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Xopenex Hfa
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- Active ingredient
- Levalbuterol Tartrate 45 µg
- Other brand names
- Dosage form
- Aerosol, Metered
- Route
- Oral
- Prescription status
- Rx (prescription)
- Pregnancy
- See Pregnancy Use Section
- Lactation
- See Lactation Use Section
- Marketed in the U.S.
- Since 2023
- Label revision date
- January 1, 2023
- FDA Insert
- Prescribing information, PDF file
- Active ingredient
- Levalbuterol Tartrate 45 µg
- Other brand names
- Dosage form
- Aerosol, Metered
- Route
- Oral
- Prescription status
- Rx (prescription)
- CSA schedule
- Not a scheduled drug
- Pregnancy
- See Pregnancy Use Section
- Lactation
- See Lactation Use Section
- Marketed in the U.S.
- Since 2023
- Label revision date
- January 1, 2023
- Manufacturer
- Praxis, LLC
- Registration number
- NDA021730
- NDC root
- 59368-411
- FDA Insert
- Prescribing information, PDF file
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Drug Overview
XOPENEX HFA is a medication that contains levalbuterol tartrate, which is a specific form of albuterol. It is primarily used to help relax the muscles in the airways, making it easier for you to breathe. This is particularly beneficial for individuals with conditions like asthma or chronic obstructive pulmonary disease (COPD), as it helps to relieve bronchospasm (tightening of the airway muscles).
Levalbuterol works by activating beta2-adrenergic receptors in the airway smooth muscle. This activation leads to a series of reactions that increase a substance called cyclic AMP, which ultimately relaxes the airway muscles and helps prevent breathing difficulties. XOPENEX HFA is delivered through a pressurized metered-dose inhaler, allowing you to inhale the medication directly into your lungs for quick relief.
Uses
Xopenex HFA (levalbuterol tartrate) is a medication used to help treat or prevent bronchospasm, which is a tightening of the muscles around the airways that can make it hard to breathe. This treatment is suitable for individuals aged 4 years and older who have reversible obstructive airway disease, a condition that can cause breathing difficulties.
Additionally, Xopenex HFA can be used to prevent bronchospasm that may occur during exercise, helping you stay active and breathe easier during physical activities.
Dosage and Administration
Before using XOPENEX HFA inhalation aerosol, make sure to shake the canister well. This medication comes in a pressurized aluminum canister that contains 200 metered actuations, which means you can take 200 individual inhalations from it.
To use it, you will inhale the medication through the blue plastic actuator mouthpiece. This method allows the medication to go directly into your lungs, where it can work effectively. Be sure to follow your healthcare provider's instructions on how often to use it for the best results.
What to Avoid
You should avoid using XOPENEX HFA if you are allergic to levalbuterol, racemic albuterol, or any of its ingredients. It's important to follow your doctor's instructions carefully; do not use this medication more often than prescribed, and never increase your dose without consulting your physician. Additionally, avoid using other inhaled or asthma medications unless directed by your doctor.
Be aware that abusing XOPENEX HFA can lead to serious risks, including cardiac arrest and even death. Always take care not to spray the medication in your eyes, and never puncture or incinerate the canister. Store the inhaler away from heat or open flames, and do not freeze it or dispose of it in a fire. Your safety is paramount, so please adhere to these guidelines.
Side Effects
You may experience some side effects while using this medication. Common reactions include nervousness, headache, dizziness, and fatigue. More serious symptoms can occur with an overdose, such as seizures, rapid heart rate (tachycardia), and even cardiac arrest, which can be life-threatening. If you notice any unusual symptoms like dry mouth, nausea, or tremors, it's important to consult your healthcare provider.
In children under 4 years old, there is a higher chance of experiencing asthma-related issues, such as increased coughing and difficulty breathing. Additionally, serious complications like maternal pulmonary edema have been reported in pregnant individuals using this medication for premature labor. Always discuss any concerns with your doctor to ensure safe use.
Warnings and Precautions
Using XOPENEX HFA can sometimes lead to unexpected breathing problems, known as paradoxical bronchospasm. If you experience sudden shortness of breath after using this medication, stop using it immediately and contact your doctor. It's important to use XOPENEX HFA only as directed; using it too often can cause serious heart or lung issues that may be life-threatening. Additionally, be aware of potential allergic reactions, which can include swelling of the face, throat, or tongue, hives, rash, or difficulty breathing. If you notice any of these symptoms, stop using the medication and call your doctor right away.
