Levalbuterol

Pronunciation

Pronunciation: LEE-val-BUE-ter-ol
Class: Sympathomimetic

Trade Names

Xopenex
- Solution for inhalation 0.31 mg per 3 mL
- Solution for inhalation 0.63 mg per 3 mL
- Solution for inhalation 1.25 mg per 3 mL

Xopenex HFA
- Aerosol 45 mg levalbuterol per actuation

Pharmacology

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

Slideshow: Flashback: FDA Drug Approvals 2013

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).

Xopenex HFA

T max in adolescents/adults (12 yr of age and older) and children (4 to 11 yr of age) is approximately 0.54 and 0.76 h, respectively. C max in adolescents/adults (12 yr of age and older) and children (4 to 11 yr of age) is approximately 0.199 and 0.163 ng/mL, respectively. AUC in adolescents/adults (12 yr of age and older) and children (4 to 11 yr of age) is approximately 0.695 and 0.579 ng•h/mL, respectively.

Elimination

The t ½ is approximately 3 to 4 h. Primary route of excretion is renal (80% to 100%) with less than 20% eliminated in the feces.

Onset

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

Peak

Approximately 1.5 h.

Duration

Approximately 5 to 8 h.

Special Populations

Renal Function Impairment

Use high doses with caution.

Children

AUC increases; use lower dose (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 Xopenex : Usual starting dosage 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 Xopenex : Recommended dosage is 0.31 mg 3 times daily by nebulization (max, 0.63 mg 3 times daily).

Adults and Children 4 yr of age and older

Inhalation aerosol Xopenex HFA : 2 inhalations (90 mcg) repeated every 4 to 6 h. In some patients, 1 inhalation every 4 h is sufficient.

General Advice

  • Xopenex
  • 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.
  • Xopenex HFA
  • Shake well before using.
  • Prime inhaler before using for the first time and when the inhaler has not been used for more than 3 days by releasing 4 test sprays into the air, away from the face.
  • Store inhaler with actuator (or mouthpiece) down.
  • Wash and dry actuator at least once/wk.

Storage/Stability

Xopenex

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.

Xopenex HFA

Store between 68° and 77°F. Protect from freezing and direct sunlight.

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 [eg, 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

Xopenex

Migraine, tachycardia (3%).

Xopenex HFA

Hypertension (less than 2%); angina; arrhythmias, including atrial fibrillation, supraventricular tachycardia, and extrasystoles; tachycardia (postmarketing).

CNS

Xopenex

Nervousness (10%); tremor (7%); anxiety, dizziness (3%).

Children 6 to 11 yr of age

Headache (12%); asthenia (3%).

Xopenex HFA

Dizziness (3%); CNS stimulation, headache, sleeplessness; nervousness, tremor (postmarketing).

Dermatologic

Xopenex Children 6 to 11 yr of age

Rash (8%); urticaria (3%).

Xopenex HFA

Acne (less than 2%).

EENT

Xopenex

Rhinitis (11%).

Children 6 to 11 yr of age

Pharyngitis, rhinitis (10%).

Xopenex HFA

Pharyngitis (8%); rhinitis (7%); conjunctivitis, ear pain, epistaxis (less than 2%); drying or irritation of the oropharynx, vertigo.

Children 4 to 11 yr of age

Pharyngitis (7%).

GI

Xopenex

Dyspepsia (3%).

Children 6 to 11 yr of age

Diarrhea (6%).

Xopenex HFA

Constipation, gastroenteritis (less than 2%); nausea (postmarketing).

Children 4 to 11 yr of age

Vomiting (11%).

Genitourinary

Xopenex HFA

Dysmenorrhea, hematuria, vaginal moniliasis (less than 2%).

Hematologic-Lymphatic

Xopenex Children 6 to 11 yr of age

Lymphadenopathy (3%).

Musculoskeletal

Xopenex

Leg cramps (3%).

Children 6 to 11 yr of age

Myalgia (2%).

Xopenex HFA

Myalgia (less than 2%).

Respiratory

Xopenex

Viral infection (12%); increased cough, sinusitis (4%); turbinate edema (3%).

Children 6 to 11 yr of age

Asthma (9%).

Xopenex HFA

Asthma (9%); lung disorder (less than 2%); dyspnea, increased cough (postmarketing).

Children 4 to 11 yr of age

Bronchitis (3%).

Miscellaneous

Xopenex

Flu syndrome (4%); accidental injury, pain (3%).

Children 6 to 11 yr of age

Fever, viral infection (9%); accidental injury (6%); pain (3%); abdominal pain (2%).

Xopenex HFA

Pain (4%); cyst, flu syndrome, herpes simplex, viral infection (less than 2%); anaphylaxis, angioedema, chest pain (postmarketing).

Children 4 to 11 yr of age

Accidental injury (9%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Xopenex

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

Xopenex HFA

Safety and efficacy not established in children younger than 4 yr of age.

Elderly

Use with caution, usually starting at the low end of the dosage range, because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.

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 hypertension.

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

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

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.
  • Advise patient to shake the inhalation aerosol well before using.
  • Advise patient to keep the activator clean by washing it at least once a week.
  • 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.

Copyright © 2009 Wolters Kluwer Health.

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