Lizine

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Lizine

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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 Lizine

Lizine: Identity and Pharmacological Classification

Property Description
Active ingredient Levocetirizine Dihydrochloride
Form Film-coated tablet, Oral solution
Pharmacological class Second-generation Antihistamine
Common purpose Symptomatic relief of allergic reactions
Origin Synthetic drug (R-enantiomer)

Lizine is a synthetic medicinal product containing the active ingredient Levocetirizine Dihydrochloride, classified as a second-generation antihistamine used for systemic relief of allergic responses. It functions to manage the core symptoms associated with histamine release. This medication is designed to counteract the effects of histamine throughout the body, providing a targeted approach to managing allergy symptoms, such as those experienced during a typical seasonal allergy flare-up. As the chemically pure active R-enantiomer of the related compound Cetirizine, Levocetirizine possesses a highly focused activity profile.


Composition, Form, and General Purpose

The medication is a single-ingredient product formulated for oral administration, typically available as a film-coated tablet and an oral solution. Lizine is distinguished by its availability in multiple forms, offering flexibility for both adult and pediatric patients who may require a liquid preparation. The active compound, Levocetirizine Dihydrochloride, is combined with inert excipients or an aqueous base to create these stable pharmaceutical preparations. The general therapeutic purpose of Lizine is to provide symptomatic relief by inhibiting the action of histamine, a key substance released during allergic reactions. The medicine is intended to ease discomfort by reducing the core inflammatory response.


Structure: Why is Levocetirizine Considered "Second-Generation" Nervously?

Levocetirizine is considered a second-generation agent because its chemical structure makes it a highly selective peripheral H1-receptor antagonist. This structural design allows the molecule to primarily target the H1-receptors located outside the central nervous system. This selectivity is a key differentiator in its classification as a non-sedating antihistamine. The focused action contributes to effective anti-allergic activity while reducing the potential for central nervous system effects often associated with older antihistamine compounds, a property recognized for improving patient tolerability.

Regulatory References

  1. NIH/MedlinePlus: Levocetirizine

What side effects are possible with Lizine?

Possible Side Effects and Safety Information

The safety profile of Lizine (Levocetirizine Dihydrochloride) is established through clinical trials and post-marketing surveillance, defining adverse reactions by frequency and physiological system involvement, as classified by government regulatory authorities.

Documented Frequencies of Adverse Reactions

Adverse reactions are formally categorized based on their rate of occurrence:

  • Common (occurring in 1% to 10% of patients): Effects primarily include Nervous System Disorders such as somnolence (drowsiness), fatigue, headache, and dizziness. Gastrointestinal effects like dry mouth are also commonly reported.
  • Uncommon (occurring in 0.1% to 1% of patients): These reactions include paresthesia (tingling sensation), agitation, and weight increase.
  • Rare and Very Rare: Less frequent but clinically significant adverse reactions include Serious Adverse Reactions such as hypersensitivity reactions (including anaphylaxis and angioedema), convulsions, aggression, depression, and tachycardia (rapid heart rate).

Key Safety Considerations

The medicine is subject to specific safety limitations defined in regulatory labeling. Use is Contraindicated in individuals with End-Stage Renal Disease (creatinine clearance less than 10 mL/min) and those on hemodialysis. This contraindication also applies to pediatric patients aged 6 months to 11 years with any degree of renal impairment.

A specific exposure-related pattern noted after long-term daily use is the documentation of severe pruritus (intense itching) upon discontinuation of the medicine. Caution is also advised regarding use with alcohol or other Central Nervous System (CNS) depressants due to the potential for enhanced drowsiness.

Overdose and Emergency Response

The official overdose profile for Lizine (Levocetirizine Dihydrochloride) is primarily defined by the risk of Central Nervous System (CNS) effects and regulator-mandated emergency actions.

In adults, the most common documented sign of overdose is somnolence (drowsiness). A distinct pattern is noted for the pediatric population, where overdose may initially manifest as agitation and restlessness, followed by the onset of drowsiness.

