Formoterol (Inhaler)

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[edit] BRAND NAMES

[edit] STRUCTURE

Formoterol.jpg

[edit] MECHANISM OF ACTION

Formoterol is a long-acting β2 adrenergic receptor agonist.

β2 receptors are the predominant adrenergic receptors in bronchial smooth muscle. The binding of Formoterol 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)

Following inhalation, a significant improvement in pulmonary function is well established after few minutes and effect should last for 12 hours.

[edit] INDICATIONS

FDA approved:

  • Treatment of asthma, in addition to concomitant treatment with an inhaled corticosteroid, in patients aged 5 years and older. (when asthma is inadequately controlled on inhaled corticosteroid alone)
  • Prevention of exercise-induced bronchospasm in patients aged 5 years and older.
  • Maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD)

[edit] DOSAGE

  • Asthma: Adults and children 5 years of age and older, 12 mcg twice daily.
    In adults, the maximum recommended daily dose is 48 mcg and in children, the maximum recommended daily dose is 24 mcg.
  • To prevent exercise-induced bronchospasm: Adults and children 5 years of age and older, 12 mcg at least 15 minutes before exercise. Additional doses should not be used for 12 hours.
  • Maintenance treatment of bronchospasm associated with COPD: 12 mcg twice daily

[edit] DOSAGE FORMS AND STRENGTHS

  • Capsules for oral inhalation: 12 mcg formoterol, for use with Aerolizerinhaler
  • Turbohaler: 6 mcg/Metered dose, 12 μg/Metered dose

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Formoterol
  • Primary treatment of status asthmaticus or acute episodes of asthma or COPD requiring intensive measures
  • Formoterol 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), diabetes, hypertension, hyperthyroidism, and a history of seizures.
  • Paradoxical bronchospasm may occur and should be treated immediately with alternative therapy
  • Do not use to treat acute symptoms
  • Long-acting beta2-adrenergic agonists increase the risk of Asthma-related death and asthma-related hospitalizations. Patients with asthma must take a concomitant inhaled corticosteroid and should not use Formoterol if asthma is adequately controlled on low or medium dose inhaled corticosteroids.
  • Formoterol is not a substitute for corticosteroids. Corticosteroids should not be stopped or reduced when Formoterol is initiated

[edit] INTERACTIONS

  • 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, Formoterol 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
  • MAO inhibitors, tricyclic antidepressants, macrolides, and drugs that prolong QTc interval: Use with extreme caution. May potentiate effect on cardiovascular system
  • Halogenated hydrocarbons: There is an elevated risk of arrhythmias in patients receiving concomitant anesthesia with halogenated hydrocarbons (halothane, chloroform, enflurane, trichloroethylene, isoflurane, desflurane, sevoflurane)

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Animal reproduction studies of formoterol in rats and rabbits revealed evidence of teratogenicity as well as other developmental toxic effects. There are no adequate and well-controlled studies in pregnant women, Formoterol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • In reproductive studies in rats, formoterol was excreted in the milk. It is not known whether formoterol is excreted in human milk, but because many drugs are excreted in human milk, caution should be exercised if formoterol is administered to nursing women.

[edit] SIDE EFFECTS

The major adverse effects of inhaled beta2-agonists occur as a result of excessive activation of the systemic beta-adrenergic receptors. The most common adverse effects in adults and adolescents include skeletal muscle tremor and cramps, insomnia, headache, tachycardia, decreases in plasma potassium, and increases in plasma glucose.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[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