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English name: Indacaterol/glycopyrrolate/mometasone furoate
Trade name: Enerzair inhalation capsules
Chinese name: Indacaterol/glycopyrrolate/mometasone furoate composite inhalation capsules
Manufacturer: Novartis Pharmaceuticals
Drug Introduction:
The world's first triple inhalation drug for asthma: Enerza IR inhalation capsule is a fixed-dose combination product composed of indacaterol acetate (IND, a LABA), glycopyrrolate (GLY, a LAMA), and mometasone furoate (MF, an ICS). It precisely combines the bronchodilator effect of IND with the antimuscarinic effect of GLY and the anti-inflammatory effect of ICS. The product is administered using the Breezhaler device with a dose confirmation mechanism, which allows for once-daily inhalation treatment using a single inhaler. Significantly reduce the rate of acute exacerbations of moderate to severe asthma.
Pharmaceutical efficacy classification name:
Triple combination asthma treatment agent
Approval date:August 2020
Characteristics:
It is a white powder.
Indications:
Bronchial asthma (when inhaled steroids, long-acting inhaled beta-2 agonists and long-acting inhaled anticholinergics are used concurrently)
Usage and Dosage:
Generally, adults should take 1 capsule (150 μg of indacaterol, 50 μg of glycopyrrolate and 80 μg of mometasone furoate) in a medium-dose energy inhalation capsule per day.
Energy Inhalation Capsules High-dose 1 capsule (150 μg of indacaterol, 50 μg of glycopyrrolate, and 160 μg of mometasone furoate) inhaled once daily depending on symptoms.
Packaging:
Medium dose capsules for inhalation
14 capsules (7 capsules 2 tablets, 1 Breeze Heller®)
Handling Precautions:
Store in blister pack protected from light and moisture.
Mechanism of action:
Indacaterol
It is a long-acting β-receptor agonist, showing high affinity for β2 receptors compared with β1 and β3 receptors.
Glycopyrrolate
It is a long-acting muscarinic receptor antagonist with high affinity for all muscarinic receptors M1 to M5. Compared with tiotropium bromide, it is slightly more selective for M3 receptors than M2 receptors.
Mometasone furoate
It is a synthetic steroid with affinity for the glucocorticoid receptor.
Bronchiectasis
Indacaterol/glycyrrhizic acid
It exhibits a concentration-dependent inhibitory effect on the contraction induced by carbamic acid in the resected trachea of guinea pigs. The combined use of indacaterol and glycopyrronium shows an additive effect.
Indacaterol
It shows a sustained inhibitory effect of 5-hydroxytryptamine on bronchoconstriction in response to methancholine in conscious guinea pigs and anesthetized ruby-throated monkeys.
Glycopyrrolate
It exhibits inhibitory effects on tracheostomy contractions induced by muscarinic receptor stimulation in guinea pigs and humans. It shows sustained inhibitory effects on soft-shell choline-induced airway contraction in rats and algae monkeys.
Anti-inflammatory effect
Mometasone furoate
Inhibits the production of interleukin-4 (IL-4) and IL-5 by human helper T cells (in vitro). In actively sensitized mice, the number of inflammatory cells (such as eosinophils) in bronchoalveolar lavage fluid or lung tissue increased through antigen induction, and IL-4 and IL-5 mRNA expression in lung tissue was suppressed.