Adult: As tab and oral solution: 5 mg once daily. Child: 2-5 years As oral solution: 1.25 mg once daily or 1.25 mg bid; ≥6-11 years As tab and oral solution: 2.5-5 mg once daily; ≥12 years Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.
Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.
Administration
May be taken with or without food.
Contraindications
ESRD (CrCl <10 mL/min) or undergoing haemodialysis. Renal impairment in children 6 months to 11 years.
Special Precautions
Patient with risk factors for urinary retention (e.g. spinal cord lesions, prostatic hyperplasia), epilepsy, predisposition for convulsion. Mild to moderate renal impairment. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: CNS depression, rebound pruritus, urinary retention, seizure aggravation. Gastrointestinal disorders: Dry mouth, abdominal pain. General disorders and administration site conditions: Fatigue, asthenia. Nervous system disorders: Headache, somnolence.
This drug may cause somnolence, fatigue, and asthenia; if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor renal function periodically.
Overdosage
Symptoms: Drowsiness. In children, initially, agitation and restlessness then followed by drowsiness. Management: Symptomatic and supportive treatment. May consider performing gastric lavage shortly after ingestion.
Drug Interactions
May increase the CNS depressant effect with other CNS depressants.
Food Interaction
Decreased rate of absorption with food. Increased CNS depressant effect with alcohol.
Lab Interference
May diminish the wheal and flare reactions to skin test antigens.
Action
Description: Mechanism of Action: Levocetirizine, the active R-enantiomer of cetirizine, is a 2nd generation antihistamine. It is a potent and selective antagonist of histamine H1-receptors on effector cells in the blood vessels, gastrointestinal and respiratory tracts. It possesses twice the binding affinity at the H1-receptor compared to cetirizine. Onset: Within 1 hour. Duration: 24 hours. Pharmacokinetics: Absorption: Rapidly and extensively absorbed. Food decreases the rate of absorption. Time to peak plasma concentration: 0.9 hours (tab); 0.5 hours (oral solution). Distribution: Volume of distribution: Approx 0.4 L/kg. Plasma protein binding: 91-92%. Metabolism: Metabolised via aromatic oxidation, N- and O-dealkylation by CYP3A4, and taurine conjugation. Excretion: Via urine (85.4%); faeces (12.9%). Elimination half-life: Approx 8-9 hours.
Chemical Structure
Levocetirizine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 1549000, Levocetirizine. https://pubchem.ncbi.nlm.nih.gov/compound/Levocetirizine. Accessed Aug. 17, 2023.
R06AE09 - levocetirizine ; Belongs to the class of piperazine derivatives used as systemic antihistamines.
References
Allerzal F.C. Tablet 5 mg (Md Healthcare Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 13/07/2023.Anon. Levocetirizine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 13/07/2023.Anon. Levocetirizine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/07/2023.Buckingham R (ed). Levocetirizine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/07/2023.Childrens Xyzal Allergy - Solution (Chattem, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 13/07/2023.Joint Formulary Committee. Levocetirizine Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/07/2023.Levocet Syrup 0.5 mg/mL (Asumed Biotech Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 13/07/2023.Levocetirizine 5 mg Film-coated Tablets (Glenmark Pharmaceuticals Europe Limited). MHRA. https://products.mhra.gov.uk. Accessed 13/07/2023.Levocetirizine Dihydrochloride (Macleods Pharmaceuticals Limited). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 13/07/2023.Levocetirizine Dihydrochloride Solution (Padagis Israel Pharmaceuticals Ltd). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 13/07/2023.Xyzal 0.5 mg/mL Oral Solution (UCB Pharma Ltd). MHRA. https://products.mhra.gov.uk. Accessed 13/07/2023.Xyzal 5 mg Film Coated Tablets (UCB Pharma Ltd). MHRA. https://products.mhra.gov.uk. Accessed 24/07/2023.Xyzal Allergy 24 Hour Tablet (Chattem, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 24/07/2023.Xyzal Film Coated Tablet/Oral Drops (UCB Farchim SA). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 24/07/2023.
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