If you find that XOPENEX HFA is not working as well as it used to, or if your symptoms worsen, seek medical attention immediately. Pregnant or nursing individuals should consult their healthcare provider before using this medication. For those with kidney issues, monitoring renal function may be necessary. Always be vigilant about your health and don’t hesitate to seek emergency help if you experience serious side effects or worsening lung symptoms.
Overdose
If you take too much XOPENEX HFA, you may experience symptoms like rapid heart rate (tachycardia) of up to 200 beats per minute, seizures, chest pain (angina), high or low blood pressure (hypertension or hypotension), nervousness, headaches, tremors, dry mouth, nausea, dizziness, fatigue, and trouble sleeping. In some cases, low potassium levels (hypokalemia) can also occur. It's important to know that serious complications, including cardiac arrest and even death, can happen with misuse of this medication.
If you suspect an overdose, stop taking XOPENEX HFA immediately and seek medical help. Treatment typically involves managing the symptoms you experience. In some cases, a specific type of beta-blocker may be used, but be aware that this can cause breathing difficulties (bronchospasm). There is not enough evidence to suggest that dialysis is helpful for an overdose of this medication, so professional medical assistance is crucial. Always reach out to a healthcare provider or call emergency services if you feel unwell after taking this medication.
Pregnancy Use
There are currently no well-controlled studies on the use of XOPENEX HFA (levalbuterol) in pregnant women, so caution is advised. While studies in pregnant rabbits showed no signs of birth defects at high doses, other forms of albuterol have been linked to serious birth defects in animal studies. The general risk of major birth defects and miscarriage in the U.S. is estimated to be between 2-4% and 15-20%, respectively.
If you have asthma that is not well controlled during pregnancy, you may face increased risks such as preeclampsia and complications for your baby, including low birth weight. It's important to work closely with your healthcare provider to manage your asthma effectively. Additionally, XOPENEX HFA is not approved for use in managing preterm labor, and its safety for this purpose has not been established. Always discuss any medications with your doctor to weigh the benefits and risks during your pregnancy.
Lactation Use
If you are breastfeeding and considering the use of XOPENEX HFA, it's important to be aware that there are no well-controlled studies confirming its safety for nursing mothers. While the exact effects of this medication on breast milk have not been established, caution is advised when using it while breastfeeding. Always discuss any concerns or questions with your healthcare provider to ensure the best care for you and your baby.
Pediatric Use
If your child is 4 years old or older, XOPENEX HFA has been shown to be safe and effective for treating asthma in this age group based on clinical trials. However, it is important to note that XOPENEX HFA is not recommended for children under 4 years of age. In studies involving younger children, there was no significant benefit observed, and some experienced more asthma-related side effects compared to those who received a placebo (a treatment with no active medication).
For children under 4, the risks may outweigh the benefits, as some reported adverse reactions related to asthma were higher in those treated with XOPENEX HFA. If you have concerns about your child's asthma treatment, it's best to consult with your healthcare provider for appropriate options.
Geriatric Use
When considering the use of XOPENEX HFA for older adults, it's important to note that clinical studies did not include enough participants aged 65 and older to fully understand how they might respond compared to younger individuals. However, based on other clinical experiences, no significant differences in responses have been reported between older and younger patients.
For older adults, healthcare providers typically recommend starting at the lower end of the dosing range. This cautious approach is due to the higher likelihood of decreased liver (hepatic), kidney (renal), or heart (cardiac) function, as well as the presence of other health conditions or medications. Always consult with your healthcare provider to ensure the safest and most effective treatment plan tailored to your needs.
Renal Impairment
If you have kidney issues, it's important to be aware of how your condition can affect the use of certain medications, such as racemic albuterol. Studies have shown that while renal impairment (kidney problems) does not change how long the medication stays in your body (its half-life), it can significantly reduce how quickly your body clears the drug—by about 67%.
Because of this, you should be cautious when using high doses of XOPENEX HFA (a type of albuterol inhaler) if you have renal impairment. Always consult your healthcare provider for guidance on the appropriate dosage and monitoring while using this medication.
