Overview
11 DESCRIPTION Levalbuterol inhalation solution, USP (concentrate) is a sterile, clear, colorless, preservative-free solution of the hydrochloride salt of levalbuterol, the (R)-enantiomer of the drug substance racemic albuterol. Levalbuterol hydrochloride is a relatively selective beta 2 -adrenergic receptor agonist [see Clinical Pharmacology (12) ] .
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action 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 release of mediators from mast cells in the airway.
Indications
- 1 INDICATIONS AND USAGE Levalbuterol inhalation solution (concentrate) is indicated for the treatment or prevention of bronchospasm in adults, adolescents, and children 6 years of age and older with reversible obstructive airway disease. Levalbuterol inhalation solution (concentrate) is a beta 2 -adrenergic agonist indicated for: • Treatment or prevention of bronchospasm in adults, adolescents, and children 6 years of age and older with reversible obstructive airway disease. ( 1 )
Common Doses
- 1.25 mg
- 3 mL
- 0.31 mg
- 0.63 mg
Dosage
2 DOSAGE AND ADMINISTRATION Levalbuterol inhalation solution (concentrate) is for oral inhalation only. Dilute with sterile normal saline before administration. Administer by nebulization using with a standard jet nebulizer (with a face mask or mouthpiece) connected to an air compressor. Do not exceed recommended dose. For dosages less than 1.25 mg, the non-concentrate (i.e., levalbuterol inhalation solution, 3 mL) formulation must be used. Children 6 to 11 Years Old: The recommended dosage of levalbuterol inhalation solution for patients 6 to 11 years old is 0.
Contraindications
- 4 CONTRAINDICATIONS Levalbuterol inhalation solution is contraindicated in patients with a history of hypersensitivity to levalbuterol or racemic albuterol. Reactions have included urticaria, angioedema, rash, bronchospasm, anaphylaxis, and oropharyngeal edema [see Warnings and Precautions (5.6) ] . • Hypersensitivity to levalbuterol or racemic albuterol. ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following serious adverse reactions are described below and elsewhere in the labeling: • Paradoxical bronchospasm [see Warnings and Precautions (5.1) ] • Cardiovascular effects [see Warnings and Precautions (5.4) ] • Immediate hypersensitivity reactions [see Warnings and Precautions (5.6) ] • Hypokalemia [see Warnings and Precautions (5.8) ] Most common adverse reactions are: palpitations, chest pain, tachycardia, headache, dizziness, tremor and nervousness.
Interactions
- 7 DRUG INTERACTIONS • Other short-acting sympathomimetic aerosol bronchodilators and adrenergic drugs: May potentiate effect. ( 7.1 ) • Beta-blockers: May block bronchodilatory effects of beta-agonists and produce severe bronchospasm. Patients with asthma should not normally be treated with beta-blockers. ( 7.2 ) • Diuretic: May worsen electrocardiographic changes or hypokalemia associated with diuretic may worsen. Consider monitoring potassium levels. ( 7.3 ) • Digoxin: May decrease serum digoxin levels. Consider monitoring digoxin levels. ( 7.