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Pronunciation
(leve al BYOO ter ole)
Generic Available (U.S.)
Yes: Excludes aerosol
Index Terms
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Treatment or prevention of bronchospasm in children and adults with reversible obstructive airway disease
Pregnancy Risk Factor
C
Pregnancy Considerations
Teratogenic effects were not observed in animal studies; however, racemic albuterol was teratogenic in some species. There are no adequate and well-controlled studies in pregnant women. This drug should be used during pregnancy only if benefit exceeds risk. Use caution if needed for bronchospasm during labor and delivery; has potential to interfere with uterine contractions.
Lactation
Excretion in breast milk unknown/use caution
Breast-Feeding Considerations
It is not known whether levalbuterol is excreted in human milk. Plasma levels following oral inhalation are low. Racemic albuterol was shown to be tumorigenic in animal studies.
Contraindications
Hypersensitivity to levalbuterol, albuterol, or any component of the formulation
Warnings/Precautions
Concerns related to adverse effects:
• Bronchospasm: Rarely, paradoxical bronchospasm may occur with use of inhaled bronchodilating agents; this should be distinguished from inadequate response.
• Hypersensitivity reactions: Immediate hypersensitivity reactions (urticaria, angioedema, rash, bronchospasm) have been reported.
Disease-related concerns:
• Asthma: Appropriate use: Optimize anti-inflammatory treatment before initiating maintenance treatment with levalbuterol. Do not use as a component of chronic therapy without an anti-inflammatory agent. Only the mildest form of asthma (Step 1 and/or exercise-induced) would not require concurrent use based upon asthma guidelines.
• Cardiovascular disease: Use with caution in patients with cardiovascular disease (arrhythmia or hypertension or HF); beta-agonists may cause elevation in blood pressure, heart rate and result in CNS stimulation/excitation. Beta2-agonists may also increase risk of arrhythmias.
• Diabetes: Use with caution in patients with diabetes mellitus; beta2-agonists may increase serum glucose.
• Glaucoma: Use with caution in patients with glaucoma; may elevate intraocular pressure.
• Hyperthyroidism: Use with caution in hyperthyroidism; may stimulate thyroid activity.
• Hypokalemia: Use with caution in patients with hypokalemia; beta2-agonists may decrease serum potassium.
• Seizures: Use with caution in patients with seizure disorders; beta-agonists may result in CNS stimulation/excitation.
Special populations:
• Pediatrics: Safety and efficacy have not been established in children <4 years of age.
Other warnings/precautions:
• Appropriate use: Do not exceed recommended dose; serious adverse events, including fatalities, have been associated with excessive use of inhaled sympathomimetics.
• Patient information: Patients must be instructed to seek medical attention in cases where acute symptoms are not relieved or a previous level of response is diminished. The need to increase frequency of use may indicate deterioration of asthma, and treatment must not be delayed. A spacer device or valved holding chamber is recommended when using a metered-dose inhaler.
Adverse Reactions
>10%:
Endocrine & metabolic: Serum glucose increased, serum potassium decreased
Neuromuscular & skeletal: Tremor (≤7%)
Respiratory: Rhinitis (3% to 11%)
Miscellaneous: Viral infection (7% to 12%)
>2% to 10%:
Central nervous system: Headache (8% to 12%), nervousness (3% to 10%), dizziness (1% to 3%), anxiety (≤3%), migraine (≤3%), weakness (3%)
Cardiovascular: Tachycardia (∼3%)
Dermatologic: Rash (≤8%)
Gastrointestinal: Diarrhea (2% to 6%), dyspepsia (1% to 3%)
Neuromuscular & skeletal: Leg cramps (≤3%)
Respiratory: Asthma (9%), pharyngitis (3% to 10%), cough (1% to 4%), sinusitis (1% to 4%), nasal edema (1% to 3%)
Miscellaneous: Flu-like syndrome (1% to 4%), accidental injury (≤3%)
<2%: Abnormal ECG, acne, anaphylaxis, angina, angioedema, arrhythmia, atrial fibrillation, chest pain, chills, constipation, conjunctivitis, cough, diaphoresis, dysmenorrhea, dyspnea, epistaxis, extrasystole, gastroenteritis, hematuria, hyper-/hypotension, hypoesthesia (hand), hypokalemia, insomnia, itching eyes, lymphadenopathy, myalgia, nausea, oropharyngeal dryness, paresthesia, supraventricular arrhythmia, syncope, vaginal moniliasis, vertigo, vomiting, wheezing, xerostomia
Note: Immediate hypersensitivity reactions have occurred (including angioedema, oropharyngeal edema, urticaria, and anaphylaxis).
