Fluticasone/Salmeterol (Inhaler)

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

[edit] MECHANISM OF ACTION

  • Fluticasone is an inhaled potent glucocorticoid, it works in the air passages of the lungs by reducing inflammation and keeping the airways open, making it easier to breathe. Glucocorticoids have multiple antiinflammatory effects, inhibiting both inflammatory cells and release of inflammatory mediators.
  • Salmeterol is a long acting Beta2 agonist (lasting for approximately 12 hours) with a slow onset of action; The onset of effective bronchodilation occurs within 10 to 30 minutes and peak effect occurs between 3 to 4 hours. Beta2 receptors are the predominant adrenergic receptors in bronchial smooth muscle. The binding of Formoterol to Beta2 adrenergic receptors in bronchial smooth muscle, activates the intracellular adenylate cyclase, an enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). The increase of cAMP determines:
    • Bronchodilation: Increased intracellular cyclic AMP (cAMP) increases the activation of cAMP-dependent protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular calcium levels within the muscle. Lower levels of calcium cause relaxation of the smooth muscle and therefore bronchodilatation.
    • Inhibition of the release of mast cell mediators

[edit] INDICATIONS

  • Treatment of asthma in patients aged 4 years and older.
  • Maintenance treatment of airflow obstruction and reducing exacerbations in patients with chronic obstructive pulmonary disease (COPD)

Fluticasone/Salmeterol combination is not indicated for the relief of acute bronchospasm

[edit] DOSAGE

  • ASTHMA:
    • Adults and children over 12 years: one inhalation of 50/100, 50/250 or 50/500 micrograms of salmeterol/fluticasone twice daily, based on asthma severity
    • Children 4 years and over: one inhalation of 50/100 micrograms of salmeterol/fluticasone twice daily.
  • Maintenance treatment of COPD: 1 inhalation of 50/250 mcg twice daily

[edit] DOSAGE FORMS AND STRENGTHS

  • DISKUS device 50/100 micrograms of salmeterol/fluticasone respectively
  • DISKUS device 50/250 micrograms of salmeterol/fluticasone respectively
  • DISKUS device 50/500 micrograms of salmeterol/fluticasone respectively

[edit] CONTRAINDICATIONS

  • Acute episodes of asthma or COPD requiring intensive measures
  • Patients with severe milk protein allergy (Anaphylactic reactions have been reported)

[edit] PRECAUTIONS AND WARNINGS

  • Long-acting beta2-adrenergic agonists (LABAs), such as Salmeterol, increase the risk of asthma-related death. They increase also the risk of asthma-related hospitalization in pediatric and adolescent patients. therefore therapy with Fluticasone/Salmeterol combination should be limited for patients not adequately controlled on a long-term asthma control medication, such as an inhaled corticosteroid, or whose disease severity clearly warrants initiation of treatment with both an inhaled corticosteroid and a LABA. Once asthma control is achieved and maintained, assess the patient at regular intervals and step down therapy (discontinue Fluticasone/Salmeterol combination) if possible without loss of asthma control and maintain the patient on a long-term asthma control medication, such as an inhaled corticosteroid. Do not use Fluticasone/Salmeterol combination for patients whose asthma is adequately controlled on low- or medium-dose inhaled corticosteroids.
  • Deterioration of Disease and Acute Episodes: Fluticasone/Salmeterol combination should not be initiated in patients during rapidly deteriorating or potentially life-threatening episodes of asthma or COPD. An inhaled, short-acting beta2-agonist (e.g. Salbutamol), should be used to relieve acute symptoms such as shortness of breath.
  • Use with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension.
  • Candida albicans infection of the mouth and pharynx. Monitor patients periodically for signs of adverse effects in the mouth and pharynx. Advise patients to rinse mouth after inhalation.
  • Potential worsening of existing tuberculosis; fungal, bacterial, viral, or parasitic infection; or ocular herpes simplex. More serious or even fatal course of chickenpox or measles in susceptible patients. Use caution in patients with the above because of the potential for worsening of these infections
  • Decreases in bone mineral density (BMD) have been observed with long-term administration of products containing inhaled corticosteroids
  • Glaucoma, increased intraocular pressure, and cataracts have been reported following the long-term administration of inhaled corticosteroids.
  • Orally inhaled corticosteroids may cause a reduction in growth velocity when administered to pediatric patients. Monitor the growth of pediatric patients
  • Paradoxical bronchospasm may occur. Treat bronchospasm immediately with a fast-acting inhaled bronchodilator (Salbutamol) and discontinue Fluticasone/Salmeterol (Inhaler).
  • Metabolic effects: Be alert to eosinophilic conditions, hypokalemia, and hyperglycemia.
  • Coexisting conditions: Use with caution in patients with convulsive disorders, thyrotoxicosis, diabetes mellitus, and ketoacidosis

