Levalbuterol

Primary Uses

Levalbuterol is used to treat or prevent bronchospasm, a condition where the muscles in the airways tighten, making it difficult to breathe. It is commonly prescribed for people with reversible obstructive airway diseases, such as:

• Asthma
• Chronic obstructive pulmonary disease (COPD)

How It Helps

This medication is a bronchodilator that works by relaxing the muscles in the lungs to open up the airways. It is used to relieve or prevent symptoms such as:

• Wheezing
• Shortness of breath
• Coughing
• Chest tightness

Levalbuterol is often used as a rescue medication to provide quick relief when symptoms suddenly worsen. In some cases, it may be used before physical activity to prevent exercise-induced breathing difficulties.

How Levalbuterol Works

Levalbuterol is a type of medication known as a bronchodilator, specifically a short-acting beta-agonist. It works by directly affecting the muscles in the lungs to improve airflow.

Targeting the Airways

When levalbuterol is inhaled, it travels into the lungs and attaches to specific sites called beta-2 receptors. These receptors are located on the smooth muscles that wrap around the bronchial tubes, which are the airways in the lungs. Once the medication binds to these receptors, it signals the muscles to relax.

Relieving Bronchospasm

In conditions like asthma or chronic obstructive pulmonary disease (COPD), these airway muscles can tighten or spasm, making the airways narrow and difficult to breathe through. This is known as bronchospasm. By relaxing these muscles, levalbuterol helps to:

• Widen the airways, a process called bronchodilation
• Increase the amount of air that can flow into and out of the lungs
• Provide quick relief from wheezing, coughing, chest tightness, and shortness of breath

Levalbuterol is the chemically active part of albuterol. It is designed to target the lungs specifically to provide rapid relief during a sudden worsening of respiratory symptoms.

Common Side Effects

Many people using levalbuterol do not experience serious side effects. Common symptoms may include:

• Nervousness or shakiness (tremors)
• Headache or dizziness
• Sore throat, runny nose, or cough
• Nausea, vomiting, or diarrhea
• Muscle aches or pain
• Dry mouth

Serious Side Effects

Contact a healthcare provider immediately if you experience any of the following serious symptoms:

• Paradoxical bronchospasm: Sudden wheezing, chest tightness, or trouble breathing immediately after using the medication.
• Heart problems: Fast, pounding, or irregular heartbeat, or chest pain.
• Low potassium levels: Leg cramps, constipation, fluttering in the chest, increased thirst, or muscle weakness.
• High blood sugar: Increased urination, extreme thirst, or blurred vision.
• Allergic reactions: Rash, hives, itching, or swelling of the face, tongue, or throat.

Paradoxical Bronchospasm

Like other inhaled medicines, levalbuterol can cause paradoxical bronchospasm, which is a sudden worsening of shortness of breath and wheezing immediately after use. This condition can be life-threatening. If this occurs, the medication should be discontinued immediately and an alternative therapy should be sought.

Cardiovascular Effects

Levalbuterol may cause significant changes in pulse rate and blood pressure. It should be used with caution in people with heart-related conditions, including:

• Coronary artery disease
• Heart rhythm disorders (arrhythmias)
• High blood pressure (hypertension)

Allergic Reactions

Immediate hypersensitivity reactions can occur. Signs of an allergic reaction may include skin rash, hives, swelling of the face or throat, and difficulty breathing. This medication is contraindicated in patients with a history of hypersensitivity to levalbuterol or racemic albuterol.

Medical Monitoring and Other Conditions

Caution is advised for individuals with certain underlying health issues, as the medication may worsen these conditions or require closer monitoring:

• Convulsive disorders: Such as epilepsy.
• Hyperthyroidism: Overactive thyroid.
• Diabetes: Inhaled beta-agonists may increase blood glucose levels.
• Low potassium: The drug may cause a decrease in serum potassium levels (hypokalemia), which can lead to adverse cardiovascular effects.

