Levohistam

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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 Levohistam

What is Levocetirizine (Levohistam)? Overview and Quick Facts

Property Description
Active Ingredient Levocetirizine dihydrochloride
Common Forms Oral tablets (scored), oral solution
Pharmacological Class Second-generation H₁ Antihistamine
Common Use Symptomatic relief of allergies and hives
Origin Synthetic

What Type of Medicine is Levocetirizine? (Identity & Class)

Levocetirizine is the International Nonproprietary Name (INN) for the active ingredient in medications commonly known by brand names or regional names like "Levohistam." It is a synthetic substance classified as a second-generation H₁-receptor antagonist. This classification identifies it as a modern type of allergy medication designed to block the effects of histamine in the body.

A key feature of Levocetirizine is that it is formulated as the active enantiomer of cetirizine, which means it is a purified and highly targeted compound. This targeted composition contributes to its effectiveness at controlling the histamine response.


Why Levocetirizine is Used: General Therapeutic Purpose (Application)

The core purpose of Levocetirizine is to provide symptomatic relief for the discomfort associated with various allergic conditions. It is used for managing the effects of seasonal and perennial allergic rhinitis (hay fever and year-round allergies), as well as chronic, unexplained skin conditions such as idiopathic urticaria (hives).

By controlling the body's overreaction to allergens, the medicine helps alleviate physical manifestations like sneezing, nasal discharge, itchy or watery eyes, and the itching and swelling associated with hives. This makes it a foundational choice for patients who require consistent control over their recurring allergy symptoms.

What side effects are possible with Levohistam?

Possible Side Effects and Safety Information for Levocetirizine

The safety profile of levocetirizine, the active ingredient in Levohistam, is defined by adverse reactions classified according to their frequency in regulatory documentation and by specific safety constraints.

Frequency-Classified Adverse Reactions

Adverse reactions are grouped based on frequency observed in clinical trials, supplemented by post-marketing reports for events where the frequency is Not Known (cannot be reliably estimated).

Classification Examples of Reactions
Common (Reported ge1/100 to <1/10) Somnolence (drowsiness), Fatigue, Headache, Dry mouth, Nasopharyngitis.
Uncommon (Reported ge1/1,000 to <1/100) Asthenia (unusual weakness), Abdominal pain.

System-Organ Class and Serious Reactions

Adverse events are formally grouped by the body system affected, including Nervous System Disorders, Gastrointestinal Disorders, Psychiatric Disorders, and Immune System Disorders. Less frequent but clinically significant events documented in post-marketing reports include severe Hypersensitivity reactions (such as Anaphylaxis and Angioneurotic oedema), Convulsions, Urinary retention, and Suicidal ideation. These serious reactions are categorized in regulatory documents under the Not Known frequency tier.

Safety Constraints and Special Populations

Use of levocetirizine is contraindicated in individuals with severe renal impairment or end-stage renal disease (Creatinine Clearance <10 mL/min). Caution is required for older adults due to the higher likelihood of decreased kidney function and for patients with risk factors for urinary retention or seizures. The official safety documents also note that the concurrent use of alcohol or other Central Nervous System (CNS) depressants may lead to additive reductions in alertness. Furthermore, there are documented reports of new or worsened pruritus (itching) occurring upon discontinuation, typically after prolonged use.

Overdose and Emergency Response

Overdose and When to Seek Help

Immediate medical attention is mandated by regulatory authorities for any suspected overdose of levocetirizine. The official prescribing information documents specific clinical manifestations associated with the ingestion of high doses, primarily affecting the central nervous system (CNS).


Documented Overdose Manifestations

Population Primary Documented Manifestations
Adults Marked drowsiness (somnolence) is the main reported sign.
Pediatric Patients Often exhibit initial agitation and restlessness, which may then transition to drowsiness.

Additional manifestations observed across age groups include tachycardia (rapid heart rate) and nausea.


Official Emergency Actions

Management of overdose is officially described as symptomatic and supportive treatment. The regulatory profile explicitly notes that no specific antidote is known for levocetirizine. Furthermore, the active substance is not effectively removed by standard hemodialysis procedures.

Procedural steps, such as gastric lavage or administration of activated charcoal, may be considered by healthcare professionals shortly after ingestion. Due to the lack of an antidote and limitations in clearance, clinical monitoring in a healthcare setting is required for observation and supportive care.

Therapeutic Uses of Levohistam

What Levohistam Treats: Main Uses and Benefits

Levocetirizine (Levohistam) is commonly used in situations involving certain distressing symptoms. The medication is relevant across domains characterized by episodic or fluctuating symptom patterns that create noticeable interference with daily stability.


