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Chlorpheniramine | CAS No: 132-22-9 | GMP-certified suppliers
A medication that provides relief from allergic conditions including rhinitis, urticaria, hay fever, common cold symptoms, and supportive management of certain asthma-related reactions.
Therapeutic categories
Primary indications
- For the treatment of rhinitis, urticaria, allergy, common cold, asthma and hay fever
Product Snapshot
- Chlorpheniramine is a small-molecule antihistamine available in multiple oral solid/liquid forms and parenteral formulations
- It is used for symptomatic management of allergic conditions including rhinitis, urticaria, hay fever, common cold, and allergy-related respiratory irritation
- It is approved in the US and Canada
Clinical Overview
Its pharmacology is based on competitive inverse agonism at the histamine H1 receptor. By occupying H1 binding sites on effector cells of the respiratory tract, vasculature, and gastrointestinal tissues, it reduces the physiologic consequences of histamine release. These include pruritus, vasodilation, increased vascular permeability, bronchoconstriction, and sensory nerve activation. Clinical benefit reflects attenuation of sneezing, rhinorrhea, and ocular symptoms associated with allergic responses.
Chlorpheniramine is a substituted alkylamine derivative with central nervous system activity. Compared with some classical antihistamines, it generally exhibits moderate sedative potential, although individual variability is notable. It is also characterized as an inhibitor and substrate of cytochrome P450 CYP2D6 and a substrate of CYP3A isoforms, which has implications for metabolic interactions and potential alteration of exposure when co‑administered with strong modifiers of these pathways.
Absorption following oral administration is typically rapid, with systemic distribution to central and peripheral tissues. The compound undergoes hepatic metabolism and is eliminated through renal pathways. Duration of action supports multiple daily dosing in most formulations. Reported adverse effects include somnolence, impaired psychomotor function, dry mouth, and anticholinergic symptoms. Chlorpheniramine is listed among agents with moderate QTc prolongation risk and is associated with serotonergic activity relevant to serotonin syndrome when combined with other serotonergic drugs.
Chlorpheniramine is available internationally in numerous single‑agent and combination over‑the‑counter products. For API procurement, sourcing should prioritize pharmacopeial‑grade material supported by validated impurity profiles, consistent polymorphic form control, and reliable documentation of residual solvent and elemental impurity compliance.
Identification & chemistry
| Generic name | Chlorpheniramine |
|---|---|
| Molecule type | Small molecule |
| CAS | 132-22-9 |
| UNII | 3U6IO1965U |
| DrugBank ID | DB01114 |
Pharmacology
| Summary | Chlorpheniramine is an H1‑receptor inverse agonist that reduces the downstream effects of histamine released during allergic responses. By competitively blocking H1 receptors on vascular, respiratory, and gastrointestinal tissues, it limits the vasodilation, permeability changes, and sensory activation associated with histamine signaling. It also interacts with monoamine transporters, though these effects are secondary to its primary antihistaminic action. |
|---|---|
| Mechanism of action | Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. |
| Pharmacodynamics | In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H<sub>1</sub>-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Chlorpheniramine, is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It competes with histamine for the normal H<sub>1</sub>-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
| Sodium-dependent serotonin transporter | Humans | inhibitor |
| Sodium-dependent noradrenaline transporter | Humans | inhibitor |
ADME / PK
| Absorption | Well absorbed in the gastrointestinal tract. |
|---|---|
| Half-life | 21-27 hours |
| Protein binding | 72% |
| Metabolism | Primarily hepatic via Cytochrome P450 (CYP450) enzymes. |
Formulation & handling
- Oral formulations need solubilization aids or salts due to low aqueous solubility and moderate lipophilicity, with food potentially improving tolerance.
- Parenteral solutions require solvents and pH control to maintain clarity and prevent precipitation of this lipophilic small molecule.
- Liquid and syrup forms should incorporate antioxidants or protective packaging to limit degradation in solution.
Regulatory status
| Lifecycle | Patent protection for the API in the United States spans from already‑expired estates to coverage extending through 2032, indicating a market that is partly mature but still supported by later‑expiring patents. With commercialization limited to the US and Canada, the product remains in a protected phase in these markets until the final US patent expires. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Chlorpheniramine is an established antihistamine with numerous packagers and generic manufacturers, indicating that originator influence in the supply chain is minimal and the market is largely generics‑driven. Branded products are primarily documented in the US and Canada, with limited evidence of broader regional branding. The core molecule’s patent protection has long expired, and the remaining listed patents relate to later formulations, supporting the presence of mature generic competition. |
|---|
Safety
| Toxicity | Oral LD50 (rat): 306 mg/kg; Oral LD50 (mice): 130 mg/kg; Oral LD50 (guinea pig): 198 mg/kg [Registry of Toxic Effects of Chemical Substances. Ed. D. Sweet, US Dept. of Health & Human Services: Cincinatti, 2010.] Also a mild reproductive toxin to women of childbearing age. |
|---|
- Demonstrates moderate acute oral toxicity across species (LD50 values: rat 306 mg/kg, mouse 130 mg/kg, guinea pig 198 mg/kg), indicating need for controlled handling and exposure minimization in production settings
- Classified as a mild reproductive toxin for women of childbearing potential
- Implement appropriate industrial hygiene controls to limit occupational exposure
US Drug Master File (USDMF)
A US Drug Master File (USDMF) is a confidential document submitted to the U.S. Food and Drug Administration (FDA) that provides detailed information about the manufacturing process of an Active Pharmaceutical Ingredient (API) or a finished pharmaceutical product. This document includes comprehensive details such as chemical properties, manufacturing facilities, production processes, packaging specifications, storage conditions, and more.
The USDMF ensures that proprietary information remains protected while allowing the FDA to review the data as part of drug approval processes. Unlike other types of DMFs used in different regions, the USDMF is specifically designed to meet the regulatory requirements set by the FDA, ensuring compliance with U.S. standards.
Chlorphenamine 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.
Chlorphenamine (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.
Chlorphenamine API manufacturers & distributors
Compare qualified Chlorphenamine API suppliers worldwide. We currently have 9 companies offering Chlorphenamine API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Auro Laboratories | Producer | India | India | CEP, CoA, GMP | 6 products |
| Chr. Olesen Group | Distributor | Denmark | India | CEP, CoA, GMP, MSDS | 252 products |
| Harika Drugs | Producer | India | India | CoA, WC | 3 products |
| Keshava Organics | Producer | India | India | CoA, USDMF, WC | 6 products |
| Kongo Chemical | Producer | Japan | Japan | CEP, CoA, FDA, USDMF | 5 products |
| Mahalaxmi Chemi Pharm | Producer | India | India | CoA | 13 products |
| Mallinckrodt | Producer | United States | Unknown | CoA, USDMF | 34 products |
| Pharm Rx Chemical Corp | Distributor | United States | India | BSE/TSE, CoA, GMP, MSDS, USDMF | 166 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
When sending a request, specify which Chlorphenamine 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 Chlorphenamine 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 Chlorphenamine API
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Technical
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Regulatory
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