L-Sitrizin

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Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

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 L-Sitrizin

Levocetirizine is the active ingredient in medications used to treat symptoms of allergies, such as seasonal allergic rhinitis (hay fever) and chronic idiopathic urticaria (hives). It is classified as a second-generation antihistamine, a class of drugs known for effective symptom relief with a lower propensity for causing drowsiness compared to older medications.

Quick Facts
Active Ingredient Levocetirizine Dihydrochloride
Form Oral tablet, Oral solution (syrup)
Pharmacological Class Second-Generation H1-Receptor Antagonist
Common Use Relief of allergy symptoms (e.g., sneezing, itching, runny nose)
Origin Active L-enantiomer of Cetirizine

Chemically, levocetirizine is the active, purified L-enantiomer of cetirizine, which means it contains the isomer primarily responsible for the therapeutic effect. This gives it a highly selective action as an H1-receptor antagonist.

The medication works by blocking the action of histamine, a substance naturally released by the body during an allergic reaction, which helps to alleviate the associated discomfort, such as itching and inflammation. It is designed for once-daily use and is clinically recognized for offering 24-hour relief, which supports its effectiveness in the long-term management of persistent allergic conditions. Available both over-the-counter and by prescription, levocetirizine is a widely used and well-studied component of allergy treatment plans worldwide.

What side effects are possible with L-Sitrizin?

Possible side effects and safety information

The safety profile of levocetirizine is officially documented across regulatory sources, classifying possible adverse reactions by frequency and affected body system. All safety information is based on controlled studies and post-marketing surveillance, distinguishing between common reactions and rare but serious concerns.


Official Adverse Reaction Categories

Adverse reactions are classified according to official frequency standards:

Frequency Classification Examples of Officially Listed Adverse Reactions
Common (up to 1 in 10) Somnolence (drowsiness), fatigue, headache, dry mouth
Uncommon (up to 1 in 100) Asthenia (lack of energy/physical weakness), abdominal pain

These effects primarily involve the Nervous System (e.g., somnolence) and the Gastrointestinal System (e.g., dry mouth).


Serious Adverse Reactions and Safety Constraints

The regulatory profile documents the potential for rare but clinically significant reactions, including severe Hypersensitivity Reactions, such as anaphylaxis or angioedema, as well as reports of convulsions and hepatitis.

Official labeling defines specific constraints for use. Levocetirizine is contraindicated in individuals with severe renal impairment (creatinine clearance less than 10 mL/min) and those with known hypersensitivity to any piperazine derivatives. Caution is advised for older adults and individuals with urinary retention predisposing factors, as the risk of adverse reactions may be increased. Concomitant use with alcohol or other CNS depressants is noted in regulatory text to potentially lead to further reductions in alertness. Furthermore, some reports indicate pruritus (itching) upon discontinuation of the medicine.

Overdose and Emergency Response

Overdose and When to Seek Help

The following information summarizes the official regulatory guidance on levocetirizine overdose and is not a substitute for professional medical advice.

Immediate medical attention is required in the event of a suspected overdose. Contact a poison control center or emergency services immediately if a dose of at least five times the recommended daily amount is known or suspected to have been taken.

Documented Overdose Manifestations

Symptoms following levocetirizine overdose are primarily related to Central Nervous System (CNS) effects and potential anticholinergic effects, as documented in regulatory prescribing information. Manifestations may include:

  • Adults: Somnolence (drowsiness), confusion, stupor, fatigue, dizziness, and headache.
  • Children: Initial agitation and restlessness may precede somnolence.

Overdose Management

Management Focus Official Guidance
Antidote No known specific antidote exists.
Treatment Treatment should be symptomatic and supportive.
Decontamination Gastric lavage may be considered following recent ingestion.
Elimination Dialysis (hemodialysis) is not effective for removing levocetirizine.

All individuals with a known or suspected overdose should be immediately transported to a medical facility for assessment and appropriate supportive care.

Therapeutic Uses of L-Sitrizin

Quick Facts on Uses

  • Relieves symptoms associated with seasonal allergic rhinitis.
  • Addresses symptoms of perennial (year-round) allergic rhinitis.
  • Supports management of chronic hives (uncomplicated skin manifestations of chronic idiopathic urticaria).

What Levocetirizine Treats: Main Uses and Benefits

Levocetirizine is a medication utilized to support the relief of symptoms related to specific allergic conditions. Its established role is in addressing the discomfort associated with both seasonal and perennial allergic rhinitis. Seasonal allergic rhinitis, commonly referred to as hay fever, can cause symptoms such as sneezing, a runny nose, and itchy, watery eyes. Perennial allergic rhinitis involves similar symptoms that occur throughout the year.

The medication is also indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria, commonly known as chronic hives. For these conditions, levocetirizine may help mitigate the associated itching and rash. Patients should discuss their individual needs and the appropriate use of this treatment with a qualified healthcare provider to ensure optimal management of their symptoms.

