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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/03/31 02:59:59」(JST)

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Emedastine (trade name Emadine) is a second generation^{[citation needed]} antihistamine used in eye drops to treat allergic conjunctivitis. It acts as a H₁ receptor antagonist. It works by blocking certain natural substances, histamines that cause allergic symptoms. It is used in form of the difumarate.^[1] The formation of emedastine difumarate is a white, crystalline, water-soluble fine powder. Emedasine is applied as an eye drop with 2 times a day. When the patients with allergic conjunctivitis were treated with 0.05% emedastin difumarate ophthalmic solution for six weeks, the signs and symptoms such as redness, itching and swelling of the eyes were relieved. Emedastine appears to be devoid of effects on adrenergic, dopaminergic and serotonin receptors. This drug was developed by alcon which is global medical company specializing in eye care products.

Emedastine is significantly selective to H1 histamine receptors (Ki=1.3 nM), whereas its affinities for other histamine receptor are low (H2: Ki=49067 nM and H3: Ki=12430 nM ) in vitro study. Tropical ocular administration of emedastine inhibits histamine-stimulated vascular permeability in the conjunctiva as a concentration dependent manner in vitro study.

The human oral bioavailability is approximately 50% and maximum plasma concentration were achieved within 1-2 hours after dosing. Emedastine is mainly metabolized by the liver. There are two primary metabolites: 5-hydroxyemedastine and 6-hydroxyemedastine. They 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. The elimination half-life of oral emedastine in plasma is 3-4 hours, whereas that of topical emedastine is 10 hours. 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.

Emedastine should not be used in patients who are hypersensitive to any other ingredients or emedastin. Benzalkonium chloride contained in the bottle of emedastines can discolor soft contact lenses, so people who wear the lenses should be careful with using it. The most common adverse effect was headache (11%). The other minor adverse effect less than 5% of patients: asthenia, burning or stinging, bad taste, blurred vision, dry eye and tearing.

References

^ Bielory, L.; Lien, K. W.; Bigelsen, S. (2005). "Efficacy and tolerability of newer antihistamines in the treatment of allergic conjunctivitis". Drugs 65 (2): 215–228. doi:10.2165/00003495-200565020-00004. PMID 15631542. edit

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1. アレルギー性鼻炎の薬物療法 pharmacotherapy of allergic rhinitis
2. アレルギー性結膜炎 allergic conjunctivitis

English Journal

Contribution of mast cells to cerebral aneurysm formation.

Ishibashi R, Aoki T, Nishimura M, Hashimoto N, Miyamoto S.SourceDepartment of Neurosurgery, Kyoto University, Graduate School of Medicine, Kyoto, Japan.
Current neurovascular research.Curr Neurovasc Res.2010 May;7(2):113-24.
Cerebral aneurysm (CA) has a high prevalence and causes a fatal subarachnoid hemorrhage. Although CA is a socially important disease, there are currently no medical treatments for CA, except for surgical procedures, because the detailed mechanisms of CA formation remain unclear. From recent studies,
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Japanese Journal

アトピー性皮膚炎モデルマウス(NC/Ngaマウス)に経口投与した抗アレルギー薬(フマル酸エメダスチン)の発症予防ならびに治療効果の検討

西村久美子,江挙,中尾裕史,坪井良治,小川秀興
日本皮膚科学会雑誌 = THE JAPANESE JOURNAL OF DERMATOLOGY 114(9), 1507-1516, 2004-08-20
NAID 10013672235

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★リンクテーブル★

リンク元	「エメダスチン」「EMADINE」
関連記事	「emedastine」

「エメダスチン」

Emedastine
Systematic (IUPAC) name
	1-(2-ethoxyethyl)-2- (4-methyl-1,4-diazepan-1-yl)- benzoimidazole
Clinical data
Trade names	Emadine
AHFS/Drugs.com	monograph
Identifiers
CAS Registry Number	87233-61-2
ATC code	S01GX06
PubChem	CID 3219
DrugBank	DB01084
ChemSpider	3106
UNII	9J1H7Y9OJV
KEGG	D07890
ChEBI	CHEBI:4779
ChEMBL	CHEMBL594
Chemical data
Formula	C17H26N4O
Molecular mass	302.415 g/mol
	SMILES O(CC)CCn1c(nc2ccccc12)N3CCCN(C)CC3;
	InChI InChI=1S/C17H26N4O/c1-3-22-14-13-21-16-8-5-4-7-15(16)18-17(21)20-10-6-9-19(2)11-12-20/h4-5,7-8H,3,6,9-14H2,1-2H3 ; Key:KBUZBQVCBVDWKX-UHFFFAOYSA-N ;
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