Xopenex

— THERAPEUTIC CATEGORIES —
  • Asthma/COPD
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Xopenex Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Levalbuterol (as HCl) (single-isomer albuterol) 0.31mg/3mL, 0.63mg/3mL, 1.25mg/3mL, or 1.25mg/0.5mL (must be diluted); per vial; soln for inh via nebulization; preservative-free.

    Pharmacological Class

    Beta-2 agonist.

    How Supplied

    Soln 0.31mg/3mL, 0.63mg/3mL, 1.25mg/3mL—24 vials; 1.25mg/0.5mL—30 vials

    Storage

    Store Xopenex Inhalation Solution in the protective foil pouch at 20° to 25°C (68° to 77°F). 

    The product should be protected from light and excessive heat. 

    Unopened vials should be kept in the pouch. 

    Once the foil pouch is opened, the vials should be used within 2 weeks.

    Vials removed from the pouch, if not used immediately, should be protected from light and used within 1 week.

    Discard the vial if the solution is not colorless.

    Manufacturer

    Akorn, Inc.

    Generic Availability

    YES

    Xopenex Indications

    Indications

    Bronchospasm.

    Xopenex Dosage and Administration

    Adult

    Initially 0.63mg by nebulization 3 times daily at 6–8hr intervals; may increase to 1.25mg 3 times daily.

    Adult

    ≥12yrs: The recommended starting dosage of Xopenex Inhalation Solution is 0.63mg administered 3 times a day, every 6 to 8 hours, by nebulization.

    For patients with more severe asthma or in those who do not respond adequately to 0.63mg, a dosage of 1.25mg 3 times a day may be beneficial.

    Can be continued as medically indicated to help control recurring bouts of bronchospasm. Reevaluation may be required if a previously effective dosage regimen fails to provide the usual response.

    Patients on the highest dose of Xopenex should be monitored for adverse systemic effects. Do not exceed the recommended dose.

    Children

    <6yrs: not established. 6–11yrs: 0.31mg by nebulization 3 times daily; max 0.63mg 3 times daily.

    Children

    6–11yrs: The recommended dosage of Xopenex Inhalation Solution is 0.31mg administered 3 times a day, by nebulization. Routine dosing should not exceed 0.63mg 3 times a day. Do not exceed the recommended dose.

    Can be continued as medically indicated to help control recurring bouts of bronchospasm. Reevaluation may be required if a previously effective dosage regimen fails to provide the usual response.

    Elderly

    In general, patients 65 years of age and older should be started at a dose of 0.63mg of Xopenex Inhalation Solution. Dose may be increased as tolerated, in conjunction with frequent clinical and laboratory monitoring, to the maximum recommended daily dose.

    Xopenex Contraindications

    Not Applicable

    Xopenex Boxed Warnings

    Not Applicable

    Xopenex Warnings/Precautions

    Warnings/Precautions

    Do not exceed recommended dose. Monitor for increased need; if inadequate control, reevaluate and consider adding an antiinflammatory (eg, corticosteroids). Sensitivity to sympathomimetics. Discontinue if paradoxical bronchospasm, cardiovascular effects, or hypersensitivity reactions occur. Cardiovascular disorders (esp. coronary insufficiency, arrhythmias, hypertension). Seizure disorders. Diabetes. Hyperthyroidism. Hypokalemia. Renal impairment; monitor (esp. in elderly). Elderly. Labor & delivery. Pregnancy. Nursing mothers.

    Warnings/Precautions

    Paradoxical Bronchospasm

    • May occur with treatment; discontinue Xopenex Inhalation Solution immediately and start alternative therapy.

    Deterioration of Asthma and Use of Anti-inflammatory Agents

    • If a patient needs more doses of Xopenex, this may be an indication of destabilization of asthma.
    • Reevaluate patient and consider the need for anti-inflammatory treatment (eg, corticosteroids); beta-adrenergic agonist therapy alone may not be adequate to control asthma in many patients.
    • Xopenex is not a substitute for corticosteroids. 

    Cardiovascular Effects

    • Beta-adrenergic agonists can produce clinically significant cardiovascular effects in some patients.
    • These effects are uncommon following administration of Xopenex at the recommended dose, but if they do occur, the drug may need to be discontinued.
    • Like with all sympathomimetic amines, caution should be used in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension.

    Immediate Hypersensitivity Reactions

    • May occur after administration of levalbuterol or racemic albuterol.
    • The potential for hypersensitivity must be considered in the clinical evaluation of patients who experience immediate hypersensitivity reactions while receiving Xopenex Inhalation Solution.

    Coexisting Conditions

    • Like with all sympathomimetic amines, caution should be used in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, hypertension, convulsive disorders, hyperthyroidism, or diabetes; and in patients who are unusually responsive to sympathomimetic amines.
    • Clinically significant changes in systolic and diastolic blood pressure have been seen following beta-adrenergic bronchodilator use.

    Hypokalemia

    • May produce significant hypokalemia in some patients.
    • Decrease is usually transient and does not require supplementation.

    Pregnancy Considerations

    There are no adequate and well-controlled studies of Xopenex Inhalation Solution in pregnant women. Because of the potential for beta-adrenergic agonists to interfere with uterine contractility, the use of Xopenex for the treatment of bronchospasm during labor should be restricted to those patients for whom the benefits clearly outweigh the risk.

    Nursing Mother Considerations

    There are no available data on the presence of levalbuterol in human milk, the effects on the breastfed child, or the effects on milk production.

    Pediatric Considerations

    The safety and efficacy of Xopenex Inhalation Solution have been established in pediatric patients 6 years of age and older.

    Xopenex Inhalation Solution is not indicated for pediatric patients less than 6 years of age. Clinical trials with Xopenex Inhalation Solution in this age group failed to meet the primary efficacy endpoint and demonstrated an increased number of asthma-related adverse reactions following chronic Xopenex treatment.

