Asitrol

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Medically reviewed

Marina Burgos

Last updated on 10/01/2026

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Asitrol

Quick Facts Description
Active ingredient Cetirizine Hydrochloride
Form Oral dosage forms (Tablet, Syrup, Oral solution)
Pharmacological class Second-generation Antihistamine (H1-receptor antagonist)
Common use Symptomatic relief of allergic conditions
Origin Synthetic metabolite of Hydroxyzine

Asitrol is a pharmaceutical preparation whose active ingredient is Cetirizine Hydrochloride, which functions as a modern, second-generation antihistamine used to manage the symptoms of various allergic conditions. The drug belongs to the pharmacological class of H1-receptor antagonists, acting selectively at peripheral receptors by specifically binding to and blocking histamine receptors to achieve its therapeutic effect. This entity is a synthetic metabolite derived from the older first-generation compound, Hydroxyzine, which chemically defines its profile of minimal central nervous system (CNS) penetration.

As a result of this classification, Asitrol offers effective relief for symptoms such as sneezing, itching, and congestion associated with allergic rhinitis or the discomfort of chronic idiopathic urticaria. Its key mechanism of effect involves blocking the action of histamine at its target receptors, the critical chemical mediator released by the body during an allergic reaction, providing general purpose symptomatic management of the body’s response to allergens.

What Type of Medicine is Asitrol (Cetirizine Hydrochloride)?

Asitrol is classified as a highly selective second-generation antihistamine because its chemical structure is engineered to primarily target histamine receptors outside of the brain, leading to minimal sedation compared to earlier generations.

The active ingredient, Cetirizine Dihydrochloride, is recognized for its potent selective inhibition of peripheral H1 receptors, which provides the foundation for its therapeutic utility in various allergic conditions. Compared to older analogues like Diphenhydramine, this classification ensures low anticholinergic effects, concentrating its anti-inflammatory activity on reducing the symptoms of immediate allergic reactions. This medicinal agent eases discomfort by effectively binding to histamine receptors.

Composition, Forms, and General Purpose

The medicinal entity is fundamentally a single-component product centered on Cetirizine Hydrochloride.

This active ingredient is made available for oral administration in several common oral dosage forms, which include the solid tablet and liquid preparations such as syrup and oral solution. The availability of both syrup and oral solution forms is a distinctive feature that facilitates accurate oral administration for the patient groups who cannot easily swallow a solid form, particularly children. These liquid forms often utilize an aqueous solution base to ensure bioavailability. The general purpose of the preparation is the symptomatic management of allergic rhinitis and chronic idiopathic urticaria by reducing associated issues like fluid leakage caused by decreased vascular permeability.

Regulatory References

  1. Cetirizine: MedlinePlus Drug Information
  2. WHO Essential Medicines List Entry for Cetirizine

What side effects are possible with Asitrol?

Possible side effects and safety information

The safety profile for Asitrol (Cetirizine Hydrochloride) is comprehensively documented in official regulatory sources, with potential adverse reactions systematically classified by incidence and affected physiological systems. The medicine's profile is characterized primarily by effects on the Nervous System and Gastrointestinal system.

Frequency Classification and System-Organ Effects

The most frequently reported effects are classified as Common, affecting up to 1 in 10 patients. These include somnolence (drowsiness), fatigue, headache, and dizziness. Gastrointestinal effects classified as Common include dry mouth and pharyngitis (sore throat).

Less frequent, Rare adverse reactions (affecting up to 1 in 1,000 patients) are also documented across various System-Organ Classes. These include abnormal hepatic function (with elevated liver enzymes and bilirubin), convulsions, and serious forms of hypersensitivity.

Serious Reactions and Safety Constraints

The regulatory safety documents specify the rare but serious potential for severe allergic events, such as anaphylactic shock and angioneurotic oedema (swelling beneath the skin).

Official cautions are noted for specific populations where drug clearance is reduced, including older adults and individuals with renal or hepatic impairment. The medicine is contraindicated in persons with a known hypersensitivity to the active substance, its precursor hydroxyzine, or other related derivatives. Additionally, specific cautions are noted regarding the risk of new onset pruritus (itching) upon discontinuation after long-term use.

Overdose and Emergency Response

Official Overdose Manifestations

The regulatory profile for Cetirizine Hydrochloride overdose describes acute manifestations primarily involving the Central Nervous System (CNS) and cardiovascular system. Documented signs include CNS depression, presenting as somnolence (drowsiness), sedation, stupor, and fatigue. Other listed signs and symptoms include dizziness, confusion, diarrhea, tremor, and headache. Severe documented manifestations include tachycardia (an abnormally fast heart rate) and urinary retention.

