Levocetirizine
Encyclopedia
Levocetirizine is a third-generation non-sedative antihistamine
Antihistamine
An H1 antagonist is a histamine antagonist of the H1 receptor that serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions...

, developed from the second-generation antihistamine cetirizine
Cetirizine
Cetirizine , a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.-Availability:...

. Chemically, levocetirizine is the active enantiomer
Enantiomer
In chemistry, an enantiomer is one of two stereoisomers that are mirror images of each other that are non-superposable , much as one's left and right hands are the same except for opposite orientation. It can be clearly understood if you try to place your hands one over the other without...

 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.

The manufacturers claim it to be more effective with fewer side effects
Adverse effect (medicine)
In medicine, an adverse effect is a harmful and undesired effect resulting from a medication or other intervention such as surgery.An adverse effect may be termed a "side effect", when judged to be secondary to a main or therapeutic effect. If it results from an unsuitable or incorrect dosage or...

 than the second-generation drugs; however, there have been no published studies supporting this assertion, although other studies have concluded it may be more effective.

History and formulations

Levocetirizine was first launched in 2001 by Belgian pharmaceutical company UCB
UCB (company)
UCB is a multinational biopharmaceutical manufacturing company headquartered in Brussels, Belgium.- History :UCB was founded on 18 January 1928 by Emmanuel Janssen, a Belgian businessman...

. It is sold under the brand name Xyzal (icon) in Austria, Finland, France, Ireland, Netherlands, Portugal, Romania, United States, South Africa and UK; Xuzal in Mexico; Xusal in Germany; and Xozal in Greece. In India, levocetirizine is marketed by GlaxoSmithKline
GlaxoSmithKline
GlaxoSmithKline plc is a global pharmaceutical, biologics, vaccines and consumer healthcare company headquartered in London, United Kingdom...

 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
Sanofi-Aventis
Sanofi S.A. is a multinational pharmaceutical company headquartered in Paris, France, the world's fourth-largest by prescription sales. Sanofi engages in the research and development, manufacturing and marketing of pharmaceutical products for sale principally in the prescription market, but the...

.Torrent Pharma launched UVNIL in rural market of INDIA. It is also available as LEZYNCET 5 mg tablets through Unichem in India. In India, generic name of Lev-Cit 5 mg is manufactured by VIP Pharmaceuticals. Also marketed in India by Croslands (Ranbaxy Laboratories Ltd.) under the brand name Teczine.
It is marked in Egypt by BORG Pharma under the brand name 'Xaltec', Allear by western pharmaceuticals and levcet by marcryl. In Pakistan Levocetirizine was first launched in liquid formulation by Novartis Consumer Health Division by the name of T-Day Syrup.

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 2.5 mg/5ml.

In Bangladesh levocetirizine is available in 5 mg tablet & 2.5 mg/ml Oral liquid formulation with the brand name of Alcet marketed by Healthcare Pharmaceuticals ltd and Seasonix marketed by Incepta Pharmaceuticals ltd.

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
Headache
A headache or cephalalgia is pain anywhere in the region of the head or neck. It can be a symptom of a number of different conditions of the head and neck. The brain tissue itself is not sensitive to pain because it lacks pain receptors. Rather, the pain is caused by disturbance of the...

, mouth dryness
Xerostomia
Xerostomia is the medical term for the subjective complaint of dry mouth due to a lack of saliva. Xerostomia is sometimes colloquially called pasties, cottonmouth, drooth, or doughmouth. Several diseases, treatments, and medications can cause xerostomia. It can also be exacerbated by smoking or...

, lightheadedness
Lightheadedness
Light-headedness is a common and often unpleasant sensation of dizziness and/or feeling that one may be about to faint, which may be transient, recurrent, or occasionally chronic. In some cases, the individual may feel as though his or her head is weightless. The individual may also feel as...

, vision problems (mainly blurred vision
Blurred vision
-Causes:There are many causes of blurred vision:* Use of atropine or other anticholinergics* Presbyopia -- Difficulty focusing on objects that are close. The elderly are common victims....

), palpitations and fatigue.

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. 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 LevoKast tablets, a formulation of levocetirizine hydrochloride and montelukast
Montelukast
Montelukast is a leukotriene receptor antagonist used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is usually administered orally...

. In India, LevoKast is a Schedule 'H' drug and can be taken on the prescription by a registered medical practitioner only. In Finland, the drug is sold over-the-counter.
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