Levocetirizine

Second-generation antihistamine

ATC code: R06AE09

Brand names: Xyzal, Xazal, Muntel, Levocet

Updated 27 May 2026 · Methodology

Indications

Allergic rhinitis

First line

First-line for seasonal and perennial allergic rhinitis under ARIA 2020 and 2022 alongside other second-generation antihistamines (bilastine, desloratadine, fexofenadine, rupatadine). Standard dose 5 mg once daily. Children 6–11 years: 2.5 mg once daily. Onset within 1 hour; effect lasts at least 24 hours.

Sources

AEMPS: Ficha técnica de Levocetirizina (2024)
EAACI: ARIA guideline 2019 update on allergic rhinitis (2020)
J Allergy Clin Immunol: Allergic Rhinitis and its Impact on Asthma (ARIA) guidelines-2016 revision. (2017)
Braz J Otorhinolaryngol: Efficacy of different oral H(1) antihistamine treatments on allergic rhinitis: a systematic review and network meta-analysis of randomized controlled trials. (2023)
J Allergy Clin Immunol: Levocetirizine improves quality of life and reduces costs in long-term management of persistent allergic rhinitis. (2004)

ICD-10: J30.9 · ICD-11: CA08.0

Chronic urticaria

First line

First-line for chronic spontaneous urticaria under /GA²LEN/EDF/ 2022 at standard dose 5 mg once daily. With insufficient response, up-dosing to 20 mg/day is acceptable (off-label, EAACI consensus). When symptoms persist at quadruple dose, add omalizumab.

Sources

ICD-10: L50.1 · ICD-11: EB00.1

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

Immune support and respiratory infection care

Not recommended

Levocetirizine is a second-generation antihistamine and the active enantiomer of cetirizine. It is prescribed for seasonal and perennial allergic rhinitis and urticaria ( 2024). Levocetirizine is prescribed for cold to relieve mucosal edema and for immunity. The Cochrane review by De Sutter 2015 did not confirm benefit of antihistamines in the common cold. If levocetirizine was prescribed for a cold without confirmed allergic rhinitis, consider seeking a second opinion.

Sources

How to read tiers A–F

AStrong evidence – first or second line in international guidelines
BRecommended in selected cases
CStudy data contradict each other
DBenefit not proven, no documented harm
FDocumented harm, or risk without benefit

Mechanism of action

The active l-enantiomer of cetirizine. A selective peripheral H1-antagonist with roughly twice the H1 affinity of racemic cetirizine. Minimal blood-brain barrier penetration – low sedation. Hardly metabolized hepatically; 85% is excreted unchanged by the kidneys, so CYP-mediated interactions are minimal.

Safety

Contraindications

Hypersensitivity to levocetirizine, cetirizine, hydroxyzine, or piperazine derivatives
End-stage renal disease (eGFR under 10)
Age under 6 months

Serious adverse effects

Rare hypersensitivity reactions (angioedema, anaphylaxis)
Hepatotoxicity (very rare)

Common adverse effects

Drowsiness (~5–8%)
Headache
Dry mouth
Fatigue

Pregnancy: can you take Levocetirizine?

AEMPS summary of product characteristics (section 4.6): there are no or limited data (fewer than 300 pregnancies) on the use of levocetirizine in pregnant women. For cetirizine, the racemate of levocetirizine, a large amount of data (more than 1,000 pregnancies) indicates no malformations and no fetal or neonatal toxicity. Animal studies do not show direct or indirect harmful effects on pregnancy, embryo-fetal development, parturition or postnatal development. If needed, the use of levocetirizine may be considered during pregnancy.

Breastfeeding: can you take Levocetirizine?

Hale L2 · Probably compatible

Compatible. Hale L2. RID 1.5%, same as cetirizine (levocetirizine is the active enantiomer). Non-sedating at standard doses.

RID, infant dose via milk: 1.5%
Maternal half-life: 8 h
Maternal peak time: 1 h
Peak milk concentration: 0.16 mg/L
Milk-to-plasma ratio: 1

Calculate RID Safe feeding window Full profile on NIH LactMed ↗

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Practical notes

Timing and administration

Take once daily, preferably in the evening (if mild drowsiness develops, it occurs during sleep). Food does not affect efficacy but slows peak concentration. Adjust in renal impairment: eGFR 30–50 – 5 mg every other day; eGFR 10–30 – 5 mg every 3–4 days; eGFR under 10 – contraindicated. Start at 2.5 mg in older adults with reduced eGFR.

