Novocetrin

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Medically reviewed

Laura Arias

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 Novocetrin

Property Description
Active ingredient Levocetirizine (as the dihydrochloride salt)
Form Film-coated tablet, Oral solution
Pharmacological class Second-Generation Histamine H1-Receptor Antagonist
Common use Symptomatic relief of allergic rhinitis and urticaria
Origin Synthetic, active isomer

What Type of Medicine is Novocetrin?

Novocetrin is a pharmaceutical product containing the active substance Levocetirizine, and it is classified as a Second-Generation Histamine H1-Receptor Antagonist, placing it within the broader group of Antihistamines. This modern classification confirms its role as an effective antiallergic agent used for symptomatic relief. The compound is the pharmacologically active portion of its predecessor, cetirizine, and its selective profile is clinically recognized for providing relief while minimizing the central nervous system effects often associated with older agents. This feature is particularly relevant for individuals needing to maintain alertness throughout the day.

Composition and Form: What is Levocetirizine?

The active ingredient is Levocetirizine, specifically the R-enantiomer, or active isomer, of the racemic compound cetirizine. This structural specificity means that the drug utilizes only the most therapeutically effective molecular form, giving it a high affinity for the target receptor. Novocetrin is prepared as a single-ingredient product designed for oral administration, typically available as a film-coated tablet and an oral solution, offering flexibility for different patient groups. This formulation ensures the medication is accessible across various ages requiring anti-allergic support.

General Purpose and Mechanism Principle

The general purpose of Novocetrin is to mitigate the physical symptoms of allergic reactions through a targeted Histamine Blocking mechanism principle. The Levocetirizine selectively binds to and occupies the body’s Histamine H1 receptors, preventing the natural histamine released during an allergic event from initiating the subsequent cascade of allergic signs. By inhibiting this action, the medication serves to reduce the core inflammatory and symptomatic effects driven by histamine, such as itching, swelling, and increased vascular permeability, thereby providing effective management of the allergic process.

What side effects are possible with Novocetrin?

Possible Side Effects and Safety Information

Novocetrin, which contains Levocetirizine, has an official safety profile organized by regulatory bodies into frequency and System-Organ Classes (SOC) based on clinical trials and post-marketing reports.

Common adverse reactions (occurring in 1 out of 100 to 1 out of 10 patients) typically involve the central nervous system and general systemic conditions. These include Somnolence (drowsiness), Fatigue, Headache, Dry Mouth, and Nasopharyngitis.

Reactions categorized as Uncommon include Asthenia (lack of strength), Abdominal Pain, and Pruritus (itching). Other adverse reactions reported during post-marketing surveillance, for which frequency cannot be accurately estimated (Not Known), affect several systems. These include severe Hypersensitivity reactions (e.g., Anaphylaxis, Angioedema), Psychiatric Disorders (e.g., Aggression, Hallucination, Suicidal ideation), and Nervous System Disorders (e.g., Convulsion, Syncope, Tremor).


Safety Considerations and Constraints

Official labeling defines specific safety constraints and population-specific considerations. The medicine is contraindicated in individuals with a known hypersensitivity to levocetirizine, cetirizine, or hydroxyzine, as well as those with severe renal impairment (creatinine clearance less than 10 mL/min).

Caution is advised for older adults due to the greater likelihood of reduced kidney function. The use of Novocetrin with alcohol or other central nervous system (CNS) depressants may lead to a further reduction in alertness and impairment of CNS performance. Additionally, the label notes a post-marketing observation of severe Pruritus developing after the discontinuation of long-term daily use.

Overdose and Emergency Response

Novocetrin Overdose and When to Seek Help

Novocetrin (cetirizine) is generally safe when taken as directed. An overdose, which is typically defined as ingesting significantly more than the prescribed or recommended dose, can lead to adverse effects, although severe toxicity is uncommon, particularly with this second-generation antihistamine.

Common Signs of Overdose

Symptoms of a Novocetrin overdose can vary but often include central nervous system effects such as pronounced drowsiness, somnolence, and sedation. In children, paradoxical reactions like restlessness, agitation, or irritability may be observed. Other potential signs include a rapid heartbeat (tachycardia) and headache.

Symptom Type Common Examples
Central Nervous System Drowsiness, somnolence, restlessness (in children)
Cardiovascular Tachycardia (rapid heartbeat)

When to Seek Immediate Medical Help

If an overdose of Novocetrin is suspected, immediate professional medical evaluation is necessary, regardless of the severity of symptoms. You should contact emergency services immediately if the individual:

  • Experiences a seizure or loss of consciousness.
  • Has severe trouble breathing or collapses.
  • Exhibits a very fast or irregular heart rate.