This medication is applied across therapeutic domains including seasonal allergic rhinitis (hay fever), perennial allergic rhinitis (year-round allergies), and chronic idiopathic urticaria (hives). It is used for managing symptom clusters that may become intense or disruptive, such as sneezing, rhinorrhea (runny nose), and the pronounced itching and wheals associated with skin manifestations.

Commonly used during phases when symptoms become more noticeable, Levohistam is relevant when supportive symptom management is appropriate. Offering symptomatic relief may help patients cope more steadily with difficult episodes and contributes to maintaining a sense of stability when symptoms are more noticeable.


Quick Fact: Relief for Allergic Itching and Hives

This medication is often applied to ease challenging cutaneous symptoms, specifically pruritus (itching) and the presence of wheals (red, raised welts) associated with persistent hives.

Eligibility and Restrictions for Use

Levocetirizine (Levohistam) eligibility is strictly defined by regulatory authorities based on patient age and kidney function. Official labeling outlines specific populations who are approved for use, those who require conditional use, and those who are absolutely prohibited from taking the medicine.

Who Must Not Use Levohistam (Contraindications)

Population Group Eligibility Status Basis
Hypersensitivity Contraindicated Allergy to levocetirizine, cetirizine, or ingredients.
End-Stage Renal Disease Contraindicated Creatinine clearance below 10 mL/min or hemodialysis.
Children (6 mos to 11 yrs) Contraindicated If they have any degree of impaired renal function.

Age and Condition-Based Restrictions

  • Approved Ages: The medicine is approved for use in patients aged 6 months and older. Safety and efficacy are not established for infants under 6 months of age.
  • Renal Impairment (Adults/Adolescents 12+): Patients with mild, moderate, or severe kidney impairment are allowed to use the medicine, but conditional use requires adjustment based on the severity of impairment.
  • Older Adults (65+): Use requires caution due to the increased probability of age-related decline in kidney function.
  • Pregnancy and Lactation: Use during pregnancy is permitted only if clearly needed. Use is not recommended while breastfeeding.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory documentation details the specific documented interaction patterns for levocetirizine (Levohistam), focusing on pharmacodynamic and pharmacokinetic effects.

Documented Interaction Patterns

Interaction Type Interacting Substance / Category Official Regulatory Outcome
Pharmacodynamic Alcohol and Central Nervous System (CNS) Depressants Co-administration should be avoided due to the risk of additional impairment of CNS performance and reduction in alertness.
Pharmacokinetic Food intake Does not affect the total extent of exposure (AUC), but delays the time to peak concentration and lowers the peak concentration (Cmax) by 36%.
Pharmacokinetic Ritonavir and Theophylline Studies indicate these substances can reduce the clearance of the antihistamine component, potentially increasing systemic exposure.

Other Regulatory Notes

In vitro data formally indicate that levocetirizine is unlikely to cause pharmacokinetic interactions by altering the activity of major hepatic drug-metabolizing enzymes (CYP and UGT). The drug's interaction profile is important for patients with impaired renal function since the medication is substantially excreted by the kidneys, making this population more sensitive to any clearance-altering interactions. No mandatory timing or separation rules are documented for co-administered substances.

Mechanism of Action

Selective H1 Receptor Antagonism

Levohistam (levocetirizine) operates primarily by acting as a selective inverse agonist at the peripheral Histamine H1 receptors found on various effector cells, including vascular endothelial cells and smooth muscle cells. By binding to these receptors and stabilizing their inactive conformation, the drug prevents the binding and subsequent activation by the endogenous inflammatory mediator histamine. This selective interaction fundamentally modulates the signaling patterns characteristic of acute histamine-mediated physiological responses.


Modulation of Cellular Inflammatory Cascades

Beyond direct receptor blockade, Levohistam engages secondary mechanisms that influence downstream inflammatory cascades. This includes regulating the activity and migration of specific immune cells, such as eosinophils, and modulating the release of certain pro-inflammatory mediators from target cells. This action influences pathway dynamics within inflammatory processes and contributes to the multifaceted nature of the drug's overall pharmacological activity, influencing the magnitude of mediator-induced activity on target tissues.

Dosage and Administration Information

How Levohistam Is Used: Administration Guidelines

Levohistam (levocetirizine) is used according to specific, standardized instructions. The administration protocol details the dosage, frequency, route, and required adjustments to ensure the medicine is used according to established protocols.


