Salmeterol

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Salmeterol is a long-acting bronchodilator. It helps the airways in the lungs to stay open. This makes it easier for air to get in and out. The effects are usually felt within 10 to 20 minutes and last for 12 hours or more.

Salmeterol is used to help prevent breathing problems. These could be caused by asthma, asthma brought on by exercise or at night and by Chronic Obstructive Pulmonary Disease (COPD).

Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Salmeterol.jpg

[edit] MECHANISM OF ACTION

Salmeterol is a long-acting β2 adrenergic receptor agonist.

β2 receptors are the predominant adrenergic receptors in bronchial smooth muscle. The binding of Salmeterol to β2 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 (such as histamine, leukotrienes, and prostaglandin D2)
  • Increased mucociliary clearance

The duration of action of Salmeterol lasts approximately 12 hours VS 4-6 hours for salbutamol

[edit] INDICATIONS

  • Treatment of asthma, in addition to concomitant treatment with an inhaled corticosteroid, in patients aged 4 years and older. (when asthma is inadequately controlled on inhaled corticosteroid alone)
  • Prevention of exercise-induced bronchospasm in patients aged 4 years and older.
  • Maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD)

Salmeterol is not indicated for the relief of acute bronchospasm

[edit] DOSAGE

  • Asthma: Adults and children 4 years of age and older, 1 inhalation (50 mcg) twice daily.
  • To prevent exercise-induced bronchospasm: Adults and children 4 years of age and older, one inhalation (50 mcg) at least 30 minutes before exercise.
  • Maintenance treatment of bronchospasm associated with COPD: 1 inhalation (50 mcg) twice daily

[edit] DOSAGE FORMS AND STRENGTHS

  • DISKUS device containing salmeterol (50 mcg) as an oral inhalation powder

[edit] CONTRAINDICATIONS

  • Primary treatment of status asthmaticus or acute episodes of asthma or COPD requiring intensive measures
  • Salmeterol is contraindicated for treatment of asthma without concomitant use of a long-term asthma control medication, such as an inhaled corticosteroid.

[edit] WARNINGS AND PRECAUTIONS

  • Use with caution in patients with underlying cardiovascular disorders.(Monitor heart rate)
  • Paradoxical bronchospasm may occur and should be treated immediately with alternative therapy
  • Patients with asthma must take a concomitant inhaled corticosteroid
  • Do not use to treat acute symptoms
  • Long-acting beta2-adrenergic agonists increase the risk of Asthma-related death and asthma-related hospitalizations

[edit] INTERACTIONS

  • Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, saquinavir, telithromycin) are potent inhibitors of Salmeterol metabolism in liver, therefore, the amount of salmeterol in the blood may increase and cause increased risk of cardiovascular adverse events. Concomitant use of Salmeterol with strong CYP3A4 inhibitors is not recommended.
  • Beta blockers: Beta blockers (medications used to slow down the heart beat), especially nonselective ones may block bronchodilatory effects of beta-agonists and produce severe bronchospasm. Patients with asthma should not normally be treated with beta blockers.
  • Nonpotassium-sparing diuretics: As with other beta-agonists, Salmeterol may produce significant hypokalemia in some patients. Co-administration of nonpotassium-sparing diuretics (such as loop diuretics or thiazide diuretics) which cause hypokalemia as a side effect, may worsen hypokalemia . Consider monitoring potassium levels

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US), Salmeterol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • In nursing mothers, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother

[edit] SIDE EFFECTS

The most common adverse reactions are: Headache, influenza, nasal congestion, pharyngitis, rhinitis, bronchitis, cough, musculoskeletal pain

  • Serious adverse effects: Paradoxical bronchospasm, arrhythmia and anaphylactic reaction in patients with severe milk protein allergy (Rare)

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

http://us.gsk.com/products/assets/us_serevent_diskus.pdf

[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