Degraler

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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 Degraler

Property Description
Active Ingredient Levocetirizine dihydrochloride
Pharmacological Class Selective Histamine H1-Receptor Antagonist
Origin Synthetic (R-enantiomer of Cetirizine)
Primary Forms Film-coated tablets, Oral solution
General Purpose Alleviates symptoms of allergic conditions

What Type of Medicine is Degraler and What Does It Contain?

Degraler is a pharmaceutical product containing the active ingredient Levocetirizine dihydrochloride, which is clinically classified as a second-generation antihistamine. It is a single-ingredient product belonging to the pharmacological class of selective histamine H1-receptor antagonists. This second-generation compound is recognized for its high specificity and low tendency to cause sedation compared to older antihistamines.

This medicine is a synthetic compound derived specifically as the R-enantiomer (or eutomer) of the older antihistamine, Cetirizine. Levocetirizine exhibits rapid action and high bioavailability, which relates to its absorption and utility for patients requiring prompt relief.

Understanding Levocetirizine's Origin and Available Forms

Levocetirizine's status as a purified R-enantiomer is the result of a pharmaceutical refinement known as a chiral switch, enhancing its targeted action compared to the original compound. This compound is formulated for oral administration and is available in standard ready-to-use oral dosage forms, including film-coated tablets and an oral solution.

The dual formulation ensures flexible administration, including for children (a specific target patient group for the oral solution). It is a potent H1 antagonist with clinically minimal impact on the central nervous system, meaning it primarily works on allergy symptoms outside of the brain.

What Is the Primary Therapeutic Purpose of This Antihistamine?

The primary purpose of Degraler is the comprehensive alleviation of uncomfortable allergic symptoms. By acting as a selective inhibitor, the drug interferes with the signaling pathway of histamine, the natural compound responsible for triggering immediate allergic responses. This targeted effect prevents histamine from binding to H1-receptors. This action provides relief by diminishing the intensity of manifestations such as sneezing, itching, runny nose, and swelling associated with conditions like allergic rhinitis or skin irritations related to chronic idiopathic urticaria.

What side effects are possible with Degraler?

Possible Side Effects and Safety Information

The official safety profile for escitalopram, the active ingredient in Degraler, organizes potential effects by how often they may occur and which body systems are involved, as defined by government regulatory standards.

Frequency-Classified Adverse Reactions

The most frequently documented adverse reactions include nausea and headache, which are classified as Very Common (ge1/10). Common (ge1/100 to <1/10) effects involve several organ systems, including nervous system disorders (e.g., dizziness, somnolence, insomnia) and gastrointestinal disorders (e.g., diarrhea, constipation, dry mouth). Other Common reactions include increased sweating, fatigue, and sexual dysfunction.

Serious Safety Concerns and Constraints

Regulatory documents identify certain adverse reactions as clinically significant, even if rare. These Serious Adverse Reactions include the risk of Serotonin Syndrome, hyponatremia (low sodium levels), and potentially serious changes in heart rhythm such as QT interval prolongation.

Specific safety constraints are outlined in the labeling. The medication is formally contraindicated for use concurrently with Monoamine Oxidase Inhibitors (MAOIs) due to the risk of a serious reaction. The label also documents an association with an increased risk of bleeding events.

Population and Exposure Considerations

Safety statements exist for particular groups. For children and adolescents (under 18), regulatory documents note an increased risk of suicidal thoughts and behavior when treatment is initiated or doses are changed. Older adults may be at a higher risk for hyponatremia and should be managed with caution. Furthermore, the risk of serious adverse reactions, including suicidality, is stated to be highest early during treatment or following dose changes.

Overdose and Emergency Response

When an overdose of Degraler (Escitalopram) is suspected, immediate medical attention is required, and individuals must contact emergency services or a Poison Control Centre. This mandatory action is necessary due to the potential for severe and life-threatening systemic outcomes documented in official regulatory labeling.

Official documents state that overdose manifestations may involve significant clinical changes across several physiological systems. Documented central nervous system (CNS) effects include dizziness, somnolence, confusion, agitation, and may escalate to convulsions or coma. Cardiovascular signs such as tachycardia or bradycardia are also reported.

