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Clemastine | CAS No: 15686-51-8 | GMP-certified suppliers
A medication that provides symptomatic relief of allergic rhinitis, mild allergic skin conditions, and temporary common cold symptoms through antihistamine activity.
Therapeutic categories
Primary indications
- For the relief of symptoms associated with allergic rhinitis such as sneezing, rhinorrhea, pruritus and acrimation
- Also for the management of mild, uncomplicated allergic skin manifestations of urticaria and angioedema
- Used as self-medication for temporary relief of symptoms associated with the common cold
Product Snapshot
- Clemastine is available in multiple formulation types including oral tablets, syrups, topical gels, and parenteral solutions for intramuscular and intravenous administration
- It is primarily indicated for symptomatic relief of allergic rhinitis, allergic skin conditions such as urticaria and angioedema, and temporary relief of common cold symptoms
- Clemastine holds approved status in key regulatory markets including the US and Canada, with some formulations under investigational use
Clinical Overview
Pharmacodynamically, clemastine competitively inhibits histamine at H1 receptor sites. This antagonism reduces the physiological effects mediated by histamine, including increased capillary permeability, vasodilation, edema formation, itch sensation, and smooth muscle constriction across gastrointestinal and respiratory systems. Unlike agents that prevent histamine release, clemastine does not affect histamine synthesis or degradation but blocks receptor binding. It also exhibits central and peripheral anticholinergic properties, contributing to its sedative effects and potential for drowsiness. Depending on dosage, CNS depression or stimulation may occur.
Mechanistically, clemastine’s selective binding to histamine H1 receptors impedes the action of endogenous histamine, providing symptomatic relief from histamine-induced allergic manifestations.
Regarding absorption, distribution, metabolism, and excretion (ADME), detailed pharmacokinetic parameters vary by formulation and patient factors but generally include oral bioavailability consistent with similar first-generation antihistamines, hepatic metabolism primarily via cytochrome P450 enzymes including CYP2D6 inhibition potential, and renal excretion of metabolites.
Safety considerations include sedation, anticholinergic side effects, and a potential for QTc interval prolongation, categorizing clemastine among agents that require caution in patients with cardiac risk. Its CNS depressant effects warrant careful use in activities requiring alertness.
Notable brands and generic formulations are available globally, often OTC for allergic rhinitis and mild dermatologic allergies.
For API sourcing, quality control should emphasize purity, consistent potency, and compliance with pharmacopeial standards relevant to antihistamine compounds. Given clemastine’s metabolic interactions, evaluation for impurities and regulatory compliance in cytochrome P450 inhibition is advised to ensure safety and efficacy in pharmaceutical formulations.
Identification & chemistry
| Generic name | Clemastine |
|---|---|
| Molecule type | Small molecule |
| CAS | 15686-51-8 |
| UNII | 95QN29S1ID |
| DrugBank ID | DB00283 |
Pharmacology
| Summary | Clemastine acts as a selective antagonist of histamine H1 receptors, inhibiting the physiological effects of endogenous histamine involved in allergic responses. It exhibits antihistaminic, anticholinergic, and sedative properties that modulate capillary permeability, vasodilation, and smooth muscle constriction. Its pharmacodynamic profile includes central and peripheral effects mediated through competitive H1 receptor blockade without preventing histamine release. |
|---|---|
| Mechanism of action | Clemastine is a selective histamine H1 antagonist and 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 | Clemastine is an antihistamine that also induces anticholinergic and sedative effects. Antihistamines competitively antagonize various physiological effects of histamine including increased capillary permeability and dilatation, the formation of edema, the "flare" and "itch" response, and gastrointestinal and respiratory smooth muscle constriction. Within the vascular tree, H1- receptor antagonists inhibit both the vasoconstrictor and vasodilator effects of histamine. Depending on the dose, H1- receptor antagonists can produce CNS stimulation or depression. Most antihistamines exhibit central and/or peripheral anticholinergic activity. Antihistamines act by competitively blocking H1- receptor sites. Antihistamines do not pharmacologically antagonize or chemically inactivate histamine, nor do they prevent the release of histamine. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
ADME / PK
| Absorption | Rapidly absorbed from the gastrointestinal tract. |
|---|---|
| Metabolism | Antihistamines appear to be metabolized in the liver chiefly via mono- and didemethylation and glucuronide conjugation. |
| Route of elimination | Urinary excretion is the major mode of elimination. |
Formulation & handling
- Clemastine is a small molecule with multiple administration routes including oral, injectable (IM/IV), and topical formulations.
- Oral formulations include immediate and extended-release tablets as well as syrups, with a low water solubility requiring formulation strategies to enhance bioavailability.
- Administration with food is recommended to reduce potential gastrointestinal irritation; alcohol should be avoided due to possible interaction effects.
Regulatory status
| Lifecycle | The API has reached patent expiry in both the US and Canada, resulting in a mature market with multiple generic options available. Ongoing competition in these regions is driven by established producers. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | The clemastine supply landscape includes multiple originator and generic manufacturers, such as Teva, Novartis, and Wockhardt, indicating established production capabilities. Branded products are primarily present in the US and Canadian markets. Patent expirations have likely led to existing generic competition, as reflected by the significant number of generic manufacturers and packagers involved. |
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Safety
| Toxicity | Oral LD<sub>50</sub> in rat and mouse is 3550 mg/kg and 730 mg/kg, respectively. Antihistamine overdosage reactions may vary from central nervous system depression to stimulation. In children, stimulation predominates initially in a syndrome which may include excitement, hallucinations, ataxia, incoordination, muscle twitching, athetosis, hyperthermia, cyanosis convulsions, tremors, and hyperreflexia followed by postictal depression and cardio-respiratory arrest. Convulsions in children may be preceded by mild depression. Dry mouth, fixed dilated pupils, flushing of the face, and fever are common. In adults, CNS depression, ranging from drowsiness to coma, is more common. |
|---|
- Handle with appropriate protective equipment to avoid ingestion and skin contact due to potential CNS effects
- Store in a secure, well-ventilated area to minimize exposure risk, considering variability in toxicity between species
- In case of accidental exposure, monitor for central nervous system stimulation or depression symptoms and initiate emergency protocols
Clemastine 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.
Clemastine (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.
Clemastine API manufacturers & distributors
Compare qualified Clemastine API suppliers worldwide. We currently have 1 companies offering Clemastine API, with manufacturing taking place in 1 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 |
|---|---|---|---|---|---|
| Sekisui Medical | Producer | Japan | Japan | CoA, JDMF, USDMF | 11 products |
When sending a request, specify which Clemastine 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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