Levocetirizine, sold under the brand name Xyzal among others, is an antihistamine used for the treatment of allergic rhinitis and long term hives of unclear cause. It is less sedating than older antihistamines. It is taken by mouth. Common side effects include sleepiness, dry mouth, cough, vomiting, and diarrhea. Use in pregnancy appears safe but has not been well studied and use when breastfeeding is of unclear safety. It is classified as a second-generation antihistamine and works by blocking histamine H1-receptors. Levocetirizine was approved for medical use in the United States in 2007. It is available as a generic medication. In 2017, it was the 175th most commonly prescribed medication in the United States, with more than three million prescriptions.
Medical uses
Levocetirizine is used for allergic rhinitis. This includes allergy symptoms such as watery eyes, runny nose, sneezing, hives, and itching.
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. Cardiac safety with repolarization may be better than some other antihistamines, as levocetirizine does not significantly prolong the QT interval in healthy individuals. However, some people may still experience some slight sleepiness, headache, mouth dryness, lightheadedness, vision problems, palpitations and fatigue.
Pharmacology
Levocetirizine is an antihistamine. It acts as an inverse agonist that decreases activity at histamine H1 receptors. This in turn prevents the release of other allergy chemicals and increase the blood supply to the area, and provides relief from the typical symptoms of hay fever.
Chemistry
Chemically, levocetirizine is the active levorotary enantiomer of cetirizine, also called the l-enantiomer of cetirizine. It is a member of the diphenylmethylpiperazine group of antihistamines.
History
Levocetirizine was first launched in 2001 by Belgian pharmaceutical company UCB.
Society and culture
Availability
On 31 January 2017, the Food and Drug Administration approved an over-the-counter version. Although the drug was authorized by the FDA in 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.
Brand names
Levocetirizine is sold under the following brand names:
Xyzal in Australia, Austria, Bulgaria, Croatia, Czech Republic, Finland, France, India, Ireland, Italy, Japan, Lithuania, Netherlands, Poland, Portugal, Romania, Taiwan, Thailand, Turkey, The Philippines, Serbia, Singapore, Slovakia, Slovenia, South Africa and UK. On May 25, 2007, the United States Food and Drug Administration approved Xyzal, where it is co-marketed by Sanofi-Aventis.
Levobert in India
Xusal in Germany, Mexico
Xozal in Greece
Xazal in Spain
Allevo in Egypt
In Hungary it is marketed as Zilola, Histisynt and Xyzal.
In Bangladesh, levocetirizine available as Alcet by Healthcare pharma, Curin by Beximco pharma and Seasonix by Incepta.
