Levocetirizine: Information from Answers.com

Levocetirizine
Systematic (IUPAC) name

2-[2-[4-[(R)-(4-chlorophenyl)-phenyl-methyl] piperazin-1-yl]ethoxy]acetic acid
Identifiers
CAS number	130018-77-8
ATC code	R06AE09
PubChem	1549000
Chemical data
Formula	C₂₁H₂₅Cl N₂O₃
Mol. mass	388.888 g/mol
Pharmacokinetic data
Bioavailability	High
Protein binding	90%
Metabolism	Hepatic 14% CYP3A4
Half life	6 to 10 hours
Excretion	Renal and fecal
Therapeutic considerations
Pregnancy cat.	B(US)
Legal status	POM(UK) ℞-only(US)
Routes	Oral

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. 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.

It is claimed to be more effective and with fewer side effects than the second-generation drugs; however, this claim is not clearly supported by the available clinical literature.^{[citation needed]}

1 History and formulations
2 Side effects
3 Research
4 Availability
5 References

History and formulations

Levocetirizine was first launched in 2001 by Belgian pharmaceutical company UCB with the brand name Xyzal 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.

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.^[1]

Research

Latest research shows levocetirizine reduces asthma attacks by 70% in children.^[2]

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

^ XOZAL technical specifications booklet.
^ Pasquali, M (2006-09). "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. http://www.ncbi.nlm.nih.gov/pubmed/16961716.

Histaminergics

Receptor
Ligands

H₁	Agonists: 2-Pyridylethylamine • Betahistine • Histamine • HTMT • UR-AK49 Antagonists: 1st Generation: Alimemazine • Azatadine • Bamipine • Bepotastine • Bromazine • Brompheniramine • Buclizine • Carbinoxamine • Chlorcyclizine • Chloropyramine • Chlorothen • Chlorpheniramine • Chlorphenoxamine • Cinnarizine • Clemastine • Clobenzepam • Clocinizine • Cyclizine • Cyproheptadine • Dacemazine • Deptropine • Dexbrompheniramine • Dexchlorpheniramine • Dimetindene • Diphenhydramine • Diphenylpyraline • Doxylamine • Embramine • Etymemazine • Histapyrrodine • Hydroxyethylpromethazine • Hydroxyzine • Iproheptine • Isopromethazine • Isothipendyl • Meclizine • Mepyramine • Mequitazine • Methafurylene • Methapyrilene • Methdilazine • Moxastine • Niaprazine • Orphenadrine • Oxatomide • Oxomemazine • p-Methyldiphenhydramine • Pheniramine • Phenyltoloxamine • Promethazine • Pyrilamine • Pyrrobutamine • Setastine • Talastine • Thenalidine • Thenyldiamine • Thiazinamium • Thonzylamine • Tolpropamine • Tripelennamine • Triprolidine; 2nd Generation: Acrivastine • Antazoline • Astemizole • Azatadine • Azelastine • Bamipine • Cetirizine • Clemizole • Clobenztropine • Deptropine • Dimebon • Ebastine • Emedastine • Epinastine • Ketotifen • Levocabastine • Loratadine • Mebhydrolin • Mizolastine • Olopatadine • Phenindamine • Pimethixene • Pyrrobutamine • Rupatadine • Terfenadine • Thenalidine • Tritoqualine; 3rd Generation: Desloratadine • Fexofenadine • Levocetirizine; Miscellaneous: Tricyclic Antidepressants (Amitriptyline, Doxepin, Trimipramine, etc) • Tetracyclic Antidepressants (Mianserin, Mirtazapine, etc) • Serotonin Antagonists and Reuptake Inhibitors (Trazodone, Nefazodone) • Typical Antipsychotics (Chlorpromazine, Thioridazine, etc) • Atypical Antipsychotics (Clozapine, Olanzapine, Quetiapine, etc)

H₂	Agonists: Amthamine • Betazole • Dimaprit • Histamine • HTMT • Impromidine • UR-AK49 Antagonists: Cimetidine • Famotidine • Lafutidine • Metiamide • Niperotidine • Nizatidine • Ranitidine • Roxatidine

H₃	Agonists: α-Methylhistamine • Cipralisant • Histamine • Imetit • Immepip • Immethridine • Methimepip • Proxyfan Antagonists: A-349,821 • A-423,579 • ABT-239 • Betahistine • Burimamide • Ciproxifan • Clobenpropit • Conessine • GSK-189,254 • Impentamine • Iodophenpropit • JNJ-5,207,852 • MK-0249 • NNC-38-1,049 • SCH-79,687 • Thioperamide • Tiprolisant • VUF-5,681

H₄	Agonists: 4-Methylhistamine • Histamine • VUF-8,430 Antagonists: JNJ-7,777,120 • Thioperamide • VUF-6,002

Reuptake
Inhibitors

Plasmalemmal

.....

Vesicular

VMAT Inhibitors

Ibogaine • Reserpine • Tetrabenazine

Enzyme
Inhibitors

Anabolism

HDC Inhibitors

α-FMH • Brocresine • Catechin • Cyanidanol-3 • McN-A-1293 • ME • Meciadanol • Naringenin • Thiazol-4-yimethoxyamine • Tritoqualine • Zy-15,029

Catabolism

HNMT Inhibitors	Amodiaquine • BW-301U • Diphenhydramine • Harmaline • Metoprine • Quinacrine • SKF-91,488 • Tacrine

DAO Inhibitors	1,4-Diamino-2-butyne • Aminoguanidine

Others

Precursors	L-Histidine

Cofactors	Vitamin B6 (Pyridoxine, Pyridoxamine, Pyridoxal → Pyridoxal Phosphate)

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Levocetirizine

Contents

History and formulations

Side effects

Research

Availability

References