DrugindexOnline^{2nd edition}

Pronouncation: (lev-al-BYOO-ter-ol)
Class: Sympathomimetic

Trade Names:
Xopenex
- Solution for inhalation 0.31 mg levalbuterol per 3 mL
- Solution for inhalation 0.63 mg levalbuterol per 3 mL
- Solution for inhalation 1.25 mg levalbuterol per 3 mL

Mechanism of Action

Pharmacology

Produces bronchodilation by relaxing bronchial smooth muscles via beta ₂ -adrenergic receptor stimulation.

Pharmacokinetics

Absorption

T _max is approximately 0.2 h. C _max is approximately 1.1 to 4.5 ng/mL (dose-dependent). AUC is approximately 3.3 to 17.4 ng•h/mL (dose dependent).

Elimination

The t _½ is approximately 3 to 4 h.

Onset

17 min (0.63 mg); 10 min (1.25 mg).

Peak

Approximately 1.5 h.

Duration

Approximately 5 to 8 h.

Special Populations

Children

AUC increases; use lower dose (children 6 to 11 yr of age).

Indications and Usage

Treatment or prevention of bronchospasm in patients with reversible obstructive airway disease.

Contraindications

Hypersensitivity to levalbuterol or racemic albuterol.

Dosage and Administration

Adults and children 12 yr of age and older

Inhalation solution Usual starting dose is 0.63 mg 3 times daily (every 6 to 8 h) by nebulization. Patients with more severe asthma or patients who do not respond adequately to the 0.63 mg dose may benefit from 1.25 mg 3 times daily.

Children 6 to 11 yr of age

Inhalation solution Recommended dose is 0.31 mg 3 times daily by nebulization (max, 0.63 mg 3 times daily).

General Advice

• Administer only via nebulizer. Not for injection or oral use.
• Medication requires no dilution before administration and is added directly into the nebulizer reservoir.
• Once vial has been opened, administer immediately or discard.
• Discard solution if not colorless.
• Discard any unused solution.
• Do not mix with other nebulized medications unless ordered by health care provider.

Storage/Stability

Store unused vials in protective foil pouch between 68° and 77°F. Once the foil pouch is opened, use vials within 2 wk. If vials are removed from pouch and not used immediately, use within 1 wk. Protect vials from light and excessive heat.

Drug Interactions

Beta-blockers (eg, propranolol)

Severe bronchospasms may be produced in asthmatic patients taking levalbuterol.

Digoxin

Plasma digoxin levels may be decreased.

Diuretics (eg, loop [eg, furosemide] and thiazide [hydrochlorothiazide])

ECG changes and hypokalemia associated with diuretic therapy may be worsened by levalbuterol administration.

MAOIs (eg, phenelzine), tricyclic antidepressants (eg, amitriptyline)

The action of levalbuterol on the vascular system may be potentiated.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Tachycardia; migraine; abnormal ECG and ECG changes; hypertension; hypotension; syncope.

CNS

Dizziness, nervousness, tremor, anxiety, hypesthesia of the hand, insomnia, paresthesia; headache (children 6 to 11 yr of age).

Dermatologic

Eczema, rash, urticaria (children 6 to 11 yr of age).

EENT

Rhinitis, sinusitis, turbinate edema, dry throat, eye itch; pharyngitis, otitis media (children 6 to 11 yr of age).

GI

Dyspepsia; diarrhea; dry mouth; gastroenteritis; nausea.

Respiratory

Increased cough; viral infection.

Miscellaneous

Flu-like symptoms, accidental injury, pain, leg cramps, lymphadenopathy, myalgia; abdominal pain, asthma, fever (children 6 to 11 yr of age).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 6 yr of age.

Hypersensitivity

Immediate hypersensitivity reactions may occur.

Special Risk Patients

Use with caution in patients with CV disorders, convulsive disorders, hyperthyroidism, or diabetes, and in patients unusually responsive to sympathomimetic amines.

Bronchospasm

Life-threatening paradoxical bronchospasm may occur.

CV effects

Clinically important CV effects, as measured by pulse rate and BP, may occur; use with caution in patients with CV disorders, especially coronary insufficiency, cardiac arrhythmias, and hypotension.

CNS effects

CNS stimulation may occur; use with caution in patients with a history of seizures or hyperthyroidism.

Deterioration of asthma

A dosage requirement increase or increased frequency of use may indicate destabilization of asthma, requiring re-evaluation of the treatment regimen.

Diabetes mellitus

Use with caution.

Overdosage

Symptoms

Seizures, angina, hypertension, hypotension, tachycardia, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise, sleeplessness, hypokalemia, cardiac arrest, death.

Patient Information

• Advise patient to review illustrated patient information leaflet. Ensure that patient, family, or caregiver can prepare, use, and clean the nebulizer without difficulty.
• Instruct patient not to mix nebulizer medications unless advised by health care provider.
• Instruct patient to use nebulizer solution immediately after opening. If solution is not used immediately, advise patient to discard the solution.
• Advise patient to discard any unused nebulizer solution.
• Instruct patient not to exceed prescribed dose. Advise patient to contact health care provider if this medication no longer seems to control asthma symptoms or if increasing doses of the medicine are needed. These may indicate worsening asthma.
• Advise patients using more than 1 inhaled medication to use this medication first if needed. Take inhaled corticosteroids or other inhaled controller medications last.
• Advise patient that if breathing symptoms worsen during or immediately after using this medication, to stop using it and inform health care provider immediately.
• Inform patient that levalbuterol is not a substitute for inhaled or oral corticosteroids and not to stop or reduce the dose of corticosteroid medication.
• Instruct patient to discontinue use and immediately notify health care provider if eye pain or discomfort, blurred vision, vision halos, or colored images develop in association with red eyes. Advise patient that these symptoms may be associated with a serious problem that will require immediate medical care.
• Advise patient to carry medical identification (eg, card, bracelet) indicating asthma or COPD.