Levosalbutamol, also known as levalbuterol, is a short-acting
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Trade names | Xopenex, other |
Other names | evalbuterol |
AHFS/Drugs.com | International Drug Names |
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Routes of administration | By mouth (tablets), inhalational (MDI) |
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Pharmacokinetic data | |
Metabolism | Hepatic |
Elimination half-life | 3.3–4 hours |
Excretion | Urinary |
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ECHA InfoCard | 100.113.688 |
Chemical and physical data | |
Formula | C13H21NO3 |
Molar mass | 239.315 g·mol−1 |
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The drug is the (R)-(−)-enantiomer of its prototype drug salbutamol. It is available in some countries in generic formulations from pharmaceutical companies including Cipla, Teva, and Dey, among others.
Medical use edit
Levosalbutamol's bronchodilator properties give it indications in treatment of COPD (chronic obstructive pulmonary disease, also known as chronic obstructive lung disease) and asthma. Like other bronchodilators, it acts by relaxing smooth muscle in the bronchial tubes, and thus shortening or reversing an acute "attack" of shortness of breath or difficulty breathing. Unlike some slower-acting bronchodilators, it is not indicated as a preventative of chronic bronchial constriction.
Comparison to salbutamol edit
A 2013 systematic review of the drug's use as a treatment for acute asthma found that it "was not superior to albuterol regarding efficacy and safety in subjects with acute asthma." The review concluded: "We suggest that levalbuterol should not be used over albuterol for acute asthma."[2] Levalbuterol is notably more costly.[4][5]
Adverse effects edit
Generally, levosalbutamol is well tolerated. Common mild side-effects include an elevated heart rate, muscle cramps, and gastric upset (including heartburn and diarrhea).[6]
Symptoms of overdose in particular include: collapse into a seizure; chest pain (possible precursor of a heart attack); fast, pounding heartbeat, which may cause raised blood pressure (hypertension); irregular heartbeat (cardiac arrhythmia), which may cause paradoxical lowered blood pressure (hypotension); nervousness and tremor; headache; dizziness and nausea/vomiting; weakness or exhaustion (medical fatigue); dry mouth; and insomnia.[6]
Rarer side effects may indicate a dangerous allergic reaction. These include: paradoxical bronchospasm (shortness of breath and difficulty breathing); skin itching, rash, or hives (urticaria); swelling (angioedema) of any part of the face or throat (which can lead to voice hoarseness), or swelling of the extremities.[6]
Pharmacology edit
Mechanism of action edit
Activation of
Levosalbutamol relaxes the smooth muscles of all airways, from the trachea to the terminal bronchioles. Increased cyclic AMP concentrations are also associated with the inhibition of the release of mediators from mast cells in the airways. Levosalbutamol acts as a functional agonist that relaxes the airway irrespective of the spasmogen involved, thereby protecting against all bronchoconstrictor challenges.
While it is recognized that
Approval and names edit
Levosalbutamol is the INN while levalbuterol is the USAN.
Levalbuterol was approved in the United States as a solution to be used with a nebulizer device in March 1999[7] and in March 2015 became available in a formulation with a metered-dose inhaler under the trade name Xopenex HFA (levalbuterol tartrate inhalation aerosol).[8]
See also edit
- Salbutamol — the racemic mixture containing both (R)-(−)- and (S)-(+)-enantiomers
References edit
- ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.
- ^ a b Jat KR, Khairwa A (April 2013). "Levalbuterol versus albuterol for acute asthma: a systematic review and meta-analysis". Pulmonary Pharmacology & Therapeutics. 26 (2): 239–248. doi:10.1016/j.pupt.2012.11.003. PMID 23207739.
- ^ Punj A, Prakash A, Bhasin A (November 2009). "Levosalbutamol vs racemic salbutamol in the treatment of acute exacerbation of asthma". Indian Journal of Pediatrics. 76 (11): 1131–1135. doi:10.1007/s12098-009-0245-4. PMID 20012785. S2CID 11566782.
- ^ Schreck DM, Babin S (November 2005). "Comparison of racemic albuterol and levalbuterol in the treatment of acute asthma in the ED". Am J Emerg Med. 23 (7): 842–7. doi:10.1016/j.ajem.2005.04.003. PMID 16291438.
- ^ Hendeles L, Hartzema A (September 2003). "Levalbuterol is not more cost-effective than albuterol for COPD". Chest. 124 (3): 1176, author reply 1176–8. doi:10.1378/chest.124.3.1176. PMID 12970057.
- ^ a b c American Society of Health-System Pharmacists (1 September 2010). "Levalbuterol Oral Inhalation". MedlinePlus. Bethesda, Maryland: U.S. National Library of Medicine, National Institutes of Health. Retrieved 7 January 2015.
- ^ "US label: levalbuterol hydrochloride Inhalation Solution" (PDF). FDA. January 2015. For updates and past labels, see FDA index page for NDA 020837.
- ^ "US label: levalbuterol tartrate inhalation aerosol" (PDF). FDA. February 2017. For updates and past labels, see FDA index page for NDA 021730.
External links edit
- "Levalbuterol". Drug Information Portal. U.S. National Library of Medicine.