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US), Fluticasone/Salmeterol combination should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Since there are no data from controlled trials on the use of Fluticasone/Salmeterol combination by nursing mothers, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account its importance to the mother.

[edit] SIDE EFFECTS

Most common adverse reactions are :

  • Risk of development of localized infections in the mouth and pharynx with Candida albicans (rinse the mouth after inhalation)
  • Dysphonia
  • Bronchitis
  • Cough
  • headaches
  • Nausea and vomiting
  • Possible development of pneumonia in patients with COPD inhaling corticosteroids, including fluticasone.

Fluticasone/Salmeterol combination can also produce paradoxical bronchospasm, which may be life threatening. If paradoxical bronchospasm occurs, it should be treated immediately with an inhaled, short-acting bronchodilator (Salbutamol).

For more serious side effects see Precautions and warnings

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

GSK US ADVAIR PRESCRIBING INFORMATION

[edit] REFERENCES

Asthma / Chronic obstructive pulmonary disease (COPD)
Adrenergics, inhalants Short acting β2-agonists Fenoterol (Berotec)   Levosalbutamol (Xopenex)   Salbutamol (Ventolin)   Terbutaline (Bricanyl)
Long acting β2-agonists (LABA) Arformoterol (Brovana)   Clenbuterol (Spiropent)   Formoterol (Foradil)   Salmeterol (Serevent)
Ultra long acting β2-agonists Indacaterol   Olodaterol   Vilanterol
Inhaled corticosteroids Beclomethasone (Inhaler)   Budesonide (Inhaler)   Ciclesonide (Inhaler)   Flunisolide (Inhalation suspension)   Fluticasone (Inhaler)   Mometasone (Inhaler)
Anticholinergics (Muscarinic antagonists) Aclidinium bromide   Glycopyrronium bromide   Ipratropium bromide   Oxitropium bromide (Inhalation suspension)   Tiotropium bromide
Mast cell stabilizers Cromoglicate   Nedocromil
Monoclonal anti-IgE antibody Omalizumab
Xanthine derivatives Aminophylline   Bamifylline   Doxofylline   Dyphylline   Theophylline
Eicosanoid inhibition Leukotriene antagonists Montelukast   Pranlukast   Zafirlukast
Thromboxane receptor antagonists Ramatroban   Seratrodast
Non-xanthine PDE4 inhibitors Ibudilast   Roflumilast
Combination products Corticosteroid + Long acting Beta2 agonist Beclomethasone/Formoterol (Inhaler)   Fluticasone/Salmeterol (Inhaler)   Fluticasone/Vilanterol   Mometasone/Formoterol
Corticosteroid + Short acting Beta2 agonist Beclomethasone/Salbutamol   Salbutamol/Flunisolide (Inhalation suspension)   Salbutamol/Flunisolide (Inhaler)
Short acting Beta2 agonist + Muscarinic antagonist Fenoterol/Ipratropium bromide (Inhaler)   Levosalbutamol/Ipratropium   Salbutamol/Ipratropium bromide