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Levocetirizine | CAS No: 130018-77-8 | GMP-certified suppliers
A medication that treats perennial allergic rhinitis and chronic idiopathic urticaria symptoms with a non-sedating antihistamine profile suitable for diverse allergy management.
Therapeutic categories
Primary indications
- Levocetirizine is indicated to treat symptoms of perennial allergic rhinitis and uncomplicated skin manifestations of chronic idiopathic urticaria
- It is also used over the counter for a variety of mild allergy symptoms
Product Snapshot
- Levocetirizine is available as oral tablets, capsules, syrups, and topical formulations including creams, gels, and shampoos
- It is primarily used for the treatment of perennial allergic rhinitis and chronic idiopathic urticaria symptoms
- Levocetirizine is approved for use in the US market
Clinical Overview
Pharmacologically, levocetirizine functions by selectively inhibiting peripheral histamine H1 receptors, thereby blocking histamine-mediated effects such as smooth muscle contraction, increased vascular endothelial permeability, stimulation of cough receptors, and neural flare responses. This results in symptom relief associated with allergic conditions. Its specificity for H1 receptors contributes to a lower incidence of sedation relative to first-generation antihistamines, although caution is advised in patient populations prone to urinary retention or tasks requiring full alertness.
Pharmacokinetic data indicate that levocetirizine is predominantly excreted via the renal route, necessitating dose adjustment or close monitoring in patients with impaired renal function. It is metabolized to a limited extent and functions as a substrate for cytochrome P450 enzymes, particularly CYP3A4, but is not a strong inducer or inhibitor, reducing the potential for significant drug-drug interactions in this pathway.
Safety evaluations, including animal studies, demonstrate a wide therapeutic window with maximal nonlethal doses exceeding 100 times typical clinical doses, supporting a generally favorable safety profile when used as directed. However, levocetirizine may have QTc prolongation potential, warranting caution in patients with cardiac risk factors or those receiving other QTc-prolonging agents.
As a diphenylmethane derivative within the piperazine class, levocetirizine APIs must meet rigorous quality standards including stereochemical purity, consistent potency, and low impurity levels. Attention to source transparency, compliance with pharmacopeial specifications, and robust stability data is critical in API procurement to ensure consistent clinical efficacy and safety.
Identification & chemistry
| Generic name | Levocetirizine |
|---|---|
| Molecule type | Small molecule |
| CAS | 130018-77-8 |
| UNII | 6U5EA9RT2O |
| DrugBank ID | DB06282 |
Pharmacology
| Summary | Levocetirizine is a second-generation antihistamine that selectively antagonizes histamine H1 receptors, mitigating allergic symptoms such as rhinitis and urticaria. Its mechanism reduces histamine-induced effects including vascular permeability and smooth muscle contraction. The drug exhibits a long duration of action and a wide therapeutic index. |
|---|---|
| Mechanism of action | Levocetirizine selectively inhibits histamine H<sub>1</sub> receptors. This action prevents histamine from activating this receptor and causing effects like smooth muscle contraction, increased permeability of vascular endothelium, histidine uptake in basophils, stimulation of cough receptors, and stimulation of flare responses in the nervous system. |
| Pharmacodynamics | Levocetirizine is a second generation histamine H<sub>1</sub> antagonist used to treat various allergic symptoms. It has a long duration of action as it is generally taken once daily, and a wide therapeutic window as animal studies show the maximal nonlethal dose is over 100x a normal dose. Patients are cautioned to avoid tasks that require complete alertness, avoid alertness, and use caution in patients with factors predisposing urinary retention. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist, inhibitor |
ADME / PK
| Absorption | Following a 5mg oral dose of levocetirizine, a C<sub>max</sub> of 0.27±0.04µg/mL with a T<sub>max</sub> of 0.75±0.50h. The AUC of levocetirizine is 2.31±0.50µg\*h/mL. Taking levocetirizine with food does not affect the AUC but delays T<sub>max</sub> by 1.25 hours and lowers C<sub>max</sub> by 36%. |
|---|---|
| Half-life | The average half life of levocetirizine is 7.05±1.54 hours. |
| Protein binding | Plasma protein binding of levocetirizine was on average 96.1% 1 hour post dose and 91.9% 6 hours post dose. |
| Metabolism | Levocetirizine is poorly metabolized with 85.8% of an oral dose being excreted as the unchanged drug. Levocetirizine can be metabolized to a dihydrodiol (M2), an N-oxide (M3), a hydroxymethoxy derivative (M4), a hydroxy derivative (M5), an O-dealkylated derivative (M6), a taurine conjugate (M8), and an N-dealkylated and aromatic hydroxylated derivative (M9). The M5 metabolite can be glucuronidated to form the M1 metabolite and the M9 metabolite can form 4-chloro-4'-hydroxybenzhydryl mercapturates (M10a and M10b). |
| Route of elimination | 168 hours post dose an average of 85.4% of a radiolabeled dose was recovered with an average of 80.8% in the urine and 9.5% in the feces. In the urine, 77% of the dose was recovered as unchanged drug, 0.5% as the M8 and M9 metabolites, 0.4% as the M10a metabolite, 0.4% as the M10b metabolite, 0.3% as the M3 metabolite, 0.3% as the M4 and M5 metabolite, 0.2% as the M2 metabolite, and 0.1% as the M1 metabolite. In the feces, 9.0% of the dose was recovered as unchanged drug, 1.0% as the M4 and M5 metabolite, and 0.1% as the M1 metabolite. |
| Volume of distribution | The volume of distribution of levocetirizine is 0.33±0.02L/kg. |
| Clearance | The average clearance of levocetirizine is 0.57±0.18mL/min/kg. |
Formulation & handling
- Levocetirizine is a small molecule primarily formulated for oral administration in various solid and liquid dosage forms.