Eligibility and Restrictions for Use

This section outlines the official population eligibility and exclusion criteria for levocetirizine, as defined by regulatory bodies (e.g., FDA, EMA). These rules determine who is permitted to use the medicine and who must not use it.

Contraindications (Who Must NOT Use)

Levocetirizine is strictly contraindicated for the following groups:

  • Patients with a known hypersensitivity to levocetirizine, any of its ingredients, or other piperazine derivatives, such as cetirizine or hydroxyzine.
  • Patients with end-stage renal disease, defined as a creatinine clearance (CLCR) of less than 10 mL/min or those undergoing hemodialysis.
  • Children aged 6 months to 11 years with any degree of impaired renal function.

Eligibility and Restrictions

Population Group Eligibility Status & Constraint
Age (Adults/Adolescents) Approved for use in adults and adolescents 12 years of age and older.
Age (Children <6 Years) Safety and efficacy are not established for infants under 6 months. The tablet formulation is not recommended for children under 6 years.
Renal Impairment Requires dose adjustment for patients 12 years and older with mild to severe renal impairment.
Hepatic Impairment No dose adjustment is needed in patients with solely impaired liver function.
Pregnancy/Lactation Use during breastfeeding is generally not recommended due to likely excretion into human milk.
Special Caution Use is restricted and requires caution in patients with predisposing factors for urinary retention (e.g., spinal cord lesion) or a history of epilepsy/convulsions.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Levocetirizine's interaction profile is primarily defined by its effects on the central nervous system (CNS) and its clearance via the kidneys, as documented in regulatory prescribing information.


Pharmacodynamic and Substance Interactions

Co-administration with alcohol (Ethanol) or other Central Nervous System (CNS) Depressants (such as sedatives or hypnotics) is officially restricted because it may lead to additive impairment of mental alertness and performance. Regulatory documents advise avoiding the concurrent use of these substances.

Pharmacokinetic Interactions

The most clinically significant pharmacokinetic interaction noted is with Ritonavir, a substance that significantly increases systemic exposure of the active compound by raising its AUC and C max and decreasing its clearance. Similarly, studies using low-dose Theophylline showed a small decrease in the clearance of the active compound. The drug is documented as unlikely to be involved in interactions via common CYP metabolic enzymes.

Population-Specific Notes

The risk of adverse reactions is greater in patients with renal impairment because levocetirizine is substantially excreted by the kidneys, increasing the clinical significance of any clearance-reducing interaction. In geriatric patients, clearance is approximately 33% lower, which also leads to higher systemic exposure.

Non-Interaction Statements

No known interactions with food or non-alcoholic drinks are officially documented in regulatory sources.

Mechanism of Action

The mechanism of action for levocetirizine is centered on its highly selective engagement with the peripheral Histamine H1 Receptor ( H1 R). It functions as an inverse agonist and antagonist, binding to the receptor and actively stabilizing its inactive conformation. This dual action suppresses both the receptor's intrinsic constitutive activity and blocks endogenous histamine from initiating signaling. This molecular blockade results in the suppression of histamine-driven signals in the vascular tissue and sensory nerves.

Beyond this primary receptor mechanism, the molecule modulates the late-phase inflammatory cascade by inhibiting the chemotaxis and subsequent accumulation of key inflammatory cells, specifically eosinophils and T-lymphocytes, in tissues. This cellular-level influence reduces the amplification and continuation of the inflammatory response.

The drug exhibits a strong peripheral preference for H1 R activity due to its low lipophilicity and efficient transport out of the central nervous system (CNS) by the P-glycoprotein system. This compartmentalization focuses the mechanism on peripheral targets, and the resulting physiological consequences, such as reduced vascular permeability, occur with low H1 R occupancy within the brain.

Dosage and Administration Information

Levocetirizine is administered through the oral route, available as a film-coated tablet, which may be scored, and as an oral solution (syrup). The standard daily dose for adults and adolescents geq 12 years of age is 5 mg, taken once daily in the evening. Some individuals may be adequately controlled by a lower dose of 2.5 mg once daily.

Administration and Timing

Tablets should be swallowed whole with liquid. The medication may be taken with or without food, as food does not significantly affect the extent of absorption. The single daily dose is typically recommended for administration in the evening.

