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Azelastine | CAS No: 58581-89-8 | GMP-certified suppliers
A medication that provides symptomatic relief for seasonal allergic rhinitis, vasomotor rhinitis, and allergic conjunctivitis, supporting reliable development of intranasal and ophthalmic allergy therapies.
Therapeutic categories
Anti-Allergic AgentsAntiallergic Agents, Excl. CorticosteroidsAntihistamines for Systemic UseAutonomic AgentsCentral Nervous System DepressantsCytochrome P-450 CYP1A2 Substrates
Generic name
Azelastine
Molecule type
small molecule
CAS number
58581-89-8
DrugBank ID
DB00972
Approval status
Approved drug
ATC code
R06AX19
Primary indications
- Intranasal azelastine is indicated for the symptomatic treatment of seasonal allergic rhinitis in patients 5 years and older and for the symptomatic treatment of vasomotor rhinitis in patients 12 years and older
- Ophthalmic azelastine solution is indicated for the treatment of itchy eyes associated with allergic conjunctivitis
- As a 0
Product Snapshot
- Azelastine is supplied as an intranasal and ophthalmic solution/spray, with additional oral solid forms available for development needs
- It is used for allergic rhinitis, vasomotor rhinitis, and allergic conjunctivitis
- It is approved in the US and Canada for both prescription and OTC allergy indications
Clinical Overview
Azelastine (CAS 58581-89-8) is a phthalazinone antihistamine used primarily in intranasal and ophthalmic formulations for the symptomatic management of allergic disease. Intranasal products are indicated for seasonal allergic rhinitis in patients five years and older and for vasomotor rhinitis in patients twelve years and older. Ophthalmic solutions are used to treat itchy eyes associated with allergic conjunctivitis. A 0.15 percent intranasal formulation is available over the counter for individuals six years and older. Combination therapy with fluticasone propionate is available in some markets for seasonal allergic rhinitis.
Azelastine is a selective antagonist of histamine H1 receptors with modest affinity for H2 receptors. Antagonism of H1 receptors on sensory nerves, smooth muscle, and glandular tissue reduces histamine-mediated symptoms such as itching, sneezing, and rhinorrhea. Additional anti‑inflammatory activity includes mast cell stabilization with reduced release of histamine, tryptase, interleukin‑6, and TNF‑alpha. Studies also demonstrate attenuation of leukotriene production and reduced concentrations of neuropeptides such as substance P and bradykinin in nasal secretions.
Intranasal onset occurs within approximately 15 minutes, while ophthalmic solutions can act within several minutes. Intranasal effects peak at 4 to 6 hours and are maintained through a typical 12‑hour dosing interval. Systemic absorption following local administration is limited but measurable. Oral bioavailability is moderate. Azelastine undergoes hepatic metabolism, including N‑demethylation to the active metabolite desmethylazelastine. Elimination occurs via renal and biliary pathways, and the terminal half‑life is prolonged relative to the dosing interval.
Safety considerations include bitter taste, local irritation, somnolence, and, rarely, epistaxis or ocular discomfort. Systemic adverse effects are uncommon at therapeutic intranasal and ophthalmic doses. As azelastine can interact with multiple cytochrome P450 pathways, clinically relevant interactions are possible with orally administered formulations, though not typically observed with topical use.
For API procurement, consistent enantiomeric composition, control of related phthalazinone impurities, and adherence to pharmacopeial specifications are key quality considerations to support global formulation and regulatory requirements.
Azelastine is a selective antagonist of histamine H1 receptors with modest affinity for H2 receptors. Antagonism of H1 receptors on sensory nerves, smooth muscle, and glandular tissue reduces histamine-mediated symptoms such as itching, sneezing, and rhinorrhea. Additional anti‑inflammatory activity includes mast cell stabilization with reduced release of histamine, tryptase, interleukin‑6, and TNF‑alpha. Studies also demonstrate attenuation of leukotriene production and reduced concentrations of neuropeptides such as substance P and bradykinin in nasal secretions.
