Indacaterol + Glycopyrronium bromide + Mometasone

Indacaterol + Glycopyrronium bromide + Mometasone is used for: Asthma

Inhalation Capsule Maintenance treatment of asthma in adults not adequately controlled w/ maintenance combination of long-acting beta2-agonist & high-dose inhaled corticosteroid w/ >1 asthma exacerbation 1 cap once-daily inhalation at the same time each day. Hepatic impairment No dose adjustment is required in patients with mild or moderate hepatic impairment. No data are available for the use of the medicinal product in patients with severe hepatic impairment, therefore it should be used in these patients only if the expected benefit outweighs the potential risk

Renal impairment No dose adjustment is required in patients with mild to moderate renal impairment. Caution should be observed in patients with severe renal impairment or end-stage renal disease requiring dialysis.

For inhalation use only. The capsules must not be swallowed. The capsules must be administered only using the inhaler provide.

Hypersensitivity to the active substances or to any of the excipients.

Discontinue use if hypersensitivity reactions & paradoxical bronchospasm occurs. Not to be used for acute asthma & bronchospasm episodes. CV disorders (CAD, acute MI, cardiac arrhythmias, HTN), convulsive disorders or thyrotoxicosis, unusually responsive to β2-adrenergic agonists; unstable ischaemic heart disease, history of MI w/in last 12 mth, NYHA class III/IV left ventricular failure, arrhythmia, uncontrolled HTN, cerebrovascular disease; known or suspected QT interval prolongation or patients treated w/ medicinal products affecting QT interval; hypokalaemia; hyperglycaemia, type I or uncontrolled type II DM; narrow-angle glaucoma or urinary retention; pulmonary TB, chronic or untreated infections. Systemic effects eg, Cushing's syndrome, Cushingoid features, adrenal suppression, decreased bone mineral density, cataracts, glaucoma, psychological or behavioural effects, psychomotor hyperactivity, sleep disorders, anxiety, depression or aggression; visual disturbance. Rinse mouth or gargle w/ water w/o swallowing to reduce risk of oropharyngeal candida infection. Avoid abrupt w/drawal. High-dose & prolonged use. Not to be used in galactose intolerance, total lactase deficiency or glucose-galactose malabsorption. Severe renal (GFR <30 mL/min/1.73 m2) or hepatic impairment; ESRD requiring dialysis. Pregnancy & lactation. Childn <18 yr; growth retardation in childn & adolescents.

Pregnancy: There are insufficient data from the use of this inhaler or its individual components (indacaterol, glycopyrronium and mometasone furoate) in pregnant women to determine whether there is a risk. Indacaterol and glycopyrronium were not teratogenic in rats and rabbits following subcutaneous or inhalation administration, respectively: Toxicology: Preclinical safety data under Actions). In animal reproduction studies with pregnant mice, rats and rabbits, mometasone furoate caused increased foetal malformations and decreased foetal survival and growth. Like other medicinal products containing beta2-adrenergic agonists, indacaterol may inhibit labour due to a relaxant effect on uterine smooth muscle. This medicinal product should only be used during pregnancy if the expected benefit to the patient justifies the potential risk to the foetus. Breast-feeding: There is no information available on the presence of indacaterol, glycopyrronium or mometasone furoate in human milk, on the effects on a breast-fed infant, or on the effects on milk production. Other inhaled corticosteroids similar to mometasone furoate are transferred into human milk. Indacaterol, glycopyrronium and mometasone furoate have been detected in the milk of lactating rats. Glycopyrronium reached up to 10-fold higher concentrations in the milk of lactating rats than in the blood of the dam after intravenous administration. A decision must be made whether to discontinue breast-feeding or to discontinue/abstain from therapy, taking into account the benefit of breast-feeding for the child and the benefit of therapy for the woman. Fertility: Reproduction studies and other data in animals did not indicate a concern regarding fertility in either males or females.

Potentiated effect on QT interval w/ MAOIs, TCAs or medicinal products prolonging QT interval. Potentiated hypokalaemic effect w/ methylxanthine derivatives, steroids or non-K-sparing diuretics. Weakened or antagonised effect by beta-adrenergic blockers. Increased systemic exposure to mometasone furoate w/ strong CYP3A4 inhibitors eg, ketoconazole, itraconazole, nelfinavir, ritonavir, cobicistat. Increased risk of systemic side effects w/ cobicistat-containing products. Potentiated AR w/ long-acting β2-adrenergic agonists.

Side effects of Indacaterol + Glycopyrronium bromide + Mometasone : Nasopharyngitis; asthma exacerbation. URTI, candidiasis, UTI; hypersensitivity; headache; tachycardia; oropharyngeal pain, cough, dysphonia; gastroenteritis; musculoskeletal pain, muscle spasms; pyrexia.

This medicinal product is a combination of indacaterol, a long-acting beta2-adrenergic agonist (LABA), glycopyrronium, a long-acting muscarinic receptor antagonist (LAMA) and mometasone furoate, an inhaled synthetic corticosteroid (ICS). Indacaterol The pharmacological effects of beta2-adrenoceptor agonists, including indacaterol, are at least in part attributable to increased cyclic-3', 5'-adenosine monophosphate (cyclic AMP) levels, which cause relaxation of bronchial smooth muscle. When inhaled, indacaterol acts locally in the lung as a bronchodilator. Indacaterol is a partial agonist at the human beta2-adrenergic receptor with nanomolar potency. In isolated human bronchus, indacaterol has a rapid onset of action and a long duration of action. Although beta2-adrenergic receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-receptors are the predominant receptors in the human heart, there are also beta2-adrenergic receptors in the human heart comprising 10% to 50% of the total adrenergic receptors. Glycopyrronium Glycopyrronium works by blocking the bronchoconstrictor action of acetylcholine on airway smooth muscle cells, thereby dilating the airways. Glycopyrronium bromide is a high-affinity muscarinic receptor antagonist. It demonstrated 4- to 5-fold selectivity for the human M3 and M1 receptors over the human M2 receptor in competition binding studies. It has a rapid onset of action, as evidenced by observed receptor association/dissociation kinetic parameters and by the onset of action after inhalation in clinical studies. The long duration of action can be partly attributed to sustained drug concentrations in the lungs, as reflected by the prolonged terminal elimination half-life of glycopyrronium after inhalation via the inhaler in contrast to the half-life after intravenous administration. Mometasone furoate Mometasone furoate is a synthetic corticosteroid with high affinity for glucocorticoid receptors and local anti-inflammatory properties. In vitro, mometasone furoate inhibits the release of leukotrienes from leukocytes of allergic patients. In cell culture, mometasone furoate demonstrated high potency in inhibition of synthesis and release of IL-1, IL-5, IL-6 and TNF-alpha. It is also a potent inhibitor of leukotriene production and of the production of the Th2 cytokines IL-4 and IL-5 from human CD4+ T-cells.