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Xylometazoline | CAS No: 526-36-3 | GMP-certified suppliers
A medication that provides temporary relief of nasal congestion associated with colds, hay fever, and other respiratory allergies to support reliable formulation of nasal products.
Therapeutic categories
Primary indications
- Xylometazoline is indicated for the temporary relief of nasal congestion due to cold, hay fever or other respiratory allergies
Product Snapshot
- Xylometazoline is supplied as nasal and topical small‑molecule formulations including sprays, solutions, gels, and drops
- It is used for short-term relief of nasal congestion associated with colds, hay fever, and other respiratory allergies
- It is approved in the US and Canada, with some investigational listings in certain markets
Clinical Overview
Xylometazoline produces localized vasoconstriction of the venous sinusoids within the nasal mucosa through activation of alpha adrenergic receptors. Its activity is most pronounced at α2B‑adrenoceptors, with additional affinity for α1A, α2A, α2C, α1B, and α1D receptor subtypes. This receptor engagement reduces mucosal edema, decreases nasal resistance, and restores nasal airflow. Comparative data indicate a slightly faster onset of action than oxymetazoline, with a similar duration of effect.
Pharmacodynamic studies report a rapid onset of subjective symptom relief, with median improvement occurring within minutes and maximal perceived benefit reached within approximately half an hour. As a topically applied agent with limited systemic exposure, formal ADME characterization is minimal; however, systemic absorption can occur, particularly with excessive dosing or compromised mucosa.
Safety considerations center on the risk of rebound congestion, rhinitis medicamentosa, and reduced decongestant effect with prolonged or high‑frequency use. Use is generally restricted to short treatment intervals to mitigate these effects. Systemic sympathomimetic reactions such as hypertension or tachycardia are uncommon but possible, particularly in sensitive populations. Early in vitro observations of antioxidant activity have been described, though these findings do not inform clinical use.
Xylometazoline is marketed globally in various OTC brands. For API procurement, manufacturers should verify compliance with pharmacopeial specifications, confirm impurity profiles appropriate to regional regulatory expectations, and ensure reliable supply chain controls for consistent particle characteristics and stability suitable for nasal formulations.
Identification & chemistry
| Generic name | Xylometazoline |
|---|---|
| Molecule type | Small molecule |
| CAS | 526-36-3 |
| UNII | WPY40FTH8K |
| DrugBank ID | DB06694 |
Pharmacology
| Summary | Xylometazoline is a sympathomimetic agent that relieves nasal congestion by activating alpha‑adrenergic receptors in the nasal mucosa, producing vasoconstriction of venous sinusoids and reducing airway resistance. It acts across multiple alpha‑1 and alpha‑2 receptor subtypes, with relative selectivity for the alpha‑2B receptor. Pharmacodynamic effects include rapid reduction of mucosal edema and increased nasal airflow, with additional in vitro evidence of antioxidant activity. |
|---|---|
| Mechanism of action | Nasal congestion is caused by various etiologies, such as rhinosinusitis and allergic or non-allergic rhinitis, leading to congestion of the venous sinusoids lining the nasal mucosa. Activation of α-adrenergic receptors leads to vasoconstriction of the blood vessels of the nasal mucosa and resumption of nasal airflow.As the most abundantly expressed in the human nasal mucosa, α<sub>1A</sub>- and α<sub>2B</sub>-adrenoceptors may play the most important role in vasoconstriction of the human nasal mucosa. Xylometazoline is a more selective agonist at α<sub>2B</sub>-adrenoceptors,with affinity at α<sub>1A</sub>-, α<sub>2A</sub>-, α<sub>2C</sub>-, α<sub>1B</sub>-, and α<sub>1D</sub>-adrenoceptors.Xylometazoline decreases nasal resistance during inspiration and expiration and increases the volume of nasal airflow. Compared to [oxymetazoline], another imidazoline nasal decongestant, xylometazoline had a slightly faster onset of action although they had a similar duration of action.In one study, subjects with nasal congestion reported relief of earache and sore throat in addition to nasal decongestion: it is speculated that oxymetazoline mediates this effect by causing vasoconstriction of the nasal mucosa that contains the venous sinuses and nasal decongestion allows breathing through the nose, providing relief from sore throat caused by mouth breathing that dries and irritates the throat. |
| Pharmacodynamics | Xylometazoline is a sympathomimetic agent that causes vasoconstriction of the nasal mucosa. In one study comprising subjects with nasal congestion associated with the common cold, the median time of onset of subjective relief of nasal congestion was about 1.7 minutes and the time of subjective peak relief of nasal congestion was 30 minutes.Previous studies reported rebound swelling, rebound nasal congestion, rhinitis medicamentosa, and shorter duration of decongestant effect from the long-term use of xylometazoline in healthy volunteers, suggesting that the drug is most effective if used temporarily. An early _in vitro_ study demonstrated xylometazoline to exert anti-oxidant actions, where it inhibited microsomal lipid peroxidation and mediated hydroxyl radical scavenging activity. This suggests that xylometazoline has a beneficial effect against oxidants, which play a role in tissue damage in inflammation. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Alpha-2A adrenergic receptor | Humans | agonist |
| Alpha-2B adrenergic receptor | Humans | agonist |
| Alpha-1A adrenergic receptor | Humans | agonist, partial agonist |
ADME / PK
| Absorption | No information is available on xylometazoline pharmacokinetics. |
|---|---|
| Half-life | No information is available on xylometazoline pharmacokinetics. |
| Protein binding | No information is available on xylometazoline pharmacokinetics. |
| Metabolism | No information is available on xylometazoline pharmacokinetics. |
| Route of elimination | No information is available on xylometazoline pharmacokinetics. |
| Volume of distribution | No information is available on xylometazoline pharmacokinetics. |
| Clearance | No information is available on xylometazoline pharmacokinetics. |
Formulation & handling
- A small‑molecule nasal decongestant formulated mainly as aqueous nasal sprays or gels, requiring solubilizers or co‑solvents due to low aqueous solubility.