Dosage Adjustment

Specific dosage modifications are required for certain populations due to the drug’s primary excretion pathway via the kidneys. For patients with mild renal impairment, the dose is reduced to 2.5 mg once daily. For moderate or severe renal impairment, both the dosage and frequency must be reduced or the interval extended, as the risk of increased systemic exposure is greater. No dose adjustment is specified for patients with solely hepatic impairment. Use is contraindicated in end-stage renal disease (creatinine clearance < 10 mL/min) and in pediatric patients aged 6 months to 11 years with impaired renal function. In the event of a missed dose, the next dose should be taken at the regularly scheduled time, and a double dose should not be taken to compensate.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Levocetirizine


Evidence for use in Seasonal and Perennial Allergic Rhinitis

Research on levocetirizine was evaluated in the context of allergic rhinitis, which includes both seasonal (hay fever) and perennial (year-round) types. This research has primarily been conducted using Randomized Controlled Trials (RCTs) to evaluate outcomes related to how symptoms evolve in the observed populations. Studies focus on outcomes linked to inflammatory or irritative states such as sneezing, runny nose, and itching, and monitored patient-reported outcomes describing perceived discomfort. Findings describe data show patterns related to the Total Symptom Score (TSS) and how symptoms evolved over short-term periods. What remains uncertain is the extent of research findings for the evaluation of nasal congestion specifically, and comparative evidence is lacking for extensive head-to-head trials against the full range of other similar allergy medications.


Evidence for use in Chronic Idiopathic Urticaria (Chronic Hives)

Levocetirizine was studied for Chronic Idiopathic Urticaria (CIU), or chronic hives. The main evidence was evaluated in placebo-controlled RCTs and subsequent Systematic Reviews. Research examined outcomes related to physical discomfort, specifically focusing on Itching Severity Scores and measurements of the size and number of the Wheals (hives). Studies reported that data show patterns related to Itching Severity Scores was observed in some studies when comparing the medicine to placebo. Findings related to the use of higher-than-standard dosing regimens was associated with certain patterns described in aggregate meta-analyses. The long-term effects are not fully established for sustained use of these regimens, as the core research is largely based on medium-term follow-up periods of up to three to six months.


Evidence in Specific Patient Populations and Research Gaps

Research has explored the medicine’s use in children with allergic rhinitis and chronic urticaria, with protocols including both older children and studies in children as young as six months. Findings describe group patterns, but the research does not determine whether an individual will respond similarly across all groups. Data for certain groups remain insufficient, particularly older adults with multiple comorbidities. A consistent limitation is that follow-up durations were limited for assessing long-term impact. Ultimately, research provides context for group patterns observed in studies, but it is important to remember that findings describe group patterns, not personal outcomes.

Key Studies & References Efficacy and safety of levocetirizine in seasonal allergic rhinitis: a systematic review and meta-analysis of randomized controlled trials

Frequently Asked Questions (FAQ)

Common questions about Levocetirizine (FAQ)


Q: How quickly does Levocetirizine start working for allergies?

A: Levocetirizine is known for rapid absorption after oral intake. According to the official product information, peak concentrations of the medicine in the blood are usually reached in about one hour after the tablet is taken.


Q: What should I do if I feel drowsy after taking Levocetirizine?

A: Drowsiness (somnolence), fatigue, and weakness have been reported as common side effects. Regulatory documents advise that individuals should be cautious about performing activities that require full mental alertness and coordination, such as driving a motor vehicle or operating machinery, if they experience these effects.


Q: Does Levocetirizine interact with alcohol?

A: Yes, official labeling advises caution. Taking the medicine concurrently with alcohol or other Central Nervous System (CNS) depressants should be avoided. This combination may lead to further impairment of mental alertness and performance.


Q: Is it normal to feel tired the morning after taking Levocetirizine?

A: Yes, tiredness or fatigue is a commonly reported side effect, along with drowsiness. This is consistent with the standard recommendation to take the single daily dose in the evening.


Q: Can I take Levocetirizine if I am taking blood pressure medication?

A: Regulatory information indicates the drug is unlikely to be involved in interactions via common metabolic enzymes. Information regarding use with specific blood pressure medications should be discussed with a qualified healthcare professional.


Q: Can I take Levocetirizine if I have asthma?

A: Levocetirizine is an antihistamine used to relieve allergy symptoms and chronic hives. The official labeling does not list asthma as a contraindication, but it is not a primary treatment for asthma itself. The decision to use this medicine for individuals with asthma should be made in consultation with a healthcare professional.


Q: Does Levocetirizine have an effect on mucus production?

A: Levocetirizine is officially indicated for the relief of symptoms associated with allergic rhinitis, such as a runny nose (rhinorrhea) and sneezing. Its action on these symptoms is related to its ability to modulate inflammation and block histamine effects.


Q: Could taking Levocetirizine interfere with allergy skin tests?

A: Since this medicine works by blocking the H1 histamine receptor in the body, it is expected to interfere with the results of tests that measure histamine release, such as allergy skin-prick tests. The potential for interference should be reviewed with a healthcare professional before allergy testing is scheduled.


Q: Can Levocetirizine be crushed or split if it is a tablet?

A: The tablets should generally be swallowed whole with liquid. However, the standard 5 mg film-coated tablet is typically scored, which allows it to be broken in half to provide a lower dose if a lower dose is needed and has been directed.


