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Cinnarizine | CAS No: 298-57-7 | GMP-certified suppliers
A medication that supports management of vertigo, Ménière’s disease, motion sickness, and related nausea by alleviating diverse vestibular symptoms across various clinical settings.
Therapeutic categories
Primary indications
- For the treatment of vertigo/meniere's disease, nausea and vomiting, motion sickness and also useful for vestibular symptoms of other origins
Product Snapshot
- Oral small‑molecule formulations available as tablets, capsules, and liquid preparations
- Used for vertigo and Ménière‑type vestibular disorders, motion sickness, and related nausea
- Marketed in multiple regions with established approvals and considered investigational in some jurisdictions
Clinical Overview
The pharmacological profile combines H1 receptor antagonism, muscarinic receptor blockade, and inhibition of L‑type and T‑type voltage‑gated calcium channels. These actions reduce excitability within the vestibular nuclei and attenuate signal transmission from the inner ear to central emetic pathways. The calcium channel–blocking activity also produces vasorelaxant effects in cerebral vasculature, which has contributed to its historical use in combination with other agents in certain neurological contexts.
The mechanism of action involves suppression of calcium‑dependent contraction in vascular smooth muscle and modulation of neurotransmission via interactions with histamine H1, muscarinic acetylcholine, and dopamine D2 receptors. These combined effects help stabilize vestibular input and diminish motion‑induced symptoms. Cinnarizine is a substrate of multiple CYP450 isoenzymes, including CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2D6, and CYP3A4, indicating potential susceptibility to metabolic interactions, although specific kinetic parameters vary by population and formulation.
Safety considerations include dose‑dependent sedation, potential anticholinergic effects, and the risk of exacerbating movement disorders in susceptible individuals due to dopaminergic receptor interactions. Cinnarizine has been associated with QTc prolongation, and concomitant use with other QT‑prolonging agents warrants caution. Long‑term use should be evaluated carefully in older adults due to possible cumulative neurological effects.
Cinnarizine is marketed in several regions under names such as Stugeron, though availability varies internationally. For API procurement, manufacturers should verify compliance with regional pharmacopeial specifications, ensure complete impurity profiling, and confirm reliable control of polymorphic form and particle size distribution when relevant to the intended dosage form.
Identification & chemistry
| Generic name | Cinnarizine |
|---|---|
| Molecule type | Small molecule |
| CAS | 298-57-7 |
| UNII | 3DI2E1X18L |
| DrugBank ID | DB00568 |
Pharmacology
| Summary | Cinnarizine acts as an H1‑receptor antagonist and a blocker of L‑ and T‑type voltage‑gated calcium channels, reducing excitability in vascular and vestibular smooth muscle. It also interacts with muscarinic and dopamine D2 receptors, contributing to its effects on vestibular signaling and nausea pathways. The combined antihistaminic and calcium channel–blocking actions underpin its use in conditions involving disordered balance and motion‑related symptoms. |
|---|---|
| Mechanism of action | Cinnarizine inhibits contractions of vascular smooth muscle cells by blocking L-type and T-type voltage gated calcium channels. Cinnarizine has also been implicated in binding to dopamine D2 receptors, histamine H1 receptors, and muscarinic acetylcholine receptors. |
| Pharmacodynamics | Cinnarizine is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities such as contraction of smooth muscle of the airways and gastrointestinal tract, vasodilatation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release and chemotaxis of eosinophils and mast cells. Competitive antagonists at histamine H1 receptors may be divided into first (sedating) and second (non-sedating) generation agents. Some, such as Cinnarizine also block muscarinic acetylcholine receptors and are used as anti-emetic agents. Cinnarizine through its calcium channel blocking ability also inhibits stimulation of the vestibular system. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
| Voltage-dependent L-type calcium channel subunit alpha-1C | Humans | inhibitor |
| Voltage-dependent L-type calcium channel subunit alpha-1D | Humans | inhibitor |
Formulation & handling
- High logP and low aqueous solubility require solubility‑enhancing strategies for oral formulations (e.g., lipid vehicles or solid dispersion approaches).
- As a lipophilic small molecule, it is typically formulated as tablets, capsules, or oral liquids, with attention to dissolution performance to ensure consistent absorption.
- Light and oxidation sensitivity reported for cinnarizine necessitate protection from light and use of stabilizing excipients during manufacturing and storage.
Regulatory status
Cinnarizine 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.
Cinnarizine API manufacturers & distributors
Compare qualified Cinnarizine API suppliers worldwide. We currently have 9 companies offering Cinnarizine 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 |
|---|---|---|---|---|---|
| Fleming Labs. | Producer | India | India | CEP, CoA, FDA, GMP, WC | 8 products |
| Gedeon Richter | Producer | Hungary | Hungary | CoA, GMP | 48 products |
| Hikal | Producer | India | India | CEP, CoA, FDA, GMP | 26 products |
| Indukern Chemie AG | Distributor | Switzerland | Unknown | CoA | 13 products |
| Janssen Pharma | Producer | Belgium | Unknown | CEP, CoA, GMP | 63 products |
| Kleem Pharmaceuticals | Producer | India | India | CoA | 22 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Unnati Pharmaceuticals Pv... | Distributor | India | India | CoA | 70 products |
| Vasudha Pharma Chem Ltd. | Producer | India | India | CEP, CoA, GMP, MSDS, USDMF, WC | 37 products |
When sending a request, specify which Cinnarizine 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 Cinnarizine 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 Cinnarizine API
Sourcing
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Technical
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