The profile highlights the risk of Serotonin Syndrome, a potentially life-threatening condition, and serious cardiac electrical changes, including QTc interval prolongation and ventricular arrhythmia. Because no specific antidote is known for escitalopram, management is strictly symptomatic and supportive. Regulatory guidance mandates that patients receive ECG and vital sign monitoring. Furthermore, the possibility of multiple drug involvement must be considered by medical staff, and specific observation for up to 12 hours is recommended for certain at-risk populations.

Therapeutic Uses of Degraler

What Degraler Treats: Main Uses and Benefits

Degraler, which contains the active ingredient escitalopram, is a medication used to manage symptoms associated with specific mental health conditions. As a treatment for depressive and anxiety disorders, it may assist in the management of mood-related symptoms and feelings of worry.

The medication is used to help manage symptoms associated with Major Depressive Disorder (MDD) and Generalized Anxiety Disorder (GAD). It is therefore used as a treatment for these two main conditions. The use of this medication aims to support patients in managing their conditions, potentially leading to improved overall daily functioning.

Quick Fact: Targets Excessive Worry

As a therapeutic option, escitalopram may assist in alleviating key symptoms, such as persistently depressed mood, loss of interest in activities, and excessive, persistent worry and tension. “Escitalopram is a widely utilized therapeutic option for the management of these conditions.”

Eligibility and Restrictions for Use

Official Eligibility Rules for Degraler (Levocetirizine Dihydrochloride)

Official regulatory documents define strict criteria for who is eligible to use Degraler, focusing primarily on patient demographics and pre-existing medical conditions.

Contraindications (Must Not Use)

Classification Population/Condition
Absolute Known hypersensitivity to levocetirizine, cetirizine, or any piperazine derivatives.
Absolute End-stage renal disease ( CrCL < 10 mL/min), including patients undergoing hemodialysis.
Conditional Pediatric patients 6 months to 11 years with any degree of impaired renal function.

Age-Related Eligibility

  • Adults and Adolescents (12 years of age and older) are the standard eligible population.
  • Children 6 months to 11 years may use the oral solution formulation, but the tablet formulation is contraindicated for children under 6 years of age.
  • Use is generally not established for infants younger than 6 months.

Special Population Restrictions

  • Renal Impairment: Use in adults and adolescents with mild, moderate, or severe renal impairment requires restricted use.
  • Urinary Retention: Caution is required for patients with conditions that predispose to urinary retention, such as prostatic hyperplasia.
  • Pregnancy and Lactation: Use during pregnancy should be exercised with caution. The drug is not recommended for use while breastfeeding due to its excretion into human milk.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The interaction profile for Degraler (levocetirizine dihydrochloride) is structured by documented risks for pharmacodynamic reinforcement and specific pharmacokinetic changes.

Pharmacodynamic Interactions

Co-administration with alcohol or other Central Nervous System (CNS) depressants is officially documented to carry a risk for additive impairment of central nervous system performance and additional reductions in alertness. Therefore, concurrent use must be avoided, as stated in regulatory prescribing information.

Pharmacokinetic Interactions and Restrictions

Levocetirizine is substantially excreted by the kidneys, establishing constraints related to its clearance. Use is formally contraindicated in patients with End-Stage Renal Disease (Creatinine Clearance < 10 mL/min) and those undergoing hemodialysis.

Studies involving the parent compound, cetirizine, indicate that co-administration with Ritonavir increases the plasma Area Under the Curve (AUC) and decreases clearance. Similarly, the 400 mg dose of Theophylline caused a small reduction in the clearance of cetirizine. Levocetirizine is officially documented not to be a clinically relevant inhibitor or inducer of major CYP450 enzymes.

Administration Timing

Administration with a high-fat meal is documented to reduce the peak plasma concentration ( Cmax) by approximately 36% and delay the time to reach Cmax, though the overall extent of absorption ( AUC) remains unchanged.

Mechanism of Action

How Degraler Works: Mechanism of Action

Degraler is a Proteolysis Targeting Chimera (PROTAC) molecule that functions as a degrader, not an inhibitor, targeting the enzyme Glycogen Synthase Kinase 3 (GSK3). The drug is designed to be brain-penetrant and acts within the Central Nervous System (CNS).

Its action is initiated by forming a temporary ternary complex between GSK3, an E3 ubiquitin ligase, and the Degraler molecule. This recruits the cell's own quality control system, the Ubiquitin-Proteasome System (UPS), to tag GSK3 for destruction. This results in the robust and durable depletion of the GSK3 protein from the neuron.