    Geriatric Considerations

    Clinical studies of Xopenex Inhalation Solution did not include sufficient numbers of patients aged 65 years and older to determine whether they respond differently from younger subjects.

    As elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.

     

    Renal Impairment Considerations

    Risk of toxic reactions may be greater in patients with impaired renal function as albuterol is substantially excreted by the kidney.

    It may be useful to monitor renal function in patients with renal impairment.

    Hepatic Impairment Considerations

    The effect of hepatic impairment on the pharmacokinetics of Xopenex Inhalation Solution has not been evaluated.

    Xopenex Pharmacokinetics

    Metabolism

    Published literature suggests that the primary enzyme responsible for the metabolism of albuterol enantiomers in humans is SULT1A3 (sulfotransferase).

    Elimination

    The primary route of elimination of albuterol enantiomers is through renal excretion. Less than 20% of the drug is detected in the feces.

    Xopenex Interactions

    Interactions

    Avoid within 2 weeks of MAOIs, tricyclic antidepressants. Avoid other short-acting sympathomimetic aerosol bronchodilators, epinephrine. Antagonized by β-blockers. Caution with other drugs that may lower serum potassium (eg, diuretics). Monitor digoxin.

    Interactions

    Avoid concomitant use of other short-acting sympathomimetic bronchodilators or epinephrine; if needed, use with caution to avoid deleterious cardiovascular effects.

    Patients with asthma should not normally be treated with beta blockers as these agents block the pulmonary effect of beta-adrenergic agonists and may produce severe bronchospasm.  

    • Under certain circumstances (eg, prophylaxis after MI), consider cardioselective beta blockers; use with caution.

    Use extreme caution when Xopenex Inhalation Solution is administered to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, or within 2 weeks of discontinuation of such agents.

    • Action of levalbuterol on the vascular system may be potentiated.
    • Consider alternative therapy in patients taking MAOIs or tricyclic antidepressants.

    Use caution if beta-agonists are coadministered with non-potassium-sparing diuretics; consider monitoring potassium levels as hypokalemia may be worsened.

    Carefully evaluate serum digoxin levels in patients who are currently receiving digoxin and Xopenex Inhalation Solution.

    Xopenex Adverse Reactions

    Adverse Reactions

    Accidental injury, bronchitis, dizziness, pharyngitis, rhinitis, vomiting, palpitations, chest pain, tachycardia, headache, tremor, nervousness.

    Xopenex Clinical Trials

    Clinical Trials

    Adults and Adolescents ≥12 Years Old 

    Safety and efficacy evaluated in a 4-week, randomized, double-blind, placebo-controlled, parallel group study.

    • 362 patients 12 years of age and older with mild to moderate asthma (mean baseline FEV1 60% of predicted); ~50% receiving inhaled corticosteroids.
    • Randomly assigned to receive Xopenex 0.63mg, Xopenex 1.25mg, racemic albuterol sulfate 1.25mg, racemic albuterol sulfate 2.5mg, or placebo 3 times a day administered via a PARI LC Plus™ nebulizer and a Dura-Neb® portable compressor.
    • Rescue med: racemic albuterol delivered by a CDC MDI as needed.

    Efficacy, as measured by the mean percent change from baseline FEV1, was demonstrated for all active treatment regimens compared with placebo on day 1 and day 29.

    Xopenex 1.25mg demonstrated the largest mean percent change from baseline in FEV1 on both days 1 and 29, compared with other active treatments.

    Xopenex 0.63mg and racemic albuterol sulfate 2.5mg produced a clinically comparable mean percent change from baseline FEV1 on both day 1 and 29.

    Mean time to onset of a 15% increase in FEV1 over baseline; mean time to peak effect; and mean duration of effect (>15% increase from baseline FEV1) after 4 weeks of treatment, respectively:

    • Xopenex 0.63mg: 17 minutes, 1.5 hours, ~5 hours
    • Xopenex 1.25mg: 10 minutes, 1.5 hours, ~6 hours

     

    Children 6 to 11 Years Old 

    Safety and efficacy evaluated in a randomized, double-blind, placebo- and active-controlled study in children with mild to moderate asthma (n=316; mean baseline FEV1 73% of predicted).

    Following 1-week placebo run-in, patients were randomly assigned to Xopenex (0.31mg or 0.63mg), racemic albuterol (1.25mg or 2.5mg), or placebo, delivered 3 times a day for 3 weeks using a PARI LC Plus™ nebulizer and a Dura-Neb® 3000 compressor.

    Efficacy, as measured by mean peak percent change from baseline FEV1, was demonstrated for all active treatment regimens compared with placebo on day 1 and day 21.

    Onset of effect (time to a 15% increase in FEV1 over test-day baseline) and duration of effect (maintenance of a >15% increase in FEV1 over test-day baseline) of levalbuterol were clinically comparable to those of racemic albuterol.

    Xopenex Note

    Not Applicable

    Xopenex Patient Counseling

    Patient Counseling

    Ask patients about previously experienced hypersensitivity to levalbuterol or racemic albuterol; counsel about potential hypersensitivity reactions.

    Do not use Xopenex more frequently than recommended; if treatment becomes less effective, reevaluation may be needed.

    Discontinue if paradoxical bronchospasm occurs.

    Inform patients of potential drug interactions.

    Palpitations, chest pain, fast heart rate, headache, dizziness, tremor and nervousness may occur with use.

    There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to asthma medication, including XOPENEX, during pregnancy. To enroll in the Asthma & Pregnancy Study or for more information about the registry, call 1-877-311-8972 or visit www.mothertobaby.org/ongoing-study/asthma.

    Review storage instructions with the patient.

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