Lertazin

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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 Lertazin

Property Description
Active ingredient Levocetirizine dihydrochloride
Form Tablet (film-coated) and Oral Solution
Pharmacological Class Second-generation Antihistamine (H1-receptor antagonist)
General Purpose Symptom relief for allergic conditions
Origin Synthetic, purified (R)-enantiomer
Status Available Over-The-Counter (OTC) or prescription, depending on the country.

Lertazin is a synthetic medicinal preparation intended for oral administration, and it is classified pharmacologically as a second-generation antihistamine. The active substance is levocetirizine dihydrochloride.


What Type of Medicine is Lertazin?

Levocetirizine falls under the therapeutic class of H1-receptor antagonists. Levocetirizine is chemically unique as the purified (R)-enantiomer of the older, racemic compound, cetirizine. This targeted synthesis makes levocetirizine highly selective and generally distinguishes it from first-generation antihistamines which carry a greater propensity for central nervous system effects. This classification means the medicine is specifically designed to interfere with a key chemical trigger of allergic reactions. This chemical refinement provides a differentiating factor within the overall antihistamine class.


Composition, Forms, and General Purpose

The composition of Lertazin centers entirely on levocetirizine, which is formulated for public use as a single product in two principal dosage forms: the film-coated tablet and the oral solution. Both forms deliver the exact same active ingredient. Levocetirizine is used for the management of allergic symptoms. The purpose of Lertazin is therefore to offer symptom relief by mitigating the physical effects of histamine release in the body, a characteristic of H1-antagonists. Its action as a selective H1-antagonist helps to reduce the physical consequences of the body's allergic response, often used for conditions like hay fever.

What side effects are possible with Lertazin?

Possible Side Effects and Safety Information

The safety profile of Lertazin (levocetirizine dihydrochloride) is established through regulatory classification, grouping possible effects by frequency and the body system affected, according to official documents like the FDA label and EMA Summary of Product Characteristics (SmPC).

Adverse Reaction Classification

Adverse reactions are categorized based on their likelihood of occurrence:

  • Common (may affect up to 1 in 10 people): Fatigue, somnolence (drowsiness), headache, dry mouth, and pharyngitis (sore throat) are most frequently reported.
  • Uncommon (may affect up to 1 in 100 people): Effects such as abdominal pain and asthenia (loss of strength) have been documented.

System-Organ Groupings

Side effects that occur less frequently are listed across various system-organ classes, including Nervous System Disorders (e.g., convulsions, tremor), Gastrointestinal Disorders (e.g., nausea, diarrhea), and Psychiatric Disorders (e.g., aggression, insomnia).

Serious Safety Considerations

Regulatory documents list certain rare but serious adverse reactions. These include severe hypersensitivity reactions, such as anaphylaxis and angioneurotic edema (swelling of the face or throat). Rare reports of systemic effects such as hepatitis and jaundice (yellowing of the skin or eyes) are also documented.

Safety Constraints

Use of this medicine is contraindicated in patients with a known history of hypersensitivity to levocetirizine, cetirizine, or any of the product components. It is also contraindicated in individuals with end-stage renal disease or severe renal impairment. Regulatory notes indicate that combining levocetirizine with alcohol or other Central Nervous System (CNS) depressants may lead to additive effects, which can result in reduced alertness.

Overdose and Emergency Response

Overdose and when to seek help

Taking an amount exceeding the prescribed or recommended dose requires immediate emergency medical attention and contact with a national Poison Control Center, as strictly mandated by regulatory authorities. The officially documented clinical manifestations of Lertazin (levocetirizine) overdose are categorized by Central Nervous System (CNS) effects, which are differentiated based on age.

In adults, the primary sign of overdose is documented as significant drowsiness (somnolence). Conversely, the official labeling notes that in children, the presentation may be biphasic: an initial phase of agitation or restlessness is explicitly described, which is subsequently followed by the state of drowsiness. This age-specific observation is critical for defining the overdose profile.

When an overdose occurs, the official management measure is symptomatic and supportive treatment. Regulatory information confirms that no specific antidote is known for levocetirizine dihydrochloride. Additionally, while general measures to remove unabsorbed drug (such as gastric lavage) may be considered following short-term ingestion, the labels clarify that standard procedures like dialysis (haemodialysis) are not effective for removing levocetirizine from the body. Immediate priority remains seeking urgent medical help as directed.