Label mentions15 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

Azithromycin
«No se han realizado estudios de interacción con levocetirizina (incluyendo estudios con inductores de CYP3A4). Los estudios realizados con el compuesto racémico cetirizina demostraron que no había…»
AEMPS, section 4.5 · Open on CIMA
Azithromycin
«DRUG INTERACTIONS: Antipyrine, Azithromycin, Cimetidine, Erythromycin, Ketoconazole, Theophylline, and Pseudoephedrine»
FDA, section 7 · Open on DailyMed
depresores del SNCclass named in the label
«En pacientes sensibles, la administración simultánea de cetirizina o levocetirizina y alcohol u otros depresores del SNC, puede producir una reducción adicional de la capacidad de atención y…»
AEMPS, section 4.5 · Open on CIMA
Diazepam
«No se han realizado estudios de interacción con levocetirizina (incluyendo estudios con inductores de CYP3A4). Los estudios realizados con el compuesto racémico cetirizina demostraron que no había…»
AEMPS, section 4.5 · Open on CIMA
Erythromycin
«No se han realizado estudios de interacción con levocetirizina (incluyendo estudios con inductores de CYP3A4). Los estudios realizados con el compuesto racémico cetirizina demostraron que no había…»
AEMPS, section 4.5 · Open on CIMA
Erythromycin
«DRUG INTERACTIONS: Antipyrine, Azithromycin, Cimetidine, Erythromycin, Ketoconazole, Theophylline, and Pseudoephedrine»
FDA, section 7 · Open on DailyMed
inductores del CYP3A4class named in the label
«No se han realizado estudios de interacción con levocetirizina (incluyendo estudios con inductores de CYP3A4). Los estudios realizados con el compuesto racémico cetirizina demostraron que no había…»
AEMPS, section 4.5 · Open on CIMA
Ketoconazole
«No se han realizado estudios de interacción con levocetirizina (incluyendo estudios con inductores de CYP3A4). Los estudios realizados con el compuesto racémico cetirizina demostraron que no había…»
AEMPS, section 4.5 · Open on CIMA
Ketoconazole
«DRUG INTERACTIONS: Antipyrine, Azithromycin, Cimetidine, Erythromycin, Ketoconazole, Theophylline, and Pseudoephedrine»
FDA, section 7 · Open on DailyMed
Pseudoephedrine
«No se han realizado estudios de interacción con levocetirizina (incluyendo estudios con inductores de CYP3A4). Los estudios realizados con el compuesto racémico cetirizina demostraron que no había…»
AEMPS, section 4.5 · Open on CIMA
Pseudoephedrine
«DRUG INTERACTIONS: Antipyrine, Azithromycin, Cimetidine, Erythromycin, Ketoconazole, Theophylline, and Pseudoephedrine»
FDA, section 7 · Open on DailyMed
Ritonavir
«En un estudio de dosis múltiple de ritonavir (600 mg dos veces al día) y cetirizina (10 mg diarios), el grado de exposición a cetirizina se incrementó en un 40%, mientras que la disposición de…»
AEMPS, section 4.5 · Open on CIMA
Ritonavir
«Ritonavir: Ritonavir increased the plasma AUC of cetirizine by about 42% accompanied by an increase in half-life (53%) and a decrease in clearance (29%) of cetirizine. The disposition of ritonavir…»
FDA, section 7 · Open on DailyMed
Theophylline
«No se han realizado estudios de interacción con levocetirizina (incluyendo estudios con inductores de CYP3A4). Los estudios realizados con el compuesto racémico cetirizina demostraron que no había…»
AEMPS, section 4.5 · Open on CIMA
Theophylline
«DRUG INTERACTIONS: Antipyrine, Azithromycin, Cimetidine, Erythromycin, Ketoconazole, Theophylline, and Pseudoephedrine»
FDA, section 7 · Open on DailyMed

Check interaction with another drug

Opens the checker prefilled with this drug. Pick the second one from your regimen.

Open checker

Summary of a multi-drug list →

Medicine list: everything you take in one place →

Frequently asked

What is Levocetirizine used for?

Levocetirizine is evaluated for the following indications with varying evidence strength: Allergic rhinitis (evidence tier A), Chronic urticaria (evidence tier A), Immune support and respiratory infection care (evidence tier F). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Levocetirizine?

Common side effects of Levocetirizine (≥ 1 in 100): Drowsiness (~5–8%), Headache, Dry mouth, Fatigue. See the Safety section for uncommon and serious reactions.

Is Levocetirizine safe during pregnancy?

Is Levocetirizine compatible with breastfeeding?

Compatible. Hale L2. RID 1.5%, same as cetirizine (levocetirizine is the active enantiomer). Non-sedating at standard doses.

Who should not take Levocetirizine?

Levocetirizine is contraindicated in: Hypersensitivity to levocetirizine, cetirizine, hydroxyzine, or piperazine derivatives; End-stage renal disease (eGFR under 10); Age under 6 months. Full list in the Safety section.

Official sources

Direct links to regulator labels. Open in a new tab.

AEMPS / CIMALabel dated 07/24/2025
FDA / DailyMedLabel dated 08/13/2026

Other drugs in this group

Loratadine, Promethazine, Rupatadine, Bilastine, Chloropyramine, Dexchlorpheniramine, Doxylamine/pyridoxine, Cetirizine