Metabolism/Transport Effects
None known.
Drug Interactions
Alpha-/Beta-Blockers: May diminish the therapeutic effect of Beta2-Agonists. Risk D: Consider therapy modification
Atomoxetine: May enhance the tachycardic effect of Beta2-Agonists. Risk C: Monitor therapy
Beta-Blockers (Beta1 Selective): May diminish the bronchodilatory effect of Beta2-Agonists. Of particular concern with nonselective beta-blockers or higher doses of the beta1 selective beta-blockers. Risk C: Monitor therapy
Beta-Blockers (Nonselective): May diminish the bronchodilatory effect of Beta2-Agonists. Risk X: Avoid combination
Betahistine: May diminish the therapeutic effect of Beta2-Agonists. Risk C: Monitor therapy
Cannabinoids: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Risk X: Avoid combination
Loop Diuretics: Beta2-Agonists may enhance the hypokalemic effect of Loop Diuretics. Risk C: Monitor therapy
MAO Inhibitors: May enhance the adverse/toxic effect of Beta2-Agonists. Risk C: Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy
Thiazide Diuretics: Beta2-Agonists may enhance the hypokalemic effect of Thiazide Diuretics. Risk C: Monitor therapy
Tricyclic Antidepressants: May enhance the adverse/toxic effect of Beta2-Agonists. Risk C: Monitor therapy
Storage
Aerosol: Store at room temperature of 20°C to 25°C (68°F to 77°F); protect from freezing and direct sunlight. Store with mouthpiece down. Discard after 200 actuations.
Solution for nebulization: Store in protective foil pouch at room temperature of 20°C to 25°C (68°F to 77°F). Protect from light and excessive heat. Vials should be used within 2 weeks after opening protective pouch. Use within 1 week and protect from light if removed from pouch. Vials of concentrated solution should be used immediately after removing from protective pouch.
Reconstitution
Concentrated solution should be diluted with 2.5 mL NS prior to use.
Compatibility
Solution for nebulization: Compatible with budesonide suspension
Mechanism of Action
Relaxes bronchial smooth muscle by action on beta2-receptors with little effect on heart rate
Pharmacodynamics/Kinetics
Onset of action (as measured by a 15% increase in FEV1):
Aerosol: 5.5-10.2 minutes
Peak effect: ∼77 minutes
Nebulization: 10-17 minutes
Peak effect: 1.5 hours
Duration (as measured by a 15% increase in FEV1):
Aerosol: 3-4 hours (up to 6 hours in some patients)
Nebulization: 5-6 hours (up to 8 hours in some patients)
Absorption: A portion of inhaled dose is absorbed to systemic circulation
Half-life elimination: 3.3-4 hours
Time to peak, serum:
Aerosol: Children: 0.8 hours, Adults: 0.5 hours
Nebulization: Children: 0.3-0.6 hours, Adults: 0.2 hours
Dosage
Metered-dose inhaler (45 mcg/puff):
Children 5-11 years:
Bronchospasm, quick relief: 1-2 puffs every 4-6 hours as needed
Exacerbation of asthma (acute, severe) (NIH Guidelines, 2007): 4-8 puffs every 20 minutes for 3 doses, then every 1-4 hours as needed
Children ≥12 years and Adults:
Bronchospasm, quick relief: 1-2 puffs every 4-6 hours
Exacerbation of asthma (acute, severe) (NIH Guidelines, 2007): 4-8 puffs every 20 minutes for up to 4 hours, then every 1-4 hours as needed
Solution for nebulization:
Children: ≤4 years:
Bronchospasm, quick relief (NIH Guidelines, 2007): 0.31-1.25 mg every 4-6 hours as needed
Exacerbation of asthma (acute, severe) (NIH Guidelines, 2007): 0.075 mg/kg (minimum: 1.25 mg) every 20 minutes for 3 doses, then 0.075-0.15 mg/kg (maximum: 5 mg) every 1-4 hours as needed
Children 5-11 years:
Bronchospasm, quick relief: 0.31-0.63 mg every 8 hours as needed
Exacerbation of asthma (acute severe) (NIH Guidelines, 2007): 0.075 mg/kg (minimum: 1.25 mg) every 20 minutes for 3 doses, then 0.075-0.15 mg/kg (maximum: 5 mg) every 1-4 hours as needed
Children ≥12 years and Adults:
Bronchospasm, quick relief: 0.63-1.25 mg every 8 hours as needed
Exacerbation of asthma (acute, severe) (NIH Guidelines, 2007): 1.25-2.5 mg every 20 minutes for 3 doses, then 1.25-5 mg every 1-4 hours as needed
Elderly: Only a small number of patients have been studied. Although greater sensitivity of some elderly patients cannot be ruled out, no overall differences in safety or effectiveness were observed. An initial dose of 0.63 mg should be used in all patients >65 years of age.
Administration: Inhalation
Metered-dose inhaler: Shake well before use; prime with 4 test sprays prior to first use or if inhaler has not been use of more than 3 days. Clean actuator (mouthpiece) weekly. A spacer device or valved holding chamber is recommended when using a metered-dose inhaler.
Solution for nebulization: Safety and efficacy were established when administered with the following nebulizers: PARI LC Jet™, PARI LC Plus™, as well as the following compressors: PARI Master®, Dura-Neb® 2000, and Dura-Neb® 3000. Concentrated solution should be diluted prior to use. Blow-by administration is not recommended, use a mask device if patient unable to hold mouthpiece in mouth for administration.
Monitoring Parameters
Asthma symptoms; FEV1, peak flow, and/or other pulmonary function tests; heart rate, blood pressure, CNS stimulation; arterial blood gases (if condition warrants); serum potassium, serum glucose (in selected patients)
Patient Education
Stress or excessive exercising may exacerbate wheezing or bronchospasm. You may experience tremor, anxiety, dizziness, headache, upset stomach, nausea, or vomiting. Paradoxical bronchospasm can occur. Notify prescriber if any of the following occur: Chest pain, tightness, palpitations, severe headache, increased nervousness, restlessness, trembling, or muscle cramps. Report unusual signs of flu or infection, leg or muscle cramps, unusual cough, persistent GI problems, or vision changes.
Geriatric Considerations
For aerosol formulation, start with low end of dosage range. Refer to dosing information for nebulization dosing specifics.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause nervousness, anxiety, and dizziness; may rarely cause insomnia
Mental Health: Effects on Psychiatric Treatment
Effects of anxiolytics may be ameliorated; cardiac effects may be potentiated with MAO inhibitors and TCAs
Nursing: Physical Assessment/Monitoring
Teach patient safe use of nebulizer.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Aerosol, for oral inhalation, as tartrate [strength expressed as base]:
Xopenex HFA™: 45 mcg/actuation (15 g) [chlorofluorocarbon free; 200 actuations]
Solution, for nebulization, as hydrochloride [strength expressed as base, preservative free]:
Xopenex®: 0.31 mg/3 mL (24s); 0.63 mg/3 mL (24s); 1.25 mg/3 mL (24s)
Solution, for nebulization, as hydrochloride [strength expressed as base, concentrate, preservative free]: 1.25 mg/0.5 mL (30s)
Xopenex®: 1.25 mg/0.5 mL (30s [DSC])
Pricing: U.S. (www.drugstore.com)
Aerosol (Xopenex HFA)
45 mcg/ACT (15): $59.99
Nebulization (Xopenex)
0.31 mg/3 mL (72): $139.98
0.63 mg/3 mL (72): $148.23
1.25 mg/3 mL (72): $136.99
References
Expert Panel Report 3, “Guidelines for the Diagnosis and Management of Asthma,” Clinical Practice Guidelines, National Institutes of Health, National Heart, Lung, and Blood Institute, NIH Publication No. 08-4051, prepublication 2007. Available at http://www.nhlbi.nih.gov/guidelines/asthma/asthgdln.htm
International Brand Names
Lexi-Comp.com
Last full review/revision January 2012
Content last modified January 2012
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