Loading AI tools
Antihistamine drug From Wikipedia, the free encyclopedia
Levocetirizine, sold under the brand name Xyzal, among others, is a second-generation antihistamine used for the treatment of allergic rhinitis (hay fever) and long-term hives of unclear cause.[3] It is less sedating than older antihistamines.[4] It is taken by mouth.[3]
| |
 | |
| Clinical data | |
|---|---|
| Trade names | Xyzal, Levazyr, others |
| Other names | Levocetirizine dihydrochloride |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607056 |
| License data | |
| Routes of administration | By mouth |
| Drug class | Second generation antihistamines |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | High |
| Protein binding | 91–92%[2] |
| Metabolism | Minimal (less than 14%, primarily CYP3A4)[2] |
| Elimination half-life | 8 to 9 hours[2] |
| Excretion | Urine: 85%[2] Feces: 12.9%[2] |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| IUPHAR/BPS | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| PDB ligand | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C21H25ClN2O3 |
| Molar mass | 388.89 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
  (what is this?) (verify) | |
Common side effects include sleepiness, dry mouth, cough, vomiting, and diarrhea.[3] Use in pregnancy appears safe but has not been well studied and use when breastfeeding is of unclear safety.[5] It is classified as a second-generation antihistamine and works by blocking histamine H1-receptors.[6][3]
Levocetirizine was approved for medical use in the United States in 2007,[3] and is available as a generic medication.[4] In 2022, it was the 152nd most commonly prescribed medication in the United States, with more than 3 million prescriptions.[7][8]
Levocetirizine is used for allergic rhinitis.[9] This includes allergy symptoms such as watery eyes, runny nose, sneezing, hives, and itching.[10]
Levocetirizine is referred to as 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.[11][12][13] However, some people may still experience some slight sleepiness, headache, mouth dryness, lightheadedness, vision problems (mainly blurred vision), palpitations and fatigue.[14]
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 increases the blood supply to the area, providing relief from the typical symptoms of hay fever. Levocetirizine, (R)-(-)-cetirizine, is essentially a chiral switch of (±)-cetirizine. This enantiomer, the eutomer, is more selective and the (S)-counterpart, the distomer, is inactive.[15][16]
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.[citation needed]
Levocetirizine was first launched in 2001 by the Belgian pharmaceutical company UCB (Union Chimique Belge).[citation needed]
In January 2017, the US Food and Drug Administration approved an over-the-counter preparation.[17] Levocetirizine had previously received authorization by the FDA as a prescription drug in 2007, having already been brought to market throughout much of Europe.[citation needed] In India, a prescription-only drug containing levocetirizine hydrochloride and montelukast is sold as Crohist MK.[citation needed]
 | This section needs additional citations for verification. (July 2020) |
Preparations of levocetirizine are sold under the following brand names:
Seamless Wikipedia browsing. On steroids.
Every time you click a link to Wikipedia, Wiktionary or Wikiquote in your browser's search results, it will show the modern Wikiwand interface.
Wikiwand extension is a five stars, simple, with minimum permission required to keep your browsing private, safe and transparent.
