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Pheniramine | CAS No: 86-21-5 | GMP-certified suppliers
A medication that provides relief from seasonal allergies, cold, and flu symptoms by reducing histamine-induced itching, redness, and swelling in over-the-counter formulations.
Therapeutic categories
Primary indications
- Pheniramine is commonly used in over-the-counter products to treat seasonal allergies or cold and flu symptoms
Product Snapshot
- Pheniramine is available in various formulation types including oral small molecules (tablet, capsule, syrup), injectable solutions, topical ointments, and ophthalmic sprays or drops
- It is primarily indicated for use in products addressing seasonal allergies and symptoms associated with cold and flu
- Pheniramine is approved for commercial distribution in key regulatory markets such as the United States and Canada
Clinical Overview
Pheniramine’s primary clinical indication is to alleviate allergic manifestations such as edema, itching, and redness caused by histamine release. Pharmacodynamically, it acts as an antagonist at histamine H1 receptors, functioning as an inverse agonist upon binding. This activity results in reduced vasodilation and capillary permeability, which lessens wheal and flare reactions commonly seen in allergic responses. Additionally, pheniramine’s central nervous system penetration contributes to sedation, a hallmark of first-generation antihistamines. Emerging evidence suggests that inverse agonism at H4 receptors may also play a role in its antipruritic and anti-inflammatory effects.
Key ADME parameters for pheniramine include its oral bioavailability in typical OTC doses, central nervous system distribution, and metabolic clearance primarily through hepatic pathways. Due to its ability to cross the blood-brain barrier, sedation and anticholinergic side effects are important safety considerations. Furthermore, pheniramine has been identified as a potential QTc-prolonging agent, warranting caution in patients with cardiac risk factors or concomitant medications that affect cardiac repolarization.
Though largely replaced in clinical allergy management by second-generation antihistamines such as cetirizine and loratadine due to improved safety and tolerability profiles, pheniramine remains utilized in certain regional OTC products and combination cold remedies.
From a sourcing and quality perspective, pharmaceutical grade pheniramine APIs should comply with established pharmacopeial standards for purity, residual solvents, and impurity profiles. Given its use in combination products, compatibility and stability testing are essential when selecting API suppliers to ensure consistent formulation performance and regulatory compliance.
Identification & chemistry
| Generic name | Pheniramine |
|---|---|
| Molecule type | Small molecule |
| CAS | 86-21-5 |
| UNII | 134FM9ZZ6M |
| DrugBank ID | DB01620 |
Pharmacology
| Summary | Pheniramine functions as an inverse agonist at histamine H1 and H4 receptors, mitigating allergic symptoms by reducing vasodilation, capillary permeability, and inflammatory responses. Its antagonism of H1 receptors in peripheral tissues decreases edema, itching, and redness, while central nervous system H1 receptor inverse agonism contributes to sedation. Additionally, H4 receptor interaction may further suppress inflammatory itch signaling. |
|---|---|
| Mechanism of action | Pheniramine competes with histamine for the histamine H1 receptor, acting as an inverse agonist once bound. The reduction in H1 receptor activity is responsible for reduced itching as well as reduced vasodilation and capillary leakage leading to less redness and edema. This can be seen in the suppression of the histamine-induced wheal (swelling) and flare (vasodilation) response. Inverse agonism of the H1 receptor in the CNS is also responsible for the sedation produced by first-generation antihistamines like pheniramine. The binding of pheniramine to H4 receptors, and subsequent inverse agonism, may also contribute to reduced itching by antagonizing inflammation. |
| Pharmacodynamics | Pheniramine acts as an antagonist to allergic symptoms stemming from inappropriate histamine release to reduce edema, itching, and redness. The same antihistamine effect also produces sedation by acting in the central nervous system. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H4 receptor | Humans | inverse agonist |
| Histamine H1 receptor | Humans | inverse agonist |
| Nuclear receptor subfamily 1 group I member 3 | Humans |
ADME / PK
| Absorption | The administration of 30.5 mg of free base pheniramine resulted in a Cmax of 173-294 ng/L with a Tmax of 1-2.5 h. |
|---|---|
| Half-life | The terminal half-life of pheniramine administered via IV is 8-17 h. |
| Metabolism | Pheniramine undergoes N-dealkylation to N-didesmethylpheniramine and N-desmethylpheniramine. |
| Route of elimination | Pheniramine is eliminated by metabolism and via renal excretion. 24.3% of pheniramine is present in the urine as the parent drug. |
Formulation & handling
- Pheniramine is a small molecule API suitable for oral, injectable, topical, nasal, and ophthalmic formulations, offering versatile route options.
- The moderate water solubility and logP near 3 suggest formulation considerations for solubilization and bioavailability enhancement in aqueous-based preparations.
- Handling should consider the solid state stability and prevention of moisture exposure to maintain the integrity of various dosage forms, especially powders and extended-release tablets.
Regulatory status
| Lifecycle | The API's primary patents have expired in both the US and Canada, indicating a mature market with potential generic competition. Products containing this API are widely available across these regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Pheniramine is supplied by multiple originator companies producing branded products primarily in the US and Canadian markets. The presence of several branded allergy eye drop formulations indicates established global distribution in these regions. Given the availability of multiple branded products and the generic nature of pheniramine, patent expirations suggest existing generic competition in the supply landscape. |
|---|
Safety
| Toxicity | Case reports involving pheniramine overdosage mention the rare possibility of arrythmias, cutaneous eruptions, and rhabdomyolysis with acute kidney injury. The administration of activated charcoal effectively prevents the absorption of pheniramine as it largely adsorbs to the charcoal, therefore this may be of benefit in cases of overdose if provided early after ingestion. |
|---|
- Handle pheniramine with care to minimize exposure, as overdose cases have been associated with arrhythmias, cutaneous eruptions, and rhabdomyolysis leading to acute kidney injury
- Use appropriate containment and avoid inhalation or skin contact during processing to reduce toxicity risk
- In case of spillage or accidental ingestion, activated charcoal may be employed promptly to limit systemic absorption
Pheniramine 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.
Pheniramine (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.
Pheniramine API manufacturers & distributors
Compare qualified Pheniramine API suppliers worldwide. We currently have 6 companies offering Pheniramine 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 |
|---|---|---|---|---|---|
| Harika Drugs | Producer | India | India | CoA, WC | 3 products |
| Keshava Organics | Producer | India | India | CoA, WC | 6 products |
| Kongo Chemical | Producer | Japan | Japan | CoA, USDMF | 5 products |
| Pharm Rx Chemical Corp | Distributor | United States | Unknown | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Tresinde Biotech | Producer | India | India | CoA, GMP | 50 products |
When sending a request, specify which Pheniramine 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 Pheniramine 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.