Therapeutic Uses of Lertazin

Lertazin (levocetirizine) is commonly applied across domains where additional symptomatic support is needed for conditions characterized by periods of heightened symptoms associated with inflammatory or irritative states. The medicine is indicated for the support of symptoms associated with seasonal and perennial allergic rhinitis, and for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria.

The medicine is relevant for managing disruptive symptom clusters in both the nasal/ocular and dermal areas. It is used for managing conditions such as hay fever, seasonal allergic rhinitis, perennial allergic rhinitis, and chronic idiopathic urticaria (hives). It is relevant for easing discomfort related to symptoms that interfere with daily functioning, including frequent sneezing, a runny nose, itchy/watery eyes, and intense skin itching (pruritus) with associated wheals or rash.

The overall benefit is that Lertazin offers symptomatic relief when symptoms become more noticeable, and may assist with managing symptom fluctuations during difficult episodes.

“Lertazin is relevant when supportive symptom management is appropriate across domains involving irritative states.”


Quick Fact: Support for Key Allergic Domains
This medicine is commonly used to help manage symptoms related to nasal irritation, ocular discomfort, and dermal swelling/itching that are characteristic of acute or recurrent allergic episodes.

Eligibility and Restrictions for Use

Who Can and Cannot Use Lertazin?

The eligibility for Lertazin (levocetirizine) use is primarily determined by age, kidney function, and known drug hypersensitivity, based on official regulatory documents.

Populations Who Must Not Use Lertazin (Contraindications)

Official regulatory information strictly prohibits the use of this medicine in the following groups:

  • Hypersensitivity: Individuals with a known allergy to the active ingredient, levocetirizine, or to its parent compound, cetirizine, or any related piperazine derivatives (such as hydroxyzine).
  • End-Stage Kidney Disease: Patients diagnosed with severe or end-stage renal disease (Creatinine Clearance less than 10 mL/min) or those requiring dialysis, as the drug is mainly cleared by the kidneys.
  • Pediatric Patients with Kidney Impairment: Children between 6 months and 11 years of age who have any degree of impaired kidney function.

Eligibility for Use by Age and Condition

Lertazin is generally allowed for adults and children 6 months of age and older. However, use is limited for the elderly and those with kidney issues:

  • Kidney Impairment: Adults and adolescents 12 years and older with mild, moderate, or severe kidney impairment require a specific dose adjustment and monitoring by a healthcare provider.
  • Breastfeeding: Use is generally advised against in women who are breastfeeding due to the expectation that the medicine will pass into breast milk.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The official interaction profile of levocetirizine is defined by specific pharmacodynamic and pharmacokinetic patterns documented in regulatory labeling.

A major pharmacodynamic interaction involves co-administration with Central Nervous System (CNS) depressants. The label states that concurrent use with alcohol or other CNS depressants should be avoided because this combination may cause additional reductions in alertness and impairment of performance.

Clearance-related restrictions are mandatory: The medicine is contraindicated in patients with end-stage renal disease (CrCl < 10 –15 mL/min) and those undergoing dialysis. This is due to its reliance on renal excretion via active tubular secretion. Formal dose adjustments are required for other stages of renal impairment, but no adjustment is needed for solely hepatic impairment.

Limited pharmacokinetic data is derived from studies with the parent racemate, cetirizine. Co-administration of the racemate with ritonavir resulted in a documented approx 40% increase in the extent of exposure (AUC), while with theophylline, a approx 16% decrease in clearance was observed.

Regarding drug-food interactions, the medicine can be taken without regard to food consumption. Food is documented to delay the rate of absorption (T max delayed) but does not reduce the overall extent of absorption (AUC).

Mechanism of Action

How Lertazin Works

Lertazin's action is primarily defined by its highly selective antagonism at the peripheral Histamine H1 receptors , which are biological targets involved in acute inflammatory responses. The drug binds to these receptors on cells like smooth muscle and endothelial cells, stabilizing them in an inactive conformation. This mechanism prevents the endogenous chemical mediator, histamine, from binding and initiating its cellular signaling sequence.

This blockade of the H1 receptor modifies early molecular steps that influence the downstream inflammatory cascade. The drug's action further limits the propagation of these effects by stabilizing certain immune cells and inhibiting the further release of other pro-inflammatory substances. This mechanism induces a more regulated state within targeted pathways by counteracting the activity of released mediators.

