Which asthma medicine works best: albuterol or levalbuterol?
Both aim to open your airways, but they work in slightly different ways. Albuterol has been around for decades and contains two parts — one helps, but the other may sometimes worsen asthma. On the other hand, levalbuterol uses only the helpful part, offering smoother relief for some people.
Even though they work differently, studies show they improve symptoms about the same.
In this article, we’ll explore how albuterol and levalbuterol work, their effectiveness, side effects, and costs.
| 🔑 Key Takeaways ➤ Albuterol has two parts but one part can stay in your body longer and may sometimes make asthma worse. ➤ Levalbuterol uses only the helpful part of albuterol, so it works the same but may lower the risk of side effects. ➤ Studies show that both medicines improve breathing about the same amount for most people. ➤ Albuterol often costs less than levalbuterol, especially for inhalers and pills. ➤ Common side effects of both include shaking, headache, and fast heartbeat, but how often they happen can differ. ➤ Levalbuterol may work at a lower dose and might cause fewer changes in heart rate. |
Mechanism of Action
Albuterol opens the airways to help breathing, but one part of it (S-albuterol) can sometimes worsen asthma, while levalbuterol contains only the helpful part (R-albuterol) for safer breathing relief.
Mechanism of Action of Albuterol
Albuterol has been used for more than 40 years as a racemic mixture made of two isomers:
- (R)-albuterol, which is the active form
- (S)-albuterol, which was classically considered inert
When inhaled, racemic albuterol produces effects that can help improve asthma, such as amplifying the action of corticosteroids and reducing inflammatory mediators.
(S)-albuterol can actually create opposite effects. When patients inhale racemic albuterol, the (S)-albuterol stays in the bloodstream 12 times longer than the (R)-albuterol. This longer persistence raises concerns because it may lead to paradoxical effects — meaning unexpected worsening of asthma symptoms seen in some clinical cases.
Mechanism of Action of Levalbuterol
Levalbuterol is the single-isomer formulation of albuterol. It contains only the (R)-albuterol isomer, which is the therapeutically active part. Levalbuterol works by binding selectively to beta2-adrenergic receptors in the airways, which leads to relaxation of airway smooth muscle and dilation of the airways.
Levalbuterol has approximately 100 times greater affinity for the beta2 receptor than (S)-albuterol. Unlike the (S)-isomer, which was once thought to be inert but is now known to cause immune cell proliferation, cytokine production, and increased intracellular calcium (all of which can lead to bronchoconstriction), levalbuterol avoids these unwanted effects. (S)-albuterol lasts longer in plasma and lung tissue due to its slower metabolism and elimination, while levalbuterol clears faster, reducing the risk of adverse effects.
Efficacy
Albuterol and levalbuterol both improve asthma symptoms, with no clear difference in how well they work.
Clinical Efficacy of Albuterol
In a large review which included seven trials and 1,625 people, the researchers found no significant differences between albuterol and levalbuterol in respiratory rate, oxygen saturation, percentage change in FEV1, or asthma scores.
In another study, 129 children aged 2–14 with acute asthma were split between albuterol and levalbuterol. Results showed no difference in asthma scores, FEV1, number of nebulizations, breathing rate, oxygen levels, emergency department time, or hospital stays.
Another study showed that albuterol improved lung function over placebo with a peak FEV1 change, but this was not significantly better than levalbuterol. And in adults, one research found albuterol had similar bronchodilation as levalbuterol but at a lower cost.
Clinical Efficacy of Levalbuterol
One review showed no clear advantage. Across the seven trials, levalbuterol did not outperform albuterol in respiratory rate, oxygen levels, lung function, or asthma scores.
In the same study with children, levalbuterol didn’t lower asthma scores, reduce the number of treatments, shorten emergency stays, or lower hospitalization rates compared to albuterol.
The same study above also found that levalbuterol led to a peak FEV1 change. Importantly, no children on levalbuterol had less than a 10% change in FEV1, while 15.8% on albuterol and 30.3% on placebo did.
In a study with adults, it showed that levalbuterol 0.63 mg worked as well as albuterol 2.5 mg, suggesting it might achieve the same effect at a lower dose and possibly with fewer heart effects.
In a study in children aged 3–11 showed that levalbuterol and albuterol both improved lung function over placebo, but the highest FEV1 was seen with levalbuterol 1.25 mg. Another study also supported that lower doses of levalbuterol (0.31 mg) worked as well as higher doses of albuterol (1.25–2.5 mg), with less impact on heart rate and potassium levels.
