available.

 

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