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Emedastine

Catalog No. DB01084 Name DrugBank
CAS Number 87233-61-2 Website http://www.ualberta.ca/
M. F. C17H26N4O Telephone (780) 492-3111
M. W. 302.41454 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 955

SYNONYMS

IUPAC name
1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-1,3-benzodiazole
IUPAC Traditional name
emedastine
Brand Name
Emadine
Synonyms
Emedastinum [INN-Latin]
Emedastina [INN-Spanish]
Emedastine difumarate

DATABASE IDS

PubChem SID 46505109
PubChem CID 3219
CAS Number 87233-61-2

PROPERTIES

Hydrophobicity(logP) 2.6
Solubility Soluble (difumarate formulation)

DETAILS

Description (English)
Item Information
Drug Groups approved
Description Emedastine is an antihistamine used in eye drops to treat allergic conjunctivitis. [Wikipedia]
Indication For the temporary relief of the signs and symptoms of allergic conjunctivitis.
Pharmacology Emedastine is a relatively selective H1-receptor antagonist.
Toxicity Somnolence and malaise have been reported following daily oral administration.
Affected Organisms
Humans and other mammals
Biotransformation Two primary metabolites, 5-hydroxyemedastine and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms. The 5'-oxoanalogs of 5-hydroxyemedastine and 6-hydroxy-emedastine and the N-oxide are also formed as minor metabolites.
Absorption Ophthalmic use of emedastine usually does not produce measurable plasma concentrations.
Half Life The elimination half-life of oral emedastine in plasma is 3-4 hours.
Elimination Approximately 44% of the oral dose is recovered in the urine over 24 hours with only 3.6% of the dose excreted as parent drug. Two primary metabolites, 5- and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms.
External Links
Wikipedia
RxList
Drugs.com

REFERENCES