Immediate emergency medical attention is required if any symptoms of severe impairment are observed. Regulator guidance states that individuals must immediately call emergency services if the person has collapsed, had a seizure, has trouble breathing, or can't be awakened. It is also advised to call a Poison Control Center for guidance.

For clinical management, symptomatic and supportive treatment is the recommended intervention, as regulatory documents explicitly state that no specific antidote is known for Levocetirizine. Treatment may include considering gastric lavage shortly after ingestion, and continuous clinical observation is required due to the potential for CNS depression. Furthermore, the drug is not effectively removed by dialysis. Concurrent use of Lizine with alcohol or other CNS depressants is noted as a factor that may heighten the risk of reduced alertness.

Therapeutic Uses of Lizine

L-Lysine, often referred to commercially as Lizine, is an essential amino acid. It is applied across domains where additional symptomatic support is needed because it plays a role in managing the fundamental building blocks of protein within the body, making it relevant in contexts involving heightened systemic burden.

This nutritional supplement may promote healthy tissue function, growth, and healing. It is commonly used across conditions presenting with acute episodes and is relevant for easing symptoms related to physical discomfort, symptoms that create noticeable physiological strain, and symptoms of increased neurological or muscular activity. The support helps patients cope more steadily with symptom fluctuations and supports general well-being during symptomatic phases.

This contributes to easing the overall symptom load and may assist with maintaining functional stability in situations where patients experience temporary physiological imbalance.

Quick Fact: Relief for Symptoms that become more disruptive during flare-ups

Regulatory References

  1. National Cancer Institute (NCI) Drug Dictionary entry for L-lysine

Eligibility and Restrictions for Use

Eligibility: Who can and cannot use Lizine?

Regulatory documentation defines strict population eligibility criteria for Lizine (Levocetirizine Dihydrochloride).

Classification Population Group or Condition
ABSOLUTELY CONTRAINDICATED Patients with known hypersensitivity to levocetirizine, cetirizine, hydroxyzine, or other piperazine derivatives.
Patients with End-Stage Renal Disease (creatinine clearance less than 10 mL/min).
Children younger than 6 months of age.
RESTRICTED / CONDITIONAL USE Patients 12 years of age and older with mild to severe renal impairment (requires dose adjustment).
Patients with predisposing factors for urinary retention (e.g., prostatic hyperplasia) or epilepsy (use with caution).
AGE ELIGIBILITY Approved for adults and adolescents 12 years of age and older.
Approved for children 6 months (oral solution) or 6 years (tablet).
PREGNANCY / LACTATION Use in pregnancy is generally authorized only if clearly needed (Pregnancy Category B). Use during lactation is not recommended by US regulators.

Lizine is contraindicated in children 6 months to 11 years of age with impaired kidney function. Patients with isolated hepatic impairment are eligible for standard use, as dose adjustments are not typically required.

What should I know about interactions with other medicines?

Interactions with other medicines and products — official regulatory information for Levocetirizine Dihydrochloride

Category Official Regulatory Documentation Statement
Medicinal product categories with documented interactions Central Nervous System (CNS) depressants.
Specific interacting medicines Alcohol (Ethanol), Ritonavir, Theophylline.
Mechanistic basis of interactions Pharmacodynamic: Additive impairment of CNS performance. Pharmacokinetic: Altered drug clearance and increased exposure.
Timing-based interaction rules No mandatory timing separation is required for food.
Population-specific interaction notes Contraindicated in End-Stage Renal Disease or severe renal impairment.
Interaction-related restrictions Avoid co-administration with alcohol and other CNS depressants.

Interaction Classifications (High-Level)

Category Official Regulatory Documentation Statement
Interaction severity classification Avoid co-administration (pharmacodynamic); Contraindicated (renal clearance restriction).
Regulatory basis FDA and EMA Prescribing Information.
Interaction-context constraints Contraindication relates directly to the drug's primary renal excretion.

