Levalbuterol

Levalbuterol is a prescription medicine used to prevent or treat the symptoms of asthma (bronchospasm).

• Levalbuterol is available under the following different brand names: Xopenex, Xopenex HFA

Adult and pediatric dosage

Nebulizer solution

• 0.31mg/3mL
• 0.63mg/3mL
• 1.25mg/3mL
• 1.25mg/0.5mL
• Aerosol
• 45mcg/actuation

Geriatric dosage

• Nebulizer solution: 0.63 mg initially in patients above 65 years
• Bronchospasm
• Adult dosage
• Nebulizer solution: 0.63 mg 3 times daily at intervals of 6-8 hours; may increase the dose to 1.25 mg 3 times daily with close monitoring for adverse effects
• Aerosol: 90 mcg (2 actuation of metered-dose inhaler) every 4-6 hours; 1 actuation every 4 hours may be sufficient; not to exceed 2 actuation every 4 hour
• Pediatric dosage
• Nebulizer solution
• Children below 6 years: Not indicated; clinical trials with levalbuterol inhalation in this age group failed to meet the primary efficacy endpoint
• Children between 6 to 12 years: 0.31 mg every 8 hours; not to exceed 0.63 mg every 8 hours as needed
• Children above 12 years: 0.63 mg 3 times daily at intervals of 6-8 hours; may increase the dose to 1.25 mg 3 times daily with close monitoring for adverse effects
• Aerosol
• Children below 4 years: Safety and efficacy not established
• Children above 4 years: 90 mcg (2 actuation of metered-dose inhaler) every 4-6 hours as needed; in some patients, 1 inhalation (45 mg of levalbuterol free base) every 4 hours may be sufficient

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

Common side effects of Levalbuterol include:

• dizziness,
• nervousness,
• tremors,
• runny nose,
• sore throat,
• chest pain or tightness,
• irregular heartbeats,
• pain, and
• vomiting.

Serious side effects of Levalbuterol include:

• wheezing,
• choking,
• other breathing problems,
• pounding heartbeats,
• worsening asthma symptoms,
• low potassium-leg cramps, constipation, irregular heartbeats, fluttering in the chest, extreme thirst, increased urination, numbness or tingling, muscle weakness, and limp feeling.

Rare side effects of Levalbuterol include:

• none 

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first

• Levalbuterol has severe interactions with no other drugs.
• Levalbuterol has serious interactions with the following drugs:
  • amisulpride
  • amitriptyline
  • amoxapine
  • chloroquine
  • clomipramine
  • desipramine
  • doxepin
  • fexinidazole
  • imipramine
  • isocarboxazid
  • lefamulin
  • linezolid
  • lofepramine
  • maprotiline
  • nortriptyline
  • phenelzine
  • protriptyline
  • tranylcypromine
  • trazodone
  • trimipramine
• Levalbuterol has moderate interactions with at least 257 other drugs.
• Levalbuterol has minor interactions with the following drugs: 
  • bendroflumethiazide
  • bumetanide
  • chlorothiazide
  • chlorthalidone
  • cyclopenthiazide
  • ethacrynic acid
  • eucalyptus
  • furosemide
  • hydrochlorothiazide
  • indapamide
  • methyclothiazide
  • metolazone
  • noni juice
  • sage
  • torsemide

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Hypersensitivity to levalbuterol or racemic albuterol

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Levalbuterol?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Levalbuterol?”

Cautions

• Risk of paradoxical bronchospasm; this should be distinguished from inadequate response; discontinue and treat with alternate therapy if it occurs
• Has a higher affinity for beta1- and beta2-adrenergic receptors than racemic albuterol has
• Risk of hypersensitivity reactions
• Use caution in hyperthyroidism; may increase thyroid activity
• Use with caution in diabetes mellitus (beta2 agonists may increase glucose)
• Risk of hypokalemia (usually transient); use with caution in hypokalemia
• Use with caution in patients with a history of seizure disorders; therapy may increase CNS activity/excitation
• Exceeding the recommended dose may result in serious adverse effects, including fatalities

Cardiovascular effects

• Use with caution in cardiovascular disorders (eg, arrhythmias, hypertension, coronary insufficiency)
• May cause elevation in blood pressure and heart rate; may cause CNS stimulation or excitation
• May increase the risk of arrhythmia and electrocardiogram changes, including ST-segment depression, prolongation of the QTc interval, or flattening of the T wave

Drug interaction overview

• Short-acting bronchodilators
• Avoid use
• If additional adrenergic drugs are to be administered by any route, use with caution to avoid deleterious additive cardiovascular effects

Beta-blockers

• Beta-adrenergic receptor blocking agents not only block the pulmonary effect of beta-adrenergic agonists but may produce severe bronchospasm in asthmatic patients.
• Therefore, patients with asthma should not normally be treated with beta-blockers.
• Under certain circumstances, cardioselective beta-blockers should be considered and may be used with caution

Diuretics

• ECG changes or hypokalemia that may result from the administration of non-potassium-sparing diuretics can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded

Digoxin

• Mean decreases of 16% and 22% in serum digoxin levels were demonstrated after single-dose IV and oral administration of racemic albuterol, respectively, to normal volunteers who had received digoxin for 10 days

Monoamine oxidase inhibitors or tricyclic antidepressants

• Use extreme caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, or within 2 weeks of discontinuation of such agents, because the action of levalbuterol on the vascular system may be potentiated
• Consider alternative therapy in patients taking MAO inhibitors or tricyclic antidepressants

Pregnancy and Lactation

• There are no adequate and well-controlled studies on pregnant women; there are clinical considerations with use in pregnant women

Pregnancy exposure registry

• Monitors pregnancy outcomes in women exposed to asthma medication 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

Clinical considerations

• In women with poorly or moderately controlled asthma, there is an increased risk of preeclampsia in the mother and prematurity, low birth weight, and small gestational age in neonate
• Closely monitor and adjust medication as necessary to maintain optimal control

Lactation

• There are no available data on the presence of levalbuterol in human milk, its effects on the breastfed child, or effects on milk production
• Developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on the breastfed child from therapy or underlying maternal condition