Emergency Actions and Management

In case of a suspected overdose, regulatory authorities mandate that individuals seek immediate medical attention or contact a Poison Control Center right away. Urgent medical help is required if severe or life-threatening symptoms, such as collapse, difficulty breathing, or seizures, occur.

Management is defined as symptomatic and supportive treatment, as official labeling confirms that no specific antidote is known. Officially described supportive measures may include the use of activated charcoal or gastric lavage shortly after ingestion. The labeling notes that pediatric patients may initially exhibit restlessness and irritability followed by somnolence, while somnolence is the most common manifestation in adults.

Therapeutic Uses of Asitrol

What Asitrol Treats: Main Uses and Benefits

Asitrol is commonly used across conditions characterized by periods of heightened symptoms that lead to the cluster of manifestations known as allergic rhinitis (hay fever). It is applied to ease symptoms related to rhino-ocular irritation, helping to address recurrent sneezing, runny nose, and the distressing itching and watering of the eyes associated with seasonal or perennial allergies. This provides support that helps ease the overall symptom burden during periods of high allergen exposure, assisting patients in maintaining comfort. The medicine is utilized for the symptoms of respiratory allergies like hay fever and itching due to hives.

The medication is applicable in conditions presenting with systemic or localized discomfort, particularly in the management of chronic urticaria (hives) and acute allergic skin manifestations, including symptoms such as pruritus (itching) and wheals (hives).

“It is commonly used when groups of symptoms appear suddenly or fluctuate, helping to address symptoms that interfere with daily comfort.”

In clinical settings, Asitrol is relevant in contexts where maintaining alertness is an important consideration. It is often used when supportive symptom management is appropriate, as its profile is relevant in situations requiring temporary assistance in symptom stabilization, and assists with maintaining functional stability when symptoms interfere with routine activities.

Quick Fact Relief for Symptom
Primary Focus Symptomatic relief for allergic conditions
Key Benefit Supports maintenance of alertness
Addresses Nasal discharge, sneezing, and itching

Regulatory References

  1. Cetirizine Injection: MedlinePlus Drug Information

Eligibility and Restrictions for Use

Eligibility Map: Who Can and Cannot Use Asitrol (Cetirizine Hydrochloride)

Official regulatory documents define strict criteria for the use of Asitrol, focusing on population-specific contraindications, age limitations, and organ function status.


Contraindicated Populations

The medicine is strictly contraindicated in patients with a history of hypersensitivity to the active substance, to the parent compound Hydroxyzine, or to any related piperazine derivatives. It is also prohibited for patients with severe renal impairment where the creatinine clearance ( CL cr) is below 10 mL/min.

Age-Group Eligibility and Restrictions

Age Group Eligibility Status
Adults Standard approved use (12 years and older).
Children (2 to 11 years) Approved for use with specific lower doses.
Infants (Under 2 years) Use not recommended due to insufficient clinical data.

Special Population Limitations

Renal Status: Patients with moderate or severe kidney impairment ( CL cr 10–49 mL/min) are subject to mandatory dose reduction and extended dosing intervals. For those with solely hepatic impairment, no dose adjustment is required. Pregnancy use requires caution and should only occur if clearly needed. The medicine is not recommended for breastfeeding mothers as the substance is known to be excreted into human milk.

What should I know about interactions with other medicines?

Interactions with other medicines and products

This section outlines the officially documented interaction patterns of Asitrol (Cetirizine Hydrochloride) as verified by government regulatory authorities.


Documented Interaction Patterns and Restrictions

Pharmacodynamic Interactions

The most prominent interaction is the pharmacodynamic reinforcement observed with substances that depress the Central Nervous System (CNS). Concurrent use with alcohol or other CNS depressants (such as sedatives or tranquilizers) may lead to an additive reduction in alertness and further impairment of CNS performance, as stated in the regulatory labeling.

Pharmacokinetic Alterations

Co-administration with a high dose of theophylline (400 mg once daily) is documented to cause a measurable decrease (16%) in the clearance of Cetirizine, which may result in increased exposure to Asitrol. Conversely, studies found no clinically significant drug interactions with tested medicines, including azithromycin, pseudoephedrine, erythromycin, or ketoconazole.

Interaction with Food

Taking Asitrol with food does not change the total amount of drug absorbed (AUC), but officially delays the rate of absorption (Tmax) and reduces the maximum concentration (Cmax) by 23%.


Population-Specific Contraindication

Asitrol is primarily eliminated by the kidneys. Therefore, it is formally contraindicated in adult patients with end-stage renal disease (ESRD) who are simultaneously requiring dialysis treatment due to the high risk of drug accumulation. Dose adjustment is recommended for all other patients with impaired renal function.

