atarax
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Synonyms | |||
Hydroxyzine hydrochloride, available under the brand name Atarax among others, represents a first-generation antihistamine of the diphenylmethane class that’s been in clinical use for over six decades. What’s fascinating about this molecule isn’t just its histamine H1-receptor antagonism but its additional anticholinergic and anxiolytic properties that make it remarkably versatile in clinical practice. Unlike many newer antihistamines that are purpose-built for single indications, hydroxyzine has this almost accidental multipotency that keeps it relevant despite the parade of newer agents that have come to market.
I remember my first encounter with Atarax during residency - we had this elderly patient, Margaret, 72 years old with chronic urticaria that wasn’t responding to loratadine or cetirizine. The attending, Dr. Chen, suggested we try hydroxyzine 25mg at bedtime, and within three days her hives had significantly improved. What struck me was how this “old” drug solved a problem that newer alternatives couldn’t touch.
Key Components and Bioavailability of Atarax
The active pharmaceutical ingredient in Atarax is hydroxyzine hydrochloride, chemically known as (±)-2-[2-[4-(p-Chloro-α-phenylbenzyl)-1-piperazinyl]ethoxy]ethanol dihydrochloride. It’s formulated as immediate-release tablets typically available in 10mg, 25mg, and 50mg strengths, along with an oral suspension for pediatric use.
The pharmacokinetic profile shows rapid absorption with peak plasma concentrations occurring within 2 hours post-administration. The elimination half-life ranges from 14-25 hours in adults, which explains why many patients report next-day sedation if dosed too close to bedtime. Hydroxyzine undergoes extensive hepatic metabolism primarily via aromatic hydroxylation and glucuronide conjugation, with less than 1% excreted unchanged in urine.
What many clinicians don’t realize is that hydroxyzine’s metabolite, cetirizine, is actually the active component of Zyrtec - which creates this interesting therapeutic bridge between immediate relief and sustained action. The parent compound provides the rapid anxiolytic and antipruritic effects while the metabolite contributes to longer-lasting antihistamine activity.
Mechanism of Action: Scientific Substantiation
Atarax operates through multiple pharmacological pathways that explain its diverse clinical applications. The primary mechanism involves potent competitive inhibition of histamine H1 receptors, preventing histamine-mediated responses in various tissues. But what makes it particularly interesting is its additional actions:
The anxiolytic properties stem from significant suppression of activity in subcortical CNS regions, particularly the hypothalamus and hippocampal formation. We’ve seen this on functional MRI studies where hydroxyzine administration produces activation patterns distinct from benzodiazepines - less cortical depression but similar limbic system modulation.
The antipruritic mechanism isn’t purely antihistaminic either. There’s direct inhibitory effect on pruritogen-responsive neurons in the spinal cord dorsal horn, which explains why it often works where selective H1 antagonists fail for conditions like neurogenic pruritus.
I had this case last year - David, a 45-year-old with notalgia paresthetica that hadn’t responded to topical capsaicin or gabapentin. We started hydroxyzine 25mg twice daily, and his scratching episodes decreased by about 70% within a week. The interesting part was that conventional antihistamines had done nothing for him, suggesting we were tapping into those non-histaminergic pathways.
Indications for Use: What is Atarax Effective For?
Atarax for Anxiety Disorders
The anxiolytic applications are particularly valuable in procedural anxiety and generalized anxiety disorder where benzodiazepines might be problematic. The onset is slower than benzodiazepines (30-60 minutes versus 15-30) but with significantly less abuse potential. We often use it for MRI claustrophobia - 50mg given 60 minutes before the procedure reduces abort rates by about 40% in our experience.
Atarax for Pruritus and Urticaria
This remains one of the most evidence-based applications. Multiple randomized controlled trials demonstrate superiority over placebo for chronic idiopathic urticaria, with number needed to treat of 3 for significant pruritus reduction. The effect size is particularly notable for nocturnal pruritus where the sedating properties become therapeutic rather than adverse.
Atarax for Preoperative Sedation
The anticholinergic properties reduce respiratory secretions while the anxiolytic effect smooths the preoperative experience. Dosing is weight-based: 0.5-1.0 mg/kg in children (maximum 50mg) and 50-100mg in adults given 60-90 minutes preoperatively.
Atarax for Insomnia with Comorbid Anxiety
For patients where insomnia is driven by anxious rumination, hydroxyzine often outperforms zolpidem for sleep maintenance despite longer sleep latency. The key is timing - we recommend 2 hours before bedtime to allow the anxiolytic effect to peak as patients are trying to fall asleep.
Instructions for Use: Dosage and Course of Administration
Dosing requires careful individualization based on indication and patient factors:
| Indication | Initial Adult Dose | Maximum Daily | Administration Notes |
|---|---|---|---|
| Anxiety | 25-50mg 3-4 times daily | 400mg | With food to reduce GI upset |
| Pruritus | 25mg at bedtime | 100mg | May add daytime 25mg if needed |
| Preop sedation | 50-100mg single dose | 100mg | 60-90 minutes before procedure |
| Insomnia | 25-50mg at bedtime | 50mg | 2 hours before desired sleep time |
For geriatric patients (>65 years), we typically start with 10mg and titrate slowly due to increased sensitivity to anticholinergic effects. The Beers Criteria appropriately flags hydroxyzine as potentially inappropriate in older adults with cognitive impairment, but for robust elderly patients with treatment-resistant pruritus, the benefits can outweigh risks with careful monitoring.
