Arformoterol

Arformoterol tartrate inhalation solution is a long-acting beta 2 -adrenergic agonist (beta 2 -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 tartrate inhalation solution is not indicated to treat acute deteriorations of chronic obstructive pulmonary disease. Arformoterol tartrate inhalation solution is not indicated to treat asthma.

Arformoterol, the (R,R)-enantiomer of formoterol, is a selective long-acting beta 2 -adrenergic receptor agonist (beta 2 -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 beta 2 -agonist than the (R,R)-enantiomer. While it is recognized that beta 2 -receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta 1 -receptors are the predominant receptors in the heart, data indicate that there are also beta 2 -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 beta 2 -agonists may have cardiac effects.

The recommended dose of arformoterol tartrate inhalation solution is one 15 mcg unit-dose vial administered twice daily (morning and evening) by nebulization. A total daily dose of greater than 30 mcg (15 mcg twice daily) is not recommended. Arformoterol tartrate inhalation solution should be administered by the orally inhaled route via a standard jet nebulizer connected to an air compressor. Arformoterol tartrate inhalation solution should not be swallowed. Arformoterol tartrate inhalation solution should be stored refrigerated in foil pouches. After opening the pouch, unused unit-dose vials should be returned to, and stored in, the pouch. An opened unit-dose vial should be used right away. If the recommended maintenance treatment regimen fails to provide the usual response, medical advice should be sought immediately, as this is often a sign of destabilization of COPD.

Arformoterol tartrate inhalation solution is contraindicated in patients with a history of hypersensitivity to arformoterol, racemic formoterol or to any other components of this product. Use of a LABA, including arformoterol tartrate inhalation solution, without an inhaled cortisteroid is contraindicated in patients with asthma. Arformoterol tartrate inhalation solution is not indicated for the treatment of asthma. Use of a LABA, including arformoterol tartrate inhalation solution, without an inhaled corticosteroid is contraindicated in patients with asthma.

LABA as monotherapy (without an inhaled corticosteroid) for asthma increases the risk of serious asthma-related events. Do not initiate arformoterol tartrate inhalation solution 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 tartrate inhalation solution, 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 tartrate inhalation solution immediately. Use with caution in patients with cardiovascular or convulsive disorders, thyrotoxicosis, or with sensitivity to sympathomimetic drugs.

Long-acting beta 2 -adrenergic agonists, such as arformoterol tartrate, as monotherapy (without inhaled corticosteroids) for asthma increase the risk of asthma-related events. Arformoterol tartrate inhalation solution is not indicated for the treatment of asthma. 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.

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.

Store arformoterol tartrate inhalation solution in the protective foil pouch under refrigeration at 36° to 46°F (2° to 8°C). Unopened foil pouches of arformoterol tartrate inhalation solution can also be stored at room temperature 68° to 77°F (20° to 25°C) for up to 6 weeks. If stored at room temperature, discard if not used after 6 weeks or if past the expiration date, whichever is sooner. Protect from light and excessive heat. After opening the pouch, unused unit-dose vials should be returned to, and stored in, the pouch.