(leve al BYOO ter ole)
- Levalbuterol Hydrochloride
- Levalbuterol Tartrate
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Aerosol, Inhalation, as tartrate [strength expressed as base]:
Xopenex HFA: 45 mcg/actuation (15 g)
Nebulization Solution, Inhalation, as hydrochloride [strength expressed as base]:
Xopenex: 0.63 mg/3 mL (3 mL [DSC]); 1.25 mg/3 mL (3 mL [DSC])
Generic: 0.63 mg/3 mL (3 mL)
Nebulization Solution, Inhalation, as hydrochloride [strength expressed as base, preservative free]:
Xopenex: 0.31 mg/3 mL (3 mL); 0.63 mg/3 mL (3 mL); 1.25 mg/3 mL (3 mL)
Xopenex Concentrate: 1.25 mg/0.5 mL (1 ea, 30 ea)
Generic: 0.31 mg/3 mL (3 mL); 0.63 mg/3 mL (3 mL); 1.25 mg/3 mL (3 mL); 1.25 mg/0.5 mL (1 ea, 30 ea)
Brand Names: U.S.
- Xopenex Concentrate
- Xopenex HFA
- Beta2 Agonist
Relaxes bronchial smooth muscle by action on beta2-receptors with little effect on heart rate
A portion of inhaled dose is absorbed to systemic circulation
Vd: Adults: 1,900 L
Hepatic to an inactive sulfate
3% to 6% excreted unchanged in urine
Onset of Action
Measured as a 15% increase in FEV1:
Aerosol: 5.5 to 10.2 minutes; Peak effect: ~77 minutes
Nebulization: 10 to 17 minutes; Peak effect: 1.5 hours
Time to Peak
Aerosol: Children: 0.8 hours, Adults: 0.5 hours
Nebulization: Children: 0.3 to 0.6 hours, Adults: 0.2 hours
Duration of Action
Measured as a 15% increase in FEV1:
Aerosol: 3 to 4 hours (up to 6 hours in some patients)
Nebulization: 5 to 6 hours (up to 8 hours in some patients)
3.3 to 4 hours
Special Populations: Children
AUC values were about 1.5-fold greater than adults.
Use: Labeled Indications
Bronchospasm: Treatment or prevention of bronchospasm in patients with reversible obstructive airway disease
Hypersensitivity to levalbuterol, albuterol, or any component of the formulation
Children ≥4 years, Adolescents, and Adults: 2 inhalations (90 mcg) every 4 to 6 hours as needed; in some patients, 1 inhalation (45 mcg) every 4 hours may be sufficient (maximum: 2 inhalations every 4 hours).
Elderly: Refer to adult dosing, starting with lowest dose; titrate cautiously
Solution for nebulization:
Asthma Guidelines (off-label; NAEPP, 2007):
Children ≤4 years: 0.31 to 1.25 mg every 4 to 6 hours as needed
Children 5 to 11 years: 0.31 to 0.63 mg every 8 hours as needed
Children 6 to 11 years: 0.31 mg 3 times daily (maximum: 0.63 mg 3 times daily)
Children ≥12 years, Adolescents, and Adults: Initial: 0.63 mg 3 times daily at intervals of 6 to 8 hours; dosage may be increased to 1.25 mg 3 times daily with close monitoring for adverse effects (maximum: 1.25 mg 3 times daily)
Elderly: Refer to adult dosing, starting with lowest dose; titrate cautiously.
Exacerbation of asthma (acute, severe) (off-label; NAEPP, 2007):
Children <12 years: 4 to 8 inhalations every 20 minutes for 3 doses, then every 1 to 4 hours as needed
Children ≥12 years, Adolescents, and Adults: 4 to 8 inhalations every 20 minutes for up to 4 hours, then every 1 to 4 hours as needed
Solution for nebulization:
Children <12 years: 0.075 mg/kg (minimum: 1.25 mg) every 20 minutes for 3 doses, then 0.075 to 0.15 mg/kg (maximum: 5 mg) every 1 to 4 hours as needed
Children ≥12 years, Adolescents, and Adults: 1.25 to 2.5 mg every 20 minutes for 3 doses, then 1.25 to 5 mg every 1 to 4 hours as needed
Dosage adjustment in renal impairment: There are no dosage adjustments provided in the manufacturer’s labeling. Use with caution.
Dosage adjustment in hepatic impairment: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).
Concentrated solution should be diluted with 2.5 mL NS prior to use.