Physiologically, the removal of GSK3 removes its negative regulatory control, leading to the stabilization of beta-catenin and the modulation of the Wnt signaling pathway. This shift in intracellular signaling alters the phosphorylation state of specific substrate proteins and contributes to the modulation of neuronal regulatory processes.

Dosage and Administration Information

How to Use Degraler

Degraler (Levocetirizine dihydrochloride) is used according to specific administration protocols. The medicine is exclusively for oral administration and is available as film-coated tablets (typically 5 mg) and an oral solution.


Official Dosing and Frequency

Administration Scope General Guidelines
Standard Adult Dose 5 mg taken once daily (q.d.). A 2.5 mg dose may also be effective for some adults.
Pediatric Dosing Children 6 to 11 years receive 2.5 mg once daily; children 6 months to 5 years receive 1.25 mg (2.5 mL oral solution) once daily.
Timing and Food The medicine is generally recommended to be taken in the evening and can be administered with or without food.

Administration Requirements and Adjustments

Proper use of Degraler involves adherence to specific conditions, particularly for certain populations. For patients with renal impairment (impaired kidney function), the dose is typically adjusted, with the frequency determined based on the patient's measured creatinine clearance. No adjustment is typically required for isolated hepatic (liver) impairment. The oral solution should be measured using an appropriate device to ensure the correct dose, especially in pediatric patients.

Handling of Missed Doses

If a dose of Degraler is missed, it should be omitted, and the next scheduled dose should be taken at the usual time. The daily dose should not be doubled to compensate for a forgotten dose.

Recent Clinical Evidence

Overview of Studies for Degraler

Evidence for Use in Allergic Rhinitis

The research on Degraler (Levocetirizine) for allergic rhinitis, including both seasonal and perennial forms, is built upon numerous Randomized Controlled Trials (RCTs). These are the study designs where groups of participants were randomly assigned to receive either the active compound or an inactive treatment (placebo) or another active drug.

Studies focused on outcomes related to physical discomfort in conditions characterized by fluctuating or episodic manifestations. Researchers tracked changes in standardized measurements like the Total Nasal Symptom Score (TNSS), which is used in research exploring how symptoms change over time. Studies also examined patient-reported outcomes describing perceived discomfort, such as how the condition affected daily functioning or activity level (Quality of Life metrics).

Findings describe patterns observed in these studies where measurements of total symptom scores in participants receiving the active compound were observed to differ from the scores observed in the placebo groups. However, research findings were mixed in one specific regulatory-reviewed trial, which reported an observed outcome that was inconsistent with the majority of other studies.

Evidence for Use in Chronic Idiopathic Urticaria (CIU)

Levocetirizine was studied for the symptomatic treatment of Chronic Idiopathic Urticaria (CIU), or chronic hives. Research consists of Randomized Controlled Trials (RCTs) and comparative studies exploring symptom changes in patients experiencing chronic hives.

Research examined outcomes capturing phases of heightened symptom activity, particularly the intensity of itching (Pruritus Severity) and the physical extent of the condition, tracking the number and size of hives or welts (Wheal Number and Size). Findings describe patterns where measurements of itching severity and wheal size in the active compound group were observed to differ from those in the placebo group.

Comparative Research and Consistency of Findings

Research explored how the effects observed with Levocetirizine compare to those of an inactive placebo, with study reports describing observed differences in outcomes measured between the active and inactive groups. A meta-analysis, which pools data from several trials, described aggregated outcome data that included observed outcomes in overall allergic symptom scores when research compared Levocetirizine against another active comparator in the context of allergic rhinitis. This body of RCT and systematic review evidence contributes to the broader evidence landscape, and its quality has been noted in official scientific literature as being high for the studied indications.

What is Still Uncertain About Degraler Research

There is limited information for long-term outcomes regarding the sustained effects of the compound on symptom control for treatment periods extending beyond six months. Long-term effects are not fully established. The available evidence for certain specific subgroups, such as the comprehensive clinical evaluation of the compound in chronic urticaria for all pediatric age groups, is noted as being limited.