Hepatic Impairment
If you have liver problems, it's important to know that the effects of these conditions on how your body processes XOPENEX HFA (a medication used for breathing issues) have not been studied. This means that there is no specific information available about how your liver health might influence the effectiveness or safety of this medication.
Because of this uncertainty, it's crucial to talk to your healthcare provider about your liver condition before using XOPENEX HFA. They may recommend monitoring your health closely or adjusting your treatment plan to ensure your safety and well-being. Always follow their guidance to manage your health effectively.
Drug Interactions
It's important to talk to your healthcare provider about all the medications you are taking, as XOPENEX HFA can interact with other medicines. This means that XOPENEX HFA might change how other medications work, and vice versa. Be sure to inform your doctor if you are using other inhaled medicines, asthma treatments, heart medications, diuretics (which help increase urination), antidepressants, or medications for chronic obstructive pulmonary disease (COPD).
While using XOPENEX HFA, you should only take other inhaled drugs and asthma medications as directed by your physician. This helps ensure that all your treatments work effectively and safely together. Always keep an open line of communication with your healthcare provider about your medications and any changes in your health.
Storage and Handling
To ensure the safety and effectiveness of your inhaler, store it in a cool, dry place at a temperature between 20° and 25°C (68° and 77°F). It's important to protect it from freezing temperatures and direct sunlight. Always keep the inhaler with the actuator mouthpiece facing down, and avoid storing it near heat sources or open flames, as exposure to temperatures above 120°F can cause the canister to burst.
Handle the inhaler carefully—do not puncture or incinerate it, and never throw the container into a fire or incinerator. Keep the inhaler out of reach of children, and remember to discard the canister when the dose indicator shows zero, which means you have used all 200 actuations. Following these guidelines will help ensure your inhaler remains safe and effective for your use.
Additional Information
XOPENEX HFA is designed for oral inhalation only and typically works for 4 to 6 hours. It's important not to use it more often than recommended. Before using XOPENEX HFA, make sure to read the FDA-approved patient labeling for important instructions. Priming the inhaler is crucial to ensure you receive the correct amount of medication with each puff.
Be aware that using XOPENEX HFA can lead to serious side effects, such as paradoxical bronchospasm (a sudden tightening of the airways), which requires you to stop using the inhaler immediately if it occurs. Always follow your doctor's guidance regarding the use of other inhaled medications while using XOPENEX HFA. If you are pregnant or nursing, consult your physician before using this medication. Additionally, be cautious, as abusing XOPENEX HFA can lead to severe health risks, including cardiac arrest and death.
FAQ
What is XOPENEX HFA?
XOPENEX HFA is a medication that contains levalbuterol tartrate, which is used to treat or prevent bronchospasm in patients aged 4 years and older with reversible obstructive airway disease.
How does XOPENEX HFA work?
Levalbuterol tartrate is a selective beta2-adrenergic receptor agonist that relaxes airway smooth muscles, increasing cyclic AMP levels, which leads to muscle relaxation and inhibits the release of mediators from mast cells.
What is the recommended dosage for XOPENEX HFA?
After priming with 4 actuations, each actuation delivers 67.8 mcg of levalbuterol tartrate. The inhaler provides 200 actuations.
How should I use my XOPENEX HFA inhaler?
Shake the inhaler well before each use, inhale deeply while pressing down on the dose indicator, and hold your breath for 10 seconds if possible.
What should I do if I experience paradoxical bronchospasm?
If you experience paradoxical bronchospasm, discontinue use of XOPENEX HFA immediately and contact your doctor.
Are there any contraindications for using XOPENEX HFA?
Do not use XOPENEX HFA if you are allergic to levalbuterol, racemic albuterol, or any of its ingredients.
What are the potential side effects of XOPENEX HFA?
Possible side effects include tachycardia, nervousness, headache, tremor, and dry mouth. In severe cases, it may lead to cardiac arrest.
Can I use XOPENEX HFA during pregnancy?
There are no adequate studies of XOPENEX HFA in pregnant women, so consult your doctor if you are pregnant or planning to become pregnant.
How should I store XOPENEX HFA?
Store XOPENEX HFA between 20° and 25°C (68° and 77°F) and protect it from freezing and direct sunlight. Do not puncture or incinerate the canister.
