Umeclidinium Bromide (3 brand names, 1 dosage form, 1 route)
Available dosage forms: POWDER.
Routes of administration: INHALATION.
Brand Names
- ANORO ELLIPTA
- INCRUSE ELLIPTA
- TRELEGY ELLIPTA
Contraindications
TRELEGY ELLIPTA is contraindicated in the following conditions: •Primary treatment of status asthmaticus or other acute episodes of COPD or asthma where intensive measures are required [see Warnings and Precautions (5.2)]. •Severe hypersensitivity to milk proteins or demonstrated hypersensitivity to fluticasone furoate, umeclidinium, vilanterol, or any of the excipients [see Warnings and Precautions (5.11), Description (11)].
Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in labeling: •Serious Asthma-Related Events – Hospitalizations, Intubations, Death [see Warnings and Precautions (5.1)] •Oropharyngeal Candidiasis [see Warnings and Precautions (5.4)] •Increased Risk of Pneumonia in COPD [see Warnings and Precautions (5.5)] •Immunosuppression and Risk of Infections [see Warnings and Precautions (5.6)] •Hypercorticism and Adrenal Suppression [see Warnings and Precautions (5.8)] •Paradoxical Bronchospasm [see Warnings and Precautions (5.10)] •Cardiovascular Effects [see Warnings and Precautions (5.12)] •Reduction in Bone Mineral Density [see Warnings and Precautions (5.13)] •Worsening of Narrow-Angle Glaucoma [see Warnings and Precautions (5.14)] •Worsening of Urinary Retention [see Warnings and Precautions (5.15)] Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice.
Mechanism of Action
TRELEGY ELLIPTA TRELEGY ELLIPTA contains fluticasone furoate, umeclidinium, and vilanterol. The mechanisms of action described below for the individual components apply to TRELEGY ELLIPTA. These drugs represent 3 different classes of medications (an ICS, an anticholinergic, and a LABA), each having different effects on clinical and physiological indices. Fluticasone Furoate Fluticasone furoate is a synthetic trifluorinated corticosteroid with anti-inflammatory activity. Fluticasone furoate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor that is approximately 29.9 times that of dexamethasone and 1.7 times that of fluticasone propionate. The clinical relevance of these findings is unknown. The precise mechanism through which fluticasone furoate affects COPD and asthma symptoms is not known. Inflammation is an important component in the pathogenesis of COPD and asthma. Corticosteroids have been shown to have a wide range of actions on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) involved in inflammation. Specific effects of fluticasone furoate demonstrated in in vitro and in vivo models included activation of the glucocorticoid response element, inhibition of pro-inflammatory transcription factors such as NFkB, and inhibition of antigen-induced lung eosinophilia in sensitized rats. These anti-inflammatory actions of corticosteroids may contribute to their efficacy. Umeclidinium Umeclidinium is a long-acting muscarinic antagonist, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparatio
Overdosage
TRELEGY ELLIPTA contains fluticasone furoate, umeclidinium, and vilanterol; therefore, the risks associated with overdosage for the individual components described below apply to TRELEGY ELLIPTA. Treatment of overdosage consists of discontinuation of TRELEGY ELLIPTA together with institution of appropriate symptomatic and/or supportive therapy. The judicious use of a cardioselective beta-receptor blocker may be considered, bearing in mind that such medicine can produce bronchospasm. Cardiac monitoring is recommended in cases of overdosage. Fluticasone Furoate Because of low systemic bioavailability (15.2%) and an absence of acute drug-related systemic findings in clinical trials, overdosage of fluticasone furoate is unlikely to require any treatment other than observation. If used at excessive doses for prolonged periods, systemic effects such as hypercorticism may occur [see Warnings and Precautions (5.8)]. Umeclidinium High doses of umeclidinium may lead to anticholinergic signs and symptoms. Vilanterol The expected signs and symptoms with overdosage of vilanterol are those of excessive beta‑adrenergic stimulation and/or occurrence or exaggeration of any of the signs and symptoms of beta-adrenergic stimulation (e.g., seizures, angina, hypertension or hypotension, tachycardia with rates up to 200 beats/min, arrhythmias, nervousness, headache, tremor, muscle cramps, dry mouth, palpitation, nausea, dizziness, fatigue, malaise, insomnia, hyperglycemia, hypokalemia, metabolic acidosis). As with all inhaled sympathomimetic medicines, cardiac arrest and even death may be associated with an overdose of vilanterol.