Levocetirizine

Levocetirizine

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Systematic (IUPAC) name
2-[2-[4-[(R)-(4-chlorophenyl)-phenyl-methyl] piperazin-1-yl]ethoxy]acetic acid
Clinical data
Pregnancy category	US: B (No risk in non-human studies)
Routes of administration	Oral
Legal status
Legal status	UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Bioavailability	High
Protein binding	90%
Metabolism	Hepatic 14% CYP3A4
Biological half-life	6 to 10 hours
Excretion	Renal and fecal
Identifiers
CAS Number	130018-77-8
ATC code	R06AE09 (WHO)
PubChem	CID 1549000
IUPHAR/BPS	1214
Chemical data
Formula	C21H25ClN2O3
Molar mass	388.888 g/mol[[]]

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 L-enantiomer of the cetirizine racemate. 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.

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, although other studies have shown it to be more effective.

History and formulations

Levocetirizine was first launched in 2001 by Belgian pharmaceutical company UCB with the brand name Xyzal (pronounced /ˈzaɪzæl/) in Austria, Finland, France, Ireland, Netherlands, Portugal, Romania, United States, UK; Xuzal in Mexico; Xusal in Germany; and Xozal in Greece. In India, levocetirizine is marketed by GlaxoSmithKline under the brand name Vozet and Xyzal. On May 25, 2007, the United States Food and Drug Administration approved Xyzal, where it is co-marketed by Sanofi-Aventis.Torrent Pharma launched UVNIL in rural market of INDIA. It is also available as LEZYNCET 5 mg tablets through Unichem in India. In India, generic name of Lev-Cit 5mg is manufactured by VIP Pharmaceuticals. Also marketed in India by Croslands (Ranbaxy Laboratories Ltd.) under the brand name Teczine. It is marked in Egypt by BORG Pharma under the brand name 'Xaltec', Allear by western pharmaceuticals and levcet by marcryl. In Pakistan Levocetirizine was first launched in liquid formulation by Novartis Consumer Health Division by the name of T-Day Syrup.

It is available as 5 mg-strength tablets and a 0.5 mg/mL oral solution.

In Pakistan levocetirizine is available in liquid formulation as well with the name of OCITRA 2.5mg/5ml.

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.

Research

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

Availability

The drug is currently available on 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. As for 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 "LevoKast" tablets, marketed by [TTK Healthcare Ltd][1]. The "LevoKast" is a formulation of Levocetirizine Hydrochloride & Montelukast. The "LevoKast" is a Schedule 'H' Drug and can be taken on the prescription by a Registered Medical Practitioner only.

References

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