Resulting Interaction Structure

Official interaction statements:

  • Co-administration with alcohol and other CNS depressants should be avoided due to the documented pharmacodynamic interaction causing additive impairment of alertness and CNS function.
  • The medicine is contraindicated for patients with End-Stage Renal Disease or severe renal impairment, as the drug is predominantly eliminated via the kidneys.
  • A pharmacokinetic interaction is documented with Ritonavir, which may lead to an increase in Levocetirizine plasma levels.
  • Co-administration with Theophylline (400 mg once daily) resulted in a minor, documented reduction in levocetirizine clearance.
  • Taking the medicine with food is noted as having a pharmacokinetic effect of delaying the rate of absorption but does not change the overall amount of drug absorbed.

Connection to the overall interaction profile (2–4 sentences): The regulatory interaction profile is defined by a central pharmacodynamic restriction requiring avoidance of co-use with substances that depress the CNS, such as alcohol. Pharmacokinetically, the structure notes specific clearance effects with agents like Ritonavir and Theophylline. Furthermore, the profile includes a stringent population-based contraindication directly tied to the drug’s substantial dependence on kidney function for elimination.

Mechanism of Action

Lizine (L-lysine) is an essential alpha-amino acid that primarily acts as a substrate for protein biosynthesis and subsequent post-translational modification pathways throughout the body. Following absorption from the small intestine via cationic amino acid transporters (e.g., CAT-1, CAT-2), Lizine is distributed systemically. Intracellularly, it serves as a necessary component for the synthesis of structural proteins, including collagen, where it is hydroxylated by lysyl hydroxylase to form hydroxylysine residues.

Beyond protein synthesis, Lizine is a precursor in the synthesis of carnitine, a molecule required for the transport of long-chain fatty acids across the inner mitochondrial membrane for beta-oxidation. Lizine can also modulate the activity of the herpes simplex virus (HSV) by acting as an antagonist to the amino acid L-arginine, which is necessary for viral protein synthesis and replication. A resulting shift in the intracellular lysine:arginine ratio inhibits the assembly of viral structural proteins, thereby modulating the infectious cycle.

Dosage and Administration Information

How to Use Lizine: Administration Guidelines

Lizine (Levocetirizine Dihydrochloride) is an oral medication with specific use instructions to ensure consistent administration. The medicine is available as a film-coated tablet and an oral solution.


Standard Dosing and Schedule

Lizine is administered once daily (qDay). The dose is typically taken in the evening.

Population Standard Dosing Regimen Maximum Daily Dose
Adults & Adolescents (ge 12 yrs) 5 mg once daily 5 mg/24 hours
Children (6 to 11 yrs) 2.5 mg once daily 2.5 mg/24 hours
Children (6 months to 5 yrs) 1.25 mg (via oral solution) once daily 1.25 mg/24 hours

Administration Context and Duration

Lizine can be taken without regard to food, meaning intake is permissible either with or without a meal. For patients using the tablet form, it must be swallowed whole with liquid; the scored tablet allows for accurate administration of the 2.5 mg dose.

For chronic conditions, continuous therapy may be used, with clinical experience supporting administration for periods of at least six months. Conversely, for temporary issues like seasonal symptoms, treatment can be stopped when symptoms subside and restarted if they return.

Population-Specific Adjustments

The dosing interval or dose amount is adjusted for patients with impaired kidney function based on their level of creatinine clearance. Conversely, no dose adjustment is required solely for patients with hepatic impairment.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Lizine

Evidence for Use in Seasonal and Perennial Allergies (Rhinitis)

Lizine (Levocetirizine Dihydrochloride) was studied for use in conditions characterized by fluctuating or episodic manifestations, such as seasonal allergic rhinitis (SAR) and perennial allergic rhinitis (PAR). Research for these conditions relies heavily on Randomized Controlled Trials (RCTs). These short-term RCTs, often double-blind and placebo-controlled, were the main research applied in studies examining patient-reported experiences. Research measured changes in scores related to physical discomfort, such as sneezing, nasal discharge, itching, and congestion, measured using formal tools like the Total Nasal Symptom Scores (TNSS).

