Levocetirizine


Concise Prescribing Info
Indications/Uses
Allergic condition.
Dosage/Direction for Use
Adult : PO 2.5-5 mg once daily in the evening.
Dosage Details
Oral
Allergic conditions
Adult: 2.5-5 mg once daily.
Child: 6 months-5 years 1.25 mg once daily. 6-11 years 2.5 mg once daily in the evening. >12 years Same as adult dose.
Renal Impairment
Patients undergoing dialysis: Contraindicated.
 CrCl (mL/min) Dosage 
 <10 Contraindicated.
10-30 2.5 mg once twice weekly.
30-50 2.5 mg every other day.
50-80 2.5 mg once daily.
Administration
May be taken with or without food.
Contraindications
ESRD (CrCl < 10 mL/min) or undergoing haemodialysis.
Special Precautions
Patient with increased risk of urinary retention (e.g. spinal cord lesion, prostatic hyperplasia), epileptic patients and at risk of convulsion. Children. Mild to moderate renal impairment. Pregnancy and lactation.
Adverse Reactions
Significant: CNS depression, rebound pruritus.
Ear and labyrinth disorders: Otitis media.
Gastrointestinal disorders: Dry mouth, diarrhoea, vomiting, constipation, abdominal pain.
General disorders and administration site conditions: Fatigue, asthenia, pyrexia.
Nervous system disorders: Headache.
Psychiatric disorders: Sleep disorder, somnolence.
Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, pharyngitis, cough.
Vascular disorders: Epistaxis.
Patient Counseling Information
This drug may cause somnolence, fatigue and asthenia, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor renal function.
Overdosage
Symptoms: Drowsiness; agitation, restlessness (children). Management: Symptomatic and supportive. Gastric lavage may be considered shortly following ingestion.
Drug Interactions
Possible additive adverse CNS effects with CNS depressants (e.g. sedatives, tranquilizers).
Food Interaction
Concomitant use with alcohol may result in additive CNS depression.
Action
Description: Levocetirizine, an antihistamine and is an active enantiomer of cetirizine. Its binding affinity to H1-receptor is twice than cetirizine. It selectively competes for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels and respiratory tract.
Onset: 1 hour.
Duration: 24 hours.
Pharmacokinetics:
Absorption: Rapid and extensive oral absorption. Time to peak plasma concentration: 0.9 hours.
Distribution: Volume of distribution: Approx 0.4 L/kg. Plasma protein binding: 91-92%.
Metabolism: Metabolised by aromatic oxidation, N- and O-dealkylation (via CYPA4) and taurine conjugation.
Excretion: Mainly via urine (85.4%); faeces (12.9%). Elimination half-life: Approx 8-9 hours.
Chemical Structure

Chemical Structure Image
Levocetirizine

Source: National Center for Biotechnology Information. PubChem Database. Levocetirizine, CID=1549000, https://pubchem.ncbi.nlm.nih.gov/compound/Levocetirizine (accessed on Jan. 22, 2020)

Storage
Store between 20-25°C.
ATC Classification
R06AE09 - levocetirizine ; Belongs to the class of piperazine derivatives used as systemic antihistamines.
References
Anon. Levocetirizine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 11/06/2019.

Anon. Levocetirizine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 21/01/2014.

Buckingham R (ed). Levocetirizine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/06/2019.

Joint Formulary Committee. Levocetirizine Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/06/2019.

Levocetirizine Dihydrochloride Solution (Camber Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 11/06/2019.

Levocetirizine Dihydrochloride Tablet, Film Coated (Micro Labs Limited). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 11/06/2019.

Levocetirizine Syrup (Unimed Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 11/06/2019.

Levocetirizine Tablet (Unimed Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 11/06/2019.

McEvoy GK, Snow EK, Miller J et al (eds). Levocetirizine Dihydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 21/01/2014.

Xyzal (UCB Farchim S.A.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 21/01/2014.

Xyzal Oral Solution and Tablets. U.S. FDA. https://www.fda.gov/. Accessed 21/01/2014.

Disclaimer: This information is independently developed by MIMS based on Levocetirizine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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