What should I do if I miss a dose?
If you miss a dose, take it as soon as you remember. If it's almost time for your next dose, skip the missed dose and continue with your regular schedule.
Packaging Info
The table below lists all NDC Code configurations of Xopenex Hfa (levalbuterol tartrate), the U.S. brand-name prescription product. Columns show Packaging, Formulation Type, and Active Ingredient Strength.
Details | ||||
|---|---|---|---|---|
| Aerosol, Metered | 45 µg | ||
Product details Regulatory status — Marketed All current FDA data sets list this NDC as actively marketed. FDA record dates for this NDC:
Active ingredients
Inactive ingredients
| ||||
FDA Insert (PDF)
This is the full prescribing document for Xopenex Hfa, submitted to the U.S. Food and Drug Administration (FDA). It contains official information for healthcare providers, including how to use the medication, possible side effects, and safety warnings.
Description
The active component of XOPENEX HFA inhalation aerosol is levalbuterol tartrate, the (R)-enantiomer of albuterol, which acts as a relatively selective beta-2-adrenergic receptor agonist. Levalbuterol tartrate is chemically designated as (R)-α-[1,1-dimethylethyl)aminomethyl]-4-hydroxy-1,3-benzenedimethanol L-tartrate (2:1 salt), with a molecular weight of 628.71 and an empirical formula of (C13H21NO3)2·C4H6O6. This compound appears as a white to light-yellow solid, is freely soluble in water, and exhibits very slight solubility in ethanol.
XOPENEX HFA inhalation aerosol is delivered via a pressurized metered-dose inhaler (MDI) equipped with a dose indicator, producing an aerosol intended for oral inhalation. The formulation includes a suspension of micronized levalbuterol tartrate, propellant HFA-134a (1,1,1,2-tetrafluoroethane), Dehydrated Alcohol USP, and Oleic Acid NF. After priming the inhaler with four actuations, each actuation releases 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 contains sufficient formulation for 200 actuations.
Uses and Indications
Xopenex HFA (levalbuterol tartrate) is indicated for the treatment or prevention of bronchospasm in patients aged 4 years and older with reversible obstructive airway disease. Additionally, it is indicated for the prevention of exercise-induced bronchospasm.
Limitations of Use: There are no specific teratogenic or nonteratogenic effects associated with Xopenex HFA as per the available data.
Dosage and Administration
XOPENEX HFA inhalation aerosol is supplied in a pressurized aluminum canister containing 200 metered actuations (or inhalations). Prior to each use, the canister must be shaken well to ensure proper mixing of the medication.
The medication is administered via inhalation using the blue plastic actuator mouthpiece. Healthcare professionals should instruct patients to follow the recommended inhalation technique to achieve optimal delivery of the medication.
Contraindications
XOPENEX HFA is contraindicated in patients with a known allergy to levalbuterol, racemic albuterol, or any of the components of XOPENEX HFA.
The use of XOPENEX HFA is also contraindicated in situations where there is a risk of abuse, as it may lead to serious adverse effects, including cardiac arrest and death.
Patients should not use XOPENEX HFA more frequently than prescribed by their healthcare provider, nor should they increase the dosage or frequency without consulting their physician. The concurrent use of other inhaled or asthma medications is contraindicated unless directed by a healthcare professional.
Additionally, XOPENEX HFA should not be sprayed in the eyes, punctured, incinerated, or stored near heat or open flame. It must not be frozen or disposed of in a fire or incinerator.
Warnings and Precautions
XOPENEX HFA has the potential to induce paradoxical bronchospasm. Healthcare professionals should instruct patients to discontinue use immediately if they experience any signs of paradoxical bronchospasm. It is important to note that sudden shortness of breath may occur immediately following the administration of XOPENEX HFA.
Overuse of XOPENEX HFA can lead to serious cardiovascular or pulmonary complications, which may be fatal. Therefore, patients must be cautioned against exceeding the recommended dosage. In cases where patients notice a decrease in the effectiveness of XOPENEX HFA for symptomatic relief, experience worsening symptoms, or find themselves needing to use the medication more frequently than usual, they should seek medical attention without delay.