- Non‑oral, locally acting API with minimal systemic exposure; suitable for nasal, topical, or ophthalmic solutions where pH and osmolarity control support mucosal tolerance.
- Chemically stable as a solid; finished products should minimize oxidation and maintain preservative effectiveness to ensure multi‑dose container stability.
Regulatory status
| Lifecycle | With patent protections expired or nearing expiry, the API in the US and Canada is in a mature stage of its lifecycle. Market dynamics are largely driven by established generic competition across both regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Xylometazoline is an established OTC decongestant with long‑expired intellectual property, so there is no active originator protection and supply is fully generic. Multiple companies market branded OTC formulations in the United States and Canada, indicating a mature, multi‑supplier landscape. The absence of remaining patent barriers supports ongoing broad generic competition. |
|---|
Safety
| Toxicity | The oral LD<sub>50</sub> is 230 mg/kg in rats and 75 mg/kg in mice. The subcutaneous LD<sub>50</sub> is 90 mg/kg in rats and 53 mg/kg in mice. The intraperitoneal LD<sub>50</sub> is 43 mg/kg in rats. Xylometazoline poisoning is documented in three pediatric patients who were exposed to a drug concentration 40 times above the adequate dosage for children due to a compounding error: these patients experienced bradypnea and sinus bradycardia with supraventricular extrasystoles and were managed with fluid management. |
|---|
- Acute toxicity is moderate to high, with oral LD50 values of 230 mg/kg in rats and 75 mg/kg in mice
- Parenteral routes show increased potency, with intraperitoneal LD50 as low as 43 mg/kg in rats
- Overexposure can produce significant cardiopulmonary effects, including bradypnea and bradyarrhythmias, as observed in cases involving excessive concentrations
Xylometazoline is a type of Adrenergic agents
Adrenergic agents are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that target the adrenergic system in the body. This system is responsible for regulating various physiological responses, including heart rate, blood pressure, and smooth muscle contraction.
Adrenergic agents can be further divided into two main groups: adrenergic agonists and adrenergic antagonists. Adrenergic agonists stimulate the adrenergic receptors, leading to an increase in sympathetic nervous system activity. This can result in effects such as vasoconstriction, bronchodilation, and increased heart rate. Adrenergic agonists are commonly used in the treatment of conditions such as asthma, hypotension, and cardiac arrest.
On the other hand, adrenergic antagonists block the adrenergic receptors, thereby inhibiting the effects of sympathetic nervous system activation. These agents are often employed to lower blood pressure, treat certain heart conditions, and manage symptoms associated with conditions like benign prostatic hyperplasia. Adrenergic antagonists can be further classified into alpha-adrenergic antagonists and beta-adrenergic antagonists, based on their selectivity for different adrenergic receptor subtypes.
Pharmaceutical companies extensively utilize adrenergic agents as key components in the development of various medications. Adrenergic APIs offer targeted effects on the adrenergic system, allowing for precise modulation of physiological responses. The understanding of adrenergic agents and their mechanisms of action is vital for the design and optimization of drugs used in the treatment of numerous medical conditions. Researchers and scientists continue to explore and innovate within this subcategory to develop new adrenergic agents with enhanced efficacy and fewer side effects, ultimately improving patient outcomes.
Xylometazoline (Adrenergic agents), 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.
Xylometazoline API manufacturers & distributors
Compare qualified Xylometazoline API suppliers worldwide. We currently have 7 companies offering Xylometazoline API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Chemische Fabrik Berg | Producer | Germany | Germany | CEP, CoA, FDA, GMP | 20 products |
| Duchefa Farma B.V. | Distributor | Netherlands | Germany | CoA, GMP, ISO9001, MSDS | 170 products |
| Ipochem | Producer | Poland | Poland | CEP, CoA, GMP | 3 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CEP, CoA, FDA, GMP, MSDS | 64 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Unnati Pharmaceuticals Pv... | Distributor | India | India | CoA | 70 products |
When sending a request, specify which Xylometazoline 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.).
Use the list above to find high-quality Xylometazoline API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Xylometazoline API
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