Hydroxyzine for Itching
Hydroxyzine is an effective first-generation antihistamine for treating pruritus, particularly useful for nighttime dosing due to its sedative properties (25-50 mg daily), while non-sedating second-generation antihistamines are preferred for daytime use. 1
Mechanism of Action
- Hydroxyzine acts as a potent H1-receptor antagonist with sedative properties, suppressing activity in key regions of the subcortical central nervous system 2
- Clinical effects typically begin within 15-30 minutes after oral administration 2
- Beyond antihistamine effects, hydroxyzine demonstrates bronchodilator activity, analgesic effects, and mild antisecretory activity 2
Clinical Applications
Mild to Moderate Pruritus (Grade 1)
- Hydroxyzine can be used alongside topical moderate/high-potency steroids 1
- Typical dosing is 10-25 mg QID or at bedtime for mild localized pruritus 1
- Can be combined with non-sedating antihistamines (cetirizine/loratadine) for 24-hour coverage 1
Moderate to Severe Pruritus (Grade 2)
- For intense or widespread pruritus with intermittent symptoms, hydroxyzine remains a viable option 1
- Often used in combination with topical steroids and/or GABA agonists (pregabalin/gabapentin) 1
- Dosing may be increased to 25-50 mg daily, particularly at night 1
Severe Pruritus (Grade 3)
- For intense, widespread, and constant pruritus limiting self-care activities, hydroxyzine can be part of a multimodal approach 1
- May need to be combined with oral corticosteroids (0.5-1 mg/kg/day of prednisone) for temporary relief of severe symptoms 1
- In cases of treatment failure, consider GABA agonists or specialist referral 1
Dosing Considerations
- For nighttime pruritus: 25-50 mg at bedtime to leverage sedative properties 1
- For daytime coverage: Consider non-sedating antihistamines instead (loratadine 10 mg daily) 1
- In renal impairment: Dose should be halved in moderate renal impairment and avoided in severe renal impairment 1
- In hepatic impairment: Should be avoided in severe liver disease due to inappropriate sedating effects 1
- Contraindicated during early pregnancy 1
Efficacy Evidence
- Real-world observational data shows significant improvement in quality of life and pruritus scores over 12 weeks of hydroxyzine treatment 3
- Studies have shown hydroxyzine to be as effective as newer antihistamines for urticaria, with 47% reduction in daily symptom scores 4
- Bedtime dosing maintains skin H1-receptor antagonism through the following morning while minimizing daytime sedation 5
Adverse Effects and Limitations
- Common side effects include sedation, drowsiness, dizziness, dry mouth, and constipation 3
- Significantly higher rates of somnolence compared to non-sedating antihistamines (40% vs. 5%) 4
- Adding hydroxyzine at night to daytime non-sedating antihistamines increases daytime somnolence without improving treatment efficacy 6
- Rare cases of worsening dermatitis in patients with sensitivities to phenothiazines or ethylenediamines 7
Special Considerations
- For chronic urticaria, guidelines recommend using non-sedating second-generation antihistamines as first-line treatment 6
- When using hydroxyzine for more than 3 weeks at high doses, consider GI prophylaxis with proton pump inhibitors 1
- In cases where hydroxyzine is ineffective, consider antiepileptic agents (pregabalin 25-150 mg daily or gabapentin 900-3600 mg daily) as second-line treatment 1
- For treatment-resistant cases, dermatology referral is recommended 1