Company:
Sepracor
Pharmacologic class:
Bronchodilator (long-acting beta2-agonist)
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Active ingredient:
Arformoterol 15 µg/2 mL; solution for inhalation
Indication:
Long-term maintenance treatment of bronchoconstriction due to chronic obstructive pulmonary disease (COPD)
Pharmacology:
Arformoterol is the (R,R) enantiomer of formoterol, a long-acting beta2 agonist.
It is twice as potent as the racemic mixture. Arformoterol is a bronchodilator that relaxes bronchial smooth muscle and inhibits the release of hypersensitivity mediators from mast cells.
Clinical trials:
Two 12-week trials involving a total of 1,456 patients were conducted to establish the safety and efficacy of arformoterol in the long-term treatment of COPD. Both studies compared three doses of arformoterol (15 µg twice daily, 25 µg twice daily, and 50 µg once daily) to placebo and included the use of salmeterol aerosol 42 µg twice daily as a comparator.
In both studies, the use of arformoterol 15 µg twice daily resulted in significantly greater post-dose bronchodilation compared with placebo.
This effect was maintained over 12 weeks. Use of the higher doses of arformoterol did not result in sufficient additional benefit on several end points (including FEV1). After the first 15-µg dose of arformoterol, the median time to onset of bronchodilation (FEV1 increased by 15%) occurred at 6.7 minutes, and peak bronchodilator effect was usually seen within one to three hours after dosing. Patients treated with arformoterol showed improvements in peak expiratory flow rates and supplemental use of ipratropium and rescue albuterol use, compared to placebo. Tolerance to the bronchodilator effect was seen after six weeks of dosing, as shown by a decrease by about one third in bronchodilator effect measured by FEV1.
Adults:
By nebulizer: 15 µg by inhalation twice daily (am and pm). Use standard jet (e.g., PARI LC PLUS) nebulizer with air compressor (e.g., PARI DURANEB 3000). Re-evaluate periodically.
Children:
Not recommended.
Contraindications:
Not for treatment of acute attacks. Do not initiate in significantly or acutely deteriorating COPD. Concomitant other long-acting beta2 agonists.
Precautions:
Do not exceed recommended dose. Cardiovascular disease (esp. coronary insufficiency, arrhythmias, hypertension). Convulsive disorders. Hepatic impairment. Hyperthyroidism. Hypokalemia.
Hyperresponsiveness to sympathomimetics. Diabetes. Ketoacidosis. Monitor potassium. Prescribe a short-acting beta2 agonist for acute symptoms; monitor for increased need. Pregnancy (Cat. C). Labor & delivery. Nursing mothers.
Interactions:
See Contraindications. Avoid other sympathomimetics (except short-acting bronchodilators). Avoid use during or within two weeks of MAOIs, tricyclics, others that prolong QTc interval. Antagonized by beta blockers. K+-depleting diuretics, theophylline, aminophylline, steroids may potentiate hypokalemia.
Adverse reactions:
Asthenia, fever, bronchitis, headache, GI upset, serum K+ changes, leukocytosis, nervousness, pain, tremor, flu syndrome; cardiovascular effects (e.g., increased pulse rate or BP; consider discontinuing if occurs); rarely: paradoxical bronchospasm, hypersensitivity reactions; increased risk of asthma-related death.
How supplied:
Vials (2 mL)—30.
For more information, call 800.739.0565 or visit www.Brovana.com