Mechanism of Action

The mechanism of Asitrol ( Cetirizine Hydrochloride) is defined by three interconnected pharmacodynamic actions. Its primary function is selective inverse agonism at the Peripheral Histamine H1 Receptor, which are G-protein coupled receptors found on vascular and sensory nerve cells. This molecular action interrupts the signaling cascade initiated by endogenous histamine, preventing the mediator from binding and initiating the H1 receptor cascade.

Secondly, the drug modulates pathways associated with late-phase inflammation by inhibiting the migration and activation of key inflammatory cells, specifically Eosinophils, into affected tissues. By interfering with this cellular trafficking, Asitrol affects the physiological conditions, reducing the processes that lead to sustained tissue swelling and inflammation.

Finally, Asitrol exhibits physiological selectivity due to its limited ability to cross the Blood-Brain Barrier (a result of being a P-glycoprotein substrate). This mechanistic trait ensures that the H1 blockade is concentrated primarily in peripheral tissues, restricting the effect on central histaminergic pathways.

Dosage and Administration Information

General Principles of Administration

Asitrol (Cetirizine Hydrochloride) is primarily intended for oral administration, available in solid forms like tablets (5 mg and 10 mg) and liquid preparations such as syrup or oral solution to facilitate dosage. For specific acute circumstances, an intravenous (IV) injection is an approved route, which must be administered by a healthcare professional in a supervised setting.

Standard Dosing and Frequency

The standard protocol for use is a single dose taken once every 24 hours for both adults and adolescents (12 years and older). The usual adult dose is 10 mg per day, which also represents the maximum daily intake for routine oral administration. The medicine may be taken with or without food, as this does not affect the extent of absorption.

Age Group Standard Oral Regimen Maximum Daily Dose (General)
Adults (12+ years) 10 mg once daily (or 5 mg starting) 10 mg
Children (6-11 years) 5 mg or 10 mg once daily 10 mg

Population-Specific Adjustments

The standard regimen is modified for certain patient groups. For older adults and patients with moderately to severely decreased renal function, the dose is typically reduced to 5 mg once daily. This adjustment is utilized because the drug is primarily eliminated through the kidneys. Liquid oral forms are measured using an appropriate device to ensure accuracy, particularly when administering the lower doses required for children or those needing an adjustment.

Recent Clinical Evidence

Overview of Studies and Clinical Evaluation

This section summarizes the structure of the official research, including the types of studies such as randomized controlled trials (RCTs) that regulatory bodies rely on for the approved uses of Asitrol. Studies in this area are typically conducted during periods of increased symptom activity and focus on short-term outcomes related to physical discomfort.


Research Evidence for Seasonal Allergic Rhinitis (Hay Fever)

The foundation of the evidence for seasonal allergy symptoms comes from short-term RCTs, supported by Systematic Reviews. Researchers studied outcomes related to functional imbalance by monitoring changes in the Total Symptom Score (TSS), which tracks patient-reported metrics like sneezing and itchy eyes. Studies report how symptoms evolved in the observed populations, and findings describe patterns observed related to these specific, short-term symptoms. Uncertainty remains regarding the long-term data for this indication, as follow-up durations were typically limited to only a few weeks.

Research Evidence for Chronic Hives (Chronic Idiopathic Urticaria)

Asitrol was studied for use in conditions associated with chronic hives, which are characterized by fluctuating manifestations. The evidence includes RCTs and smaller double-blind crossover studies. The outcomes that research examined were specific to hives, focusing on the size and number of wheals and the severity of pruritus (itching). Some studies explored research scenarios for patients designated as refractory; however, some of these studies had sample sizes that were modest. The long-term effects are not fully established for use over periods extending beyond a few months.

Study Focus on Special Patient Groups and Research Gaps

Research has explored how the medicine was evaluated in both the Pediatric population (children) and older adults. The evidence indicates that the medicine was studied across a broad age range. However, specific subgroup findings for individuals with multiple pre-existing health conditions are still emerging. Official summaries note that follow-up durations were limited in many of the core trials. Data for certain groups remain insufficient, and comparative evidence against some newer alternatives is lacking in some research areas.

How should Asitrol be stored and disposed of?

How to Store and Dispose of Asitrol

Official regulatory documents define strict environmental controls for the storage and disposal of this medicine (Cetirizine Hydrochloride).

Storage Requirements

The product must be stored at controlled room temperature, typically 20°C to 25°C (68°F to 77°F), while being protected from excessive moisture. It is mandatory to keep the medicine in its original container and ensure the container remains tightly closed. The product must also be protected from freezing. To ensure child safety, the medicine must be stored out of the sight and reach of children at all times.

Disposal Instructions

Unused or expired product should be disposed of by utilizing a community drug take-back program. If no take-back program is available, the medicine should be mixed with an unappealing substance, sealed in a bag, and discarded in the household trash. The medicine must not be flushed down a toilet or drain.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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