Formoterol Fumarate Dihydrate (3 brand names, 1 dosage form, 1 route)
Available dosage forms: AEROSOL, METERED.
Routes of administration: INHALATION.
Brand Names
- BREYNA
- BUDESONIDE AND FORMOTEROL FUMARATE DIHYDRATE
- SYMBICORT
Contraindications
The use of budesonide and formoterol fumarate dihydrate inhalation aerosol is contraindicated in the following conditions: Primary treatment of status asthmaticus or other acute episodes of asthma or COPD where intensive measures are required. Hypersensitivity to any of the ingredients in budesonide and formoterol fumarate dihydrate inhalation aerosol.
Adverse Reactions
LABA use may result in the following: Serious asthma-related events – hospitalizations, intubations, death [see Warnings and Precautions (5.1)]. Cardiovascular and central nervous system effects [see Warnings and Precautions (5.12)]. Systemic and inhaled corticosteroid use may result in the following: Candida albicans infection [see Warnings and Precautions (5.4)] Pneumonia or lower respiratory tract infections in patients with COPD [see Warnings and Precautions (5.5)] Immunosuppression [see Warnings and Precautions (5.6)] Hypercorticism and adrenal suppression [see Warnings and Precautions (5.8 )] Growth effects in pediatric patients [see Warnings and Precautions (5.14 )] Glaucoma and cataracts [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 to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
Drug Interactions
In clinical studies, concurrent administration of budesonide and formoterol fumarate dihydrate inhalation aerosol and other drugs, such as short-acting beta2-agonists, intranasal corticosteroids, and antihistamines/decongestants has not resulted in an increased frequency of adverse reactions. No formal drug interaction studies have been performed with budesonide and formoterol fumarate dihydrate inhalation aerosol.
Mechanism of Action
Budesonide and Formoterol Fumarate Dihydrate Inhalation Aerosol Budesonide and formoterol fumarate dihydrate inhalation aerosol contains both budesonide and formoterol; therefore, the mechanisms of action described below for the individual components apply to budesonide and formoterol fumarate dihydrate inhalation aerosol. These drugs represent two classes of medications (a synthetic corticosteroid and a long-acting selective beta2-adrenoceptor agonist) that have different effects on clinical, physiological, 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 form 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 in COPD and asthma. Studies in asthmatic patients have shown a favorable ratio between topical anti-inflammatory activity and systemic corticosteroid effects over a wide range of doses of budesonide. This i
Overdosage
Budesonide and Formoterol Fumarate Dihydrate Inhalation Aerosol Budesonide and formoterol fumarate dihydrate inhalation aerosol contains both budesonide and formoterol; therefore, the risks associated with overdosage for the individual components described below apply to budesonide and formoterol fumarate dihydrate inhalation aerosol. In pharmacokinetic studies, single doses of 960/54 mcg (12 actuations of budesonide and formoterol fumarate dihydrate inhalation aerosol 80/4.5) and 1280/36 mcg (8 actuations of 160/4.5), were administered to patients with COPD. A total of 1920/54 mcg (12 actuations of budesonide and formoterol fumarate dihydrate inhalation aerosol 160/4.5) was administered as a single dose to both healthy subjects and patients with asthma. In a long-term active-controlled safety study in adolescent and adult asthma patients 12 years of age and older, budesonide and formoterol fumarate dihydrate inhalation aerosol 160/4.5 was administered for up to 12 months at doses up to twice the highest recommended daily dose. There were no clinically significant adverse reactions observed in any of these studies. Budesonide The potential for acute toxic effects following overdose of budesonide is low. If used at excessive doses for prolonged periods, systemic corticosteroid effects such as hypercorticism may occur [see Warnings and Precautions (5)]. Budesonide at five times the highest recommended dose (3200 mcg daily) administered to humans for 6 weeks caused a significant reduction (27%) in the plasma cortisol response to a 6-hour infusion of ACTH compared with placebo (+1%). The corresponding effect of 10 mg prednisone daily was a 35% reduction in the plasma cortisol response to ACTH. Formoterol An overdose of formoterol 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,