Levalbuterol Tartrate
FDA Drug Information • Also known as: Levalbuterol Tartrate Hfa Inhalation, Xopenex Hfa
- Brand Names
- Levalbuterol Tartrate Hfa Inhalation, Xopenex Hfa
- Route
- ORAL
- Dosage Form
- AEROSOL, METERED
- Product Type
- HUMAN PRESCRIPTION DRUG
Description
11 DESCRIPTION The active component of Levalbuterol tartrate HFA inhalation aerosol is levalbuterol tartrate, the (R)-enantiomer of albuterol. Levalbuterol tartrate is a relatively selective beta 2 -adrenergic receptor agonist [see Clinical Pharmacology (12) ]. Levalbuterol tartrate has the chemical name (R)-α 1 -[[(1,1-dimethylethyl)amino]methyl]-4-hydroxy-1,3-benzenedimethanol L-tartrate (2:1 salt), and it has the following chemical structure: The molecular weight of levalbuterol tartrate is 628.71, and its empirical formula is (C 13 H 21 NO 3 ) 2 · C 4 H 6 O 6 . It is a white to light-yellow solid, freely soluble in water and very slightly soluble in ethanol. Levalbuterol tartrate is the generic name for (R)-albuterol tartrate in the United States. Levalbuterol tartrate HFA inhalation aerosol is a pressurized metered-dose aerosol inhaler (MDI) fitted with a dose indicator, which produces an aerosol for oral inhalation. It contains a suspension of micronized levalbuterol tartrate, propellant HFA-134a (1,1,1,2-tetrafluoroethane), Dehydrated Alcohol USP, and Oleic Acid NF. After priming with 4 actuations, each actuation of the inhaler delivers 67.8 mcg of levalbuterol tartrate (equivalent to 51.6 mcg of levalbuterol free base) from the valve and 59 mcg of levalbuterol tartrate (equivalent to 45 mcg of levalbuterol free base) from the actuator mouthpiece. Each 15 g canister provides 200 actuations (or inhalations). The following chemical structure Levalbuterol tartrate is a relatively selective beta2-adrenergic receptor agonist [see Clinical Pharmacology (12)]. Levalbuterol tartrate has the chemical name (R)-α1-[[(1,1-dimethylethyl)amino]methyl]-4-hydroxy-1,3-benzenedimethanol L-tartrate (2:1 salt).
What Is Levalbuterol Tartrate Used For?
1 INDICATIONS AND USAGE Levalbuterol tartrate HFA inhalation aerosol is a beta 2 -adrenergic agonist indicated for the treatment or prevention of bronchospasm in patients 4 years of age and older with reversible obstructive airway disease. ( 1.1 ) 1.1 Bronchospasm Levalbuterol tartrate HFA inhalation aerosol is indicated for the treatment or prevention of bronchospasm in adults, adolescents, and children 4 years of age and older with reversible obstructive airway disease.
Dosage and Administration
2 DOSAGE AND ADMINISTRATION For Oral Inhalation Only ( 2.2 ) Adults and children 4 years of age and older: 2 inhalations repeated every 4 to 6 hours; in some patients, 1 inhalation every 4 hours may be sufficient. ( 2.1 ) Prime Levalbuterol tartrate HFA inhalation aerosol before using for the first time and when the inhaler has not been used for more than 3 days. To prime Levalbuterol tartrate HFA inhalation aerosol, release 4 sprays into the air away from the face. ( 2.2 ) At least once a week, wash the actuator with warm water and let it air-dry completely. ( 2.2 ) 2.1 Recommended Dosages The recommended dosage of Levalbuterol tartrate HFA inhalation aerosol for adults and children 4 years of age and older is 2 inhalations (90 mcg of levalbuterol free base) repeated every 4 to 6 hours; in some patients, 1 inhalation (45 mcg of levalbuterol free base) every 4 hours may be sufficient. More frequent administration or a larger number of inhalations is not routinely recommended. If a previously effective dosage regimen fails to provide the usual response, this may be a marker of destabilization of asthma and requires reevaluation of the patient and the treatment regimen, giving special consideration to the possible need for anti-inflammatory treatment, e.g., corticosteroids. 2.2 Administration Information For oral inhalation only Shake well before use. Avoid spraying in the eyes. Prime the 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. To maintain proper use of Levalbuterol tartrate HFA inhalation aerosol, it is critical to wash the actuator with warm water and air-dry thoroughly at least once a week. The inhaler may cease to deliver levalbuterol tartrate if not properly cleaned and dried thoroughly. Keep the plastic actuator clean to prevent medication build-up and blockage. If the actuator becomes blocked with levalbuterol tartrate, wash the actuator to remove the blockage The canister is fitted with a dose indicator, which indicates how many inhalations remain. The dose indicator display will move after every tenth actuation. When nearing the end of the usable inhalations, the color behind the number in the dose indicator window changes to red. Discard the inhaler when the dose indicator display window shows zero, corresponding to the use of 200 actuations.
Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS Use of Levalbuterol tartrate HFA inhalation aerosol may be associated with the following: 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 (≥ 2% and > placebo) are accidental injury, bronchitis, dizziness, pain, pharyngitis, rhinitis, and vomiting. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, call 1-800-399-2561 or contact 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 a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adult s and Adolescents 12 Years of Age and Older Adverse reaction information concerning Levalbuterol tartrate HFA inhalation aerosol in adults and adolescents is derived from two 8-week, multicenter, randomized, double-blind, active- and placebo-controlled trials in 748 adult and adolescent patients with asthma that compared Levalbuterol tartrate HFA inhalation aerosol, a marketed albuterol HFA inhalation aerosol inhaler, and an HFA-134a placebo inhaler. Table 1 lists the incidence of all adverse reactions (whether considered by the investigator to be related or unrelated to drug) from these trials that occurred at a rate of 2% or greater in the group treated with Levalbuterol tartrate HFA inhalation aerosol and more frequently than in the HFA-134a placebo inhaler group. Table 1: Adverse Reaction Incidence (% of Patients) in Two 8-Week Clinical Trials in Adults and Adolescents ≥ 12 Years of Age* Body System Preferred Term Levalbuterol tartrate HFA inhalation aerosol 90 mcg (n=403) Racemic Albuterol HFA 180 mcg (n=179) Placebo (n=166) Respiratory System Asthma 9% 7% 6% Pharyngitis 8% 2% 2% Rhinitis 7% 2% 3% Body as a Whole Pain 4% 3% 4% Central Nervous System Dizziness 3% 1% 2% * This table includes all adverse reactions (whether considered by the investigator to be related or unrelated to drug) from these trials that occurred at a rate of 2% or greater in the group treated with Levalbuterol tartrate HFA inhalation aerosol and more frequently than in the HFA‑134a placebo inhaler group. Adverse reactions reported by less than 2% and at least 2 or more of the adolescent and adult patients receiving Levalbuterol tartrate HFA inhalation aerosol and by a greater proportion than receiving HFA-134a placebo inhaler include cyst, flu syndrome, viral infection, constipation, gastroenteritis, myalgia, hypertension, epistaxis, lung disorder, acne, herpes simplex, conjunctivitis, ear pain, dysmenorrhea, hematuria, and vaginal moniliasis. There were no significant laboratory abnormalities observed in these studies. Pediatric Patients 4 to 11 Years of Age Adverse reaction information concerning Levalbuterol tartrate HFA inhalation aerosol in children is derived from a 4-week, randomized, double-blind trial of Levalbuterol tartrate HFA inhalation aerosol, a marketed albuterol HFA inhaler, and an HFA-134a placebo inhaler in 150 children aged 4 to 11 years with asthma. Table 2 lists the adverse reactions reported for Levalbuterol tartrate HFA inhalation aerosol in children at a rate of 2% or greater and more frequently than for placebo. Table 2: Adverse Reaction Incidence (% of Patients) in a 4-Week Clinical Trial in Children 4-11 Years of Age Body System Preferred Term Levalbuterol tartrate HFA inhalation aerosol 90 mcg (n=76) Racemic Albuterol HFA 180 mcg (n=39) Placebo (n=35) Digestive System Vomiting 11% 8% 6% Body as a Whole Accidental injury 9% 10% 6% Respiratory System Pharyngitis 7% 13% 6% Bronchitis 3% 0% 0% * This table includes all adverse reactions (whether considered by the investigator to be related or unrelated to drug) from...
