Epinastine

249.31

249.31

1312995-182-4

DTXSID2048371

S01GX10|R - Respiratory system|S - Sensory organs

41.6

3.5

Solid

1.32 g/cm3

205-208 °C

428°C at 760 mmHg

212.7ºC

1.727

1.63e-01 g/L

Ⅲ

3077

9

P264, P270, P273, P301+P312, P330, P391, P501

H302

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P273, P301+P312, P330, P391, and P501|Aggregated GHS information provided by 2 companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

64%

For the prevention of itching associated with allergic conjunctivitis.|FDA Label

Epinastine is an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes. Epinastine is indicated for the prevention of itching associated with allergic conjunctivitis. Epinastine is a topically active, direct H₁-receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H₁-receptor and has affinity for the histamine H2 receptor. Epinastine also possesses affinity for the a1-, a2-, and 5-HT₂ -receptors. Epinastine does not penetrate the blood/brain barrier and, therefore, is not expected to induce side effects of the central nervous system.

Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood. (See all compounds classified as Histamine H1 Antagonists.)

The absolute bioavailability of epinastine is about 40%.|Epinastine is mainly excreted unchanged. The renal elimination is mainly via active tubular secretion.|56 L/hr [patients with allergic conjunctivitis receiving one drop of ELESTAT® ophthalmic solution in each eye twice daily for seven days]

Mainly excreted unchanged, less than 10% metabolized.

12 hours

Epinastine 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.

3-amino-9,13b-dihydro-1H-benz(c,f)imidazo(1,5a)azepine

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients