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Betahistine API Manufacturers & Suppliers
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Producer
Produced in
India|
Employees: >600
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Audit Report:
Certifications:
GMP
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FDA|
MSDS|
CoA|
WHO-GMPAll certificates
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CoA
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Producer
Produced in
Spain|
Employees: 50
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Audit Report:
Certifications:
GMP
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USDMF|
EDMF/ASMF|
MSDS|
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JDMF
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CoA
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coa
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coa|
EDQM certificate 2017|
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ISO
coa
EDQM certificate 2017
WC
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Betahistine | CAS No: 5638-76-6 | GMP-certified suppliers
A medication that helps reduce recurrent vertigo episodes in adults with Ménière's disease, supporting reliable treatment supply for neuro‑otologic disorder management.
Therapeutic categories
Antivertigo PreparationsHistamine AgentsHistamine AgonistsHistamine AntagonistsMiscellaneous Central Nervous System AgentsMiscellaneous Therapeutic Agents
Generic name
Betahistine
Molecule type
small molecule
CAS number
5638-76-6
DrugBank ID
DB06698
Approval status
Approved drug, Investigational drug
ATC code
N07CA01
Primary indications
- Betahistine is indicated for the reduction of recurrent vertigo episodes associated with Ménière's disease in patients 18 years old and above
Product Snapshot
- Betahistine is an oral small‑molecule API supplied primarily in multiple tablet and solution formats
- It is used for products targeting recurrent vertigo associated with Ménière’s disease
- It is approved in Canada, with additional investigational use in other markets
Clinical Overview
Betahistine (CAS 5638-76-6) is an aralkylamine derivative used for the reduction of recurrent vertigo episodes associated with Ménière's disease in adults. Ménière’s disease is characterized by episodic vertigo, tinnitus, and fluctuating hearing loss, arising from disturbances in inner ear fluid regulation. Although previously approved in the United States and later withdrawn due to limited evidence of efficacy, betahistine remains marketed in several regions, including Canada.
Betahistine exhibits pharmacologic actions similar to endogenous histamine. Its therapeutic effect is attributed to combined H1‑receptor agonism and H3‑receptor antagonism. Stimulation of H1 receptors within the microvasculature of the inner ear promotes vasodilation and increases capillary permeability, which is thought to support normalization of endolymphatic pressure. This action may help reduce labyrinthine distension that contributes to vertigo and auditory symptoms.
Through antagonism of presynaptic H3 receptors, betahistine increases histamine turnover and enhances release of additional neurotransmitters such as serotonin in the brainstem. These effects modulate vestibular nuclei activity and may reduce asymmetry in vestibular signaling, supporting central compensation mechanisms involved in vertigo recovery.
Absorption following oral administration is rapid, and betahistine is extensively metabolized, primarily to an inactive metabolite excreted in urine. The compound has a short plasma half‑life, and accumulation is not expected with routine dosing. Protein binding is low. No major cytochrome‑mediated interactions have been identified.
Betahistine is generally well tolerated, with gastrointestinal discomfort and headache being the most frequently reported adverse effects. Caution is advised in patients with a history of peptic ulcer disease or bronchial asthma due to its histaminergic activity. Serious toxicity is uncommon at therapeutic doses.
In global procurement, API sourcing should prioritize manufacturers with demonstrated control of impurities characteristic of aralkylamine derivatives, validated analytical methods, and compliance with regional GMP expectations to ensure consistent quality and reproducibility for finished dosage development.
Betahistine exhibits pharmacologic actions similar to endogenous histamine. Its therapeutic effect is attributed to combined H1‑receptor agonism and H3‑receptor antagonism. Stimulation of H1 receptors within the microvasculature of the inner ear promotes vasodilation and increases capillary permeability, which is thought to support normalization of endolymphatic pressure. This action may help reduce labyrinthine distension that contributes to vertigo and auditory symptoms.
Through antagonism of presynaptic H3 receptors, betahistine increases histamine turnover and enhances release of additional neurotransmitters such as serotonin in the brainstem. These effects modulate vestibular nuclei activity and may reduce asymmetry in vestibular signaling, supporting central compensation mechanisms involved in vertigo recovery.
Absorption following oral administration is rapid, and betahistine is extensively metabolized, primarily to an inactive metabolite excreted in urine. The compound has a short plasma half‑life, and accumulation is not expected with routine dosing. Protein binding is low. No major cytochrome‑mediated interactions have been identified.
Betahistine is generally well tolerated, with gastrointestinal discomfort and headache being the most frequently reported adverse effects. Caution is advised in patients with a history of peptic ulcer disease or bronchial asthma due to its histaminergic activity. Serious toxicity is uncommon at therapeutic doses.
In global procurement, API sourcing should prioritize manufacturers with demonstrated control of impurities characteristic of aralkylamine derivatives, validated analytical methods, and compliance with regional GMP expectations to ensure consistent quality and reproducibility for finished dosage development.
Identification & chemistry
| Generic name | Betahistine |
|---|---|
| Molecule type | Small molecule |
| CAS | 5638-76-6 |
| UNII | X32KK4201D |
| DrugBank ID | DB06698 |
Pharmacology
| Summary | Betahistine modulates histaminergic signaling to address vertigo associated with Ménière’s disease. It acts as an H1‑receptor agonist to enhance inner‑ear microcirculation and reduce endolymphatic pressure, and as an H3‑receptor antagonist to increase histamine and other neurotransmitter release in vestibular pathways. These combined effects help normalize vestibular nucleus activity and reduce vertigo symptoms. |
|---|---|
| Mechanism of action | Vertigo is a disturbing sensation of movement caused by dysfunction of the labyrinth (inner ear), vestibular nerve, cerebellum, brainstem, or Central Nervous System (CNS). Vestibular forms of vertigo are often accompanied by auditory dysfunctions such as hyperacusis, hearing loss, and tinnitus.In most cases, adaptive mechanisms of the CNS lead to functional recovery after episodes of vertigo, however, syndromes such as Ménière's disease tend to cause the recurrence of vertigo symptoms. This significantly impacts the quality of life and the ability to carry out daily activities. **H1-receptor activity** The mechanism of action of betahistine is multifactorial. Ménière's disease is thought to result from a disruption of endolymphatic fluid homeostasis in the ear.Betahistine mainly acts as a histamine H1-receptor agonist. The stimulation of H1-receptors in the inner ear causes a vasodilatory effect leading to increased permeability of blood vessels and a reduction in endolymphatic pressure; this action prevents the rupture of the labyrinth, which can contribute to the hearing loss associated with Ménière's disease. Betahistine is also purported to act by reducing the asymmetrical functioning of sensory vestibular organs and increasing vestibulocochlear blood flow, relieving symptoms of vertigo. **H3-receptor activity** In addition to the above mechanisms, betahistine also acts as a histamine H3-receptor antagonist, increasing the turnover of histamine from postsynaptic histaminergic nerve receptors, subsequently leading to an increase in H1-agonist activity. H3-receptor antagonism elevates levels of neurotransmitters including serotonin in the brainstem, inhibiting the activity of vestibular nuclei, thus restoring proper balance and decreasing vertigo symptoms. |
| Pharmacodynamics | Through its actions on the histamine receptors, betahistine provides relief from vertigo associated with Ménière's disease. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | agonist |
| Histamine H3 receptor | Humans | antagonist |
ADME / PK
| Absorption | When given orally, betahistine is rapidly and almost completely absorbed from the gastrointestinal tract.In the fasted state, Cmax is achieved within 1 hour of administration; in the fed state, Cmax is delayed, but the total drug absorption is similar. Food, therefore, has little effect on the absorption of betahistine. |
|---|---|
| Half-life | The half-life of betahistine is 3-4 hours. |
| Protein binding | The plasma protein binding of betahistine is reported to be less than 5%. |
| Metabolism | Betahistine is metabolized primarily into the inactive metabolite 2-pyridylacetic acid. There is both clinical and in vitro evidence that monoamine oxidase enzymes are responsible for the metabolism of betahistine. |
| Route of elimination | Betahistine is mainly excreted in the urine; with approximately 85-91% being detected in urine samples within 24 hours of administration. |
| Volume of distribution | In a pharmacokinetic study of rats, betahistine was found to be distributed throughout the body.Human data for betahistine's volume of distribution is not readily available. |
Formulation & handling
- High aqueous solubility and low logP support simple oral solid and liquid formulations without complex solubilization strategies.
- Oral-only small‑molecule API with good intrinsic dissolution; excipient selection may focus on controlling GI tolerability rather than absorption enhancement.
- Chemically stable solid; hygroscopicity is modest, so standard moisture control during processing and storage is typically sufficient.
Regulatory status
| Lifecycle | In Canada, the API’s lifecycle is largely shaped by the timing of its patent and data‑protection expiry. As these protections near or reach expiration, the market typically shifts toward a more mature phase with increasing generic participation. |
|---|
| Markets | Canada |
|---|
Supply Chain
| Supply chain summary | Betahistine was originally developed by a single originator but is now supplied predominantly by multiple generic manufacturers, as reflected by the Canadian market’s reliance on products from established generic firms. The molecule is marketed in many regions, including Europe and Canada, though it is not approved in the United States. Patent expiry occurred long ago, and widespread generic availability indicates a fully mature competitive landscape for the active ingredient. |
|---|
Safety
| Toxicity | Symptoms of an overdose with betahistine (< 640 mg) include dry mouth, nausea, dyspepsia, abdominal pain, and somnolence. Serious complications such as convulsions, pulmonary or cardiac effects may occur with higher doses (> 640 mg), especially during intentional overdoses and combination with other drugs. In the case of an overdose with betahistine, provide supportive therapy, and contact the local poison control center for further management. |
|---|
High Level Warnings:
- Overexposure to betahistine has produced dose‑dependent gastrointestinal effects such as dry mouth, nausea, dyspepsia, abdominal discomfort, and CNS depression including somnolence
- High-dose exposures (›640 mg) have been associated with serious adverse events, including convulsions and pulmonary or cardiac complications, particularly when other substances are involved
- Handling should account for its potential to elicit CNS and cardiopulmonary effects at elevated concentrations, warranting controls that limit accidental ingestion or inhalation
Betahistine is a type of Anti-vertigo agents
Anti-vertigo agents are a category of pharmaceutical active pharmaceutical ingredients (APIs) that are used to treat vertigo, a condition characterized by a sensation of dizziness, spinning, or loss of balance. These APIs are specifically designed to target the underlying causes of vertigo and provide relief to patients suffering from this debilitating condition.
The primary mechanism of action of anti-vertigo agents involves their ability to modulate the central nervous system (CNS) and peripheral vestibular system. By acting on specific receptors and neurotransmitters in the brain and inner ear, these APIs help regulate the balance and coordination signals transmitted by the vestibular system, thus reducing the symptoms of vertigo.
Some commonly used anti-vertigo APIs include meclizine, betahistine, and dimenhydrinate. Meclizine, for instance, is an antihistamine that blocks histamine receptors in the brain and effectively alleviates vertigo symptoms. Betahistine, on the other hand, acts as a histamine H1 receptor agonist and H3 receptor antagonist, improving blood flow in the inner ear and reducing the frequency and severity of vertigo episodes. Dimenhydrinate, a combination of diphenhydramine and 8-chlorotheophylline, exerts its anti-vertigo effects by blocking histamine receptors and exerting a sedative effect on the CNS.
Anti-vertigo agents are available in various formulations, including oral tablets, sublingual tablets, and transdermal patches, providing options for patients with different preferences and needs. These APIs have shown efficacy in managing vertigo and are commonly prescribed by healthcare professionals. However, it is important to note that these medications may have potential side effects, such as drowsiness, dry mouth, or gastrointestinal disturbances, which should be considered when prescribing them to patients.
In conclusion, anti-vertigo agents are a vital category of pharmaceutical APIs that play a crucial role in the management of vertigo. By targeting the underlying causes of this condition, these APIs provide symptomatic relief and improve the quality of life for individuals suffering from vertigo.
Betahistine API manufacturers & distributors
Compare qualified Betahistine API suppliers worldwide. We currently have 6 companies offering Betahistine API, with manufacturing taking place in 5 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 |
|---|---|---|---|---|---|
| Grunenthal | Producer | Germany | Germany | CEP, CoA, GMP | 1 products |
| Kanto Chemical | Producer | Japan | Japan | CoA, JDMF | 3 products |
| LEBSA | Producer | Spain | Spain | BSE/TSE, CoA, Other, EDMF/ASMF, GMP, Other, Other, ISO9001, MSDS, USDMF | 18 products |
| PharmaZell | Producer | Germany | India | CoA, FDA, GDP, GMP, MSDS, WHO-GMP | 31 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| ZCL Chemicals | Producer | India | India | CoA, Other, FDA, ISO9001, WC | 30 products |
When sending a request, specify which Betahistine 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 Betahistine 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 Betahistine API
Sourcing
What matters most when sourcing GMP-grade Betahistine?
Key considerations include securing GMP-compliant material from manufacturers with a track record of supplying Betahistine to regulated markets such as Canada. Consistent quality documentation, including evidence of regulatory inspections and validated processes, is essential given the mature, multi‑generic supply environment. It is also important to confirm that the specifications and dossier support align with Canadian regulatory expectations.
Which documents are typically required when sourcing Betahistine API?
Request the core API documentation set: CoA (6 companies), Other (4 companies), GMP (3 companies), FDA (2 companies), MSDS (2 companies). Confirm versions and validity dates match the destination market to avoid delays in qualification.
Which manufacturers are known to produce Betahistine API?
Known or reported manufacturers for Betahistine: PharmaZell. Evaluate their GMP history, scale, and regional coverage before requesting dossiers or allocating demand.
How can I request quotes for Betahistine API from GMP suppliers?
Submit quote requests through the supplier listings with your specs and required documents (specifications, target volume, delivery timeline, and destination). Providing consistent details upfront speeds comparable offers and clarifies technical feasibility.
Is a GMP audit report available for Betahistine manufacturers?
Audit reports may be requested for Betahistine: 3 GMP audit reports available. Confirm the scope and recency of any audit before relying on it for qualification decisions.
How many suppliers offer Betahistine API on Pharmaoffer?
Reported supplier count for Betahistine: 6 verified suppliers. Filter listings by certifications, regions, and delivery options to match your qualification plan.
Which countries are known to manufacture Betahistine API?
Production countries reported for Betahistine: India (2 producers), Spain (1 producer), China (1 producer). Knowing the manufacturing geography helps anticipate logistics lead times and import compliance needs.
Which certifications do suppliers of Betahistine usually hold?
Common certifications for Betahistine suppliers: CoA (6 companies), Other (4 companies), GMP (3 companies), FDA (2 companies), MSDS (2 companies). Always verify issuing authorities and expiry dates when reviewing audit packages.
Technical
What is Betahistine (CAS 5638-76-6) used for?
Betahistine is used to reduce recurrent vertigo episodes associated with Ménière’s disease in adults. It acts through H1‑receptor agonism to promote inner‑ear vasodilation and through H3‑receptor antagonism to modulate vestibular signaling. These combined effects help normalize endolymphatic pressure and support central compensation mechanisms involved in vertigo control.
Which therapeutic class does Betahistine fall into?
Betahistine belongs to the following therapeutic categories: Antivertigo Preparations, Histamine Agents, Histamine Agonists, Histamine Antagonists, Miscellaneous Central Nervous System Agents. This positioning helps teams compare alternative APIs, anticipate pharmacology expectations, and align early research priorities.
What conditions is Betahistine mainly prescribed for?
The primary indications for Betahistine: Betahistine is indicated for the reduction of recurrent vertigo episodes associated with Ménière's disease in patients 18 years old and above. These use cases frame the target patient populations and help prioritize formulation and safety evaluations.
How does Betahistine work?
Vertigo is a disturbing sensation of movement caused by dysfunction of the labyrinth (inner ear), vestibular nerve, cerebellum, brainstem, or Central Nervous System (CNS). Vestibular forms of vertigo are often accompanied by auditory dysfunctions such as hyperacusis, hearing loss, and tinnitus.In most cases, adaptive mechanisms of the CNS lead to functional recovery after episodes of vertigo, however, syndromes such as Ménière's disease tend to cause the recurrence of vertigo symptoms. This significantly impacts the quality of life and the ability to carry out daily activities.
**H1-receptor activity**
The mechanism of action of Betahistine is multifactorial. Ménière's disease is thought to result from a disruption of endolymphatic fluid homeostasis in the ear.Betahistine mainly acts as a histamine H1-receptor agonist. The stimulation of H1-receptors in the inner ear causes a vasodilatory effect leading to increased permeability of blood vessels and a reduction in endolymphatic pressure; this action prevents the rupture of the labyrinth, which can contribute to the hearing loss associated with Ménière's disease. Betahistine is also purported to act by reducing the asymmetrical functioning of sensory vestibular organs and increasing vestibulocochlear blood flow, relieving symptoms of vertigo.
**H3-receptor activity**
In addition to the above mechanisms, Betahistine also acts as a histamine H3-receptor antagonist, increasing the turnover of histamine from postsynaptic histaminergic nerve receptors, subsequently leading to an increase in H1-agonist activity. H3-receptor antagonism elevates levels of neurotransmitters including serotonin in the brainstem, inhibiting the activity of vestibular nuclei, thus restoring proper balance and decreasing vertigo symptoms.
What should someone know about the safety or toxicity profile of Betahistine?
Betahistine is generally well tolerated at therapeutic doses, with gastrointestinal discomfort and headache reported most often. Overexposure can produce dose‑dependent gastrointestinal effects and CNS depression, including somnolence, and very high doses have been associated with convulsions and cardiopulmonary complications, particularly when other substances are involved. Caution is advised in individuals with peptic ulcer disease or bronchial asthma due to its histaminergic activity. Handling and use should minimize accidental ingestion or inhalation because elevated concentrations can elicit CNS and cardiopulmonary effects.
What are important formulation and handling considerations for Betahistine as an API?
Betahistine’s high aqueous solubility and low logP allow straightforward development of oral solid or liquid dosage forms without specialized solubilization approaches. Excipient selection can focus on maintaining gastrointestinal tolerability rather than enhancing absorption, as food has minimal impact on uptake. The API is a chemically stable solid with modest hygroscopicity, so routine moisture control during processing and storage is generally adequate. Standard handling conditions are suitable, with no specialized containment indicated by the provided information.
Is Betahistine a small molecule?
Betahistine is classified as a small molecule. That classification shapes process design, impurity profiling, and analytical control strategies.
Are there special stability concerns for oral Betahistine?
Oral Betahistine is a chemically stable solid with only modest hygroscopicity, so standard moisture control during processing and storage is usually adequate. Its high aqueous solubility and low logP do not introduce special stability risks for solid or liquid formulations. No unusual degradation or handling concerns are noted beyond routine protection from excess moisture.
Regulatory
Where is Betahistine approved or in use globally?
Betahistine is reported as approved in the following major regions: Canada. Understanding geographic coverage informs regulatory filings, supply planning, and risk assessments before escalating procurement.
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Betahistine procurement?
Pharmaoffer's Smart Sourcing Service coordinates compliant suppliers, documentation, and competitive quotes for Betahistine. It centralizes outreach, follow-ups, and document validation to shorten procurement timelines.
Is Betahistine included in the PRO Data Insights coverage?
PRO Data Insights coverage for Betahistine: 1703 verified transactions across 418 suppliers and 260 buyers worldwide. Use the dataset to benchmark suppliers and monitor regulatory activity where available.
Where can I access the API market report for Betahistine?
Market report availability for Betahistine: Report Available. The report highlights demand trends, pricing drivers, and supplier landscape insights for procurement planning.
