Levalbuterol

XOPENEX HFA is a beta 2 -adrenergic agonist indicated for the treatment or prevention of bronchospasm in patients 4 years of age and older with reversible obstructive airway disease.

Activation of beta 2 -adrenergic receptors on airway smooth muscle leads to the activation of adenylate cyclase and to an increase in the intracellular concentration of cyclic-3', 5'-adenosine monophosphate (cyclic AMP). The increase in cyclic AMP is associated with the activation of protein kinase A, which in turn, inhibits the phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in muscle relaxation. Levalbuterol relaxes the smooth muscles of all airways, from the trachea to the terminal bronchioles. Increased cyclic AMP concentrations are also associated with the inhibition of the release of mediators from mast cells in the airways. Levalbuterol acts as a functional antagonist to relax the airway irrespective of the spasmogen involved, thus protecting against all bronchoconstrictor challenges.

For Oral Inhalation Only. Adults and children 4 years of age and older: 2 inhalations repeated every 4 to 6 hours, in some patients, 1 inhalation every 4 hours may be sufficient. Prime XOPENEX HFA before using for the first time and when the inhaler has not been used for more than 3 days. To prime XOPENEX HFA, release 4 sprays into the air away from the face. At least once a week, wash the actuator with warm water and let it air-dry completely.

XOPENEX HFA is contraindicated in patients with a history of hypersensitivity to levalbuterol, racemic albuterol, or any other component of XOPENEX HFA. Reactions have included urticaria, angioedema, rash, bronchospasm, anaphylaxis, and oropharyngeal edema. Hypersensitivity to levalbuterol, racemic albuterol or any other component of XOPENEX HFA Inhalation Aerosol.

Life-threatening paradoxical bronchospasm may occur. Discontinue XOPENEX HFA immediately and treat with alternative therapy. Need for more doses of XOPENEX HFA than usual may be a sign of deterioration of asthma and requires reevaluation of treatment. XOPENEX HFA is not a substitute for corticosteroids. Cardiovascular effects may occur. Consider discontinuation of XOPENEX HFA if these effects occur. Use with caution in patients with underlying cardiovascular disorders. Excessive use may be fatal. Do not exceed recommended dose. Immediate hypersensitivity reactions may occur. Discontinue XOPENEX HFA immediately. Hypokalemia and changes in blood glucose may occur.

Use of XOPENEX HFA may be associated with the following: Paradoxical bronchospasm Cardiovascular effects Immediate hypersensitivity reactions Hypokalemia Most common adverse reactions (≥ 2% and > placebo) are accidental injury, bronchitis, dizziness, pain, pharyngitis, rhinitis, and vomiting.

Other short-acting sympathomimetic aerosol bronchodilators or epinephrine should not be used concomitantly with XOPENEX HFA. If additional adrenergic drugs are to be administered by any route, they should be used with caution to avoid deleterious cardiovascular effects. Other short-acting sympathomimetic aerosol bronchodilators and adrenergic drugs: May potentiate effect. Beta-blockers: May block bronchodilatory effects of beta-agonists and produce severe bronchospasm. Patients with asthma should not normally be treated with beta-blockers. Diuretics: May worsen electrocardiographic changes or hypokalemia associated with diuretics may worsen. Consider monitoring potassium levels. Digoxin: May decrease serum digoxin levels. Consider monitoring digoxin levels. Monoamine oxidase inhibitors (MAOs) or tricyclic antidepressants: May potentiate effect of albuterol on the cardiovascular system.

Store between 20° and 25°C (68° and 77°F, see USP controlled room temperature). Protect from freezing temperatures and direct sunlight. Exposure to temperatures above 120°F may cause bursting. Store inhaler with the actuator mouthpiece down. Do not store near heat or open flame.