Trial reports compared the measurements captured during the study period to those captured for patients receiving an inactive placebo. The evidence contributes to understanding symptom patterns, particularly focusing on episodes where symptoms become more noticeable. While trials up to six months exist, the majority of the research is restricted to short-term observation periods (2–4 weeks), and long-term data for use beyond six months remain limited.


Evidence for Use in Chronic Hives (Idiopathic Urticaria)

For conditions involving periods of heightened symptoms, such as chronic idiopathic urticaria (CIU), Lizine was also studied using controlled clinical trials. The research primarily monitored outcomes related to the physical manifestation of hives (wheals) and the perceived level of itching (pruritus) by monitoring scores like the Urticaria Activity Score (UAS) over short- to intermediate-duration intervals. The findings describe patterns observed in the studies, where measured outcomes for patients receiving Lizine varied compared to those receiving placebo. Studies monitored markers of allergic reactions in the skin during the study period. Data for certain groups, such as patients with CIU that is refractory (non-responsive) to standard doses, remain insufficient.


Evidence in Pediatric and Other Specific Populations

Specific trials were conducted in children aged 6 years and older. A distinct line of research was also conducted on the oral solution formulation for a very young pediatric population (infants and young children, 1 to 2 years old). This research examined temporary physiological imbalance related to recurrent cough associated with allergic symptoms. However, the available evidence is limited, and certainty remains low regarding outcomes in the youngest children compared to the volume of evidence available for adults and older children. Comparative evidence is lacking against other agents in the same therapeutic area.

Key Studies & References

  1. Efficacy of levocetirizine in infants and young children with recurrent cough associated with allergic symptoms
  2. Consensus on the clinical use of levocetirizine in pediatric allergic diseases

Frequently Asked Questions (FAQ)

Common questions about Lizine (FAQ)


Q: What is Lizine and what is it used for?

Lizine is a medicine approved for the treatment of acute herpes labialis (cold sores). According to the official product information, it is designed to manage and reduce the severity of these oral herpes flare-ups.


Q: Does Lizine work for other types of herpes or infections?

Regulatory documents state that Lizine is specifically indicated only for the treatment of acute herpes labialis (cold sores). Its use for other types of herpes infections or other conditions is not covered by the official approved indications.


Q: Can Lizine be used by children?

Official product information indicates that Lizine is not recommended for use in children and adolescents under 12 years of age. Use in patients younger than 12 has not been established in clinical studies. Questions regarding use in a child should be discussed with a healthcare professional.


Q: Is Lizine safe for pregnant women or those who are breastfeeding?

According to the official product information, use during pregnancy and lactation is not recommended. This is a standard precautionary measure. The decision to use this medicine during pregnancy or breastfeeding should be made in consultation with a healthcare professional.


Q: What should I do if I forget to use a dose of Lizine?

The official instructions indicate that if a dose is missed, it should be applied when remembered, and then treatment should continue as scheduled. Product labeling also states that a double application should not be used to compensate for a missed dose. Detailed instructions are provided in the 'How to use Lizine' section.


Q: How soon after applying Lizine should I expect to see improvement?

Studies and official information indicate that Lizine is intended to reduce the healing time of the cold sore. While individual results vary, the medicine works to interfere with the virus's replication. Clinical studies suggest that adhering to the prescribed regimen is necessary to achieve the treatment's intended benefits.

How should Lizine be stored and disposed of?

How to Store and Dispose of Lizine

Official labeling requires Lizine (Levocetirizine Dihydrochloride) to be stored at Controlled Room Temperature, which is defined as 20 C to 25 C (68 F to 77 F), with permitted short excursions up to 30 C.


Storage Requirements

The medication must remain safety sealed in its original carton or container, and should not be used if the protective seal is missing or torn. It is a mandatory requirement that Lizine be kept out of reach of children.

Disposal

Disposal of any unused or expired product must be carried out in accordance with local regulations for pharmaceutical waste, which often involves community take-back programs.

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

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