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Namespace Prefixes

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Statements

Subject Item
n2:DB00751
rdf:type
n3:Drug
n3:description
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.
n3:dosage
n17:271B57D4-363D-11E5-9242-09173F13E4C5 n17:271B57D5-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Walther G, Daniel H, Bechtel WD, Brandt K: New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine. Arzneimittelforschung. 1990 Apr;40(4):440-6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/1972625 # Schilling JC, Adamus WS, Kuthan H: Antihistaminic activity and side effect profile of epinastine and terfenadine in healthy volunteers. Int J Clin Pharmacol Ther Toxicol. 1990 Dec;28(12):493-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/1982280
n3:group
investigational approved
n3:halfLife
12 hours
n3:indication
For the prevention of itching associated with allergic conjunctivitis.
n3:manufacturer
n7:271B57D1-363D-11E5-9242-09173F13E4C5
owl:sameAs
n16:DB00751 n29:DB00751
dcterms:title
Epinastine
adms:identifier
n9:PA164764489 n10:Epinastine n19:3128 n20:DB00751 n21:51032 n22:3241 n24:D01713 n25:0023-9201-05 n26:46509056
n3:mechanismOfAction
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 H<sub>2</sub>-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.
n3:packager
n7:271B57D0-363D-11E5-9242-09173F13E4C5
n3:patent
n30:7429602
n3:routeOfElimination
Epinastine is mainly excreted unchanged. The renal elimination is mainly via active tubular secretion.
n3:synonym
Epinastin Epinastinum Epinastina (+-)-Epinastine Epinastine 3-amino-9,13b-dihydro-1H-Dibenz(c,F)imidazo(1,5-a)azepine
n3:proteinBinding
64%
n3:salt
n3:synthesisReference
Akiharu Isowaki, Tomoko Nakajima, Akira Ohtori, "Percutaneously Absorptive Ophthalmic Preparation Comprising Epinastine." U.S. Patent US20090143359, issued June 04, 2009.
n5:hasConcept
n6:M0150487
foaf:page
n12:epinastine.html n27:elestat.htm n28:ele1680.shtml
n3:IUPAC-Name
n4:271B57DA-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B57E0-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B57DF-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B57DC-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B57DD-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B57DE-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B57D8-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B57F0-363D-11E5-9242-09173F13E4C5 n4:271B57D9-363D-11E5-9242-09173F13E4C5 n4:271B57D6-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B57D7-363D-11E5-9242-09173F13E4C5
n13:hasATCCode
n14:R06AX24 n14:S01GX10
n3:H-Bond-Acceptor-Count
n4:271B57E6-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B57E7-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B57E1-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B57E2-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B57E4-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B57E3-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B57E5-363D-11E5-9242-09173F13E4C5
n3:absorption
The absolute bioavailability of epinastine is about 40%.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
80012-43-7
n3:category
n3:clearance
* 56 L/hr [patients with allergic conjunctivitis receiving one drop of ELESTAT® ophthalmic solution in each eye twice daily for seven days]
n3:containedIn
n18:271B57D2-363D-11E5-9242-09173F13E4C5 n18:271B57D3-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n4:271B57EB-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B57ED-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B57EE-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B57EF-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B57EA-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B57E9-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B57EC-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B57DB-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B57E8-363D-11E5-9242-09173F13E4C5