Treatment for overdose is generally supportive and symptomatic, as there is no specific antidote. Always store this and all medications securely away from children to prevent accidental ingestion.

Therapeutic Uses of Novocetrin

What Novocetrin Treats: Main Uses and Benefits

Novocetrin is commonly used in situations involving certain distressing symptoms across two primary therapeutic domains associated with allergic responses, providing support that helps ease the overall symptom burden and manage specific allergic conditions.


Key Therapeutic Focus

The medication is used for managing the symptomatic relief of Seasonal Allergic Rhinitis, including hay fever and Perennial Allergic Rhinitis, and is commonly used across conditions presenting with chronic or persistent manifestations such as Chronic Urticaria (hives). It helps address symptom clusters that may become intense or disruptive, such as runny nose, frequent sneezing, nasal itching, watery eyes, and intense skin itching (pruritus) with wheals.

“It is commonly applied in scenarios where additional management of discomfort is required during phases when symptoms become more noticeable.”

Applicable in conditions characterized by episodic or fluctuating symptom patterns, Novocetrin may help patients cope more steadily with symptom fluctuations when symptoms interfere with daily functioning, and contributes to improved comfort during periods of heightened symptoms.


The medication is considered relevant for easing Pruritus (Intense Skin Itching), which is a hallmark symptom of chronic hives, supporting patients during episodes of heightened discomfort and providing supportive relief when symptoms interfere with routine activities.

Regulatory References

  1. LEVOCETIRIZINE DIHYDROCHLORIDE tablet - DailyMed - NIH

Eligibility and Restrictions for Use

Novocetrin eligibility is determined by strict criteria set forth in official government regulatory documents (e.g., FDA, EMA). These rules define both absolute prohibitions and populations requiring conditional use or restricted dosing.

Contraindications and Non-Eligibility

Novocetrin is contraindicated in patients with a known hypersensitivity to the active substance, its excipients, or related compounds (e.g., hydroxyzine). It is also absolutely prohibited for patients with severe renal impairment (typically defined as creatinine clearance less than 10 mL/min). Use in children under six years of age is generally not recommended due to lack of established safety and efficacy data.

Restricted and Conditional Use

Use is restricted for patients with moderate to severe renal impairment (CrCl ge 10 mL/min but le 50 mL/min), who must receive a mandatory dose reduction. Older adults are advised to use Novocetrin with caution, as dose adjustments may be necessary due to a higher likelihood of decreased kidney function. Pregnancy and lactation are also categorized as restricted use; the drug is not recommended for women who are breastfeeding and is only advised during pregnancy when clearly needed.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory information for Novocetrin (Levocetirizine) outlines specific pharmacodynamic and pharmacokinetic interaction patterns, strictly focusing on documented changes in alertness, CNS performance, and drug exposure.


Pharmacodynamic Avoidance Requirements

The co-administration of Novocetrin with substances that depress the Central Nervous System (CNS) must be avoided due to the documented potential for additive impairment of CNS performance and an additional reduction in alertness. This restriction applies specifically to:

  • Alcohol (Ethanol): Concurrent use should be avoided.
  • Other CNS Depressants: Includes sedatives, tranquilizers, and hypnotics, which should also be avoided due to the risk of pharmacodynamic reinforcement.

Pharmacokinetic and Absorption Changes

Official labeling addresses pharmacokinetic changes related to co-administered substances and food:

  • Ritonavir: Co-administration with the drug's predecessor, cetirizine, resulted in a significant increase in the active drug's exposure (AUC). This potential for increased exposure is relevant when levocetirizine is taken concurrently with Ritonavir.

  • Food: While food does not alter the overall extent of absorption (AUC), administration with a meal results in a delay in the time to reach peak concentration (Tmax) and a reduction in the peak concentration (Cmax) by approximately 36%.

  • Metabolic Interactions: In vitro data indicate that levocetirizine is unlikely to be involved in metabolic interactions through major cytochrome P450 (CYP) isoenzymes (including 1A2, 2C9, 2C19, 2D6, and 3A4).

Mechanism of Action

️ How Novocetrin Works: Mechanism of Action

Novocetrin operates through a multimodal mechanism that targets key regulatory points within the central nervous system, primarily the spinal cord, to influence nociceptive signal propagation.


️ Presynaptic Inhibition of Calcium Channels

Novocetrin acts as a selective inhibitor of presynaptic voltage-gated N-type calcium channels (Cav2.2). By restricting the critical influx of calcium ions, the drug reduces the release of excitatory neurotransmitters (like glutamate) from the afferent neurons. This initial step modifies the early molecular signaling, influencing the systemic physiological process of nociceptive signal propagation.