Drug Interactions
7 DRUG INTERACTIONS Other short-acting sympathomimetic aerosol bronchodilators or epinephrine should not be used concomitantly with Levalbuterol tartrate HFA inhalation aerosol. If additional adrenergic drugs are to be administered by any route, they should be used with caution to avoid deleterious cardiovascular effects. Other short-acting sympathomimetic aerosol bronchodilators and adrenergic drugs : May potentiate effect. ( 7 ) Beta-blockers : May block bronchodilatory effects of beta-agonists and produce severe bronchospasm. Patients with asthma should not normally be treated with beta-blockers. ( 7.1 ) Diuretics : May worsen electrocardiographic changes or hypokalemia associated with diuretics may worsen. Consider monitoring potassium levels. ( 7.2 ) Digoxin : May decrease serum digoxin levels. Consider monitoring digoxin levels. ( 7.3 ) Monoamine oxidase inhibitors (MAOs) or tricyclic antidepressants : May potentiate effect of albuterol on the cardiovascular system. Consider alternative therapy in patients taking MAO inhibitors or tricyclic antidepressants. ( 7.4 ) 7.1 Beta-blockers Beta-blockers: Beta-adrenergic receptor blocking agents not only block the pulmonary effect of beta-adrenergic agonists, such as Levalbuterol tartrate HFA inhalation aerosol, but may produce severe bronchospasm in asthmatic patients. Therefore, patients with asthma should not normally be treated with beta-blockers. However, under certain circumstances, e.g., as prophylaxis after myocardial infarction, there may be no acceptable alternatives to the use of beta-adrenergic blocking agents in patients with asthma. In this setting, cardioselective beta-blockers should be considered, although they should be administered with caution. 7.2 Diuretics The ECG changes or hypokalemia that may result from the administration of non-potassium-sparing diuretics (such as loop and thiazide diuretics) can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded. Although the clinical significance of these effects is not known, caution is advised in the coadministration of beta-agonists with non-potassium-sparing diuretics. Consider monitoring potassium levels. 7.3 Digoxin Mean decreases of 16% to 22% in serum digoxin levels were demonstrated after single-dose intravenous and oral administration of racemic albuterol, respectively, to normal volunteers who had received digoxin for 10 days. The clinical significance of these findings for patients with obstructive airway disease who are receiving Levalbuterol tartrate HFA inhalation aerosol and digoxin on a chronic basis is unclear. Nevertheless, it would be prudent to carefully evaluate the serum digoxin levels in patients who are currently receiving digoxin and Levalbuterol tartrate HFA inhalation aerosol. 7.4 Monoamine Oxidase Inhibitors or Tricyclic Antidepressants Levalbuterol tartrate HFA inhalation aerosol should be administered with extreme caution to patients being treated...
Contraindications
4 CONTRAINDICATIONS Levalbuterol tartrate HFA inhalation aerosol is contraindicated in patients with a history of hypersensitivity to levalbuterol, racemic albuterol, or any other component of Levalbuterol tartrate HFA inhalation aerosol. Reactions have included urticaria, angioedema, rash, bronchospasm, anaphylaxis, and oropharyngeal edema. Hypersensitivity to levalbuterol, racemic albuterol or any other component of Levalbuterol tartrate HFA inhalation aerosol. ( 4 )
Pregnancy and Breastfeeding
8.1 Pregnancy Risk Summary There are no adequate and well-controlled studies of Levalbuterol tartrate HFA inhalation aerosol in pregnant women. There are clinical considerations with the use of Levalbuterol tartrate HFA inhalation aerosol 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 750 times the maximum recommended human daily inhalation dose (MRHDID) of levalbuterol tartrate 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 population(s) are unknown. In the U.S. general population, the estimated risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk 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 for gestational age in the neonate. Pregnant women should be closely monitored and medication adjusted as necessary to maintain optimal control. Labor or Delivery Because of the potential for beta-adrenergic agonists to interfere with uterine contractility, the use of Levalbuterol tartrate HFA inhalation aerosol for the treatment of bronchospasm during labor should be restricted to those patients in whom the benefits clearly outweigh the risk. Levalbuterol tartrate HFA inhalation aerosol has not been approved for the management of preterm labor. The benefit:risk ratio when levalbuterol tartrate is administered for tocolysis has not been established. Serious adverse reactions, including maternal pulmonary edema, have been reported...
Overdosage
10 OVERDOSAGE 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/minute, 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 tartrate HFA inhalation aerosol. Treatment consists of discontinuation of Levalbuterol tartrate HFA inhalation aerosol together with appropriate symptomatic therapy. The judicious use of a cardioselective 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 tartrate HFA inhalation aerosol.
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING Levalbuterol tartrate HFA inhalation aerosol is supplied as a pressurized aluminum canister in a box: NDC 0591-2927-54: Canister labeled with a net weight of 15 grams containing 200 metered actuations (or inhalations) Each canister is fitted with a dose indicator and is supplied with a blue plastic actuator mouthpiece, a red mouthpiece cap, and patient’s instructions. Shake well before using . Store between 20° and 25°C (68° and 77°F; see USP controlled room temperature). Protect from freezing temperatures and direct sunlight. Store inhaler with the actuator mouthpiece down. Contents under pressure Do not puncture or incinerate. Do not store near heat or open flame. Exposure to temperatures above 120°F may cause bursting. Never throw container into fire or incinerator. Keep out of reach of children. The blue actuator supplied with Levalbuterol tartrate HFA inhalation aerosol should not be used with any other product canisters. Actuators from other products should not be used with a Levalbuterol tartrate HFA inhalation aerosol canister. The correct amount of medication in each actuation cannot be assured after 200 actuations, even though the canister is not completely empty. When the dose indicator display window shows a red zone, approximately 20 inhalations are left, and a refill is required. The canister should be discarded when the dose indicator display window shows zero, indicating that 200 actuations have been used.
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.