Drug information of Levalbuterol


Drug group:

Beta2 Agonist use for Bronchospasm

Mechanism of effect

Beta2-receptor agonist with some beta1 activity; relaxes bronchial smooth muscle


Absorption:A portion of inhaled dose is absorbed to systemic circulation
Metabolism:Metabolized primarily in the gastrointestinal tract via SULT1A3 (sulfotransferase)
Excretion:Urine (80% to 100%), feces (<20%)
Onset of Action:
Measured as a 15% increase in FEV1:
Metered-dose inhaler: 5.5 to 10.2 minutes; Peak effect: 76 to 78 minutes
Nebulization solution: 10 to 17 minutes; Peak effect: 1.5 hours
Time to Peak:
Nebulization solution: Children: 0.3 to 0.6 hours, Adults: 0.2 hours
Duration of Action:
Measured as a 15% increase in FEV1:
Metered-dose inhaler: 3 to 4 hours (up to 6 hours in some patients)
Nebulization solution: 5 to 6 hours (up to 8 hours in some patients)
Half-Life Elimination:
3.3 to 4 hours

Drug indications



Nebulizer solution: 0.63-1.25 mg 3 times daily q6-8hr
Aerosol: 90 mcg (2 actuations of metered-dose inhaler) q4-6hr
Bronchospasm (PEDIATRIC)
Nebulizer solution:
<6 years: Not indicated; clinical trials with levalbuterol inhalation in this age group failed to meet the primary efficacy endpoint
≥6 to <12 years: 0.31 mg q8hr; not to exceed 0.63 mg q8hr PRN
>12 years: 0.63-1.25 mg q8hr PRN
<4 years: Safety and efficacy not established
≥4 years: 90 mcg (2 actuations of metered-dose inhaler) q4-6hr PRN; in some patients, 1 inhalation (45 mg of levalbuterol free base) q4hr may be sufficient

Drug contraindications

Hypersensitivity to this drug

Hypersensitivity to levalbuterol or racemic albuterol

Side effects

Headache , Flu-like symptoms , Tremor , rhinitis , nervousness

Headache ,Vomiting ,Viral infection ,Rhinitis ,Tachycardia ,Nervousness , dizziness , migraine , anxiety , pain ,Skin rash , urticaria ,Diarrhea , dyspepsia ,Lymphadenopathy ,Tremor ,leg cramps , weakness , myalgia ,Pharyngitis , asthma , cough , sinusitis , flu-like symptoms , bronchitis , nasal mucosa swelling ,Fever , accidental injury ,Decreased serum potassium, increased heart rate, increased serum glucose, paradoxical bronchospasm,Hypersensitivity reaction ,Acne vulgaris, anaphylaxis, angina pectoris, angioedema, atrial fibrillation, cardiac arrhythmia, chest pain, chills, constipation, conjunctivitis, dry throat, dysmenorrhea, dyspnea, ECG abnormality, epistaxis, extrasystoles, eye pruritus, gastroenteritis, gastroesophageal reflux disease, hematuria, hyperesthesia (hand), hypertension, hypokalemia, hypotension, insomnia, metabolic acidosis, nausea, otalgia, paresthesia, pulmonary disease, supraventricular cardiac arrhythmia, syncope, vertigo, voice disorder, vulvovaginal candidiasis, xerostomia

Beta-Blockers (Beta1 Selective)
Beta-Blockers (Nonselective)
Cannabinoid-Containing Products
Loop Diuretics
Monoamine Oxidase Inhibitors
QT-prolonging Agents (Highest Risk)
Short-acting bronchodilators
Thiazide and Thiazide-Like Diuretics
Tricyclic Antidepressants


-Cardiovascular disorder (eg, arrhythmias, hypertension, coronary insufficiency)
-Risk of paradoxical bronchospasm
-Has higher affinity for beta1- and beta2-adrenergic receptors than racemic albuterol
-Risk of hypersensitivity reactions
-Risk of hypokalemia
-Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy

Points of recommendation

-Use with caution in diabetes mellitus (beta2 agonists may increase glucose)
- Use with caution in hyperthyroidism; may stimulate thyroid activity.
- Use with caution in patients with renal impairment; drug clearance is decreased.
- Use with caution in patients with seizure disorders

Pregnancy level


Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.
This drug should not be used during pregnancy unless the benefit outweighs the risk to the fetus

Breast feeding warning

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

Developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from therapy or from underlying maternal condition

Related drugs

Arformoterol , Bitolterol

Drug forms

Xopenex, Xopenex HFA

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