Postsynaptic Receptor Modulation

This secondary mechanism involves Novocetrin acting as a partial agonist at mu-opioid receptors and an agonist at alpha2-adrenergic receptors. These interactions engage distinct inhibitory G-protein coupled cascades to hyperpolarize the receiving neuron and enhance the activity of descending inhibitory pathways. This contributes to a dampened state within the targeted spinal circuits, leading to a reduction in neuronal excitability.

Dosage and Administration Information

How to Use Novocetrin

Novocetrin, containing Levocetirizine, is an anti-allergic medication used according to specific administration rules. The medication is provided for oral use in the form of a 5 mg film-coated tablet and a 0.5 mg/mL oral solution.


Standard Dosing and Frequency

The standard regimen for adults and adolescents (12 years and older) is 5 mg taken once daily. This 5 mg dose is generally considered the maximum recommended daily intake. To align with the drug's 24-hour action profile, the dose is recommended to be taken in the evening.

Age Group Standard Daily Dose Dosing Form
Adults and Adolescents (12 yrs and older) 5 mg once daily Tablet or Solution
Children (6 to 11 yrs) 2.5 mg once daily Tablet (halved) or Solution
Infants and Children (6 mos to 5 yrs) 1.25 mg once daily Oral Solution

Administration Conditions

Novocetrin can be taken with or without food, offering flexibility in timing. Tablets should be swallowed whole with liquid. For conditions like Chronic Urticaria, usage may extend to long-term therapy, lasting up to one year.

Special Population Rules

Dosage adjustments are a mandatory procedural step for patients 12 years and older with renal impairment. The dose and dosing frequency must be reduced systematically based on the patient's creatinine clearance to prevent drug accumulation. Conversely, no dose adjustment is typically necessary for isolated hepatic (liver) impairment. If a dose is missed, patients should take the next dose at the scheduled time, without doubling up to compensate.

Recent Clinical Evidence

The evidence for Novocetrin (Levocetirizine) is derived from clinical research, primarily involving studies that evaluate symptom patterns in people with specific allergic conditions. This research framework helps to contextualize the available data regarding its use.

Evidence Studies for Allergic Rhinitis (SAR/PAR)

This section summarizes studies that examined outcomes in both seasonal allergic rhinitis (SAR) and perennial allergic rhinitis (PAR).

Research explored outcomes in conditions characterized by fluctuating or episodic manifestations, such as hay fever and year-round nasal allergies. These studies primarily utilized controlled trial designs, including those comparing the compound to a placebo or to other agents. Outcomes measured focused on patient-reported outcomes describing perceived discomfort, such as the Total Nasal Symptom Score (TNSS). Research also examined outcomes reflecting daily functioning or activity level and specific quality of life assessments.

Research highlights measured differences in patient-reported outcomes in the active treatment groups compared to placebo groups. The research provides context for understanding symptom patterns in patients with both acute seasonal episodes and chronic perennial symptoms.

The evidence level for this indication is classified as High, reflecting the weight of Randomized Controlled Trial (RCT) data. Data for extended periods, such as continuous use beyond six months, appears to be limited.

Evidence Studies for Chronic Urticaria (Hives)

This segment reviews the research foundation, primarily through placebo-controlled trials, which were designed to evaluate outcomes related to physical discomfort, specifically the severity of pruritus (itching) and the presence of wheals in patients with chronic hives.

Novocetrin was evaluated in research contexts involving fluctuating or unstable skin symptoms, such as Chronic Idiopathic Urticaria (CIU). Studies monitored outcomes related to physical discomfort, specifically using scales to measure the intensity of pruritus (intense skin itching) and the number and size of wheals (hives). These controlled trials typically examined temporary physiological imbalance during episodes where symptoms become more noticeable.

The studies describe symptom patterns observed in the populations over defined time intervals. Research describes the short-term symptom changes measured by skin discomfort scores. Findings describe group patterns for outcomes related to inflammatory or irritative states.

Frequently Asked Questions (FAQ)

Common questions about Novocetrin (FAQ)


Q: What is the main difference between Novocetrin and other similar medicines?

A: The medicine is classified as a second-generation H1-receptor antagonist. Official regulatory documents describe its selective profile, which works to minimize the central nervous system effects that are often associated with older agents in the same class.


Q: Do you take Novocetrin for pain or just for inflammation?

A: According to official product information, the medicine is officially indicated for the symptomatic treatment of allergic rhinitis (such as hay fever) and chronic urticaria (hives). Its use is defined by regulatory bodies for these specific allergic and dermatologic conditions.


Q: How quickly can a person expect Novocetrin to start working?

A: Studies show that the maximum concentration of the active ingredient in the bloodstream (peak plasma concentration) is generally reached within about one hour after the medicine is taken orally by healthy adults.


Q: Are there common foods or drinks that should be avoided when taking Novocetrin?