Side Effects
Albuterol and levalbuterol can both cause side effects, but the specific symptoms and how often they happen can vary between the two medicines.
Albuterol Side Effects
Albuterol has a wide range of side effects, from mild to rare and serious.
Very common (10% or more):
- Tremor (up to 24.2%)
- Headache (up to 18.8%)
- Excitement (up to 20%)
- Nervousness (up to 15%)
Common (1–10%):
- Palpitations
- Tachycardia
- Migraine
- Dizziness
- Shakiness
- Emotional ups and downs
- Hyperkinesia
- Skin infections (1.7%)
- Pruritus
- Rash
- Urticaria
- Sweating
- Gastroenteritis
- Nausea
- Oropharyngeal pain
- Vomiting
- Urinary tract infection
- Muscle cramps
- Back pain
- Tenseness
- Asthma exacerbation (13%)
- Bronchitis
- Sinusitis
- Upper respiratory infections
Uncommon (0.1–1%):
- Somnolence
- Drowsiness
- Epigastric pain
- Stomach ache
- Loss of appetite
- Myalgia (muscle pain)
- Sleepiness
- Sleep disturbance
- Dilated pupils
- Conjunctivitis
Rare (0.01–0.1%):
- Myocardial ischemia
- Arrhythmias (atrial fibrillation, supraventricular tachycardia)
- Hallucinations
- Sore mouth
- Nephritis
Very rare (<0.01%):
- Cardiovascular collapse
- Thrombopenia
- Angioedema
- Bronchospasm
- Paradoxical bronchospasm
- Insomnia
Frequency not reported (but observed):
- Angina
- Hypertension
- Hypotension
- Altered taste
- Glossitis
- Tongue ulceration
- Mouth or throat irritation
- Weakness
- Pulmonary edema
Levalbuterol Side Effects
Levalbuterol has its own pattern of side effects.
Serious (need immediate medical help):
- Fast heartbeat
- Chest pain or tightness
- Dizziness
- Lightheadedness
- Fainting
- Troubled breathing
Overdose symptoms:
- Chest pain
- Irregular or fast heartbeat
- Dry mouth
- General illness
- Headache
- Impaired consciousness
- Seizures
- Nausea
- Nervousness
- Sleeplessness
- Sweating
- Tremor
More common (1–10%):
- Anxiety
- Body aches
- Chills
- Congestion
- Cough
- Fever
- Dry or sore throat
- Hoarseness
- Runny or stuffy nose
- Migraines
- Leg cramps
- Muscle tightness
- Loss of appetite
Less common:
- Skin blemishes
- Bloody nose
- Burning, dry, or itching eyes
- Cough with mucus
- Cramps
- Diarrhea
- Ear pain
- Excessive tearing
- Eye itch
- Heavy menstrual bleeding
- Muscle pain
- Night sweats
- Numbness or tingling in hands or legs
- Painful cold sores
- Pimples
- Stomach pain
- Vaginal yeast infection
- Weight loss
Other reported:
- Hypertension
- Tachycardia
- Arrhythmias (atrial fibrillation, supraventricular tachycardia)
- Metabolic changes (blood glucose, potassium)
- Metabolic acidosis
- Central nervous system stimulation
- Hyperesthesia
- Dyspepsia
- Gastroenteritis
- Vomiting
- Constipation
- Asthma
- Pharyngitis
- Bronchitis
- Sinusitis
- Asthma exacerbation
- Wheezing
- Acne
- Sweating
- Rash
- Urticaria
- Hematuria
- Dysmenorrhea
- Vaginal moniliasis
- Insomnia
Cost
According to CostPlusDrugs, albuterol and levalbuterol come in different forms and strengths, with albuterol generally costing less than levalbuterol.
