Levalbuterol Side Effects: What to Expect and When to Call Your Doctor

Levalbuterol (Xopenex, Xopenex HFA) is generally well-tolerated, but like all medications, it can cause side effects. Knowing what to expect — and which symptoms require immediate attention — helps you use it safely and confidently. This guide covers the full spectrum of levalbuterol side effects based on clinical data and prescribing information.

Why Does Levalbuterol Cause Side Effects?

Levalbuterol works by stimulating beta2-adrenergic receptors in your airways, causing the smooth muscle to relax and your airways to open. However, beta2 receptors are also found in other parts of the body — including the heart, blood vessels, and skeletal muscles — which is why levalbuterol can cause effects beyond just bronchodilation.

One reason some patients are prescribed levalbuterol instead of racemic albuterol is that the inactive S-enantiomer in albuterol may contribute to some side effects — levalbuterol, being the pure R-enantiomer, may theoretically cause fewer such effects at equivalent doses. In practice, most side effects are similar between the two drugs.

Common Side Effects of Levalbuterol

These side effects are generally mild and often improve after the first few uses or as your body adjusts:

Tremors (shakiness): One of the most common side effects, caused by beta2 receptor stimulation in skeletal muscle. Usually mild and short-lived.

Nervousness or anxiety: Feels similar to a caffeine rush. Common especially with higher doses or first-time use.

Headache: Reported in clinical trials; usually mild.

Dizziness: May occur, particularly shortly after inhalation.

Fast or pounding heartbeat (tachycardia/palpitations): Beta2 stimulation can affect the heart rate. Usually temporary.

Sore throat: Can occur with inhaler use due to direct deposition of medication.

Runny nose or nasal congestion: More common with HFA inhaler use.

Chest pain: Mild chest discomfort can occur; distinguish from cardiac chest pain (see serious side effects below).

Serious Side Effects: When to Call Your Doctor or 911

Seek immediate medical attention for any of the following:

Paradoxical bronchospasm: If your breathing gets WORSE immediately after using levalbuterol instead of better, stop using it and call your doctor or emergency services immediately. This is a rare but serious reaction.

Severe chest pain or irregular heartbeat: Significant cardiovascular effects require immediate evaluation. Call 911 if you experience severe chest pain, a racing or irregular heartbeat that doesn't improve, or feel faint.

Severe allergic reaction (anaphylaxis): Signs include hives, facial swelling (angioedema), severe rash, difficulty breathing, and throat swelling. Call 911 immediately.

Very high blood pressure: If your systolic BP is 180 or higher or diastolic is 120 or higher, seek medical attention.

Severe hypokalemia (low potassium): Symptoms include leg cramps, extreme weakness, muscle fluttering in the chest, or numbness/tingling. This is especially a risk if you're also on diuretics.

Need for more doses than usual: If your rescue inhaler is becoming less effective or you need it more frequently, this may signal worsening asthma or COPD and requires re-evaluation — not just more doses.

Side Effects in Children

Levalbuterol is not approved for children under 4 years (HFA inhaler) or under 6 years (nebulizer solution) due to increased risk of side effects including unusual fast breathing and worsening asthma. In approved age groups, children may experience tremors, nervousness, and rapid heart rate similar to adults. Unusual fast breathing in young children is a warning sign requiring immediate medical evaluation.

Tips to Minimize Side Effects

Use the lowest effective dose — don't take more than prescribed

Rinse your mouth after using the inhaler to reduce sore throat

Use a spacer with the HFA inhaler for better drug delivery to the lungs (reducing systemic absorption)

Inform your doctor about all medications you take — especially beta-blockers, diuretics, MAOIs, and digoxin

Levalbuterol vs. Albuterol: Are Side Effects Really Different?

One reason levalbuterol was developed was the hypothesis that the S-enantiomer of racemic albuterol might contribute to side effects. In clinical trials, the incidence of systemic beta-adrenergic adverse reactions (tremor, nervousness) was low and comparable across levalbuterol and placebo groups — and similar to albuterol. For most patients, the side effect profiles are clinically equivalent.

For more on drug interactions that can worsen side effects, see our guide on Levalbuterol drug interactions. If you need help finding Levalbuterol in stock near you, visit medfinder.com.