Intranasal onset occurs within approximately 15 minutes, while ophthalmic solutions can act within several minutes. Intranasal effects peak at 4 to 6 hours and are maintained through a typical 12‑hour dosing interval. Systemic absorption following local administration is limited but measurable. Oral bioavailability is moderate. Azelastine undergoes hepatic metabolism, including N‑demethylation to the active metabolite desmethylazelastine. Elimination occurs via renal and biliary pathways, and the terminal half‑life is prolonged relative to the dosing interval.
Safety considerations include bitter taste, local irritation, somnolence, and, rarely, epistaxis or ocular discomfort. Systemic adverse effects are uncommon at therapeutic intranasal and ophthalmic doses. As azelastine can interact with multiple cytochrome P450 pathways, clinically relevant interactions are possible with orally administered formulations, though not typically observed with topical use.
For API procurement, consistent enantiomeric composition, control of related phthalazinone impurities, and adherence to pharmacopeial specifications are key quality considerations to support global formulation and regulatory requirements.
Identification & chemistry
| Generic name | Azelastine |
|---|---|
| Molecule type | Small molecule |
| CAS | 58581-89-8 |
| UNII | ZQI909440X |
| DrugBank ID | DB00972 |
Pharmacology
| Summary | Azelastine is a selective histamine H1‑receptor antagonist that reduces histamine‑mediated allergic symptoms, with minor activity at H2 receptors. It also stabilizes mast cells and suppresses additional inflammatory mediators, including leukotrienes, substance P, and bradykinin. These combined actions attenuate the neurogenic and inflammatory pathways that drive rhinitis and allergic conjunctivitis. |
|---|---|
| Mechanism of action | Azelastine is primarily a selective antagonist of histamine H1-receptors, with a lesser affinity for H2-receptors, used for the symptomatic treatment of allergies.Histamine H1-receptors are G-protein-coupled receptors with 7 transmembrane spanning domainsthat are found on nerve endings, smooth muscle cells, and glandular cells.Following allergen exposure in sensitized individuals, IgE-receptor cross-linking on mast cells results in the release of histamine, which binds to H1-receptors and contributes to typical allergic symptoms such as itching, sneezing, and congestion. Though its primary mode of action is thought to be via H1-receptor antagonism, azelastine (like other second-generation antihistamines) appears to affect other mediators of allergic symptomatology. Azelastine has mast cell-stabilizing properties that prevent the release of interleukin-6, tryptase, histamine, and TNF-alphafrom mast cells, and has been shown to reduce mediators of mast cell degranulation such as leukotrienes in the nasal lavage of patients with rhinitis,as well as inhibiting their production and release from eosinophils (potentially via inhibition of phospholipase A<sub>2</sub> and leukotriene C<sub>4</sub> synthase).Additionally, patients using oral azelastine were observed to have significantly reduced concentrations of substance P and bradykinin in nasal secretions, both of which may play a role in nasal itching and sneezing in patients with allergic rhinitis. |
| Pharmacodynamics | Azelastine antagonizes the actions of histamine, resulting in the relief of histamine-mediated allergy symptoms.Onset of action occurs within 15 minutes with intranasal formulations and as quickly as 3 minutes with ophthalmic solutions.Intranasal formulations have a relatively long-duration of action, with peak effects observed 4-6 hours after the initial dose and efficacy maintained over the entirety of the standard 12 hour dosing interval. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
| Histamine H2 receptor | Humans | inhibitor |
| Phospholipase A2 | Humans | inhibitor |
ADME / PK
| Absorption | Systemic bioavailability of azelastine hydrochloride following intranasal administration is approximately 40%, reaching Cmax within 2-3 hours.When administered at doses greater than the recommended maximum, greater than proportional increases in both Cmax and AUC were observed. |
|---|---|
| Half-life | Based on intravenous and oral administration, azelastine demonstrated an elimination half-life of 22 hours.Its primary active metabolite, desmethylazelastine, has an elimination half-life of 54 hours. |
| Protein binding | In-vitro studies in human plasma indicate that the plasma protein binding of azelastine and desmethylazelastine are approximately 88% and 97%, respectively. |
| Metabolism | Azelastine hydrochloride is oxidatively metabolized to its main, and biologically active, metabolite desmethylazelastine by the cytochrome P450 enzyme system.Though labels for azelastine state that specific CYP enzyme involvement has not been elucidated, it has been suggested that the N-demethylation of azelastine is primarily catalyzed by CYP3A4, CYP2D6, and CYP1A2. |
| Route of elimination | After an oral dose of radio-labeled azelastine hydrochloride, approximately 75% was excreted in the feces, with less than 10% as unchanged azelastine hydrochloride. |
| Volume of distribution | After intravenous and oral administration, the steady-state volume of distribution is 14.5 L/kg. |
| Clearance | Based on intravenous and oral administration, azelastine demonstrated a plasma clearance of 0.5 L/h/kg. |
Formulation & handling
- Low aqueous solubility and moderate lipophilicity support use in nasal and ophthalmic solutions/suspensions with solubilizers or viscosity enhancers to maintain uniformity and residence time.