Q: Why is Levocetirizine sometimes taken at night?

A: The single daily dose of this medicine is generally recommended for administration in the evening. This timing is likely due to the risk of the common side effect of drowsiness (somnolence), allowing any sedative effects to occur while sleeping.


Q: What is the potential for rebound symptoms after stopping Levocetirizine?

A: Official warnings note that there have been reports of severe itching (pruritus) occurring after the medicine is discontinued. This can happen within a few days, particularly if the medicine was used continuously for a long period.


Q: What is the typical duration of Levocetirizine treatment for chronic conditions?

A: Research indicates that the medicine is considered suitable for the long-term management of persistent allergic conditions. Clinical studies examining chronic hives (urticaria) have followed patients for medium-term periods of up to three to six months.


Q: What are the most common reasons doctors prescribe Levocetirizine?

A: The medicine is officially indicated for relieving symptoms associated with seasonal and perennial allergic rhinitis (hay fever). It is also used to treat the skin manifestations of chronic idiopathic urticaria (chronic hives).


Q: Does Levocetirizine cause weight gain?

A: Official post-marketing experience reports have listed weight increase as an adverse reaction that has been reported in patients using the drug.


Q: Is Levocetirizine safe for elderly people to use?

A: Official documents advise that caution is required when used in older adults. The clearance of the drug from the body is naturally lower in this population, which increases the overall systemic exposure and may lead to a higher risk of adverse reactions.


Q: What are some less common but possible side effects of Levocetirizine?

A: While drowsiness is common, other less common effects may include a lack of energy (asthenia), abdominal pain, or dizziness. Serious but rare reactions like convulsions and hepatitis have also been reported in official documents.


Q: Does Levocetirizine treat the root cause of allergies or just the symptoms?

A: Levocetirizine works by blocking the action of histamine, a natural substance released during an allergic reaction. Its official indication is for the relief of symptoms associated with allergic conditions, rather than curing the underlying allergy itself.


Q: What happens if I stop taking Levocetirizine suddenly?

A: Reports indicate that some patients, especially those who have used the medicine long-term, may experience severe itching (pruritus) when the treatment is abruptly stopped.


Q: Can people with kidney problems use Levocetirizine?

A: Use is contraindicated for patients with end-stage renal disease (very severe kidney impairment). For patients with mild to severe impairment, a reduced dosage and/or frequency is required because the drug is primarily eliminated by the kidneys.


Q: Are there any long-term side effects associated with continuous Levocetirizine use?

A: While the core research studies have focused on medium-term follow-up (up to three to six months), the long-term effects are not fully established. Post-marketing reports have included events like weight increase and new-onset itching upon discontinuation.


Q: Is Levocetirizine safe to use during pregnancy (general information)?

A: Official labeling indicates that use during pregnancy should be reviewed with a healthcare professional. While animal studies have not shown harm to the fetus, there are no adequate and well-controlled studies in pregnant women.


Q: Can Levocetirizine cause dizziness or lightheadedness?

A: Yes, dizziness has been reported as an adverse reaction in post-marketing experience with the drug.


Q: Does the effectiveness of Levocetirizine change with age?

A: Due to changes in the body's ability to clear the drug, the clearance of the medicine is approximately 33% lower in older adults. This alteration in clearance requires caution and may affect the drug's overall profile compared to younger adults.


Q: Are there any studies comparing Levocetirizine's effectiveness to placebos?

A: Yes, the effectiveness of the drug, particularly for conditions like chronic hives, has been evaluated in placebo-controlled Randomized Controlled Trials (RCTs).


Q: Is Levocetirizine used to prevent allergic reactions or just treat them?

A: Levocetirizine is officially indicated for the relief of symptoms associated with allergic conditions. It is used to treat the symptoms once they occur, not to prevent the underlying allergic reaction from happening.


Q: How does Levocetirizine affect the central nervous system?

A: The drug is efficiently transported out of the central nervous system (CNS), which generally results in a lower potential for CNS effects compared to older antihistamines. However, it can still cause side effects such as somnolence and is classified as a CNS depressant.

How should L-Sitrizin be stored and disposed of?

Storage and Disposal of Levocetirizine

Levocetirizine tablets and oral solution must be stored at controlled room temperature, specifically between 20 C and 25 C (68 F and 77 F). The official label permits temporary temperature excursions up to 30 C.

Storage Requirement Rule
Temperature Controlled Room Temperature: 20 C – 25 C
Container Store in the original container; oral solution bottle must be tightly closed
Protection Keep out of the sight and reach of children
Light Levocetirizine oral solution must be protected from light

Disposal of any unused or expired product must be carried out in accordance with local requirements. Unused medicine should generally not be disposed of via household refuse or wastewater.

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

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