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| Clinical data | |
|---|---|
| Trade names | Xyzal, Levazyr, others |
| Other names | Levocetirizine dihydrochloride |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607056 |
| License data | |
| Routes of administration | By mouth |
| Drug class | Second generation antihistamines |
| ATC code | |
| Legal status | |
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| Pharmacokinetic data | |
| Bioavailability | High |
| Protein binding | 91–92%[2] |
| Metabolism | Minimal (less than 14%, primarilyCYP3A4)[2] |
| Eliminationhalf-life | 8 to 9 hours[2] |
| Excretion | Urine: 85%[2] Feces: 12.9%[2] |
| Identifiers | |
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| CAS Number | |
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| IUPHAR/BPS | |
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| UNII | |
| KEGG | |
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| ChEMBL | |
| PDB ligand | |
| CompTox Dashboard(EPA) | |
| Chemical and physical data | |
| Formula | C21H25ClN2O3 |
| Molar mass | 388.89 g·mol−1 |
| 3D model (JSmol) | |
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Levocetirizine, sold under the brand nameXyzal, among others, is a second-generationantihistamine used for the treatment ofallergic rhinitis (hay fever) and long-termhives of unclear cause.[3] It is less sedating than older antihistamines.[4] It is takenby mouth.[3]
Common side effects include sleepiness, dry mouth, cough, vomiting, and diarrhea.[3] Use inpregnancy appears safe but has not been well studied and use whenbreastfeeding is of unclear safety.[5] It is classified as a second-generation antihistamine and works by blockinghistamine H1-receptors.[6][3]
Levocetirizine was approved for medical use in the United States in 2007,[3] and is available as ageneric medication.[4] In 2023, it was the 158th most commonly prescribed medication in the United States, with more than 3 million prescriptions.[7][8]
Levocetirizine is used for allergic rhinitis.[9] This includes allergy symptoms such as watery eyes, runny nose, sneezing, hives, and itching.[10]
Levocetirizine is referred to as a non-sedating antihistamine as it does not enter the brain in significant amounts and is therefore unlikely to cause drowsiness. Cardiac safety with repolarization may be better than some other antihistamines, as levocetirizine does not significantlyprolong the QT interval in healthy individuals.[11][12][13] However, some people may still experience some slightsleepiness,headache,mouth dryness,lightheadedness, vision problems (mainlyblurred vision),palpitations andfatigue.[14]
On 16 May 2025, the U.S. Food and Drug Administration (FDA) issued a Drug Safety Communication regarding a rare but severe itching, known aspruritus, that can occur after discontinuing long-term use of levocetirizine or cetirizine. This itching has been reported in patients who used these medicines daily, typically for at least a few months and often for years, and did not experience itching before starting the medication.[15]
Levocetirizine is an antihistamine. It acts as aninverse agonist that decreases activity at histamine H1 receptors. This in turn prevents the release of other allergy chemicals and increases the blood supply to the area, providing relief from the typical symptoms of hay fever. Levocetirizine, (R)-(-)-cetirizine, is essentially achiral switch of (±)-cetirizine. This enantiomer, theeutomer, is more selective and the (S)-counterpart, thedistomer, is inactive.[16][17]
Chemically, levocetirizine is the active levorotaryenantiomer ofcetirizine, also called thel-enantiomer of cetirizine. It is a member of thediphenylmethylpiperazine group of antihistamines.[citation needed]
Levocetirizine was first launched in 2001 by the Belgian pharmaceutical companyUCB (Union Chimique Belge).[citation needed]
In January 2017, the USFood and Drug Administration approved an over-the-counter preparation.[18] Levocetirizine had previously received authorization by the FDA as a prescription drug in 2007, having already been brought to market throughout much of Europe.[citation needed] In India, a prescription-only drug containing levocetirizine hydrochloride andmontelukast is sold as Crohist MK.[citation needed]
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Preparations of levocetirizine are sold under the following brand names:
The variable efficacy and durability of response of different antihistamines arise from differing modulatory effects on the H(1)-receptor. Conclusion: These findings support both the short-term and long-term use of levocetirizine in the clinical management of allergic rhinitis. The World Health Organization (WHO) ARIA Guidelines (Allergic Rhinitis and its Impact on Asthma), recommend using a combination of a non-sedating antihistamine with a decongestant, or glucocorticosteroids for treating allergic rhinitis - with the order and combination of treatment depending on severity and duration of symptoms.