Serious allergic reactions, including but not limited to swelling of the face, throat, or tongue, hives, rash, or respiratory difficulties, may occur. Patients should be advised to call their healthcare provider and discontinue the use of XOPENEX HFA immediately upon experiencing any of these symptoms.
For patients who are pregnant or nursing, it is essential to consult with their healthcare provider regarding the use of XOPENEX HFA to ensure safety for both the patient and the child.
Monitoring renal function may be beneficial in patients with pre-existing renal impairment to prevent potential complications associated with the use of XOPENEX HFA.
In the event of serious side effects or worsening lung symptoms, patients should be instructed to seek emergency medical assistance promptly by contacting their healthcare provider or visiting the nearest hospital emergency room.
Side Effects
Patients may experience a range of adverse reactions associated with the use of XOPENEX HFA. Serious adverse reactions can occur, particularly in the context of overdosage, which may lead to symptoms indicative of excessive beta-adrenergic receptor stimulation. These symptoms include seizures, angina, hypertension or hypotension, tachycardia with rates reaching up to 200 beats per minute, arrhythmias, nervousness, headache, tremor, dry mouth, palpitations, nausea, dizziness, fatigue, malaise, and sleeplessness. Additionally, hypokalemia may occur, and there have been reports of cardiac arrest and even death associated with the abuse of XOPENEX HFA.
In pediatric patients, particularly those under the age of 4 years, there is an increased incidence of asthma-related adverse reactions when treated with XOPENEX HFA compared to placebo. In a clinical trial, 12% of subjects receiving XOPENEX HFA reported asthma-related adverse reactions, including asthma, cough, hypoxia, status asthmaticus, and tachypnea, compared to 4% in the placebo group. Notably, one subject in the XOPENEX HFA group discontinued treatment due to asthma, while no subjects in the placebo group did.
Pregnant patients may also experience serious adverse reactions, including maternal pulmonary edema, during or following treatment for premature labor with beta-2 agonists, such as racemic albuterol. It is essential for healthcare providers to monitor patients closely for these adverse reactions and to weigh the benefits against the potential risks when prescribing XOPENEX HFA.
Drug Interactions
XOPENEX HFA has the potential to influence the pharmacological effects of other medications, and conversely, other medications may alter the efficacy of XOPENEX HFA.
Patients are advised to inform their healthcare provider if they are concurrently using any of the following classes of medications:
Inhaled Medicines and Asthma Medications
The use of other inhaled drugs or asthma medications should be closely monitored and taken only as prescribed by a physician during the course of treatment with XOPENEX HFA.
Cardiovascular Medications
Heart medications may interact with XOPENEX HFA, necessitating careful consideration and monitoring by the healthcare provider.
Diuretics
Medications that increase urination (diuretics) may also have interactions with XOPENEX HFA. Patients should discuss their use with their healthcare provider to ensure safe and effective treatment.
Antidepressants
The concomitant use of antidepressants may affect the action of XOPENEX HFA. Patients should inform their healthcare provider about any antidepressants they are taking.
COPD Treatments
Patients receiving treatment for chronic obstructive pulmonary disease (COPD) should consult their healthcare provider regarding the use of XOPENEX HFA in conjunction with their COPD medications.
Overall, it is essential for patients to adhere to their healthcare provider's instructions regarding the use of XOPENEX HFA alongside other medications to avoid potential interactions and ensure optimal therapeutic outcomes.
Packaging & NDC
The table below lists all NDC Code configurations of Xopenex Hfa (levalbuterol tartrate), the U.S. brand-name prescription product. Columns show Packaging, Formulation Type, and Active Ingredient Strength.
Details | ||||
|---|---|---|---|---|
| Aerosol, Metered | 45 µg | ||
Product details Regulatory status — Marketed All current FDA data sets list this NDC as actively marketed. FDA record dates for this NDC:
Active ingredients
Inactive ingredients
| ||||
Pediatric Use
Pediatric patients 4 years of age and older have demonstrated established safety and efficacy for XOPENEX HFA in an adequate and well-controlled clinical trial. In contrast, XOPENEX HFA is not indicated for pediatric patients less than 4 years of age. A clinical trial involving 196 pediatric patients with asthma or reactive airway disease, including 68 patients aged birth to <2 years and 128 patients aged 2 to <4 years, showed no statistically significant difference in the primary efficacy endpoint between treatment groups.
