Levocetirizine

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Levocetirizine chemical structure
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 C21H25N2ClO3 
Mol. weight 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.

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Legal status

POM(UK)

Routes Oral

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.[citation needed]

Contents

[edit] History & formulations

Xyzal® was first launched in 2001 by Belgian pharmaceutical company UCB.

It is available as 5mg strength tablets and marketed under brand names Xyzal® in the United Kingdom or Xusal® in Europe.

[edit] 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 machnines. You should also make sure you know how this medicine affects you before you perform potentially hazardous activites.

[edit] Research

Latest research shows levoceterizine reduces asthma attacks by 70% in children.[1]

[edit] Availability

Although the drug is available in the U.S., and most countries of Europe, it comes at a higher price than second generation antihistamines and treatment with levoceterizine is costly in poorer countries of Eastern Europe.

[edit] External links

[edit] References

  1. ^ http://www.medicalnewstoday.com/medicalnews.php?newsid=48201/ levoceterizine prevents asthma


Antihistamines (primarily R06) edit
Aminoalkyl ethers:

Bromazine, Carbinoxamine, Clemastine, Chlorphenoxamine, Diphenylpyraline, Diphenhydramine, Doxylamine

Substituted alkylamines:

Brompheniramine, Chlorphenamine, Dexbrompheniramine , Dexchlorpheniramine, Dimetindene, Pheniramine, Talastine

Substituted ethylene diamines:

Chloropyramine, Histapyrrodine, Mepyramine, Methapyrilene

Phenothiazine derivatives:

Alimemazine, Hydroxyethylpromethazine, Isothipendyl, Mequitazine, Methdilazine, Oxomemazine, Promethazine

Piperazine derivatives:

Buclizine, Cetirizine, Chlorcyclizine, Cinnarizine, Cyclizine, Hydroxyzine, Levocetirizine, Meclozine, Oxatomide

Others for systemic use:

Acrivastine, Antazoline, Astemizole, Azatadine , Azelastine, Bamipine, Cyproheptadine, Deptropine, Desloratadine, Ebastine, Epinastine, Ketotifen, Loratadine, Mebhydrolin, Mizolastine, Phenindamine, Pimethixene, Pyrrobutamine, Rupatadine, Terfenadine, Triprolidine

For topical use:

Bamipine, Chloropyramine, Chlorphenoxamine, Clemastine, Dimetindene, Diphenhydramine, Isothipendyl, Mepyramine , Promethazine, Thenalidine

Antiallergic agents
excluding corticosteroids
:

Antazoline, Azelastine , Fexofenadine

Other antiallergics:

Emedastine, Epinastine, Ketotifen, Olopatadine

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