Levocetirizine
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| Image:Levocetirizine vector.svg | |
| Levocetirizine
| |
| Systematic (IUPAC) name | |
| 2-[2-[4-[(R)-(4-chlorophenyl)-phenyl-methyl] piperazin-1-yl]ethoxy]acetic acid | |
| Identifiers | |
| CAS number | |
| ATC code | R06 |
| PubChem | |
| 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. |
B |
| Legal status | |
| Routes | Oral |
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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.[1]
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
nl:Levocetirizineth:ลีโวเซทิไรซีน
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
