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PubChem
| Name: | azelastine |
|---|---|
| PubChem Compound ID: | 2267 |
| Molecular formula: | C22H24ClN3O |
| Molecular weight: | 381.898 g/mol |
| Synonyms: |
37932-96-0; 4-((4-Chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone hydrochloride; Spectrum2_000649; 79307-93-0; BRN 0900747; Spectrum3_001984; Azelastina [INN-Spanish]; KBio3_002992; Azelastine; 4-(p-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)-phthalazinone.
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DrugBank
Identification
| Name: | azelastine |
|---|---|
| Name (isomeric): | DB00972 |
| Drug Type: | small molecule |
| Synonyms: |
Azelastine Hydrochloride; Azelastina [INN-Spanish]; Azelastinum [INN-Latin]
|
| Brand: | Optivar, Astelin |
| Category: | Histamine H1 Antagonists, Platelet Aggregation Inhibitors, Anti-Allergic Agents, Histamine H1 Antagonists, Non-Sedating, Bronchodilator Agents, Lipoxygenase Inhibitors |
| CAS number: | 58581-89-8 |
Pharmacology
| Indication: | For the symptomatic treatment of seasonal allergic rhinitis and non-allergic rhinitis, as well as symptomatic relief of ocular itching associated with allergic conjunctivitis. |
|---|---|
| Pharmacology: |
Azelastine is a relatively selective histamine H1 antagonist, which inhibits the release of histamine and other mediators from cells (e.g. mast cells) involved in the allergic response. It has some affinity to H2 receptors. Based on in vitro studies using human cell lines, inhibition of other mediators involved in allergic reactions (e.g. leukotrie...
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| Mechanism of Action: | Azelastine competes with histamine for the H1-receptor sites on effector cells and acts as an antagonist by inhibiting the release of histamine and other mediators involved in the allergic response. |
| Absorption: | Absorption of azelastine following ocular administration was relatively low. Systemic bioavailability is approximately 40% after nasal administration. |
| Protein binding: | In-vitro studies in human plasma indicate that the plasma protein binding of azelastine and N-desmethylazelastine are approximately 88% and 97%, respectively. |
| Biotransformation: | Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system, however the exact cytochrome P450 isoenzyme involved has not been determined. The major metabolite, desmethylazelastine, also has H1-receptor antagonist activity. |
| Route of elimination: | Approximately 75% of an oral dose of radiolabeled azelastine hydrochloride was excreted in the feces with less than 10% as unchanged azelastine. Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system. |
| Half Life: | Elimination half-life (based on intravenous and oral administration) is 22 hours. Elimination half-life of the active metabolite, desmethylazelastine, is 54 hours (after oral administration of azelastine). |
| Clearance: | 0.5 L/h/kg [symptomatic patients] |
| Affected organisms: | Humans and other mammals |
Interactions
| Drug interaction: |
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Targets
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