Arformoterol (Inhalation suspension)

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[edit] BRAND NAMES

[edit] STRUCTURE

Arformoterol.jpg

[edit] MECHANISM OF ACTION

Arformoterol, the (R,R)-enantiomer of formoterol, is a selective long-acting beta2-adrenergic receptor agonist (beta2-agonist) that has two-fold greater potency than racemic formoterol (which contains both the (S,S) and (R,R)-enantiomers).

The (S,S)-enantiomer is about 1,000-fold less potent as a beta2-agonist than the (R,R)-enantiomer. While it is recognized that beta2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-receptors are the predominant receptors in the heart, data indicate that there are also beta2-receptors in the human heart comprising 10% to 50% of the total beta-adrenergic receptors.

The precise function of these receptors has not been established, but they raise the possibility that even highly selective beta2-agonists may have cardiac effects.

The pharmacologic effects of beta2-adrenoceptor agonist drugs, including arformoterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cyclic AMP). Increased intracellular cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.

In vitro tests show that arformoterol is an inhibitor of the release of mast cell mediators, such as histamine and leukotrienes, from the human lung. Arformoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-responsiveness. The relevance of these in vitro and animal findings to humans is unknown.

[edit] INDICATIONS

Arformoterol (Inhalation suspension) is a long-acting beta2-adrenergic agonist (beta2-agonist) indicated for:

  • Long-term, twice daily (morning and evening) administration in the maintenance treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema.


Important limitations of use:

  • Arformoterol (Inhalation suspension) is not indicated to treat acute deteriorations of chronic obstructive pulmonary disease.
  • Arformoterol (Inhalation suspension) is not indicated to treat asthma.

[edit] DOSAGE

For oral inhalation only.

  • A total daily dose of greater than 30 mcg is not recommended.
  • One 15 mcg/2 mL vial every 12 hours.
  • For use with a standard jet nebulizer (with a face mask or mouthpiece) connected to an air compressor.

[edit] CONTRAINDICATIONS

Arformoterol (Inhalation suspension) is contraindicated in patients with a history of hypersensitivity to arformoterol, racemic formoterol or to any other components of this product.

All LABA, including Arformoterol (Inhalation suspension), are contraindicated in patients with asthma without use of a long-term asthma control medication.

[edit] WARNINGS AND PRECAUTIONS

  • Do not initiate Arformoterol (Inhalation suspension) in acutely deteriorating patients.
  • Do not use for relief of acute symptoms. Concomitant short-acting beta2-agonists can be used as needed for acute relief.
  • Do not exceed the recommended dose. Excessive use of Arformoterol (Inhalation suspension), or use in conjunction with other medications containing long-acting beta2-agonists, can result in clinically significant cardiovascular effects, and may be fatal.
  • Life-threatening paradoxical bronchospasm can occur. Discontinue Arformoterol (Inhalation suspension) immediately. (5.4)
  • Use with caution in patients with cardiovascular or convulsive disorders, thyrotoxicosis, or with sensitivity to sympathomimetic drugs.

[edit] INTERACTIONS

  • Other adrenergic drugs may potentiate effect. Use with caution.
  • Xanthine derivatives, steroids, diuretics, or non-potassium sparing diuretics may potentiate hypokalemia or ECG changes. Use with caution.
  • MAO inhibitors, tricyclic antidepressants and drugs that prolong the QTc interval may potentiate effect on the cardiovascular system. Use with extreme caution.
  • Beta-blockers may decrease effectiveness. May block bronchodilatory effects of beta-agonists. Use with caution and only when medically necessary.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). There are no adequate and well-controlled studies of Arformoterol (Inhalation suspension) in pregnant women. Arformoterol has been shown to be teratogenic in rats and rabbits. Arformoterol also caused neonatal mortality and developmental delays in rats. Because animal reproduction studies are not always predictive of human response, Arformoterol (Inhalation suspension) should be used during pregnancy, only if the potential benefit justifies the potential risk to the fetus.
  • Nursing Mothers: In reproductive studies in rats, arformoterol was excreted in the milk. It is not known whether arformoterol is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Arformoterol (Inhalation suspension) is administered to a nursing woman.

[edit] SIDE EFFECTS

Most common adverse reactions (≥2% incidence and more common than placebo) are pain, chest pain, back pain, diarrhea, sinusitis, leg cramps, dyspnea, rash, flu syndrome, peripheral edema and lung disorder.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

http://www.respistory.com/c/brovana-approved-labeling-text.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