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Mepyramine | CAS No: 91-84-9 | GMP-certified suppliers
A medication that provides relief from allergic conditions, hypersensitivity reactions, and pruritic skin disorders through systemic and topical antihistamine effects.
Therapeutic categories
Primary indications
- Indicated for the treatment of allergic conditions, symptomatic relief of hypersensitivity reaction, and treatment of pruritic skin disorders
Product Snapshot
- Mepyramine is available in multiple formulation types including oral tablets, chewable forms, capsules, liquid solutions, creams, gels, and ophthalmic preparations
- It is primarily used for allergic conditions, hypersensitivity reactions, and pruritic skin disorders
- Mepyramine holds approved status in both the US and Canadian pharmaceutical markets, including veterinary approvals
Clinical Overview
Pharmacologically, mepyramine functions as an inverse agonist at the histamine H1 receptor, a G protein-coupled receptor. By binding to this receptor, mepyramine stabilizes its inactive state, thereby inhibiting Gq/11-mediated intracellular signaling pathways. This mechanism results in the suppression of histamine-induced physiological responses, including edema, vasodilation (flare), and pruritus. The compound’s sedative effects are attributable to its ability to readily cross the blood-brain barrier, exerting activity at subcortical central nervous system sites.
In terms of absorption, distribution, metabolism, and excretion (ADME), mepyramine is known to rapidly permeate the central nervous system, contributing to its drowsiness side effect profile. It also acts as an inhibitor of cytochrome P450 CYP2D6, although the strength of this interaction is not fully quantified. The QTc prolongation potential has been noted but requires further elucidation with clinical data.
Safety considerations primarily concern its sedative properties, which may impair cognitive and motor functions. This effect necessitates caution in patient populations where CNS depression is a risk. Mepyramine has historically been included in over-the-counter combination formulations for cold and menstrual symptom relief; however, in several jurisdictions, it remains classified as an unapproved prescription medication for cough, cold, or allergic conditions. Veterinary approval exists in certain contexts.
Notable usage includes formulation in both systemic and topical anti-allergic preparations. Given its chemical class and pharmacological profile, thorough evaluation of drug-drug interactions, especially with other CNS depressants and CYP2D6 substrates, is recommended.
For API sourcing, regulatory compliance with pharmacopeial standards is essential. Manufacturers should ensure the API meets established purity criteria and confirm absence of contaminants that could influence its pharmacological or toxicological properties. Due to its CNS activity and potential for sedation, consistent batch-to-batch quality and proper impurity profiling are critical to maintain therapeutic safety and efficacy.
Identification & chemistry
| Generic name | Mepyramine |
|---|---|
| Molecule type | Small molecule |
| CAS | 91-84-9 |
| UNII | HPE317O9TL |
| DrugBank ID | DB06691 |
Pharmacology
| Summary | Mepyramine acts as an inverse agonist at histamine H1 receptors, stabilizing the receptor in an inactive state and inhibiting Gq/11-mediated signaling pathways. This interaction reduces the effects of histamine, including edema, flare, and pruritus associated with allergic and hypersensitivity reactions. Additionally, Mepyramine exhibits sedative effects through central nervous system activity at the subcortical level. |
|---|---|
| Mechanism of action | Mepyramine is a histamine H1 receptor inverse agonist. It binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling. Mepyramine competes with histamine for binding at H<sub>1</sub>-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The sedative properties of Mepyramine occur at the subcortical level of the CNS. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
Formulation & handling
- Mepyramine is a small molecule primarily formulated for oral administration in various solid and liquid dosage forms, with additional topical and ophthalmic applications.
- The API demonstrates moderate water solubility and lipophilicity (LogP 3.04), suggesting consideration for solubility enhancement in formulation development.
- Handling should account for food and alcohol interactions, advising administration with food and avoidance of alcohol to optimize therapeutic effectiveness.
Regulatory status
| Lifecycle | The API's primary patents have expired in both the US and Canada, enabling generic competition and marking the product as mature in these markets. Consequently, the API is widely available through multiple manufacturers with established regulatory approvals. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Mepyramine includes multiple originator companies producing branded products primarily in the US and Canadian markets. The presence of several branded formulations indicates an established market, with no indication of recent patent expiry, suggesting that generic competition may already exist or be developing. Global presence outside North America appears limited based on available data. |
|---|
Safety
| Toxicity | The signs and symptoms that are produced after the acute overdosage of Mepyramine include Convulsions, Coma, Ataxia, Hyperpyrexia, Tremor, Extrapyramidal effects, Excitement. |
|---|
- Mepyramine may cause central nervous system toxicity including convulsions, coma, and extrapyramidal symptoms upon acute overdosage
- Handle with care to avoid exposure that could lead to neurological adverse effects such as ataxia, tremor, and hyperpyrexia
- Use appropriate protective equipment and containment measures to minimize risk of accidental ingestion or inhalation
Mepyramine 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.
Mepyramine (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.
Mepyramine API manufacturers & distributors
Compare qualified Mepyramine API suppliers worldwide. We currently have 5 companies offering Mepyramine 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 |
|---|---|---|---|---|---|
| Chr. Olesen Group | Distributor | Denmark | India | CEP, CoA, GMP, MSDS | 252 products |
| Keshava Organics | Producer | India | India | CoA, USDMF, WC | 6 products |
| Pharm Rx Chemical Corp | Distributor | United States | India | BSE/TSE, CoA, GMP, MSDS, USDMF | 166 products |
| Rochem International, Inc... | Distributor | United States | United States | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF | 144 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
When sending a request, specify which Mepyramine 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 Mepyramine 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.
