Formoterol Fumarate (10 brand names, 4 dosage forms, 1 route)
Available dosage forms: SOLUTION, POWDER, AEROSOL, METERED, POWDER, METERED.
Routes of administration: INHALATION.
Brand Names
- BEVESPI AEROSPHERE
- BREZTRI AEROSPHERE
- DUAKLIR PRESSAIR
- DULERA
- FORADIL
- FORADIL CERTIHALER
- FORMOTEROL FUMARATE
- PERFOROMIST
- SYMBICORT AEROSPHERE
- TRIMBOW
Dosage and Administration
BREZTRI AEROSPHERE should be administered as 2 inhalations twice daily, in the morning and in the evening, by oral inhalation. Do not take more than two inhalations twice daily. After inhalation, rinse mouth with water without swallowing [see Warnings and Precautions (5.4)]. Priming Before Use Priming BREZTRI AEROSPHERE is essential to ensure appropriate drug content in each actuation. Prime BREZTRI AEROSPHERE before using for the first time. Prime BREZTRI AEROSPHERE by releasing 4 sprays into the air away from the face, shaking well before each spray. Re-prime BREZTRI AEROSPHERE if the inhaler has not been used for more than 7 days, is dropped, or after weekly rinsing. Prime BREZTRI AEROSPHERE by releasing 2 sprays into the air away from the face, shaking well before each spray. Dose counter BREZTRI AEROSPHERE canister has an attached dose indicator (also known as puff indicator), which indicates how many inhalations (puffs) remain. The dose indicator display has a pointer which will move after every actuation. When nearing the end of the usable inhalations, the pointer is in the yellow zone. BREZTRI AEROSPHERE should be discarded when the pointer is at zero in the red zone of the dose indicator.
Contraindications
BREZTRI AEROSPHERE 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) ] . •Hypersensitivity to budesonide, glycopyrrolate, formoterol, or any of the excipients [see Warnings and Precautions (5.11) and Description (11)].
Adverse Reactions
The following adverse reactions are discussed in greater detail in other sections of the labeling. •Serious asthma-related events – hospitalizations, intubations, death [see Warnings and Precautions (5.1)] •Oropharyngeal candidiasis infection [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)] •Hypersensitivity reactions including anaphylaxis [see Contraindications (4) and Warnings and Precautions (5.11)] •Cardiovascular effects [see Warnings and Precautions (5.12)] •Reduction in bone mineral density [see Warnings and Precautions (5.13)] •Growth effects in pediatric patients [see Warnings and Precautions (5.14)] •Worsening of narrow-angle glaucoma and cataracts [see Warnings and Precautions (5.15) ] •Worsening of urinary retention [see Warnings and Precautions (5.16) ] 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.
Drug Interactions
No formal drug interaction studies have been performed with BREZTRI AEROSPHERE.
Mechanism of Action
BREZTRI AEROSPHERE BREZTRI AEROSPHERE contains budesonide, glycopyrrolate, and formoterol fumarate. The mechanism of action described below for the individual components applies to BREZTRI AEROSPHERE. These drugs represent three different classes of medications (a synthetic corticosteroid, an anticholinergic, and a long-acting selective beta2-adrenoceptor agonist) that have different effects on clinical physiology and inflammatory indices of COPD and asthma. Budesonide Budesonide is an anti-inflammatory corticosteroid that exhibits potent glucocorticoid activity and weak mineralocorticoid activity. In standard in vitro and animal models, budesonide has approximately a 200-fold higher affinity for the glucocorticoid receptor and a 1000-fold higher topical anti-inflammatory potency than cortisol (rat croton oil ear edema assay). As a measure of systemic activity, budesonide is 40 times more potent than cortisol when administered subcutaneously and 25 times more potent when administered orally in the rat thymus involution assay. In glucocorticoid receptor affinity studies, the 22R epimer of budesonide was two times as active as the 22S epimer. In vitro studies indicated that the two forms of budesonide do not interconvert. Inflammation is an important component in the pathogenesis of COPD and asthma. Corticosteroids have a wide range of inhibitory activities against multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, and cytokines) involved in allergic and non-allergic-mediated inflammation. These anti-inflammatory actions of corticosteroids may contribute to their efficacy. Glycopyrrolate Glycopyrrolate is a long-acting antimuscarinic agent 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 the M3 receptor at the smooth mus
Overdosage
BREZTRI AEROSPHERE contains budesonide, glycopyrrolate, and formoterol fumarate; therefore, the risks associated with overdosage for the individual components described below apply to BREZTRI AEROSPHERE. Treatment of overdosage consists of discontinuation of BREZTRI AEROSPHERE 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 medication can produce bronchospasm. Cardiac monitoring is recommended in case of overdosage. Budesonide If used at excessive doses for prolonged periods, systemic corticosteroid effects, such as hypercorticism may occur [see Warnings and Precautions (5.8)]. Glycopyrrolate High doses of glycopyrrolate, a component of BREZTRI AEROSPHERE, may lead to anticholinergic signs and symptoms such as nausea, vomiting, dizziness, lightheadedness, blurred vision, increased intraocular pressure (causing pain, vision disturbances or reddening of the eye), obstipation, or difficulties in voiding. Formoterol Fumarate An overdose of formoterol fumarate would likely lead to an exaggeration of effects that are typical for beta2-agonists: seizures, angina, hypertension, hypotension, tachycardia, atrial and ventricular tachyarrhythmias, nervousness, headache, tremor, palpitations, muscle cramps, nausea, dizziness, sleep disturbances, metabolic acidosis, hyperglycemia, hypokalemia. As with all sympathomimetic medications, cardiac arrest, and even death may be associated with overdosage of formoterol fumarate.