Description
Azelastine, a phthalazine derivative, is an antihistamine and mast cell stabilizer available as a nasal spray for hay fever and as eye drops for allergic conjunctivitis. Azelastine is also available as a combination product of azelastine hydrochloride and fluticasone propionate called Dymista®. Dymista® is indicated in patient over 12 years old for symptomatic relief of seasonal allergic rhinitis.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: 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).
- Uses/Sources: For the symptomatic treatment of seasonal allergic rhinitis and non-allergic rhinitis, as well as symptomatic relief of ocular itching associated with allergic conjunctivitis.
- Route of Exposure: Absorption of azelastine following ocular administration was relatively low. Systemic bioavailability is approximately 40% after nasal administration.
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Potassium voltage-gated channel subfamily H member 2 Multidrug resistance protein 1 Alpha-1A adrenergic receptor Histamine H1 receptor Alpha-1B adrenergic receptor Cytochrome P450 2D6 Histamine H3 receptor |
2540229 17723160 19209282 11231118 9585822 22985961 8829888 10478514 11752352 21381763 |
Azelastine Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Aortic Valve Insufficiency | 10.27 |
|
Keloid | 9.93 |
|
Liver Cirrhosis, Experimental | 9.43 |
|
Left ventricular hypertrophy | 8.18 |
|
Abortion, Spontaneous | 7.65 |
|
Fibrosis | 6.88 |
|
Liver Cirrhosis | 6.81 |
|
Hypertension | 6.8 |
|
Schizophrenia | 6.76 |
|
Bethlem myopathy | 6.42 |
|
Ossification of the posterior longitudinal ligament of the spine | 6.42 |
|
Scleroatonic muscular dystrophy | 6.42 |
|
Ehlers-Danlos syndrome type 3 | 6.28 |
|
Inflammatory Bowel Disease 13 | 6.15 |
|
Ehlers-Danlos Syndrome | 6.08 |
|
Poisoning | 6.05 |
|
Ehlers-Danlos Syndrome, Type VII, Autosomal Dominant | 5.94 |
|
Hyperostosis, Cortical, Congenital | 5.94 |
|
Osteogenesis imperfecta, type 2A | 5.94 |
|
Osteogenesis imperfecta, type 3 | 5.94 |
|