A: Concurrent use with alcohol and other Central Nervous System (CNS) depressants is stated in official documents to be avoided. Regulatory documents note this is due to the potential for an additive reduction in alertness and impairment of CNS performance.


Q: What is the list of conditions that Novocetrin is officially approved to treat?

A: The medicine is officially indicated for the symptomatic treatment of allergic rhinitis, which includes both seasonal and persistent types. It is also approved for the treatment of chronic urticaria (hives).


Q: What research is available about the long-term effects of Novocetrin?

A: Clinical experience is available for continuous use for up to one year, particularly for chronic urticaria. Official warnings note that severe itching (pruritus) has been reported in post-marketing surveillance after discontinuing the medicine following long-term daily use.


Q: Does Novocetrin have an effect on sleep patterns?

A: Official labeling lists both drowsiness (somnolence) and fatigue as common adverse reactions that can occur. Furthermore, post-marketing reports include less frequent observations of insomnia among the psychiatric disorders listed.


Q: Is Novocetrin classified as a controlled substance?

A: No. Official regulatory databases indicate the active ingredient in Novocetrin is not classified as a controlled substance under the US Controlled Substances Act (CSA).


Q: What is the patient experience generally like when starting Novocetrin?

A: The most common adverse reactions reported in clinical trials include drowsiness (somnolence), fatigue, headache, dry mouth, and inflammation of the nasopharynx. These are the physical effects most frequently noted by patients when starting treatment.


Q: What kind of tests or monitoring might be required while taking Novocetrin?

A: For patients with known or suspected renal (kidney) impairment, official labeling indicates that dosage adjustments are required. These adjustments are typically based on an estimate of the patient's creatinine clearance, which measures kidney function.


Q: What is the expected duration of treatment with Novocetrin for common conditions?

A: The duration of treatment is guided by the type of condition. The duration model for intermittent allergic rhinitis suggests use can align with the presence and reappearance of symptoms. For chronic conditions like urticaria, official clinical experience supports continuous use extending up to one year.


Q: Is Novocetrin known to interfere with driving or operating machinery?

A: The medicine may cause drowsiness (somnolence), fatigue, or other CNS depression, which can impair mental alertness. Official labeling describes the potential for reduced alertness, noting this is relevant for activities such as driving or operating machinery.


Q: Is Novocetrin known to cause changes in appetite or weight?

A: Post-marketing surveillance reports have included observations of increased appetite and increased weight. Regulatory documents categorize these as adverse reactions of 'Not Known' frequency.


Q: Is there a generic version of Novocetrin available?

A: Yes. Regulatory documents list the active ingredient, levocetirizine dihydrochloride, as the generic name associated with the product.


Q: How long does Novocetrin stay in the system after the last dose?

A: The elimination half-life in adults is approximately eight to nine hours. This is the time it takes for half of the drug to be eliminated from the body.


Q: Does Novocetrin contain lactose or gluten?

A: The film-coated tablet formulation contains the excipient lactose monohydrate. Regulatory information notes that the medicine is not recommended for patients with rare hereditary problems of galactose intolerance. Information regarding gluten content is not explicitly addressed in the core regulatory documents.


Q: What is the purpose of the black box warning on Novocetrin, if it has one?

A: Official labeling does not contain a Black Box Warning (BBW). However, the FDA has provided a safety communication regarding the risk of severe itching (pruritus) upon discontinuation following long-term use.


Q: What is the information available about Novocetrin's use in patients with heart conditions?

A: Post-marketing surveillance reports list adverse reactions in the cardiac disorders class, including palpitations and tachycardia. These reports are categorized by regulatory documents with a reported frequency of 'Not Known.'


Q: Can Novocetrin cause problems with fertility?

A: Official regulatory documents state that no clinical data are available regarding the effect of the medicine on human fertility.


Q: Is Novocetrin a newly approved drug or has it been available for a while?

A: The prescription form of the medicine (Levocetirizine dihydrochloride) was first approved by the US FDA in May 2007.

How should Novocetrin be stored and disposed of?

How to Store and Dispose of Novocetrin?

The official storage and disposal guidelines for Novocetrin are defined to maintain product stability and safety, based strictly on regulatory documentation.

Official Storage Requirements

Novocetrin must be stored at controlled room temperature, specifically between 20° and 25°C (68° and 77°F), with a regulatory limit stating storage must be below 30°C. It is mandatory to store the medication in a dry place and protect it from light. The container's safety seal must be intact upon use.

Handling and Safety

Consistent with official labeling, the product must be kept out of the sight and reach of children. The stated shelf-life is 24 months when stored under these specified conditions.

Disposal Instructions

Regulatory documents state that there are no special requirements for the disposal of unused or expired Novocetrin, meaning it is not classified as a hazardous pharmaceutical waste.

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

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