The primary efficacy endpoint was the mean change in the Pediatric Asthma Caregiver Assessment (PACA) total score from baseline over a 4-week treatment period. The results indicated no statistical difference in PACA total score changes between XOPENEX HFA and placebo.
Safety data revealed an increased incidence of asthma-related adverse reactions in patients under 4 years treated with XOPENEX HFA compared to placebo, with 8 subjects reporting such reactions versus 3 in the placebo group. Additionally, one subject in the XOPENEX HFA group discontinued treatment due to asthma, while no subjects in the placebo group did. Other adverse reactions observed were consistent with those reported in the clinical trial population of patients aged 4 years and older.
Geriatric Use
Clinical studies of XOPENEX HFA did not include a sufficient number of subjects aged 65 and older to determine whether they respond differently from younger patients. However, other reported clinical experience has not identified significant differences in responses between elderly patients and their younger counterparts.
In general, dose selection for geriatric patients should be approached with caution. It is advisable to start at the low end of the dosing range, taking into account the increased likelihood of decreased hepatic, renal, or cardiac function, as well as the presence of concomitant diseases or other drug therapies. Careful monitoring of these patients is recommended to ensure safety and efficacy.
Pregnancy
There are no adequate and well-controlled studies of XOPENEX HFA in pregnant women. Clinical considerations regarding the use of XOPENEX HFA in this population should be taken into account see Clinical Considerations. Animal studies have shown that following oral administration of levalbuterol HCl to pregnant rabbits, there was no evidence of teratogenicity at doses up to 25 mg/kg/day, which is approximately 750 times the maximum recommended human daily inhalation dose (MRHDID) of levalbuterol tartrate for adults on a mg/m² basis. However, it is important to note that racemic albuterol sulfate has demonstrated teratogenic effects 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) is 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. Women with poorly or moderately controlled asthma may experience an increased risk of preeclampsia, as well as prematurity, low birth weight, and small for gestational age neonates. Therefore, pregnant women should be closely monitored, and medication should be adjusted as necessary to maintain optimal control.
Due to the potential for beta-adrenergic agonists to interfere with uterine contractility, the use of XOPENEX HFA for the treatment of bronchospasm during labor should be limited to those patients in whom the benefits clearly outweigh the risks. XOPENEX HFA has not been approved for the management of preterm labor, and 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 during or following treatment of premature labor with beta2-agonists, including racemic albuterol.
In developmental studies, the oral administration of levalbuterol HCl to pregnant New Zealand White rabbits during the period of organogenesis found no evidence of teratogenicity at doses up to 25 mg/kg/day. In a rat developmental study, a racemic albuterol sulfate (comprising approximately 50% levalbuterol)/HFA-134a formulation administered by inhalation did not produce any teratogenic effects at exposures approximately 160 times the MRHDID (on a mg/m² basis at a maternal dose of 10.5 mg/kg). However, other developmental studies with racemic albuterol sulfate resulted in teratogenic effects in mice and rabbits at doses slightly higher than the human therapeutic range. Specifically, in a rabbit development study, orally administered albuterol sulfate induced cranioschisis in 7 of 19 fetuses (37%) at approximately 1500 times the MRHDID (on a mg/m² basis at a maternal dose of 50 mg/kg). In a mouse developmental study, subcutaneously administered albuterol sulfate produced cleft palate formation in 5 of 111 (4.5%) fetuses at an exposure approximately 2 times the MRHDID for adults (on a mg/m² basis at a maternal dose of 0.25 mg/kg/day) and in 10 of 108 (9.3%) fetuses at approximately 20 times the MRHDID (on a mg/m² basis at a maternal dose of 2.5 mg/kg/day). Similar effects were not observed at approximately 0.2 times the MRHDID of levalbuterol tartrate for adults on a mg/m² basis (i.e., less than the therapeutic dose). Cleft palate also occurred in 22 of 72 (30.5%) fetuses from females treated subcutaneously with isoproterenol (positive control).
Lactation
There are no adequate and well-controlled studies of XOPENEX HFA in nursing mothers. Clinical considerations with the use of XOPENEX HFA in nursing mothers should be taken into account. The potential for excretion in breast milk has not been established. Caution should be exercised when administering XOPENEX HFA to nursing mothers.
