Levocetirizine

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Levocetirizine
Ball-and-stick model of the levocetirizine molecule
Clinical data
Trade namesXyzal, Levazyr, others
Other namesLevocetirizine dihydrochloride
AHFS/Drugs.comMonograph
MedlinePlusa607056
License data
Second generation antihistamines
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityHigh
Protein binding91–92%[2]
MetabolismMinimal (less than 14%, primarily CYP3A4)[2]
Elimination half-life8 to 9 hours[2]
ExcretionUrine: 85%[2]
Feces: 12.9%[2]
Identifiers
  • 2-(2-{4-[(R)-(4-Chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid
JSmol)
  • Clc1ccc(cc1)[C@H](N2CCN(CCOCC(=O)O)CC2)c3ccccc3
  • InChI=1S/C21H25ClN2O3/c22-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)24-12-10-23(11-13-24)14-15-27-16-20(25)26/h1-9,21H,10-16H2,(H,25,26)/t21-/m1/s1 checkY
  • Key:ZKLPARSLTMPFCP-OAQYLSRUSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Levocetirizine, sold under the brand name Xyzal, among others, is a second-generation

by mouth.[3]

Common side effects include sleepiness, dry mouth, cough, vomiting, and diarrhea.

histamine H1-receptors.[6][3]

Levocetirizine was approved for medical use in the United States in 2007.

generic medication.[4] In 2021, it was the 190th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[7][8]

Medical uses

Levocetirizine is used for allergic rhinitis.[9] This includes allergy symptoms such as watery eyes, runny nose, sneezing, hives, and itching.[10]

Side effects

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

fatigue.[14]

Pharmacology

Levocetirizine is an antihistamine. It acts as an

distomer, is inactive.[15][16]

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.[citation needed]

History

Levocetirizine was first launched in 2001 by the Belgian pharmaceutical company UCB (Union Chimique Belge).[citation needed]

Society and culture

Availability

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]

Brand names

Different brands (Actavis, Glenmark, UCB) Levocetirizine tablets and oral solution

Preparations of levocetirizine are sold under the following brand names:

  • Xyzal
    Sanofi-Aventis
    .
  • Xazal in Spain.[18]
  • Zobral in Cyprus.
  • Levobert in India.
  • Xusal in Germany and Mexico.
  • Xozal in Greece.
  • Degraler in Chile.
  • Allevo in Egypt.
  • Zilola, Histisynt, and Xyzal (UCB) in Hungary.
  • Alcet, Curin, and Seasonix in Bangladesh.
  • Vozet and Uvnil in India.
  • T-Day Syrup in Pakistan.
  • Curin in Nepal.[19]
  • Zenaro in the Czech Republic and
    Slovakia
    .
  • Xuzal and Zival in Chile.
  • Cezera, Levosetil, Robenan, and Xyzal in Serbia.[20]
  • Rinozal and Xyzal in Ireland.
  • Xycet in Morocco.[21]

References

  1. ^ "Xyzal Allergy 24HR- levocetirizine dihydrochloride tablet". DailyMed. 10 March 2023. Archived from the original on 30 June 2023. Retrieved 6 July 2023.
  2. ^ a b c d e f "Levocetirizine dihydrochloride- levocetirizine dihydrochloride tablet, film coated". DailyMed. 6 December 2021. Retrieved 9 July 2023.
  3. ^ a b c d e "Levocetirizine Dihydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 1 April 2019. Retrieved 22 March 2019.
  4. ^
    ISBN 9780857113382
    .
  5. ^ "Levocetirizine Pregnancy and Breastfeeding Warnings". Drugs.com. Archived from the original on 22 March 2019. Retrieved 3 March 2019.
  6. PMID 18662584
    .
  7. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  8. ^ "Levocetirizine - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  9. S2CID 26620889
    . The variable efficacy and durability of response of different antihistamines arise from differing modulatory effects on the H(1)-receptor. Conclusion: These findings support both the short-term and long-term use of levocetirizine in the clinical management of allergic rhinitis. The World Health Organization (WHO) ARIA Guidelines (Allergic Rhinitis and its Impact on Asthma), recommend using a combination of a non-sedating antihistamine with a decongestant, or glucocorticosteroids for treating allergic rhinitis - with the order and combination of treatment depending on severity and duration of symptoms.
  10. ^ "Levocetirizine Oral". WebMD. Archived from the original on 16 August 2019. Retrieved 21 August 2017.
  11. S2CID 36218027
    .
  12. PMID 20455340
    .
  13. PMID 25785934
    .
  14. ^ XOZAL technical specifications booklet.
  15. S2CID 11304832
    .
  16. S2CID 40716352
    .
  17. ^ "Prescription to Over-the-Counter (OTC) Switch List". Food and Drug Administration. Archived from the original on 24 April 2019. Retrieved 9 February 2017.
  18. ^ "Xazal 5 mg Comprimidos Recubierno con película".
  19. ^ "Curin". Archived from the original on 22 October 2012. Retrieved 29 August 2012.
  20. ^ "Medicines and Medical Devices Agency of Serbia". Archived from the original on 21 September 2020. Retrieved 23 August 2020.
  21. ^ "XYCET 5MG, Comprimé enrobé". Medicament.ma. 7 October 2020. Retrieved 12 September 2023.
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