- It is suitable for buccal, topical, and transdermal routes, but injectable formulations are not indicated.
- The drug shows moderate water solubility and can be taken with or without food; avoid co-administration with alcohol.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is commercially available in the United States, with initial patent protection expired in March 2013 and subsequent patent coverage extending until October 2027. The market is currently in a mature phase with ongoing patent protections influencing product exclusivity. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Levocetirizine involves a limited number of originator companies primarily focusing on the US market, as reflected by the branded products available. Multiple branded allergy relief formulations are present, indicating established market penetration in the US. Patent protection is active until 2027, suggesting that generic competition is currently limited but may increase upon patent expiry. |
|---|
Safety
| Toxicity | Patients experiencing an overdose may present with drowsiness. Children may become agitated and restless before drowsiness. Patients should be treated with supportive measures. Dialysis will not assist in removing the drug from the body. The maximal nonlethal dose in mice and rats is 240mg/kg. |
|---|
- Overdose may cause central nervous system depression, including drowsiness
- Pediatric cases can exhibit initial agitation and restlessness
- Supportive care is the primary treatment approach
Levocetirizine is a type of Antihistamines
Antihistamines are a vital subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) widely used in the treatment of allergies and allergic reactions. These compounds work by blocking the action of histamines, which are responsible for triggering allergic symptoms such as itching, sneezing, runny nose, and watery eyes.
Antihistamines can be classified into two main categories: first-generation and second-generation antihistamines. First-generation antihistamines, such as diphenhydramine and chlorpheniramine, have been in use for several decades. They are effective in relieving allergy symptoms but are associated with drowsiness and other side effects due to their ability to cross the blood-brain barrier.
On the other hand, second-generation antihistamines, including cetirizine, loratadine, and fexofenadine, offer similar allergy relief with fewer sedative effects. These newer antihistamines are preferred for their improved safety profiles, making them suitable for use during the day without causing significant drowsiness.
Antihistamines are available in various forms, including tablets, capsules, syrups, and topical creams. They are extensively used to manage conditions such as hay fever, hives, allergic rhinitis, and insect bites. Moreover, antihistamines may also be combined with decongestants or other medications to provide relief from nasal congestion and sinus symptoms.
As pharmaceutical APIs, antihistamines are produced through meticulous synthesis and manufacturing processes, adhering to strict quality standards. These APIs serve as the active components in various branded and generic pharmaceutical formulations, making them crucial in the pharmaceutical industry's production of allergy medications.
In conclusion, antihistamines are a significant subcategory of pharmaceutical APIs widely used for alleviating allergy symptoms. Their classification into first- and second-generation antihistamines offers options based on efficacy and sedative effects. By blocking histamines, antihistamines provide relief from common allergic reactions, making them essential in the development of effective allergy medications.
Levocetirizine (Antihistamines), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
Levocetirizine API manufacturers & distributors
Compare qualified Levocetirizine API suppliers worldwide. We currently have 6 companies offering Levocetirizine API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Cipla | Producer | India | India | CoA, GMP, USDMF, WC | 164 products |
| Glochem | Producer | India | India | CoA, USDMF | 14 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Sichuan Benepure | Producer | China | China | CoA | 23 products |
| Sun Pharma | Producer | India | India | CoA, USDMF | 219 products |
| Symed Labs | Producer | India | India | CoA, GMP, USDMF, WC | 28 products |
When sending a request, specify which Levocetirizine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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