Renal Impairment
In patients with renal impairment, the pharmacokinetics of racemic albuterol may be significantly altered. A study evaluating five subjects with creatinine clearance ranging from 7 to 53 mL/min demonstrated that while renal disease did not affect the half-life of racemic albuterol, there was a notable 67% decline in its clearance compared to healthy volunteers.
Given this substantial reduction in clearance, caution is advised when administering high doses of XOPENEX HFA to patients with reduced kidney function. Monitoring of these patients is recommended to ensure safe and effective use of the medication.
Hepatic Impairment
The effect of hepatic impairment on the pharmacokinetics of XOPENEX HFA has not been evaluated. Therefore, no specific dosage adjustments or monitoring requirements can be recommended for patients with compromised liver function. Caution should be exercised when prescribing XOPENEX HFA to this patient population, and clinical judgment should guide the decision-making process. Regular monitoring of liver function may be warranted in patients with known hepatic impairment to ensure safety and efficacy.
Overdosage
In cases of overdosage, the expected symptoms primarily reflect excessive stimulation of beta-adrenergic receptors. Healthcare professionals should be vigilant for the occurrence or exacerbation of symptoms typically associated with adverse reactions. These may include seizures, angina, hypertension or hypotension, tachycardia with rates reaching up to 200 beats per minute, arrhythmias, nervousness, headache, tremor, dry mouth, palpitations, nausea, dizziness, fatigue, malaise, and sleeplessness. Additionally, hypokalemia may also be observed.
Given the sympathomimetic nature of XOPENEX HFA, it is critical to note that severe outcomes such as cardiac arrest and even death can occur, particularly in instances of abuse.
Management of overdosage involves the immediate discontinuation of XOPENEX HFA, accompanied by appropriate symptomatic therapy tailored to the patient's clinical presentation. In certain cases, the judicious use of a cardioselective beta-receptor blocker may be considered; however, it is essential to recognize that such medications can potentially induce bronchospasm.
Currently, there is insufficient evidence to ascertain the efficacy of dialysis in the management of XOPENEX HFA overdosage. Therefore, healthcare professionals should proceed with caution and prioritize symptomatic treatment and monitoring.
Nonclinical Toxicology
No information is available regarding teratogenic effects associated with levalbuterol tartrate. Reproduction studies conducted with racemic albuterol sulfate in rats indicated no evidence of impaired fertility at oral doses up to 50 mg/kg/day, which is approximately 750 times the maximum recommended human dose on a mg/m² basis for adults.
Although specific carcinogenesis studies with levalbuterol tartrate have not been performed, racemic albuterol sulfate has been assessed for its carcinogenic potential. In a two-year study involving Sprague-Dawley rats, dietary administration of racemic albuterol sulfate resulted in a significant dose-related increase in the incidence of benign leiomyomas of the mesovarium at doses of 2 mg/kg/day and higher, which corresponds to approximately 30 times the maximum recommended human dose for adults and about 15 times for children on a mg/m² basis. Conversely, in an 18-month study with CD-1 mice and a 22-month study with golden hamsters, dietary administration of racemic albuterol sulfate did not demonstrate any evidence of tumorigenicity. The doses administered in the CD-1 mice study reached up to 500 mg/kg/day (approximately 3800 times the maximum recommended human dose for adults and about 1800 times for children on a mg/m² basis), while the doses in the golden hamster study were up to 50 mg/kg/day (approximately 500 times the maximum recommended human dose for adults and about 240 times for children on a mg/m² basis).
Levalbuterol HCl has been shown to be non-mutagenic in the Ames test and the CHO/HPRT Mammalian Forward Gene Mutation Assay. Additionally, it was not found to be clastogenic in the in vivo micronucleus test conducted in mouse bone marrow. Racemic albuterol sulfate also did not exhibit clastogenic properties in an in vitro chromosomal aberration assay using CHO cell cultures.