Albuterol Cost Breakdown
| Product | Form | Strength | Quantity / Volume | Price | Retail Price | Savings |
| Albuterol HFA (Ventolin generic) | Inhaler | 90 mcg | 1 inhaler (18g) | $46.38 | $54.34 | $7.96 |
| Albuterol Sulfate (AccuNeb generic) | Nebulization solution | 0.63 mg/3mL | Box of 25 vials | $16.41 | $38.00 | $21.59 |
| Albuterol Sulfate (AccuNeb generic) | Nebulization solution | 1.25 mg/3mL | Pack (75 mL) | $17.54 | $44.27 | $26.73 |
| Albuterol Sulfate (Proventil generic) | Tablet | 2 mg (30 ct) | 30 tablets | $9.87 | $150.00 | $140.13 |
| Albuterol Sulfate (Proventil generic) | Tablet | 4 mg (30 ct) | 30 tablets | $9.89 | $159.00 | $149.11 |
| Albuterol Sulfate (Proventil generic) | Syrup | 2 mg/5mL | 473 mL bottle | $17.80 | $58.00 | $40.20 |
| Albuterol Sulfate (Proventil generic) | Nebulization solution | 0.083% | 90 mL pack | $12.75 | $52.92 | $40.17 |
| Albuterol Sulfate (Proventil generic) | Nebulization solution | 2.5 mg/0.5mL | Box of 30 vials | $20.10 | $40.00 | $19.90 |
Levalbuterol Cost Breakdown
| Product | Form | Strength | Quantity / Volume | Price | Retail Price | Savings |
| Levalbuterol HCl (Xopenex generic) | Nebulization solution | 0.63 mg/3mL | 30 x 3mL vials (90 mL) | $15.48 | $188.00 | $172.52 |
| Levalbuterol HCl (Xopenex generic) | Nebulization solution | 1.25 mg/3mL | 25 x 3mL vials (75 mL) | $18.86 | $199.00 | $180.14 |
Wrap Up
Albuterol contains two isomers, one that may stay longer in blood and sometimes cause issues. Levalbuterol uses only the helpful isomer, offering similar airway opening with fewer unwanted effects, such as tremor. Both work fast and improve airflow equally well; cost and side effects will guide your decision.
When picking between them, think about price and how your body reacts. Which matters more to you? If budget matters most, albuterol may suit you. If you want to reduce side effects, levalbuterol could be better. Talk to your doctor to match treatment to your needs.
Frequently Asked Questions
How quickly do they work?
They usually start working in about 15 minutes to help you breathe easier.
How long do the effects last?
The effects can last around 4 to 6 hours after a dose.
Can kids use them?
Yes! Albuterol can be used in babies and older, while levalbuterol is for kids 4 years and up.
Can I take these with other medicines?
Be careful with drugs like azithromycin or beta blockers. Always check with your doctor before mixing medicines.
Are they safe during pregnancy?
There’s no clear proof they’re safe, so they should only be used if really needed. Albuterol has been studied more in pregnancy.
Is levalbuterol a rescue inhaler?
Yes! It’s used for quick relief during an asthma attack or sudden breathing trouble.
Sources
- Ameredes, B. T., & Calhoun, W. J. (2009). Levalbuterol versus albuterol. Current Allergy and Asthma Reports, 9(5), 401–409. https://doi.org/10.1007/s11882-009-0058-6
- Jat, K. R., & Khairwa, A. (2013). Levalbuterol versus albuterol for acute asthma: A systematic review and meta-analysis. Pulmonary Pharmacology & Therapeutics, 26(2), 239–248. https://doi.org/10.1016/j.pupt.2012.11.003
- Dachs, R., Darby-Stewart, A., & Graber, M. A. (2008). Albuterol vs. levalbuterol for asthma treatment in children. American Family Physician, 77(9), 1214–1216. Retrieved from https://www.aafp.org/pubs/afp/issues/2008/0501/p1214.html
- Berger, W. E., Milgrom, H., Skoner, D. P., Tripp, K., Parsey, M. V., & Baumgartner, R. A.; Xopenex Pediatric Asthma Group. (2006). Evaluation of levalbuterol metered dose inhaler in pediatric patients with asthma: A double-blind, randomized, placebo- and active-controlled trial. Current Medical Research and Opinion, 22(6), 1217–1226. https://doi.org/10.1185/030079906X112534
- Nelson, H. S., Bensch, G., Pleskow, W. W., Reasner, D. S., Rollins, T. E., & Rubin, P. D. (1998). Improved bronchodilation with levalbuterol compared with racemic albuterol in patients with asthma. Journal of Allergy and Clinical Immunology, 102(6), 943–952. https://doi.org/10.1016/S0091-6749(98)70332-X
- Gawchik, S. M., Saccar, C. L., Noonan, M., Reasner, D. S., & DeGraw, S. S. (1999). The safety and efficacy of nebulized levalbuterol compared with racemic albuterol and placebo in the treatment of asthma in pediatric patients. Journal of Allergy and Clinical Immunology, 103(4), 615–621. https://doi.org/10.1016/S0091-6749(99)70473-4