First-generation antihistamine with anxiolytic activity
ATC code: N05BB01 (Hydroxyzine)
An antagonist of peripheral and central H1 histamine receptors with weak additional antagonism of 5-HT2 serotonin and D2 dopamine receptors. Central action produces sedation and anxiolysis without dependence, unlike benzodiazepines. Anticholinergic effect is moderate. Metabolized to cetirizine – an active second-generation, non-sedating metabolite, which extends the antihistamine duration.
Second line
Used in anxiety, emotional tension, and sleep disturbance linked to anxiety. Compared with benzodiazepines, it carries no dependence or abuse risk and can be used longer. 2020 lists hydroxyzine as a second-line option in generalized anxiety disorder when SSRIs are unsuitable. Standard dose 25–100 mg daily in 2–3 divided doses; for acute episodes, single doses up to 100 mg. In patients over 65, start at the minimum dose given anticholinergic effects.
Second line
Previously considered standard for urticaria with marked itching and accompanying anxiety. Current /GA²LEN 2022 guidance does not recommend first-generation antihistamines as preferred agents due to sedation and anticholinergic effects. Use is uncommon – reserved for urticaria with severe sleep disruption where sedation is welcomed, in short courses.
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Contraindicated in T1 due to associations with fetal cardiac defects described in a 2017 Danish cohort. In T3, linked to CNS depression and neonatal withdrawal.
The cetirizine metabolite passes into milk. Cetirizine or loratadine (second-generation, minimal sedation) are preferred during lactation.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Hydroxyzine is evaluated for the following indications with varying evidence strength: Acute symptomatic anxiety (evidence tier B), Chronic urticaria (evidence tier D). See the full indication matrix with dosing and citations above on this page.
Common side effects of Hydroxyzine (≥ 1 in 100): Drowsiness, sedation, Dry mouth, Headache, Fatigue, Constipation. See the Safety section for uncommon and serious reactions.
FDA category C. Contraindicated in T1 due to associations with fetal cardiac defects described in a 2017 Danish cohort. In T3, linked to CNS depression and neonatal withdrawal.
The cetirizine metabolite passes into milk. Cetirizine or loratadine (second-generation, minimal sedation) are preferred during lactation.
Hydroxyzine is contraindicated in: Hypersensitivity to hydroxyzine or cetirizine; QT prolongation, congenital or acquired long-QT syndrome; Combination with QT-prolonging drugs (antiarrhythmics, methadone, antipsychotics, some antibiotics); Severe hepatic impairment; Pregnancy (especially T1). Full list in the Safety section.