Levocetirizine

Levocetirizine

File:Levocetirizine vector.svg
Clinical data
Pregnancy category	B
Routes of administration	Oral
ATC code	R06AE09 (WHO)
Legal status
Legal status	UK: POM (Prescription only)
Pharmacokinetic data
Bioavailability	High
Protein binding	90%
Metabolism	Hepatic 14% CYP3A4
Elimination half-life	6 to 10 hours
Excretion	Renal and fecal
Identifiers
IUPAC name 2-[2-[4-[(R)-(4-chlorophenyl)-phenyl-methyl] piperazin-1-yl]ethoxy]acetic acid
CAS Number	130018-77-8
PubChem CID	1549000
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C21H25ClN2O3
Molar mass	388.888 g/mol

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

File:Xyzal.jpg

Xyzal

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. Levocetirizine works by blocking histamine receptors. It does not prevent the actual release of histamine from mast cells, but prevents it binding to its 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 hayfever.

It is claimed to be more effective and with fewer side effects than the second generation drugs.

History & formulations

Levocetirizine was first launched in 2001 by Belgian pharmaceutical company UCB with the brand name Xyzal; in the UK, Ireland, Austria, France and The Netherlands Xuzal; in Mexico, and Xusal or Xozal elsewhere in Europe. In India, levocetirizine is marketed by GlaxoSmithKline under the brand name Vozet. Last May 2007, the United States Food and Drug Administration has approved Xyzal, where it is co-marketed by Sanofi-Aventis.

It is available as 5mg strength tablets.

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 or fatigue. It should be used with caution when working with machines. You should also make sure you know how this medicine affects you before you perform potentially hazardous activities.

Research

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

Availability

Although the drug was only authorized by the US FDA on 25 May 2007 U.S., it is already available in most European countries. Based on previous pricing patterns for new drugs, it will likely enter the market at a higher price than currently available third and second generation antihistamines.

References

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