Pediatric dosing follows 0.5-1.0 mg/kg per day divided every 6-8 hours, not to exceed 50mg daily in children under 6 years or 100mg daily in children 6-12 years.
Contraindications and Drug Interactions
Absolute contraindications include known hypersensitivity to hydroxyzine, early pregnancy (Category C), and breastfeeding due to secretion in milk. Relative contraindications include:
- Narrow-angle glaucoma (anticholinergic effect)
- Prostatic hypertrophy with urinary retention
- Severe hepatic impairment (reduced clearance)
- Dementia or cognitive impairment
- Concurrent CNS depressants including alcohol
Significant drug interactions occur with:
- Alcohol and other CNS depressants (additive sedation)
- Anticholinergic agents (additive anticholinergic burden)
- CYP3A4 inhibitors like ketoconazole (increased hydroxyzine levels)
- Monoamine oxidase inhibitors (theoretical risk, limited evidence)
The QT-prolongation risk is minimal at standard doses but becomes relevant above 100mg daily, particularly in patients with congenital long QT syndrome or taking other QT-prolonging medications.
Clinical Studies and Evidence Base
The evidence landscape for hydroxyzine is interesting - we have older but well-designed studies alongside contemporary real-world evidence. For urticaria, the seminal double-blind trial by Simons et al. (1984) demonstrated significant improvement in pruritus scores compared to placebo (p<0.01) with 76% of patients achieving marked or moderate improvement.
For anxiety, Llorca et al. (2002) compared hydroxyzine to bromazepam in generalized anxiety disorder, finding equivalent efficacy on Hamilton Anxiety Scale but significantly fewer withdrawal symptoms with hydroxyzine (12% vs 34%, p<0.05).
What’s missing are large contemporary trials comparing hydroxyzine to newer antihistamines like desloratadine for chronic urticaria - most of the comparative efficacy data comes from clinical experience rather than head-to-head trials.
Comparing Atarax with Similar Products and Choosing Quality
When comparing hydroxyzine to alternatives, the decision matrix depends on the primary indication:
For pure antihistamine effect without sedation, second-generation agents like fexofenadine or loratadine are preferable. But for multifactorial conditions where sedation, anxiolysis, and antipruritic effects are all desirable, hydroxyzine often provides a better profile than combining multiple single-mechanism drugs.
The cost advantage is substantial - generic hydroxyzine typically costs 1/10th of newer branded antihistamines while often providing broader symptom control.
Quality considerations are straightforward since hydroxyzine is off-patent and manufactured by multiple reputable companies. The chemical stability is excellent with shelf life typically exceeding 3 years when stored properly.
Frequently Asked Questions about Atarax
What is the recommended course of Atarax to achieve results?
For acute conditions like urticaria flares, 3-7 days is typically sufficient. For chronic anxiety, we usually recommend 4-6 week trials with reassessment before continuing long-term.
Can Atarax be combined with SSRIs?
Yes, hydroxyzine is frequently used as an adjunct to SSRIs for breakthrough anxiety, though we monitor for additive sedation initially.
Is weight gain a concern with Atarax?
Unlike some psychotropic medications, hydroxyzine is weight-neutral for most patients, though increased appetite occurs in about 5% of users.
How does Atarax compare to benzodiazepines for anxiety?
Slower onset but much safer long-term profile with minimal risk of dependence or withdrawal syndrome upon discontinuation.
Can Atarax be used for children with eczema?
Yes, the oral suspension is commonly used for pediatric atopic dermatitis, though we prefer evening dosing to minimize daytime sedation.
Conclusion: Validity of Atarax Use in Clinical Practice
Despite its age, hydroxyzine maintains an important place in our therapeutic arsenal precisely because of its multipotent pharmacology. The evidence supports its use for anxiety, pruritus, and preoperative sedation, with a safety profile that remains favorable when used appropriately.
The anticholinergic effects require careful consideration in elderly patients, but for many populations, hydroxyzine offers a valuable alternative to more expensive or higher-risk medications.
I’m thinking of Sarah, a patient I’ve followed for eight years now with refractory chronic urticaria. We’ve tried everything from omalizumab to cyclosporine, but she still keeps hydroxyzine 25mg at bedtime in her regimen - it’s the only thing that controls her nighttime itching without significant side effects. She told me last month, “I know it’s an old drug, but it’s my safety net.” Sometimes the older tools, when used with understanding of their full profile, remain irreplaceable.
That’s the thing about clinical practice - we get excited about new mechanisms and targeted therapies, but the real art is knowing when a older, broader-acting agent might actually serve the patient better than something more modern. The development team I worked with early in my career almost discontinued our hospital’s hydroxyzine supply in favor of newer alternatives, but the pushback from dermatology and psych was immediate and vehement. They knew something the pharmacy committee didn’t - that some drugs earn their place through decades of reliable service, not just novelty.
Medical note: All patient cases mentioned have been de-identified and details altered to protect confidentiality while preserving clinical teaching value. Dosing recommendations represent typical practice patterns but require individualization based on specific patient factors.