Ball-and-stick model of the levocetirizine molecule
Clinical data
Trade names Xyzal, Levazyr
AHFS/Drugs.com Monograph
MedlinePlus a607056
  • US: B (No risk in non-human studies)
Routes of
ATC code R06AE09 (WHO)
Legal status
Legal status
Pharmacokinetic data
Bioavailability High
Protein binding 90%
Metabolism Hepatic 14% CYP3A4
Biological half-life 6 to 10 hours
Excretion Renal and fecal
CAS Number 130018-77-8 N
PubChem (CID) 1549000
ChemSpider 1266001 YesY
KEGG D07402 YesY
Chemical and physical data
Formula C21H25ClN2O3
Molar mass 388.888 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

Levocetirizine (as levocetirizine dihydrochloride) is a third-generation non-sedative antihistamine, developed from the second-generation antihistamine cetirizine. Chemically, levocetirizine is the active enantiomer of cetirizine. It is the R-enantiomer of the cetirizine racemate. Levocetirizine is an inverse agonist that decreases activity at histamine H1 receptors. This in turn prevents the release of other allergy chemicals and increased blood supply to the area, and provides relief from the typical symptoms of hay fever. It does not prevent the actual release of histamine from mast cells.

The manufacturers claim it to be more effective with fewer side effects than the second-generation drugs; however, there have been no published studies supporting this assertion. A study part-funded by the manufacturer UCB concluded it may be more effective than some other second- and third-generation anti-histamines, but didn't compare it to cetirizine.[1]


Levocetirizine was first launched in 2001 by Belgian pharmaceutical company UCB.

Brand names

It is sold under the brand names:

Side effects

Levocetirizine is called a non-sedating antihistamine as it does not enter the brain in significant amounts, and is therefore unlikely to cause drowsiness. However, some people may experience some slight sleepiness, headache, mouth dryness, lightheadedness, vision problems (mainly blurred vision), palpitations and fatigue.[4]


Latest research shows levocetirizine reduces asthma attacks by 70% in children.[5]


The drug is currently available by prescription in the United States. Although the drug was only authorized by the FDA on 25 May 2007, it was already available in most European countries. Like many new drugs it entered the market at a higher price than currently available third and second generation antihistamines. In India, one form of the drug is available as Crohist MK tablets and syrup, a formulation of levocetirizine hydrochloride and montelukast. In India, Crohist MK is a Schedule 'H' drug and may only be prescribed by a registered medical practitioner. In Finland, Hungary, China, and Kuwait[6] the drug is sold over-the-counter.

Different brands (Actavis, Glenmark, UCB) Levocetirizine tablets and oral solution.


  1. Grant, JA; Riethuisen, JM; Moulaert, B; DeVos, C; Gamalero, C.; Descalzi, D.; Folli, C.; Passalacqua, G.; Canonica, G.W. (February 2002). "A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjects". Ann Allergy Asthma Immunol. 88 (2): 190–197. doi:10.1016/S1081-1206(10)61995-3. PMID 11868924.
  2. https://web.archive.org/web/20121022184859/http://beximco-pharma.com/allergic-disorders/147-curin.html. Archived from the original on October 22, 2012. Retrieved August 29, 2012. Missing or empty |title= (help)
  3. http://www.fass.se/LIF/substance?substanceId=ID11EHWRUFGBA53CSR
  4. XOZAL technical specifications booklet.
  5. Pasquali, M; Baiardini, I; Rogkakou, A; Riccio, AM; Gamalero, C; Descalzi, D; Folli, C; Passalacqua, G; Canonica, GW (September 2006). "Levocetirizine in persistent allergic rhinitis and asthma: effects on symptoms, quality of life and inflammatory parameters". Clinical & Experimental Allergy. 36 (9): 1161–7. doi:10.1111/j.1365-2222.2006.02548.x. PMID 16961716.
  6. On different names: http://www.hazipatika.com/gyogyszerkereso/termek/sefaller_5_mg_filmtabletta/54120
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