Salmeterol Xinafoate (9 brand names, 2 dosage forms, 1 route)
Available dosage forms: POWDER, AEROSOL, METERED.
Routes of administration: INHALATION.
Brand Names
- ADVAIR DISKUS 100/50
- ADVAIR DISKUS 250/50
- ADVAIR DISKUS 500/50
- ADVAIR HFA
- AIRDUO DIGIHALER
- AIRDUO RESPICLICK
- FLUTICASONE PROPIONATE AND SALMETEROL XINAFOATE
- SEREVENT
- WIXELA INHUB
Indications and Usage
ADVAIR HFA is indicated for treatment of asthma in adult and adolescent patients aged 12 years and older. ADVAIR HFA should be used for patients not adequately controlled on a long-term asthma control medication such as an inhaled corticosteroid (ICS) or whose disease warrants initiation of treatment with both an ICS and long-acting beta2-adrenergic agonist (LABA). Limitations of Use ADVAIR HFA is not indicated for the relief of acute bronchospasm.
Contraindications
ADVAIR HFA is contraindicated in the following conditions: •Primary treatment of status asthmaticus or other acute episodes of asthma where intensive measures are required [see Warnings and Precautions (5.2)]. •Hypersensitivity to any of the ingredients [see Warnings and Precautions (5.11), Adverse Reactions (6.2), Description (11)].
Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in the labeling: •Serious asthma-related events – hospitalizations, intubations, death [see Warnings and Precautions (5.1)] •Oropharyngeal candidiasis [see Warnings and Precautions (5.4)] •Pneumonia in patients with 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)] •Cardiovascular and central nervous system effects [see Warnings and Precautions (5.12)] •Reduction in bone mineral density [see Warnings and Precautions (5.13)] •Growth effects [see Warnings and Precautions (5.14)] •Glaucoma and cataracts [see Warnings and Precautions (5.15)]
Drug Interactions
ADVAIR HFA has been used concomitantly with other drugs, including short-acting beta2-agonists, methylxanthines, and nasal corticosteroids, commonly used in patients with asthma without adverse drug reactions [see Clinical Pharmacology (12.2)]. No formal drug interaction trials have been performed with ADVAIR HFA.
Mechanism of Action
ADVAIR HFA ADVAIR HFA contains both fluticasone propionate and salmeterol. The mechanisms of action described below for the individual components apply to ADVAIR HFA. These drugs represent 2 different classes of medications (a synthetic corticosteroid and a LABA) that have different effects on clinical, physiologic, and inflammatory indices of asthma. Fluticasone Propionate Fluticasone propionate is a synthetic trifluorinated corticosteroid with anti-inflammatory activity. Fluticasone propionate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor that is 18 times that of dexamethasone, almost twice that of beclomethasone-17-monopropionate (BMP), the active metabolite of beclomethasone dipropionate, and over 3 times that of budesonide. Data from the McKenzie vasoconstrictor assay in man are consistent with these results. The clinical significance of these findings is unknown. Inflammation is an important component in the pathogenesis of 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. These anti-inflammatory actions of corticosteroids contribute to their efficacy in asthma. Salmeterol Xinafoate Salmeterol is a selective LABA. In vitro studies show salmeterol to be at least 50 times more selective for beta2‑adrenoceptors than albuterol. Although beta2-adrenoceptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-adrenoceptors are the predominant receptors in the heart, there are also beta2-adrenoceptors in the human heart comprising 10% to 50% of the total beta-adrenoceptors. The precise function of these receptors has not been established, but their presence raises the possibility that even selective beta2-agonists may have cardiac effects. The pharmacologic effects of beta2-adrenoceptor a
Overdosage
No human overdosage data has been reported for ADVAIR HFA. ADVAIR HFA contains both fluticasone propionate and salmeterol; therefore, the risks associated with overdosage for the individual components described below apply to ADVAIR HFA. Treatment of overdosage consists of discontinuation of ADVAIR HFA 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 cases of overdosage. Fluticasone Propionate Chronic overdosage of fluticasone propionate may result in signs/symptoms of hypercorticism [see Warnings and Precautions (5.8)]. Salmeterol The expected signs and symptoms with overdosage of salmeterol 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). Overdosage with salmeterol can lead to clinically significant prolongation of the QTc interval, which can produce ventricular arrhythmias. As with all inhaled sympathomimetic medicines, cardiac arrest and even death may be associated with an overdose of salmeterol.