pharmacopeia
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/api/v1/drug/levalbuterol

Mechanism of action

Sourced from openFDA

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.

Indications

Sourced from openFDA
  • 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.

Contraindications

Sourced from openFDA
  • 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) ] .contraindicated

Dosage & administration

Sourced from openFDA

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 0.31 mg administered three times a day, by nebulization. Routine dosing should not exceed 0.63 mg three times a day. Adults and Adolescents ≥ 12 Years Old: The recommended starting dosage of levalbuterol inhalation solution for patients 12 years of age and older is 0.63 mg administered three times a day, every 6 to 8 hours, by nebulization. Patients 12 years of age and older with more severe asthma or patients who do not respond adequately to a dose of 0.63 mg of levalbuterol inhalation solution may benefit from a dosage of 1.25 mg three times a day. Patients receiving the highest dose of levalbuterol inhalation solution should be monitored closely for adverse systemic effects, and the risks of such effects should be balanced against the potential for improved efficacy. The use of levalbuterol inhalation solution can be continued as medically indicated to help control recurring bouts of bronchospasm. During this time, most patients gain optimal benefit from regular use of the inhalation solution.

Warnings & precautions

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• Life-threatening paradoxical bronchospasm may occur. Discontinue levalbuterol inhalation solution immediately and treat with alternative therapy. ( 5.1 ) • Need for more doses of levalbuterol inhalation solution than usual may be a sign of deterioration of asthma and requires reevaluation of treatment. ( 5.2 ) • Levalbuterol inhalation solution is not a substitute for corticosteroids. ( 5.3 ) • Cardiovascular effects may occur. Consider discontinuation of levalbuterol inhalation solution if these effects occur. Use with caution in patients with underlying cardiovascular disorders. ( 5.4 ) • Excessive use may be fatal. Do not exceed recommended dose. ( 5.5 ) • Immediate hypersensitivity reactions may occur. Discontinue levalbuterol inhalation solution immediately. ( 5.6 ) • Hypokalemia and changes in blood glucose may occur. ( 5.7 , 5.8 ) 5.1 Paradoxical Bronchospasm Levalbuterol inhalation solution can produce paradoxical bronchospasm, which may be life-threatening. If paradoxical bronchospasm occurs, levalbuterol inhalation solution should be discontinued immediately and alternative therapy instituted. It should be recognized that paradoxical bronchospasm, when associated with inhaled formulations, frequently occurs with the first use of a new vial. 5.2 Deterioration of Asthma Asthma may deteriorate acutely over a period of hours or chronically over several days or longer.

Adverse reactions

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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. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Mylan at 1-877-446-3679 (1-877-4-INFO-RX) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of the drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adults and Adolescents 12 Years of Age and Older Adverse reaction information concerning levalbuterol inhalation solution in adults and adolescents is derived from one 4-week, multicenter, randomized, double-blind, active-, and placebo-controlled trial in 362 patients with asthma 12 years of age and older. Adverse reactions reported in ≥ 2% of patients receiving levalbuterol inhalation solution or racemic albuterol and more frequently than in patients receiving placebo are listed in Table 1.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to asthma medication, including levalbuterol inhalation solution during pregnancy. To enroll in MotherToBaby Pregnancy Studies’ Asthma & Pregnancy Study or for more information about the registry, call 1-877- 311-8972 or visit www.mothertobaby.org/ongoing-study/asthma. Risk Summary There are no adequate and well-controlled studies of levalbuterol inhalation solution (concentrate) in pregnant women. There are clinical considerations with the use of levalbuterol inhalation solution (concentrate) in pregnant women [see Clinical Considerations]. Following oral administration of levalbuterol HCl to pregnant rabbits, there was no evidence of teratogenicity at doses up to 25 mg/kg/day [approximately 108 times the maximum recommended human daily inhalation dose (MRHDID) of levalbuterol HCl for adults on a mg/m 2 basis]; however, racemic albuterol sulfate was teratogenic in mice (cleft palate) and rabbits (cranioschisis) at doses slightly higher than the human therapeutic range ( see Data ). The estimated background risk of major birth defects and miscarriage for the indicated populations(s) are unknown. In the U.S.

Pharmacokinetics

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Metabolism
Adults and Adolescents ≥ 12 Years Old The inhalation pharmacokinetics of levalbuterol inhalation solution were investigated in a randomized cross-over study in 30 healthy adults following administration of a single dose of 1.25 mg and a cumulative dose of 5 mg of levalbuterol inhalation solution and a single dose of 2.5 mg and a cumulative dose of 10 mg of racemic albuterol sulfate inhalation solution by nebulization using a PARI LC Jet™ nebulizer with a Dura-Neb ® 2000 compressor.

Overdosage

Sourced from openFDA

The expected symptoms with overdosage are those of excessive beta-adrenergic receptor stimulation and/or occurrence or exaggeration of any of the symptoms listed under Adverse Reactions (6) , e.g., seizures, angina, hypertension or hypotension, tachycardia with rates up to 200 beats/min., arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise, and sleeplessness. Hypokalemia also may occur. As with all sympathomimetic medications, cardiac arrest and even death may be associated with the abuse of levalbuterol inhalation solution. Treatment consists of discontinuation of levalbuterol inhalation solution together with appropriate symptomatic therapy. The judicious use of a cardio selective beta-receptor blocker may be considered, bearing in mind that such medication can produce bronchospasm. There is insufficient evidence to determine if dialysis is beneficial for overdosage of levalbuterol inhalation solution.

Approval history

Sourced from openFDA
  • Mar 11, 2005NDANDA021730Lupin
  • Mar 20, 2009ANDAANDA078309Mylan Speciality Lp
  • Apr 26, 2013ANDAANDA090297Teva Pharms Usa
  • Mar 22, 2016ANDAANDA203653Ritedose Corp
  • Dec 30, 2016ANDAANDA207625Luoxin Aurovitas
  • Jan 31, 2017ANDAANDA207628Luoxin Aurovitas
  • Nov 5, 2018ANDAANDA207820Sun Pharm

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
6,541 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Dyspnoea76912%
  2. 2Device Delivery System Issue5638.6%
  3. 3Drug Dose Omission By Device4947.6%
  4. 4No Adverse Event4907.5%
  5. 5Pneumonia4286.5%
  6. 6Asthma4026.1%
  7. 7Fatigue4006.1%
  8. 8Cough3926.0%
  9. 9Drug Ineffective3875.9%
  10. 10Nausea3715.7%
  11. 11Headache3685.6%
  12. 12Off Label Use3515.4%
  13. 13Diarrhoea2734.2%
  14. 14Pain2694.1%
  15. 15Dizziness2664.1%

Literature

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Recent PubMed references pinned to Levalbuterol as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 941 ClinicalTrials.gov registrations naming Levalbuterol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Levalbuterol work?
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.
What is Levalbuterol used for?
According to FDA labeling, Levalbuterol carries indications including: 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Levalbuterol?
Levalbuterol is classified as beta2-Adrenergic Agonist, Adrenergic beta2-Agonists, Bronchodilation.
What are the brand names for Levalbuterol?
Levalbuterol is marketed under brand names including Xopenex.
What are the contraindications for Levalbuterol?
Levalbuterol labeling lists contraindications including: 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) ] .. Always consult the full prescribing information and a clinician.
Note. Data for levalbuterol is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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