Hydroxyzine
Hydroxyzine is a first-generation antihistamine with anxiolytic, sedative, and anticholinergic properties. It is used in the treatment of anxiety, insomnia, pruritus, and as an adjunct in allergic and psychoneurotic conditions.
Classification
- Drug class: H1-antihistamine (first-generation)
- ATC code: N05BB01
- Subtypes:
- Hydroxyzine hydrochloride (Atarax®)
- Hydroxyzine pamoate (Vistaril®)
Mechanism of Action
- Antagonist at histamine H1 receptors in the CNS and periphery
- Also has effects on muscarinic, serotonergic, and dopaminergic receptors
- Produces sedation, anxiolysis, and antiemetic effects
Indications
- Anxiety disorders (short-term treatment)
- Preoperative sedation
- Insomnia (off-label)
- Urticaria and pruritus
- Allergic rhinitis
- Tinnitus-related distress (off-label)
Dosage (Adults)
- Anxiety: 25–50 mg up to 4 times daily
- Pruritus: 25 mg at night or every 6–8 hours
- Sedation: 50–100 mg at bedtime
- Titrate based on sedation and tolerability
Adverse Effects
- Common: Drowsiness, dry mouth, headache, dizziness, blurred vision
- Anticholinergic: Constipation, urinary retention, confusion (especially in elderly)
- Rare but serious: QT prolongation, seizures (at high doses)
Contraindications
- Hypersensitivity to hydroxyzine or cetirizine (its active metabolite)
- Prolonged QT interval or history of torsades de pointes
- First trimester of pregnancy (teratogenic risk)
Precautions
- Use with caution in elderly (Beers Criteria)
- Avoid in renal or hepatic impairment without dose adjustment
- Caution with other CNS depressants (alcohol, opioids, benzodiazepines)
Drug Interactions
- CNS depressants: Additive sedation
- QT-prolonging drugs: Increased risk of arrhythmia
- MAO inhibitors: Avoid concomitant use
Clinical Notes
- Considered a non-addictive alternative to benzodiazepines for anxiety or sleep
- Onset of action: ~15–30 minutes
- May impair psychomotor performance; avoid driving
Synonyms and Brand Names
- Hydroxyzine hydrochloride: Atarax®
- Hydroxyzine pamoate: Vistaril®
- Metabolite: Cetirizine (second-generation antihistamine)