- Oral tablet formulations may require dissolution-enhancing strategies due to poor water solubility but have no specific food‑related absorption constraints beyond CNS depression with alcohol.
- Solid API is chemically stable and suitable for standard handling; solution formulations generally require pH control and antimicrobial preservation for multi‑dose nasal and ocular products.
Regulatory status
| Lifecycle | Most U.S. patents covering the API have already expired, with the remaining protection ending between late 2024 and mid‑2028, indicating a transition toward later‑stage lifecycle status. With commercialization in the United States and Canada, the product is positioned in a mature North American market where generic entry is expected to increase as remaining patents expire. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Azelastine’s supply chain includes multiple manufacturers and packagers, with the originator products historically associated with Meda and widely distributed in the US and Canada under brands such as Astelin and Astepro. The presence of several other manufacturers indicates an established generic market, especially as key patents have already expired or will expire in the near term. Remaining later‑dated US patents suggest continued protection for certain formulations, but overall conditions support ongoing or increasing generic competition. |
|---|
Safety
| Toxicity | Overdosage of intranasal or ophthalmic azelastine is unlikely to result in clinically significant adverse effects aside from increased drowsiness.If overdose does occur, employ general supportive measures. Oral ingestion of antihistamines, including non-oral formulations of azelastine, can cause serious adverse effects in children - for this reason, these products should be kept out of the reach of children. The oral LD<sub>50</sub> in rats is 580 mg/kg. |
|---|
High Level Warnings:
- Excess exposure may increase CNS depressive effects
- Drowsiness is the primary manifestation reported in non‑clinical overdose settings
- Oral ingestion presents higher systemic risk, particularly in juvenile models, with a reported rat oral LD50 of approximately 580 mg/kg
Azelastine is a type of Anti-allergy agents
Anti-allergy agents, also known as antihistamines, are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of allergies. These substances work by blocking the effects of histamine, a chemical released by the body's immune system during an allergic reaction.
Antihistamines act on histamine receptors, preventing them from binding to target cells and thus inhibiting the release of allergic symptoms such as itching, sneezing, and watery eyes. These APIs can be classified into two generations based on their characteristics.
First-generation antihistamines, such as diphenhydramine and chlorpheniramine, are known for their sedative properties due to their ability to cross the blood-brain barrier. Although effective in relieving allergy symptoms, they often cause drowsiness, impairing daily activities.
Second-generation antihistamines, including cetirizine and loratadine, were developed to address the sedative side effects of their predecessors. These newer APIs have a higher selectivity for peripheral histamine receptors and a reduced ability to penetrate the central nervous system, resulting in reduced sedation.
Anti-allergy APIs are available in various formulations, including oral tablets, liquids, nasal sprays, and eye drops. They are widely used to alleviate allergic reactions caused by pollen, dust mites, pet dander, and other environmental allergens. These agents provide relief from symptoms such as itching, runny nose, congestion, and hives.
