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20-September-2008 09:55:57 - Levocetirizine Levocetirizine Systematic IUPAC name 2-2-4-R-4-chlorophenyl-phenyl-methyl piperazin-1-ylethoxyacetic acid Identifiers CAS number 130018-77-8 ATC code R06AE09 PubChem 1549000 Chemical data Formula C21H25ClN2O3 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. BUS Legal status POMUK ℞-onlyUS Routes Oral Xyzal 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; however, this claim is not clearly supported by the available clinical literature.citation needed Contents 1 History formulations 2 Side Effects 3 Research 4 Availability 5 References History formulations Levocetirizine was first launched in 2001 by Belgian pharmaceutical company UCB with the brand name Xyzal in the UK, Ireland, Austria, France, The Netherlands and Romania, Xuzal in Mexico, and Xusal in Germany and Xozal in Greece. In India, levocetirizine is marketed by GlaxoSmithKline under the brand name Vozet. On May 25, 2007, the United States Food and Drug Administration 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, 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 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 ^ 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. v d e Histamine antagonists H1 or non-selective Alkylamines Bepotastine Bamipine Brompheniramine Chlorpheniramine Dexbrompheniramine Dexchlorpheniramine Dimethindene Metron S Pheniramine Pyrrobutamine Talastine Thenaldine Tolpropamine Triprolidine Ethanolamines Aminoalkyl ethers Bietanautine Bromazine/Bromodiphenhydramine Carbinoxamine Chlorphenoxamine Clemastine Diphenylpyraline Diphenhydramine Doxylamine Embramine p-Methyldiphenhydramine Moxastine Orphenadrine Phenyltoloxamine Setastine Ethylenediamines Chloropyramine Chlorothen Histapyrrodine Methafurylene Mepyramine Methapyrilene Pyrilamine Talastine Thenyldiamine Thonzylamine Tripelennamine Pyribenzamine Phenothiazine Tricyclics Ahistan Etymemazine Hydroxyethylpromethazine Isopromethazine Isothipendyl Mequitazine Methdilazine Oxomemazine Promethazine Thiazinamium Other Tricyclics Azatadine Clobenzepam Cyproheptadine Deptropine Isothipendyl Loratidine Piperazine Buclizine Chlorcyclizine Cinnarizine Clocinizine Hydroxyzine Niaprazine Oxatomide Benzhydryl compounds Cyclizine, Meclizine Others including selective, 2nd gen, 3rd gen Antazoline Astemizole Azatadine Azelastine Bepottastine Bamipine Cetoxine Clemizole Clobenztropine Deptropine Desloratadine Dimebon Ebastine Emedastine Epinastine Ketotifen Levocabastine Loratadine Mebhydrolin Mizolastine Phenindamine Pimethixene Pyrrobutamine Rupatadine Thenalidine Tritoqualine Alkylamine Acrivastine Tricyclic Olopatadine Piperazine Levocetirizine, Cetirizine Benzhydryl compounds Fexofenadine, Terfenadine H2 Cimetidine Famotidine Ranitidine Roxatidine Lafutidine Niperotidine Nizatidine H3 A-349,821 ABT-239 Burimamide Ciproxifan Clobenpropit Conessine Impentamine Iodophenpropit Thioperamide VUF-5681 H4 JNJ 7777120 Thioperamide VUF-6002 Retrieved from http://en..org/wiki/Levocetirizine Categories: H1 receptor antagonists | Carboxylic acids | Organochlorides | Aromatic compoundsHidden categories: All articles with statements | Articles with statements since February 2007 Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Español Français Nederlands Polski ไทย This page was last modified on 25 June 2008, at 05:51
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