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FDA : Cµî±Þ
(epinastine; )
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Mechanism of Action
Epinastine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
Pharmacology
Epinastine¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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.
Protein Binding
Epinastine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 64%
Half-life
Epinastine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 12 hours
Absorption
Epinastine¿¡ ´ëÇÑ Absorption Á¤º¸ The absolute bioavailability of epinastine is about 40%.
Pharmacokinetics
Epinastine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
Èí¼öÀ² : ¾à 40%
»ýü³»ÀÌ¿ë·ü : ¾à 39%
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Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 1.9 ½Ã°£
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Biotransformation
Epinastine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Mainly excreted unchanged, less than 10% metabolized.
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸]
Drug Target
[Drug Target]
Description
Epinastine¿¡ ´ëÇÑ Description Á¤º¸ Epinastine is used for the prevention of itching associated with allergic conjunctivitis. It has a multi-action 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 Form
Epinastine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Solution / drops Ophthalmic
Drug Category
Epinastine¿¡ ´ëÇÑ Drug_Category Á¤º¸ AntihistaminesHistamine H1 AntagonistsOphthalmics
Smiles String Canonical
Epinastine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ NC1=NCC2N1C1=CC=CC=C1CC1=CC=CC=C21
Smiles String Isomeric
Epinastine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ NC1=NC[C@H]2[N@]1C1=CC=CC=C1CC1=CC=CC=C21
InChI Identifier
Epinastine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C16H15N3/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16/h1-8,15H,9-10H2,(H2,17,18)/f/h17H2
Chemical IUPAC Name
Epinastine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ Not Available
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