Second-generation antihistamine
ATC code: R06AE09 (Levocetirizine)
Brand names
Xyzal, Xazal, Muntel, Levocet
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.
First line
First-line for seasonal and perennial allergic rhinitis under ARIA 2020 and 2022 alongside other second-generation antihistamines (bilastine, , , ). 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.
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.
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
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.
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FDA category B. Large pregnancy data set for cetirizine without described teratogenic effects. Levocetirizine and cetirizine are preferred for allergic rhinitis and urticaria in pregnancy per ACOG 2017.
Compatible. Hale L2. RID 1.5%, same as cetirizine (levocetirizine is the active enantiomer). Non-sedating at standard doses.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
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.
Common side effects of Levocetirizine (≥ 1 in 100): Drowsiness (~5–8%), Headache, Dry mouth, Fatigue. See the Safety section for uncommon and serious reactions.
FDA category B. FDA category B. Large pregnancy data set for cetirizine without described teratogenic effects. Levocetirizine and cetirizine are preferred for allergic rhinitis and urticaria in pregnancy per ACOG 2017.
Compatible. Hale L2. RID 1.5%, same as cetirizine (levocetirizine is the active enantiomer). Non-sedating at standard doses.
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.