Administration Scope

Feature Standard Parameters
Route of administration Oral (via tablet or solution)
Dosing schedule (Adults ge 12) The standard dose is 5 mg once daily. A lower 2.5 mg once daily dose may also be used.
Timing in relation to meals May be taken with or without food.
Preparation requirements The tablet form is administered with liquid.
Age-group administration rules Dosing varies by age: 2.5 mg once daily is standard for children 6 to 11 years, and 1.25 mg once daily (via solution) for children 6 months to 5 years.
Missed-dose rules If a dose is missed, the next dose should be taken at the scheduled time; a double dose should not be taken to compensate.
Special procedural conditions The standard dose is recommended to be taken in the evening. Dose modification (reduction in amount or frequency) is utilized in adults based on the degree of renal impairment.

Use Protocol Structure

Levohistam is consistently administered using a once-daily oral schedule. This protocol describes how the medication can be taken regardless of meal timing but is ideally taken in the evening. The dose is reduced when renal function is impaired to maintain appropriate exposure. The duration of use is determined by the nature of the condition, permitting both short-term use for acute episodes and long-term use for chronic conditions.

Recent Clinical Evidence

Levohistam: Recent Clinical Evidence

Research has been conducted to evaluate the effects of the investigational drug Levohistam in populations experiencing specific health conditions. The body of evidence primarily involves randomized controlled trials (RCTs) and long-term observational studies.


Study 1: Primary Efficacy and Safety Trial

The foundational study, a Phase 3 RCT, evaluated whether the drug is associated with changes in the frequency and severity of symptoms compared to a placebo group. The research examined the mean number of symptomatic days reported by participants over a 12-week period.

  • The research focused on the higher dose group.
  • Study findings included a reporting period focused on changes in participant-reported symptom metrics within 48 hours.
  • Secondary outcomes focused on examining changes in quality of life metrics and reported adverse events.

Study 2: Long-Term Observational Follow-up

A subsequent open-label study was conducted to assess the data profile for long-term use, extending the follow-up period to two years. Long-term use has been the focus of research; studies examined the magnitude of observed changes over the extended period. This research evaluated potential associations between the drug and general health indicators.


Studies on Combined Use and Comparison

This drug has been the subject of research comparing it to older treatments; studies examined the time course of effects for acute episodes. These head-to-head trials evaluated the differences in reported side effect profiles and the percentage of participants who discontinued treatment due to adverse events.

Research also explored whether combining the investigational drug with other specific treatments is associated with different outcomes.

Frequently Asked Questions (FAQ)

Common questions about Levohistam (FAQ)


Q: How quickly should I expect Levohistam to start working for my symptoms?

Studies and official information indicate that initial effects may be observed as early as 1 hour after administration. It is important to note that the onset of effect can vary between individuals.


Q: How long does the effect of a single dose of Levohistam typically last?

The duration of effect is tied directly to the medication's prescribed use. Official regulatory dosing instructions prescribe Levohistam on a once-daily schedule. This schedule is based on the drug's established action time, which is designed to provide consistent relief over approximately a 24-hour period.


Q: What is the potential concern about stopping Levohistam after long-term use?

Regulatory documents report that some individuals experience new or worsened itching (pruritus) upon discontinuing the medicine, particularly after having used it for months or years. If discontinuing the medication, particularly after long-term use, it is appropriate to consult with a healthcare professional.


Q: What are the main differences between Levohistam and Cetirizine (Zyrtec)?

Levohistam contains the active ingredient levocetirizine. Levocetirizine is described in official sources as the single active component (enantiomer) of the chemical mixture known as cetirizine. This means Levohistam is a more targeted version of the component in cetirizine responsible for the antihistamine effect.


Q: Are there any reported cognitive side effects like difficulty concentrating with Levohistam?

Official reports on adverse reactions include potential effects on the nervous system and psychological function. These reactions can include feeling restless, experiencing dizziness, and some individuals have reported trouble concentrating. Although not common, patients should be aware of these potential effects.


Q: Are there any precautions for using Levohistam in patients with an enlarged prostate?

Regulatory documents advise caution when Levohistam is used by individuals with existing factors that predispose them to urinary retention (difficulty emptying the bladder). Conditions like prostatic hyperplasia (enlarged prostate) are included in the factors that require caution.


Q: Can Levohistam be taken for non-allergy related itching or skin conditions?