In summary, anti-allergy agents are a vital category of APIs used to manage allergic reactions. They block the effects of histamine, providing relief from allergy symptoms. The development of second-generation antihistamines has significantly reduced sedative side effects, improving patient comfort. These APIs are available in different formulations, catering to the diverse needs of allergy sufferers.
Azelastine API manufacturers & distributors
Compare qualified Azelastine API suppliers worldwide. We currently have 9 companies offering Azelastine 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 |
|---|---|---|---|---|---|
| Cipla | Producer | India | India | CoA, GMP, WC | 164 products |
| Coral Drugs | Producer | India | India | BSE/TSE, CEP, CoA, FDA, GMP, ISO9001, USDMF, WC, WHO-GMP | 25 products |
| Curia | Producer | United States | Italy | CoA, EDMF/ASMF, GMP, MSDS, USDMF | 106 products |
| Euticals | Producer | Italy | Unknown | CoA, USDMF | 48 products |
| Evonik TC | Producer | Germany | Germany | CEP, CoA, FDA, GMP, KDMF | 7 products |
| Gedeon Richter | Producer | Hungary | Hungary | CoA, USDMF | 48 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| MSN Labs. | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 119 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
When sending a request, specify which Azelastine 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 Azelastine 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 Azelastine API
Sourcing
What matters most when sourcing GMP-grade Azelastine?
Key considerations include confirming GMP compliance and ensuring the material meets US and Canadian regulatory requirements. Verifying the manufacturer’s authorization, quality documentation, and batch traceability is essential given the multi‑source supply chain. It is also important to account for the established generic market and any remaining formulation‑specific patent protections that may affect availability.
Which documents are typically required when sourcing Azelastine API?
Request the core API documentation set: CoA (9 companies), GMP (7 companies), USDMF (5 companies), FDA (5 companies), WC (3 companies). Confirm versions and validity dates match the destination market to avoid delays in qualification.
Which manufacturers are known to produce Azelastine API?
Known or reported manufacturers for Azelastine: Global Pharma Tek, Coral Drugs, Tenatra Exports Private Limited. Evaluate their GMP history, scale, and regional coverage before requesting dossiers or allocating demand.
How can I request quotes for Azelastine 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 Azelastine manufacturers?
Audit reports may be requested for Azelastine: 3 GMP audit reports available. Confirm the scope and recency of any audit before relying on it for qualification decisions.
How many suppliers offer Azelastine API on Pharmaoffer?
Reported supplier count for Azelastine: 9 verified suppliers. Filter listings by certifications, regions, and delivery options to match your qualification plan.
Which countries are known to manufacture Azelastine API?
Production countries reported for Azelastine: India (5 producers), Italy (1 producer), Germany (1 producer). Knowing the manufacturing geography helps anticipate logistics lead times and import compliance needs.
Which certifications do suppliers of Azelastine usually hold?
Common certifications for Azelastine suppliers: CoA (9 companies), GMP (7 companies), USDMF (5 companies), FDA (5 companies), WC (3 companies). Always verify issuing authorities and expiry dates when reviewing audit packages.
Technical
What is Azelastine (CAS 58581-89-8) used for?
Azelastine is used for symptomatic relief of allergic rhinitis and allergic conjunctivitis. Intranasal formulations treat seasonal allergic rhinitis in patients five years and older and vasomotor rhinitis in patients twelve years and older. Ophthalmic solutions are used to relieve itchy eyes associated with allergic conjunctivitis. A combination intranasal product with fluticasone propionate is also available for seasonal allergic rhinitis in some markets.
Which therapeutic class does Azelastine fall into?
Azelastine belongs to the following therapeutic categories: Anti-Allergic Agents, Antiallergic Agents, Excl. Corticosteroids, Antihistamines for Systemic Use, Autonomic Agents, Central Nervous System Depressants. This positioning helps teams compare alternative APIs, anticipate pharmacology expectations, and align early research priorities.
What conditions is Azelastine mainly prescribed for?
