Combination of | |
---|---|
Beclometasone dipropionate | Glucocorticoid |
Formoterol fumarate dihydrate | Long-acting β2 agonist |
Glycopyrronium bromide | Antimuscarinic |
Clinical data | |
Trade names | Trimbow, Trydonis, Riarify, others |
AHFS/Drugs.com | UK Drug Information |
Routes of administration | Inhalation |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
CAS Number |
Beclometasone/formoterol/glycopyrronium, sold under the brand name Trimbow among others, is an inhalable fixed-dose combination medication for the treatment of chronic obstructive pulmonary disease (COPD) and asthma. It contains beclometasone dipropionate, formoterol fumarate dihydrate, and glycopyrronium bromide. [3] [4]
Side effects include oral candidiasis (a fungal infection of the mouth caused by a yeast called Candida), muscle spasms and dry mouth. [3] [4]
Beclometasone/formoterol/glycopyrronium was approved for use in the European Union in July 2017, and in April 2018. [3] [4] [5]
Trimbow is indicated for the maintenance treatment in adults with moderate to severe chronic obstructive pulmonary disease (COPD) and asthma who are not adequately treated by a combination of an inhaled corticosteroid and a long-acting beta2-agonist or a combination of a long-acting beta2-agonist and a long-acting muscarinic antagonist. [3]
Trydonis and Riarify are indicated for the maintenance treatment in adults with moderate to severe chronic obstructive pulmonary disease (COPD) who are not adequately treated by a combination of an inhaled corticosteroid and a long-acting beta2-agonist. [4] [5]
Beclometasone belongs to a group of anti-inflammatory medicines known as corticosteroids. [3] [4] It works in a similar way to naturally occurring corticosteroid hormones, reducing the activity of the immune system. [3] [4] This leads to a reduction in the release of substances that are involved in the inflammation process, such as histamine, thereby helping to keep the airways clear and allowing the patient to breathe more easily. [3] [4]
Formoterol is a long-acting beta-2 agonist. [3] [4] It attaches to receptors (targets) known as beta-2 receptors in the muscles of the airways. [3] [4] By attaching to these receptors, it causes the muscles to relax, which keeps the airways open and helps with the patient's breathing. [3] [4]
Glycopyrronium bromide is a muscarinic receptor antagonist. [3] [4] It opens the airways by blocking muscarinic receptors in muscle cells in the lungs. [3] [4] Because these receptors help control the contraction of the airway muscles, blocking them causes the muscles to relax, helping to keep the airways open and allowing the patient to breathe more easily. [3] [4]
Trimbow was approved for medical use in the European Union in July 2017, and Trydonis was approved for medical use in the European Union in April 2018. [3] [4]
The combination of beclometasone, formoterol, and glycopyrronium bromide has been shown to be effective at relieving symptoms of COPD in three main studies involving over 5,500 participants whose symptoms were not controlled well enough by either combinations of two other COPD medicines or by a muscarinic receptor antagonist alone. [3] [4]
In the first study lasting a year, after 26 weeks of treatment the combination improved participants' FEV1 (the maximum volume of air a person can breathe out in one second) by 82 ml before a dose and 261 ml after a dose. [3] [4] By comparison, the FEV1 increased by 1 and 145 ml before and after dosing respectively in participants treated with a medicine containing only two of the active substances found in the combination (beclometasone plus formoterol). [3] [4]
In the second study lasting a year, participants treated with the combination had 20% fewer exacerbations (flare-ups of symptoms) a year than participants treated with tiotropium (a muscarinic receptor antagonist). [3] [4] In this study, the combination was as effective as tiotropium plus a combination of beclometasone and formoterol at reducing the number of exacerbations. [3] [4]
In the third study lasting a year, participants treated with the combination had 15% fewer exacerbations a year than participants treated with a combination of indacaterol (a long-acting beta-2 agonist) and glycopyrronium. [3] [4]
A bronchodilator or broncholytic is a substance that dilates the bronchi and bronchioles, decreasing resistance in the respiratory airway and increasing airflow to the lungs. Bronchodilators may be originating naturally within the body, or they may be medications administered for the treatment of breathing difficulties, usually in the form of inhalers. They are most useful in obstructive lung diseases, of which asthma and chronic obstructive pulmonary disease are the most common conditions. Although this remains somewhat controversial, they might be useful in bronchiolitis and bronchiectasis. They are often prescribed but of unproven significance in restrictive lung diseases.
Bronchospasm or a bronchial spasm is a sudden constriction of the muscles in the walls of the bronchioles. It is caused by the release (degranulation) of substances from mast cells or basophils under the influence of anaphylatoxins. It causes difficulty in breathing which ranges from mild to severe.
Ipratropium bromide, sold under the trade name Atrovent among others, is a type of anticholinergic medication which is applied by different routes: inhaler, nebulizer, or nasal spray, for different reasons.
Salmeterol is a long-acting β2 adrenergic receptor agonist (LABA) used in the maintenance and prevention of asthma symptoms and maintenance of chronic obstructive pulmonary disease (COPD) symptoms. Symptoms of bronchospasm include shortness of breath, wheezing, coughing and chest tightness. It is also used to prevent breathing difficulties during exercise.
Budesonide/formoterol, sold under the brand name Symbicort among others, is a fixed-dose combination medication used in the management of asthma or chronic obstructive pulmonary disease (COPD). It contains budesonide, a steroid and formoterol, a long-acting β2-agonist (LABA). The product monograph does not support its use for sudden worsening or treatment of active bronchospasm. However, a 2020 review of the literature does support such use. It is used by breathing in the medication.
