Levocetirizine
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| Trade names | Xyzal, Levazyr |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607056 |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Bioavailability | High |
| Protein binding | 90% |
| Metabolism | Hepatic 14% CYP3A4 |
| Biological half-life | 6 to 10 hours |
| Excretion | Renal and fecal |
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| Formula | C21H25ClN2O3 |
| Molar mass | 388.888 g/mol |
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Levocetirizine (as levocetirizine dihydrochloride) is a third-generation, non-sedating antihistamine, developed from the second-generation antihistamine cetirizine. Chemically, levocetirizine is the active enantiomer of cetirizine. It is the R-enantiomer of the cetirizine. Levocetirizine is an inverse agonist that decreases activity at histamine H1 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 hay fever. It does not prevent the actual release of histamine from mast cells.
The manufacturers claim it to be more effective with fewer side effects than previous second-generation drugs; however, there have been no published studies supporting this assertion. A study part-funded by the manufacturer UCB concluded it may be more effective than some other second- and third-generation anti-histamines, but didn't compare it to cetirizine.
Levocetirizine was first launched in 2001 by Belgian pharmaceutical company UCB.
It is sold under the following brand names:
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.
The drug is currently available by prescription in the United States. On 31 January 2017, the Food and Drug Administration approved Xyzal as an over-the-counter drug. Although the drug was only authorized by the FDA on 25 May 2007, it was already available in most European countries. Like 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 Crohist MK tablets and syrup, a formulation of levocetirizine hydrochloride and montelukast. In India, Crohist MK is a Schedule 'H' drug and may only be prescribed by a registered medical practitioner. In Finland, Hungary, China, The United States and Kuwait the drug is sold over-the-counter.
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Wikipedia