Physiologically, the mechanism restricts the effect of mediator activity by reducing the histamine-driven contraction of smooth muscles and lowering microvascular permeability (the passage of fluid across blood vessel walls), resulting in adjustments that characterize the drug's overall action.

Dosage and Administration Information

Official Administration Guidelines for Lertazin

Lertazin (levocetirizine dihydrochloride) is approved for oral administration, utilizing either the 5 mg film-coated tablet or the oral solution (2.5 mg/5 mL). The fundamental use pattern across approved age groups is a once-daily dose taken in the evening.

Dosage and Frequency

Population Standard Dosing Regimen Frequency and Timing
Adults and Adolescents (12 years and older) 5 mg once daily (or 2.5 mg for some) Once daily, in the evening
Children 6 to 11 years 2.5 mg once daily Once daily, in the evening
Children 6 months to 5 years 1.25 mg once daily (oral solution) Once daily, in the evening

The medicine is designed for administration without regard to food consumption. The 5 mg tablet is scored, allowing it to be broken for the purpose of administering the 2.5 mg dose when appropriate.

Procedural Constraints

The most significant constraint on Lertazin's use relates to kidney function. For patients 12 years and older with decreased renal function, the dose and frequency must be adjusted according to the degree of impairment (creatinine clearance, CrCl), requiring extended intervals or reduced amounts (e.g., 2.5 mg once daily for mild impairment). Administration is not appropriate for pediatric patients (6 months to 11 years) with impaired kidney function, or for adults with end-stage renal disease (CrCl < 10 mL/min). The duration of use may range from short-term to continuous therapy, based on the nature of the condition. If a dose is missed, the standard procedure involves skipping the missed dose and continuing with the next scheduled dose, without taking a double amount.

Recent Clinical Evidence

Research Evidence / Overview of Studies

This section outlines the types of research and key findings from clinical and preclinical studies that evaluated Lertazin, a potent, second-generation antihistamine.


Summary of Clinical Studies

Studies were conducted to assess Lertazin's potential role in relieving symptoms associated with various allergic conditions, primarily seasonal and perennial allergic rhinitis and chronic urticaria (hives). Randomized, double-blind, placebo-controlled trials form the majority of the clinical data.

Studies were studied for its potential association with the earliest time points of change and continued lessening of acute symptoms. The focus of the research was primarily on measurements of short-term drug activity, using changes in standardized symptom scores as primary endpoints. Initial findings reported a numerical response in a majority of subjects, and studies also investigated an association with an improvement in overall quality of life.


Safety and Tolerability Profiles

Studies evaluated the tolerability in adult and pediatric populations, though specific patient subgroups were often excluded from initial research. The research protocols required regular monitoring for potential side effects. Reported side effects in the clinical trials were generally classified as mild to moderate and included temporary gastrointestinal discomfort and headache.

Mechanism of Action (Preclinical Research)

Preclinical investigations explored whether the compound’s activity, as defined by receptor binding studies, was linked to a reduction in the experience of pain and inflammation associated with histamine release. Preclinical studies in animal models and in vitro settings focused on the activity of the compound, confirming its high selectivity for the H1-receptor.

Combination Therapy

Some research has examined the difference in findings regarding symptom control and quality of life over time when Lertazin is used as a monotherapy versus when it is combined with other older generation antihistamines in difficult-to-treat cases.

Frequently Asked Questions (FAQ)

Common questions about Lertazin (FAQ)


Q: How long does it typically take before Lertazin starts working?

The official product information indicates that Lertazin acts rapidly. The highest concentration of the medicine in the blood, known as peak plasma concentration, is typically reached in approximately 0.9 hours after taking the tablet form in adults. For the oral solution, this peak concentration is reached even faster, in about 0.5 hours.


Q: What information is available about Lertazin use during pregnancy?

According to the official drug prescribing information, Lertazin is assigned to Pregnancy Category B. This classification means that while initial studies in animals showed no harm to the fetus, research in pregnant women is limited. Official sources state that this medicine is intended for use during pregnancy only if it is clearly needed.


Q: Is Lertazin considered a controlled substance?

Official documents confirm that Lertazin (levocetirizine) is not classified as a controlled substance. It is not listed under the U.S. Controlled Substances Act (CSA) schedule.


Q: Are there warnings about driving or operating machinery while on Lertazin?

