Azusaleon 1%
Azusaleon 1% Uses, Dosage, Side Effects, Food Interaction and all others data.
Azusaleon 1% is a topically active antihistamine that antagonizes both histamine H1 and H2 receptors. Moreover, it has mast cell stabilizing activity and prevents the release of inflammatory mediators from blood vessel. Azusaleon 1% does not penetrate the blood-brain barrier and therefore is not expected to induce side effects of the central nervous system.
Azusaleon 1% is an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes. Azusaleon 1% is indicated for the prevention of itching associated with allergic conjunctivitis. Azusaleon 1% is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell. Azusaleon 1% is selective for the histamine H1-receptor and has affinity for the histamine H2 receptor. Azusaleon 1% also possesses affinity for the a1-, a2-, and 5-HT2 -receptors. Azusaleon 1% does not penetrate the blood/brain barrier and, therefore, is not expected to induce side effects of the central nervous system.
| Trade Name | Azusaleon 1% |
| Availability | Prescription only |
| Generic | Epinastine |
| Epinastine Other Names | Epinastin, Epinastina, Epinastine, épinastine, Epinastinum |
| Related Drugs | prednisone, cetirizine ophthalmic, dexamethasone ophthalmic, prednisolone ophthalmic, azelastine ophthalmic, doxylamine |
| Type | |
| Formula | C16H15N3 |
| Weight | Average: 249.3104 Monoisotopic: 249.126597495 |
| Protein binding | 64% |
| Groups | Approved, Investigational |
| Therapeutic Class | Ophthalmic Non-Steroid drugs |
| Manufacturer | |
| Available Country | Japan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Azusaleon 1% ophthalmic solution is used for the prevention of itching associated with allergic conjunctivitis.
Azusaleon 1% is also used to associated treatment for these conditions: Seasonal Allergic Conjunctivitis
How Azusaleon 1% works
Azusaleon 1% has a multiaction effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.
Dosage
Azusaleon 1% dosage
The recommended dosage is one drop in each eye twice a day. Treatment should be continued throughout the period of exposure (i.e., until the pollen season is over or until exposure to the offending allergen is terminated), even when symptoms are absent.
Side Effects
Most frequently reported side effects are mild burning sensation, folliculosis, hyperemia, pruritus, cold symptoms and upper respiratory infections.
Precaution
For ophthalmic use only, Patients should be advised not to wear contact lenses if their eye is red.
Food Interaction
No interactions found.Elimination Route
The absolute bioavailability of epinastine is about 40%.
Half Life
12 hours
Clearance
- 56 L/hr [patients with allergic conjunctivitis receiving one drop of ELESTAT® ophthalmic solution in each eye twice daily for seven days]
Elimination Route
Azusaleon 1% is mainly excreted unchanged. The renal elimination is mainly via active tubular secretion.
Pregnancy & Breastfeeding use
Use in pregnancy: There are no adequate and well-controlled studies in pregnant women. Azusaleon 1% should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Use in lactation: It is not known whether Azusaleon 1% is excreted in human milk. Caution should be exercised when Azusaleon 1% is administered to a nursing mother.
Contraindication
Contraindicated in patients who are hypersensitive to Azusaleon 1% or to any of the components of Azusaleon 1% Hydrochloride.
Special Warning
Pediatric Use: Safety and effectiveness in pediatric patients below the age of 3 years have not been established.
Geriatric Use: No overall differences in safety or effectiveness have been observed between elderly and younger patients.
Storage Condition
Store in a cool and dry place, away from light. Keep out of reach of children.
Innovators Monograph
You find simplified version here Azusaleon 1%
Azusaleon 1% contains Epinastine see full prescribing information from innovator Azusaleon 1% Monograph, Azusaleon 1% MSDS, Azusaleon 1% FDA label