Metered-dose inhaler: Shake well before use, avoid spraying in the eyes; prime with 4 test sprays prior to first use or if inhaler has not been used for 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.
Solution for nebulization: Compatible with budesonide suspension (NIH, 2007)
Aerosol: Store at 20°C to 25°C (68°F to 77°F); protect from freezing and direct sunlight. Store with mouthpiece down. Discard after 200 actuations (15 g canister) or 80 actuations (8.4 g canister). Do not puncture or incinerate.
Solution for nebulization: Store in protective foil pouch at 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.
AtoMOXetine: May enhance the tachycardic effect of Beta2-Agonists. Monitor therapy
AtoMOXetine: May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Atosiban: Beta2-Agonists may enhance the adverse/toxic effect of Atosiban. Specifically, there may be an increased risk for pulmonary edema and/or dyspnea. 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. Monitor therapy
Beta-Blockers (Nonselective): May diminish the bronchodilatory effect of Beta2-Agonists. Avoid combination
Betahistine: May diminish the therapeutic effect of Beta2-Agonists. Monitor therapy
Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. Monitor therapy
Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Monitor therapy
Highest Risk QTc-Prolonging Agents: QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying) may enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Management: Avoid such combinations when possible. Use should be accompanied by close monitoring for evidence of QT prolongation or other alterations of cardiac rhythm. Consider therapy modification
Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Avoid combination
Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in patients receiving linezolid. Specific dose adjustment recommendations are not presently available. Consider therapy modification
Loop Diuretics: Beta2-Agonists may enhance the hypokalemic effect of Loop Diuretics. Monitor therapy
Loxapine: Agents to Treat Airway Disease may enhance the adverse/toxic effect of Loxapine. More specifically, the use of Agents to Treat Airway Disease is likely a marker of patients who are likely at a greater risk for experiencing significant bronchospasm from use of inhaled loxapine. Management: This is specific to the Adasuve brand of loxapine, which is an inhaled formulation. This does not apply to non-inhaled formulations of loxapine. Avoid combination
MAO Inhibitors: May enhance the adverse/toxic effect of Beta2-Agonists. Monitor therapy
Mifepristone: May enhance the QTc-prolonging effect of QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying). Management: Though the drugs listed here have uncertain QT-prolonging effects, they all have some possible association with QT prolongation and should generally be avoided when possible. Consider therapy modification
Moderate Risk QTc-Prolonging Agents: QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying) may enhance the QTc-prolonging effect of Moderate Risk QTc-Prolonging Agents. Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Thiazide Diuretics: Beta2-Agonists may enhance the hypokalemic effect of Thiazide Diuretics. Monitor therapy
Tricyclic Antidepressants: May enhance the adverse/toxic effect of Beta2-Agonists. Monitor therapy
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% (Limited to important or life-threatening): Abnormal ECG, acne, anaphylaxis, angina, angioedema, arrhythmia, atrial fibrillation, chest pain, dysmenorrhea, epistaxis, extrasystole, gastroenteritis, gastroesophageal reflux disease, hematuria, hypertension, hypoesthesia (hand), hypokalemia, lymphadenopathy, metabolic acidosis, myalgia, nausea, oropharyngeal dryness, paresthesia, supraventricular arrhythmia, syncope, vaginal moniliasis
Note: Immediate hypersensitivity reactions have occurred (including angioedema, oropharyngeal edema, urticaria, and anaphylaxis).
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, anaphylaxis, oropharyngeal edema) have been reported.
• 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 (NAEPP, 2007). If patients need more doses than usual, this may be a sign of asthma destabilization; patient should be reevaluated.
• 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; beta2-agonists 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.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
• 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.
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)
Pregnancy Risk Factor
Adverse events were not observed in animal reproduction studies. Congenital anomalies (cleft palate, limb defects) have rarely been reported following maternal use of racemic albuterol during pregnancy. Multiple medications were used in most cases, no specific pattern of defects has been reported, and no relationship to racemic albuterol has been established. Beta-agonists may interfere with uterine contractility if administered during labor.
Uncontrolled asthma is associated with adverse events on pregnancy (increased risk of perinatal mortality, pre-eclampsia, preterm birth, low birth weight infants). Other beta2-receptor agonists are currently preferred for the treatment of asthma during pregnancy (NAEPP, 2005).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience rhinorrhea, emesis, tremors, or pharyngitis. Have patient report immediately to prescriber signs of hypokalemia, angina, tachycardia, severe dizziness, syncope, significant anxiety, intolerable headache, or considerable dyspnea (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.