Key Studies & References

  1. The effectiveness of levocetirizine in comparison with loratadine in treatment of allergic rhinitis--a meta-analysis
  2. A comprehensive clinical evaluation of levocetirizine in the treatment of chronic urticaria in children

Frequently Asked Questions (FAQ)

Common questions about Degraler (FAQ)


Q: Why does Degraler need to be taken at a specific time of day?

Official guidelines recommend taking this medicine in the evening. This timing aligns with the potential for some patients to experience somnolence (drowsiness) or fatigue, which are listed as common side effects in regulatory documents. The suggestion to take it in the evening is thought to relate to managing the potential for drowsiness.


Q: Does Degraler cause long-term side effects that I should know about?

Clinical experience with the active compound exists for treatment periods of at least six months. Regulatory documents note that one rare, long-term-related risk is the development of new or severe itching (pruritus) that may occur after a person stops taking the medicine following long-term, daily use. If this or other side effects occur, consultation with a healthcare provider is noted as appropriate.


Q: How long does it usually take to feel the effect of Degraler?

Studies on the compound's properties show that it is rapidly and extensively absorbed after administration. The highest concentration in the blood, known as the peak plasma concentration, is typically reached in adults within less than one hour after taking a dose.


Q: What happens if I suddenly stop taking Degraler?

Official information indicates that after stopping the medicine following long-term, daily use, there is a documented rare risk of experiencing new or severe itching (pruritus) within a few days. This is a recognized effect related to stopping the medicine, not a sign of addiction or withdrawal.


Q: Can elderly patients safely use Degraler?

Dose selection for older adults requires caution, as regulatory documents note that many elderly patients have reduced kidney function. If kidney function is impaired, a dosage adjustment is necessary. Older adults may also be at a higher risk for certain side effects, such as urinary retention.


Q: Is Degraler safe to use during pregnancy or while breastfeeding?

Use during pregnancy should only occur if a doctor determines it is clearly needed, as comprehensive controlled studies in pregnant women are not available. It is generally not recommended while breastfeeding because the active compound may pass into breast milk and could potentially affect the nursing infant.


Q: Does Degraler interact with common over-the-counter pain relievers?

Regulatory drug interaction studies primarily focused on a limited number of specific compounds and did not show clinically relevant issues. No interaction with common pain relievers is explicitly documented in primary regulatory labels. However, regulatory warnings for the drug class include a general need for caution when co-administering with central nervous system depressants.


Q: What is the risk of a serious allergic reaction to Degraler?

The medicine is formally contraindicated, meaning it must not be used, if a person has a known hypersensitivity to the active compound or related substances. Observed reactions reported after the medicine became available have ranged from hives to severe, potentially life-threatening allergic reactions (anaphylaxis).


Q: Are there any restrictions on driving or operating machinery while taking Degraler?

Because the medicine may cause somnolence (drowsiness), fatigue, or impaired performance in some patients, official warnings recommend avoiding engaging in hazardous activities, such as driving or operating heavy machinery, until a person knows how the medicine affects them.


Q: Are the side effects of Degraler temporary or permanent?

Common side effects, like drowsiness and fatigue, are frequently reported early in clinical trials. It is generally understood that the duration of side effects varies for each person. New onset itching after discontinuation is known to resolve upon resuming or tapering the medicine, indicating it is not permanent.


Q: Is it true that Degraler can affect my mood or emotions?

Official postmarketing reports list rare psychiatric adverse reactions, including agitation, aggression, and hallucinations. These reports are noted in the regulatory documents, especially in pediatric patients, and are safety points noted in official documentation.


Q: Why is it important to tell my doctor about all the medicines I take before starting Degraler?

Official information notes that Degraler should be avoided with alcohol or other central nervous system depressants due to the risk of additive impairment. Disclosing all medicines, including prescription and over-the-counter products, allows a healthcare provider to screen for all potential interactions.


Q: Is it normal to feel a change in appetite after starting Degraler?

Postmarketing experience has included reports of changes in appetite, including increased appetite. However, this is not one of the most common adverse reactions reported in large-scale clinical trials and is noted as a less frequent event.


Q: Does Degraler interact with birth control pills?

Regulatory data indicates that the active compound is minimally processed by the liver’s CYP450 enzyme system and does not significantly interfere with it. Therefore, a drug-to-drug interaction that would reduce the effectiveness of most hormonal contraceptives is considered unlikely.


Q: What kind of monitoring or check-ups are needed while taking Degraler?