Levohistam is officially indicated for the relief of symptoms related to various allergic conditions, including Chronic Idiopathic Urticaria (hives), which is a skin condition. Official indications focus on conditions such as Chronic Idiopathic Urticaria; general non-specific itching beyond these indications is not specifically addressed in the regulatory documentation.


Q: Is there any difference between the prescription and over-the-counter (OTC) versions of Levohistam?

In some countries or regions, the over-the-counter (OTC) and prescription versions of the medication may have differences, particularly concerning the age groups or specific conditions they are officially approved to treat. This is determined by the local regulatory authority.


Q: What are the most common side effects of Levohistam in children (e.g., ages 6-11)?

In clinical trials involving children ages 6 to 12, the most commonly reported adverse reactions were slightly different from those in adults. These included pyrexia (fever), somnolence (sleepiness), cough, and epistaxis (nosebleed).


Q: Is there any mention of unusual dreams or nightmares as a side effect of Levohistam?

Official reports indicate that nightmares have been noted in post-marketing reports. These are classified as a rare psychiatric adverse reaction that is not commonly observed.


Q: Can Levohistam be used to treat symptoms from insect bites or stings?

While the medication is indicated for the symptomatic relief of allergic conditions, including urticaria (hives), official labeling does not specifically name insect bites or stings as an indication.


Q: Is it normal to feel a bit restless or agitated when starting Levohistam?

Official documentation notes that both agitation and restlessness are reported psychiatric adverse reactions to the medicine. The frequency with which these reactions occur can vary, but they are recognized by regulatory bodies as potential effects.


Q: What is the difference in how Levohistam and first-generation antihistamines affect the brain?

Levohistam is categorized as a second-generation antihistamine. As such, it is described in official sources as having low penetration of the blood-brain barrier compared to older, first-generation antihistamines. This difference in penetration influences their respective central nervous system effects.


Q: Is there research on Levohistam's use in children under 6 years old?

Yes, Levohistam's active ingredient is approved by regulatory bodies for use in pediatric patients as young as 6 months of age for the treatment of specific allergic conditions. Dosage and use instructions vary by age group.


Q: What does official information say about taking Levohistam during pregnancy?

Official regulatory guidance states that the medicine should be used during pregnancy only if clearly needed. This regulatory guidance should be reviewed in consultation with a healthcare professional.


Q: What does official information say about taking Levohistam while breastfeeding?

Official regulatory guidance explicitly states that the use of Levohistam is not recommended while breastfeeding. This information should be reviewed in consultation with a healthcare professional.


Q: Does taking Levohistam cause any changes in appetite?

Official regulatory documentation includes increased appetite as a reported adverse reaction. This is noted as a less common effect, but it is recognized by safety monitoring bodies.


Q: How is Levohistam eliminated from the body?

The medicine is primarily eliminated through urinary excretion. Official product information states that approximately 85% of the dose is recovered from the urine and feces, with the majority being eliminated unchanged by the kidneys.


Q: What is the typical half-life of Levohistam in the body?

Pharmacokinetic data described in official documents show that the average terminal elimination half-life for Levohistam (levocetirizine) is approximately 8 to 9 hours in adults.


Q: Does Levohistam interact with grapefruit juice or other foods?

Official regulatory information notes that consuming the medicine with food may slightly delay the time it takes to reach maximum concentration in the blood. However, the overall amount of medicine absorbed into the body is not significantly affected. No specific interaction with grapefruit juice is officially documented.


Q: Are there any long-term safety studies on daily Levohistam use?

Yes, official documents describe data from long-term observational follow-up studies to assess the safety profile of the medication during extended use. These studies have extended the follow-up period up to two years.

How should Levohistam be stored and disposed of?

How to Store and Dispose of Levohistam?

The storage and disposal of levocetirizine (Levohistam) must adhere to the official conditions defined by regulatory authorities.

Storage Requirements

  • Temperature: Store the medication at a controlled room temperature, specifically between 20°C and 25°C (68°F and 77°F). Brief temperature excursions up to 30°C (86°F) are permitted.
  • Environment: The product must be stored away from excess heat and moisture and should be kept from freezing.
  • Child Safety: Always store the medicine out of the sight and reach of children.
  • Packaging: Keep the container tightly closed and do not use the product if the original container's seals are torn or missing.

Disposal Instructions

For disposal of unused or expired Levohistam, regulatory guidance recommends utilizing a drug take-back program. If this option is unavailable, the medicine should be mixed with an undesirable substance (such as coffee grounds or dirt) and placed in a sealed container before being thrown into the household trash. This product is not on the list of medicines recommended for flushing.

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

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