The primary indications for Azelastine: Intranasal Azelastine is indicated for the symptomatic treatment of seasonal allergic rhinitis in patients 5 years and older and for the symptomatic treatment of vasomotor rhinitis in patients 12 years and older, Ophthalmic Azelastine solution is indicated for the treatment of itchy eyes associated with allergic conjunctivitis, As a 0. These use cases frame the target patient populations and help prioritize formulation and safety evaluations.
How does Azelastine work?
Azelastine is primarily a selective antagonist of histamine H1-receptors, with a lesser affinity for H2-receptors, used for the symptomatic treatment of allergies.Histamine H1-receptors are G-protein-coupled receptors with 7 transmembrane spanning domainsthat are found on nerve endings, smooth muscle cells, and glandular cells.Following allergen exposure in sensitized individuals, IgE-receptor cross-linking on mast cells results in the release of histamine, which binds to H1-receptors and contributes to typical allergic symptoms such as itching, sneezing, and congestion.
Though its primary mode of action is thought to be via H1-receptor antagonism, Azelastine (like other second-generation antihistamines) appears to affect other mediators of allergic symptomatology. Azelastine has mast cell-stabilizing properties that prevent the release of interleukin-6, tryptase, histamine, and TNF-alphafrom mast cells, and has been shown to reduce mediators of mast cell degranulation such as leukotrienes in the nasal lavage of patients with rhinitis,as well as inhibiting their production and release from eosinophils (potentially via inhibition of phospholipase A2 and leukotriene C4 synthase).Additionally, patients using oral Azelastine were observed to have significantly reduced concentrations of substance P and bradykinin in nasal secretions, both of which may play a role in nasal itching and sneezing in patients with allergic rhinitis.
What should someone know about the safety or toxicity profile of Azelastine?
Azelastine has a generally favorable safety profile when used intranasally or ophthalmically, with most adverse effects limited to bitter taste, local irritation, and occasional somnolence. Excess exposure can increase central nervous system depressive effects, and drowsiness is the primary manifestation noted in non‑clinical overdose settings. Oral ingestion carries higher systemic risk, reflected by a rat oral LD50 of about 580 mg/kg. Systemic adverse effects and drug interactions are uncommon at therapeutic topical doses.
What are important formulation and handling considerations for Azelastine as an API?
Important considerations include managing its low aqueous solubility, which may require solubilizers or dissolution‑enhancing approaches in oral, nasal, or ophthalmic formulations. Nasal and ophthalmic solutions or suspensions typically need pH control and appropriate preservatives for multi‑dose use, as well as viscosity enhancers to support uniformity and residence time. The solid API is chemically stable and can be handled with standard procedures.
Is Azelastine a small molecule?
Azelastine is classified as a small molecule. That classification shapes process design, impurity profiling, and analytical control strategies.
Are there special stability concerns for oral Azelastine?
Oral Azelastine has no unusual stability concerns beyond those related to its poor aqueous solubility. Tablets may require dissolution‑enhancing strategies to ensure adequate release. The API itself is chemically stable in solid form, and no special food‑related or storage‑related stability issues are noted for oral use.
Regulatory
Where is Azelastine approved or in use globally?
Azelastine is reported as approved in the following major regions: Canada, US. Understanding geographic coverage informs regulatory filings, supply planning, and risk assessments before escalating procurement.
What’s the regulatory and patent landscape for Azelastine right now?
Azelastine is regulated for use in both Canada and the United States. Patent considerations are jurisdiction‑specific and generally focus on particular formulations, delivery systems, or manufacturing processes rather than the underlying active ingredient.
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Azelastine procurement?
Pharmaoffer's Smart Sourcing Service coordinates compliant suppliers, documentation, and competitive quotes for Azelastine. It centralizes outreach, follow-ups, and document validation to shorten procurement timelines.
Is Azelastine included in the PRO Data Insights coverage?
PRO Data Insights coverage for Azelastine: 766 verified transactions across 252 suppliers and 111 buyers worldwide. Use the dataset to benchmark suppliers and monitor regulatory activity where available.
Where can I access the API market report for Azelastine?
Market report availability for Azelastine: Report Available. The report highlights demand trends, pricing drivers, and supplier landscape insights for procurement planning.