Official warnings caution against performing tasks that require complete mental alertness, such as driving a vehicle or operating heavy machinery. This caution is included because fatigue, drowsiness (somnolence), and loss of strength (asthenia) have been reported.


Q: What is the risk of dependence or withdrawal with Lertazin?

Official postmarketing reports have documented cases of new onset, severe itching (pruritus) that may occur a few days after stopping the medicine, especially following long-term use. The product label suggests consulting a healthcare provider if symptoms occur, as improvement has been noted when the medicine is restarted or tapered.


Q: What is the purpose of the boxed warning (if any) on Lertazin?

Lertazin does not currently have a Boxed Warning, which is the most stringent type of warning mandated by the FDA. However, the FDA has required the addition of a specific warning regarding the risk of severe itching upon discontinuation after long-term use.


Q: Can patients with kidney problems use Lertazin?

Official documents state that use is prohibited (contraindicated) for patients with end-stage renal disease (severe kidney failure). For adults and adolescents 12 years and older with mild to moderate kidney issues, a specific dose adjustment and monitoring may be necessary. The medicine is also prohibited for children under 12 years of age with any degree of impaired kidney function.


Q: What is the difference between brand-name Lertazin and generic versions?

The FDA has determined that generic versions of Lertazin contain the same active ingredient and are considered equally effective as the brand-name product. The primary differences are typically related to cost and the non-active ingredients, such as the fillers used in the formulation.


Q: Can Lertazin be used for anxiety that is not related to its main use?

Official information states the drug is only indicated for allergic rhinitis and chronic idiopathic urticaria, which are its approved uses. Postmarketing surveillance reports have documented cases of psychiatric effects, including anxiety and aggression, but these are noted as potential adverse reactions, not indications for use.


Q: Is Lertazin known to cause any skin reactions or rashes?

Studies show Lertazin is indicated to help manage the skin-related symptoms of chronic idiopathic urticaria (hives or itching). However, rare but serious side effects, including severe hypersensitivity reactions and swelling of the face or throat (angioneurotic edema), are listed in the official adverse reactions section.


Q: Does Lertazin affect birth control pills?

Official regulatory drug labels and interaction resources do not list a specific interaction between Lertazin and hormonal oral contraceptives (birth control pills).


Q: Does Lertazin interact with caffeine?

Official drug interaction resources generally do not list a specific interaction with caffeine. The official label does warn that the medicine should be avoided with alcohol or other central nervous system (CNS) depressants due to potential additive effects on alertness.


Q: Can Lertazin be taken with antacids or heartburn medication?

The official drug label notes that Lertazin can be taken without regard to food consumption. No specific interaction between Lertazin and common antacids or heartburn medication is listed in the official prescribing information.


Q: Why is Lertazin sometimes called by its generic name?

Regulatory and scientific sources often refer to the medicine by its generic name, which is levocetirizine dihydrochloride. The generic name is the standardized, non-proprietary chemical name for the drug's active ingredient and is used to ensure clarity across all medical and pharmacological references.


Q: Does taking Lertazin require regular blood tests or monitoring?

Routine blood tests or clinical monitoring are not explicitly mandated for all patients in the standard prescribing information. However, the initial research protocols for the drug did require regular monitoring of certain lab parameters, such as kidney and liver function.


Q: Can Lertazin be used by children?

Lertazin is generally allowed for children 6 months of age and older for certain indications, with specific lower doses outlined in the label. However, official safety information states that use is not appropriate (contraindicated) for children between 6 months and 11 years of age who have any degree of impaired kidney function.

How should Lertazin be stored and disposed of?

Storage and Stability

Lertazin, like all prescription medications, must be stored according to the conditions stated in its official product labeling to maintain its stability and effectiveness. If no specific temperature is stated, the product should be kept at controlled room temperature, which is typically between 68 F and 77 F (20 C and 25 C), with permissible short excursions. It is essential to keep the medicine in its original container and away from heat, moisture, and excessive light. Keep all medicines secured and out of the reach of children.

Disposal of Unused Medicine

The most recommended method for disposing of expired or unused Lertazin is by using a drug take-back program or an authorized mail-back envelope. If these options are not readily available and Lertazin is not on the federal flush list, it can typically be thrown in your household trash. To prepare for trash disposal, mix the medicine with an undesirable substance like dirt or used coffee grounds, place the mixture in a sealed container, and then discard it in the trash. Always remove or scratch out all personal information on the packaging before disposal.

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

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