Formoterol, also known as eformoterol, is a long-acting β2 agonist (LABA) used as a bronchodilator in the management of asthma and chronic obstructive pulmonary disease (COPD). Formoterol has an extended duration of action compared to short-acting β2 agonists such as salbutamol (albuterol), which are effective for 4 h to 6 h. Formoterol has a relatively rapid onset of action compared to other LABAs, and is effective within 2-3 minutes. The 2022 Global Initiative for Asthma report recommends a combination formoterol/inhaled corticosteroid inhaler as both a preventer and reliever treatment for asthma in adults. In children, a short-acting β2 adrenergic agonist is still recommended.
Glycopyrronium bromide is a medication of the muscarinic anticholinergic group. It does not cross the blood–brain barrier and consequently has few to no central effects. It is given by mouth, via intravenous injection, on the skin, and via inhalation. It is a synthetic quaternary ammonium compound. The cation, which is the active moiety, is called glycopyrronium (INN) or glycopyrrolate (USAN).
Beta2-adrenergic agonists, also known as adrenergic β2 receptor agonists, are a class of drugs that act on the β2 adrenergic receptor. Like other β adrenergic agonists, they cause smooth muscle relaxation. β2 adrenergic agonists' effects on smooth muscle cause dilation of bronchial passages, vasodilation in muscle and liver, relaxation of uterine muscle, and release of insulin. They are primarily used to treat asthma and other pulmonary disorders. Bronchodilators are considered an important treatment regime for chronic obstructive pulmonary disease (COPD) and are usually used in combination with short acting medications and long acting medications in a combined inhaler.
Bronchoconstriction is the constriction of the airways in the lungs due to the tightening of surrounding smooth muscle, with consequent coughing, wheezing, and shortness of breath.
Long-acting β adrenoceptor agonists (LABAs) are beta-adrenergic agonists usually prescribed for moderate-to-severe persistent asthma and chronic obstructive pulmonary disease (COPD). They are designed to reduce the need for shorter-acting β2 agonists such as salbutamol (albuterol), as they have a duration of action of approximately 12 hours in comparison with the 4-to-6-hour duration of salbutamol, making them candidates for sparing high doses of corticosteroids or treating nocturnal asthma and providing symptomatic improvement in patients with COPD. With the exception of formoterol, long-acting β2 agonists are not recommended for the treatment of acute asthma exacerbations because of their slower onset of action compared to salbutamol. Their long duration of action is due to the addition of a long, lipophilic side-chain that binds to an exosite on adrenergic receptors. This allows the active portion of the molecule to continuously bind and unbind at β2 receptors in the smooth muscle in the lungs.
Indacaterol is an ultra-long-acting beta-adrenoceptor agonist developed by Novartis. It needs to be taken only once a day, unlike the related drugs formoterol and salmeterol. It is licensed only for the treatment of chronic obstructive pulmonary disease (COPD). It is delivered as an aerosol formulation through a dry powder inhaler.
Aclidinium bromide (INN) is a long-acting, inhaled muscarinic antagonist (LAMA) approved in the United States on July 24, 2012 as a maintenance treatment for chronic obstructive pulmonary disease (COPD).
Tiotropium bromide, sold under the brand name Spiriva among others, is a long-acting bronchodilator used in the management of chronic obstructive pulmonary disease (COPD) and asthma. Specifically it is used during periods of breathing difficulty to prevent them from getting worse, rather than to prevent them from happening. It is used by inhalation through the mouth. Onset typically begins within half an hour and lasts for 24 hours.
Vilanterol is an ultra-long-acting β2 adrenoreceptor agonist (ultra-LABA), which was approved in May 2013 in combination with fluticasone furoate for sale as Breo Ellipta by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease (COPD).. The combination is also approved for the treatment of asthma in Canada, Europe, Japan and New Zealand.
Indacaterol/glycopyrronium bromide, sold under the brand name Ultibro Breezhaler among others, is a fixed-dose combination medication for inhalation consisting of the following two active ingredients:
Aclidinium bromide/formoterol, sold under the brand names Duaklir and Brimica, is a fixed-dose combination medication for inhalation, used in the management of chronic obstructive pulmonary disease (COPD). It consists of aclidinium bromide, a long-acting muscarinic antagonist, and formoterol, a long-acting β2 agonist.
Fluticasone furoate/umeclidinium bromide/vilanterol, sold under the brand name Trelegy Ellipta among others, is a fixed-dose combination inhaled medication that is used for the maintenance treatment of chronic obstructive pulmonary disease (COPD). The medications work in different ways: fluticasone furoate is an inhaled corticosteroid (ICS), umeclidinium is a long-acting muscarinic antagonist (LAMA), and vilanterol is a long-acting beta-agonist (LABA).
Glycopyrronium bromide/formoterol, sold under the brand name Bevespi Aerosphere, is a combination medication for the maintenance treatment of chronic obstructive pulmonary disease (COPD). It is a combination of glycopyrronium bromide and formoterol. It is inhaled.
Indacaterol/glycopyrronium bromide/mometasone, sold under the brand name Enerzair Breezhaler among others, is an inhalable fixed-dose combination medication for the treatment of asthma. It contains indacaterol as acetate, glycopyrronium bromide, and mometasone furoate.
Budesonide/glycopyrronium bromide/formoterol, sold under the brand name Breztri Aerosphere among others, is an inhalable fixed-dose combination medication for the treatment of chronic obstructive pulmonary disease (COPD). It contains budesonide, glycopyrronium bromide, and formoterol fumarate dihydrate. It is inhaled.