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Doxylamine | CAS No: 469-21-6 | GMP-certified suppliers
A medication that provides short-term sleep aid, nighttime relief of cold and allergy symptoms, and prevention of pregnancy-related morning sickness when combined with vitamin B6.
Therapeutic categories
Primary indications
- Used alone as a short-term sleep aid, in combination with other drugs as a night-time cold and allergy relief drug
- Also used in combination with Vitamin B6 (pyridoxine) to prevent morning sickness in pregnant women
Product Snapshot
- Doxylamine is available in multiple oral formulations including tablets (standard, extended, delayed, chewable, film-coated), capsules (gelatin coated, liquid-filled), syrups, powders for solution, and topical patches
- It is primarily indicated for short-term use as a sleep aid, as a component in night-time cold and allergy relief combinations, and in combination with Vitamin B6 for prevention of morning sickness during pregnancy
- Doxylamine is approved for human and veterinary use in the US and Canadian markets
Clinical Overview
Clinically, doxylamine is employed as a short-term hypnotic agent and as an adjunct in combination products for nighttime relief of cold and allergy symptoms such as hay fever and urticaria. It is also used in combination with pyridoxine (vitamin B6) for the prevention of nausea and vomiting during pregnancy, specifically targeting morning sickness. Historically, doxylamine was utilized in the management of parkinsonism and has applications in veterinary medicine.
The pharmacological mechanism involves competitive inhibition at peripheral and central H1 receptors, thereby mitigating histamine-induced allergic responses. Its anticholinergic activity contributes to its efficacy as an antiemetic and sedative. Doxylamine displays a high sedative potency, reportedly exceeding that of some barbiturates such as phenobarbital and many prescription hypnotics, which is attributed to its central nervous system depressant effects.
Key pharmacokinetic parameters include rapid oral absorption and extensive distribution due to lipophilicity, with metabolism primarily hepatic and elimination via renal excretion of metabolites. Specific ADME data, such as half-life and bioavailability, require reference to detailed pharmacokinetic studies.
Safety considerations highlight its anticholinergic side effects, including dry mouth, dizziness, and potential confusion, particularly in elderly populations. It is also identified as a potential QTc-prolonging agent, warranting caution in patients with cardiac arrhythmias or those receiving other QTc-prolonging medications. Overdose risk includes pronounced sedation and anticholinergic toxicity.
Notable brand formulations primarily incorporate doxylamine as a component of combination cold remedies or as standalone over-the-counter sleep aids in various international markets, with regulatory approval for human and veterinary use.
From a sourcing perspective, ensuring high purity and consistent quality of doxylamine API is crucial due to its potent pharmacodynamic profile and safety considerations. Manufacturers and purchasers should verify compliance with pharmacopeial standards and regulatory guidelines, including identity, potency, and impurity limits, to support safe and effective pharmaceutical formulation.
Identification & chemistry
| Generic name | Doxylamine |
|---|---|
| Molecule type | Small molecule |
| CAS | 469-21-6 |
| UNII | 95QB77JKPL |
| DrugBank ID | DB00366 |
Pharmacology
| Summary | Doxylamine is an ethanolamine-class antihistamine that primarily exerts its effects through competitive antagonism of histamine H1 receptors. It possesses significant sedative and anticholinergic properties, targeting muscarinic acetylcholine receptors in addition to H1 receptors. Its pharmacodynamic profile supports use as a short-term sleep aid and for relief of allergic symptoms. |
|---|---|
| Mechanism of action | Like other antihistamines, doxylamine acts by competitively inhibiting histamine at H1 receptors. It also has substantial sedative and anticholinergic effects. |
| Pharmacodynamics | Doxylamine is an antihistamine commonly used as a sleep aid. This drug is also used to relieve symptoms of hay fever (allergic rhinitis), hives (rash or itching), and other allergic reactions. Doxylamine is a member of the ethanolamine class of antihistamines and has anti-allergy power far superior to virtually every other antihistamine on the market, with the exception of diphenhydramine (Benadryl). It is also the most powerful over-the-counter sedative available in the United States, and more sedating than many prescription hypnotics. In a study, it was found to be superior to even the barbiturate, phenobarbital for use as a sedative. Doxylamine is also a potent anticholinergic. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
| Nuclear receptor subfamily 1 group I member 3 | Humans | |
| Muscarinic acetylcholine receptor | Humans | antagonist |
ADME / PK
| Absorption | Readily absorbed via the gastrointestinal tract. |
|---|---|
| Half-life | 10 hours |
| Metabolism | Hepatic. |
Formulation & handling
- Doxylamine is a small molecule primarily formulated for oral administration in various solid and liquid dosage forms.
- Due to its moderate water solubility and LogP, formulation optimization may be needed to enhance bioavailability in oral products.
- Avoidance of co-administration with alcohol is recommended due to potential additive sedative effects.
Regulatory status
| Lifecycle | The API has several patents expired in the US as of 2019 and 2021, with additional patents protecting formulations until 2033. It is marketed in the US and Canada, indicating a mature market with ongoing patent protection for specific formulations. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Doxylamine is supplied by multiple packagers serving primarily the US and Canadian markets, with several branded products available. The presence of patents extending until 2033 indicates ongoing patent protection, suggesting limited current generic competition in these regions. The manufacturing landscape includes originator companies maintaining global brand presence, particularly in North America. |
|---|
Safety
| Toxicity | Signs of overdose include wheezing, tightness in the chest, fever, itching, bad cough, blue skin color, fits, swelling of face, lips, tongue, or throat. |
|---|
- Overdose may result in respiratory distress, central nervous system symptoms, and localized swelling
- Handle with appropriate respiratory protection to prevent inhalation of dust or aerosols
- Use caution to avoid skin or mucous membrane contact due to potential for hypersensitivity reactions
Doxylamine 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.
Doxylamine (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.
Doxylamine API manufacturers & distributors
Compare qualified Doxylamine API suppliers worldwide. We currently have 4 companies offering Doxylamine 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 |
|---|---|---|---|---|---|
| Corden Pharma | Producer | Germany | Italy | CoA, GMP, USDMF | 45 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Sigma-Aldrich | Producer | United States | Ireland | CEP, CoA, FDA, USDMF | 13 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001, MSDS | 757 products |
When sending a request, specify which Doxylamine 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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