Asthma Deterioration

Asthma may deteriorate acutely over a period of hours or chronically over several days. If a patient requires more frequent doses of levalbuterol than usual, it may be a sign of destabilized asthma and requires a medical evaluation of the treatment plan.

Pregnancy

There are no adequate and well-controlled studies of levalbuterol use in pregnant women. While animal studies on related medications have shown potential risks at very high doses, it is unknown if levalbuterol causes harm to a human fetus. Healthcare providers typically only prescribe this medication during pregnancy if the clinical benefit to the mother outweighs the potential risk to the fetus.

Labor and Delivery

Levalbuterol belongs to a class of drugs that may interfere with uterine contractions. Because of this potential effect, its use during labor and delivery is generally restricted to cases where it is clearly necessary for the mother's respiratory health.

Breastfeeding

It is currently unknown whether levalbuterol passes into human breast milk. Because many drugs are excreted in human milk and there is a potential for adverse reactions in nursing infants, caution is recommended. Patients should consult their doctor to decide whether to continue breastfeeding or stop using the medication, based on the importance of the treatment to the mother's health.

Available Forms

Levalbuterol is administered by inhalation and is available in the following delivery formats:

• Inhalation Solution: This liquid form is intended for use with a standard jet nebulizer connected to an air compressor. It is typically supplied in unit-dose vials.
• Metered-Dose Inhaler: This is a pressurized aerosol device that delivers the medication as a spray for oral inhalation.

FDA Approval Status

Levalbuterol was first approved by the U.S. Food and Drug Administration (FDA) in 1999 as an inhalation solution for use with a nebulizer. A metered-dose inhaler (MDI) formulation was later approved in 2005. It is available only with a prescription from a healthcare provider and is not sold over-the-counter.

Approved Indications

The FDA has approved levalbuterol for the treatment or prevention of bronchospasm in individuals with reversible obstructive airway disease. The approved age groups depend on the specific formulation used:

• Inhalation Solution: Generally approved for use in adults and children 6 years of age and older.
• Metered-Dose Inhaler: Approved for use in adults and children 4 years of age and older.

Regulatory Oversight and Safety

There are currently no boxed warnings or Risk Evaluation and Mitigation Strategies (REMS) associated with levalbuterol. The FDA continues to monitor the safety of the medication through the FDA Adverse Event Reporting System (FAERS). In 2018, the FDA identified a potential signal of serious risk regarding vocal cord dysfunction associated with levalbuterol. Such signals are part of routine surveillance to determine if further investigation or changes to product labeling are necessary to ensure patient safety.

Using the Inhaler

Levalbuterol is available as a metered-dose inhaler (MDI) that delivers the medication directly into the lungs. To ensure the correct dose is received, the inhaler must be used properly. It is important to shake the inhaler well before each use.

Priming the Device

Before using a new inhaler for the first time, or if the inhaler has not been used for more than three days, it must be primed. Priming involves spraying the medication into the air, away from the face. For levalbuterol, this usually requires four test sprays.

Administration Steps

• Remove the cap and check the mouthpiece for any foreign objects.
• Exhale completely through the mouth.
• Place the mouthpiece in the mouth and close the lips around it.
• While breathing in deeply and slowly, press down firmly on the top of the canister to release one puff of medication.
• Hold your breath for about 10 seconds, then breathe out slowly.
• If a second puff is prescribed, wait at least one minute before repeating the steps.

Cleaning and Maintenance

To prevent the inhaler from clogging, the plastic actuator should be cleaned at least once a week. Remove the canister and rinse the plastic mouthpiece with warm running water for at least 30 seconds. Allow the actuator to air dry completely before reassembling the device. Do not get the metal canister wet.

Storage and Safety

The inhaler canister is pressurized and should be kept away from open flames or high heat. Do not puncture or burn the canister, even if it appears empty. Keep track of the number of sprays used to ensure the inhaler is replaced before it runs out of medication.