In terms of animal pharmacology and toxicology, the propellant HFA-134a was rapidly absorbed and eliminated in both animals and humans, with an elimination half-life ranging from 3 to 27 minutes in animals and 5 to 7 minutes in humans. The time to maximum plasma concentration and mean residence time were both extremely short, resulting in a transient presence of HFA-134a in the bloodstream without evidence of accumulation. Toxicological assessments in animals indicated that HFA-134a exhibited no detectable toxicological activity at exposure levels less than 380 times the maximum human exposure, based on AUC value comparisons. Observed toxicological effects at very high doses included ataxia, tremors, dyspnea, and salivation, which are similar to effects produced by structurally-related chlorofluorocarbons (CFCs) previously used in metered-dose inhalers.
Postmarketing Experience
Postmarketing experience has identified several common adverse effects associated with the use of inhaled beta-agonists. Reports indicate that patients may experience palpitations, chest pain, rapid heart rate, tremor, and nervousness. These events have been documented through voluntary reporting and surveillance programs.
Patient Counseling
Patients should be advised to read the FDA-approved patient labeling, which includes the Patient Information and Instructions for Use, to ensure they understand the proper use of XOPENEX HFA. It is important to inform patients that the action of XOPENEX HFA typically lasts for 4 to 6 hours, and they should not use the medication more frequently than recommended.
Healthcare providers should instruct patients not to increase the dose or frequency of doses of XOPENEX HFA without first consulting their physician. Patients must be made aware that if they find that treatment with XOPENEX HFA becomes less effective for symptomatic relief, if their symptoms worsen, or if they need to use the product more frequently than usual, they should seek medical attention immediately.
Priming the inhaler is essential to ensure appropriate levalbuterol content in each actuation. Patients should be instructed to shake the inhaler well before use and to prime XOPENEX HFA before using it for the first time or if it has not been used for more than 3 days. This can be done by releasing 4 test sprays into the air, away from the face.
To maintain proper dosing and prevent actuator orifice blockage, patients should be advised to wash the actuator in warm water and air-dry it thoroughly at least once a week. Detailed cleaning instructions are included in the FDA-approved patient labeling, which patients should be encouraged to review.
Patients should store the canister between 20° and 25°C (68° and 77°F), protecting it from freezing temperatures and direct sunlight. It is crucial to inform patients that XOPENEX HFA can produce paradoxical bronchospasm, and they should discontinue use immediately if this occurs.
While using XOPENEX HFA, patients should only take other inhaled drugs and asthma medications as directed by their physician. Additionally, common adverse effects associated with inhaled beta-agonists, such as palpitations, chest pain, rapid heart rate, tremor, and nervousness, should be communicated to patients to ensure they are aware of potential side effects.
Storage and Handling
The product is supplied in a canister format, with specific handling and storage requirements to ensure safety and efficacy. It should be stored at a controlled room temperature between 20° and 25°C (68° and 77°F), in accordance with USP guidelines. It is essential to protect the product from freezing temperatures and direct sunlight.
For optimal performance, the inhaler must be stored with the actuator mouthpiece facing down. Care should be taken to avoid puncturing or incinerating the canister, as well as keeping it away from heat sources and open flames. Exposure to temperatures exceeding 120°F may lead to bursting of the canister.
The container should never be disposed of in fire or incinerators. Additionally, it is crucial to keep the product out of reach of children. The canister must be discarded once the dose indicator display window shows zero, which indicates that all 200 actuations have been used.
Additional Clinical Information
XOPENEX HFA is indicated for oral inhalation use only, with an expected duration of action lasting 4 to 6 hours. Clinicians should advise patients not to exceed the recommended frequency of use. It is crucial for patients to read the FDA-approved patient labeling, which includes important instructions for use. Patients must be informed that priming the inhaler is essential to ensure the correct levalbuterol content in each actuation.
Patients should be cautioned about the potential for paradoxical bronchospasm, which may occur with XOPENEX HFA; if this happens, they should discontinue use immediately. Additionally, patients are advised to follow their physician's directions regarding the use of other inhaled drugs and asthma medications while using XOPENEX HFA. Pregnant or nursing patients should consult their physicians regarding the use of this medication. It is important to note that the abuse of XOPENEX HFA may be associated with serious adverse effects, including cardiac arrest and death.
FDA Insert (PDF)
This document is the official FDA-approved prescribing information for Xopenex Hfa as submitted by Praxis, LLC. It includes detailed information about indications, dosage, contraindications, warnings, and clinical pharmacology.