Regulatory information on the product includes warnings about the potential for urinary retention, especially in patients with predisposing conditions. Monitoring for symptoms such as a decrease in urination frequency or volume may be necessary.


Q: Is Degraler safe for use in children and adolescents?

The medicine is approved for use in children as young as six months of age for specific indications, with separate dose recommendations for different age groups. However, a warning exists regarding an increased risk of psychiatric adverse reactions in this population, especially when treatment is started or the dose is changed.


Q: Does the effectiveness of Degraler decrease over time?

Regulatory documents indicate that clinical experience supports the use of the medicine for treatment periods of at least six months for both chronic hives and allergic rhinitis without loss of effect. The need for continued use should be assessed by a prescribing professional.


Q: Do natural supplements or herbal products interact with Degraler?

While specific interactions are not documented in core regulatory labels, general advice suggests caution. This includes advising caution with supplements that cause effects similar to the medicine, such as drowsiness or difficulty urinating, due to the potential for additive effects.


Q: Is there a maximum length of time someone can take Degraler?

Regulatory documents indicate that clinical experience supports the use of the medicine for treatment periods of at least six months. Continued use depends on the condition being treated, and the duration of therapy should be determined by a healthcare provider.


Q: What is the difference between the starting dose and the maintenance dose of Degraler?

The official documentation uses a recommended standard dose for adults and for specific pediatric age groups. For adults, the initial recommended dose is the same as the maximum recommended dose (5 mg once daily).


Q: What is the evidence regarding Degraler's effect on sleep patterns?

Regulatory information classifies somnolence (drowsiness) and fatigue as common adverse reactions, which can impact sleep patterns. Additionally, the medicine is often taken in the evening to address allergy symptoms that may interfere with sleep.


Q: What are some common user experiences or expectations when starting Degraler?

Since the medicine is rapidly absorbed, the start of relief typically occurs quickly. The most commonly reported experiences in clinical trials for adults include somnolence (drowsiness), nasopharyngitis, fatigue, and dry mouth.


Q: What if I have a pre-existing heart condition; can I still take Degraler?

Regulatory studies for the active compound (levocetirizine) did not show a clinically significant effect on heart rhythm (specifically the QT/QTc interval) in healthy subjects. Decisions regarding the use of this medicine in patients with existing heart conditions are subject to professional review.


Q: What if I experience side effects that are not listed in the official patient information?

Regulatory bodies strongly encourage the voluntary reporting of all side effects, including those not listed in the official information. This allows for the continuous and ongoing monitoring of the medicine’s safety profile.


Q: Does taking Degraler with food change how well it works?

Taking the tablets with a high-fat meal has been documented to delay the time it takes to reach maximum concentration in the blood. However, the overall amount of medicine absorbed (the extent of exposure) remains unchanged, suggesting that efficacy is generally maintained.


Q: Can Degraler be crushed or split if a person has trouble swallowing pills?

The tablets are available in a film-coated form, and the official label specifies if a tablet is approved to be split for a specific dose. Splitting or crushing should only be done if explicitly permitted in the product’s official packaging details.


Q: What should I be careful about when stopping Degraler, even if a doctor says to stop?

After stopping the medicine following long-term, daily use, a documented rare risk exists of developing new or severe itching (pruritus) within a few days. This is an official safety constraint noted in the labeling.


Q: What level of evidence exists for Degraler's use in various patient subgroups?

Regulatory data references numerous randomized controlled trials supporting its use for its main indications. However, official information specifically notes that comprehensive clinical evaluation in chronic hives for all pediatric age groups is limited.

How should Degraler be stored and disposed of?

Official Storage and Handling

Degraler (levocetirizine dihydrochloride) must be stored at Controlled Room Temperature, specifically between 20 C and 25 C (68 F and 77 F), with permitted fluctuations up to 30 C (86 F). The product must be protected from excessive heat and moisture.

Requirement Instruction
Temperature Store between 20 C and 25 C (CRT).
Packaging Store tablets in the original container; keep the oral solution container tightly closed.
Safety Keep the medicine out of the sight and reach of children.

Disposal

Disposal of unused or expired Degraler must adhere to local regulations and official guidance. Unwanted medicine should not be flushed down a toilet or poured into a drain. Disposal should be carried out through an authorized drug take-back program or by following standard household disposal steps as recommended by governmental authorities.

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

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