Skip to Content

Levalbuterol

Pronunciation

Pronunciation

(leve al BYOO ter ole)

Index Terms

  • Levalbuterol Hydrochloride
  • Levalbuterol Tartrate
  • Levosalbutamol
  • R-albuterol

Dosage Forms

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
  • Xopenex Concentrate
  • Xopenex HFA

Pharmacologic Category

  • Beta2 Agonist

Pharmacology

Relaxes bronchial smooth muscle by action on beta2-receptors with little effect on heart rate

Absorption

A portion of inhaled dose is absorbed to systemic circulation

Distribution

Vd: Adults: 1,900 L

Metabolism

Hepatic to an inactive sulfate

Excretion

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)

Half-Life Elimination

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

Contraindications

Hypersensitivity to levalbuterol, albuterol, or any component of the formulation

Dosing: Adult

Bronchospasm:

Metered-dose inhaler: 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)

Solution for nebulization: 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)

Exacerbation of asthma (acute, severe) (off-label; NAEPP, 2007):

Metered-dose inhaler: 4 to 8 inhalations every 20 minutes for up to 4 hours, then every 1 to 4 hours as needed

Solution for nebulization: 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

Dosing: Geriatric

Refer to adult dosing, starting with lowest dose; titrate cautiously.

Dosing: Pediatric

Bronchospasm:

Metered-dose inhaler: Children ≥4 years and Adolescents: 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)

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

Manufacturer’s labeling:

Children 6 to 11 years: 0.31 mg 3 times daily (maximum: 0.63 mg 3 times daily)

Children ≥12 years and Adolescents: Refer to adult dosing.

Exacerbation of asthma (acute, severe) (off-label; NAEPP, 2007):

Metered-dose inhaler:

Children <12 years: 4 to 8 inhalations every 20 minutes for 3 doses, then every 1 to 4 hours as needed

Children ≥12 years and Adolescents: Refer to adult dosing.

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 and Adolescents: Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling. Use with caution.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Reconstitution

Concentrated solution should be diluted with 2.5 mL NS prior to use.

Administration

Inhalation:

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.

Compatibility

Solution for nebulization: Compatible with budesonide suspension (NIH, 2007)

Storage

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.

Drug Interactions

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 and Thiazide-Like Diuretics: Beta2-Agonists may enhance the hypokalemic effect of Thiazide and Thiazide-Like Diuretics. Monitor therapy

Tricyclic Antidepressants: May enhance the adverse/toxic effect of Beta2-Agonists. Monitor therapy

Adverse Reactions

>10%:

Endocrine & metabolic: Serum glucose increased, serum potassium decreased

Neuromuscular & skeletal: Tremor (≤7%)

Respiratory: Rhinitis (3% to 11%)

Miscellaneous: Viral infection (≤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).

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, anaphylaxis, oropharyngeal edema) 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 (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.

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.

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)

Pregnancy Risk Factor

C

Pregnancy Considerations

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).

Patient Education

• 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, vomiting, tremors, or pharyngitis. Have patient report immediately to prescriber signs of low potassium (muscle pain or weakness, muscle cramps, or an abnormal heartbeat), angina, tachycardia, severe dizziness, passing out, severe anxiety, severe headache, difficulty breathing, wheezing, or cough (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.

Hide