関: emedastine difumarate

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/03/13 16:17:49」(JST)

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Emedastine (trade name Emadine) is a second generation^{[citation needed]} antihistamine used in eye drops to alleviate the symptoms of allergic conjunctivitis. It acts as a H₁ receptor antagonist. It works by blocking the action of histamine that causes allergic symptoms. It is used in form of the difumarate.^[2] The emedastine difumarate is a white, crystalline, water-soluble fine powder. Emedastine eye drops is usually applied twice a day to the affected eye. When the patients with allergic conjunctivitis were treated with 0.05% emedastine 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.

Pharmacodynamics

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

Pharmacokinetics

The human oral bioavailability is approximately 50% and maximum plasma concentration was 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, 6-hydroxyemedastine 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.^[1]

Contraindications

Emedastine should not be used in patients who are hypersensitive to emedastine or any other excipients of the preparation. Benzalkonium chloride contained in the bottle of emedastine solution can discolor soft contact lenses, so people who wear contact lenses should be careful using it.

Adverse events

The most common adverse effect was headache (11%). The other minor adverse effects encountered in less than 5% of patients were asthenia, burning or stinging sensation, unpleasant taste, blurred vision, eye dryness and tearing.

References

^ ^a ^b "Emadine (emedastine difumarate ophthalmic solution) 0.05%. Full Prescribing Information" (PDF). Alcon Laboratories, Inc. 6201 South Freeway Fort Worth, Texas 76134, USA. Retrieved 5 January 2016.
^ 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.

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UpToDate Contents

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1. アレルギー性結膜炎：マネージメント allergic conjunctivitis management
2. アトピー性角結膜炎 atopic keratoconjunctivitis
3. アレルギー性鼻炎の薬物療法 pharmacotherapy of allergic rhinitis

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,
PMID 20334612

[Antihistamines in the treatment of allergic rhinitis--update 2008/2009].

Kruszewski J.SourceKlinika Chorob Infekcyjnych i Alergologii, Wojskowy Instytut Medyczny w Warszawie.
Otolaryngologia polska. The Polish otolaryngology.Otolaryngol Pol.2009 Sep;63(7):5-10.
The following paper reviews the latest news on antihistamines used in the treatment of allergic rhinitis. It describes the new results of investigations on clinical application of H3 and H4 receptors in therapy of allergic diseases as well as the effect of emedastine on histamine-induced tissue remo
PMID 20564892

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

フマル酸エメダスチンおよび種々選択的H1受容体拮抗・アレルギー性疾患治療薬のモルモットにおけるヒスタミン誘発および受身皮膚アナフィラキシー反応に及ぼす影響

大平明良,滝沢俊明,堀琢弥 [他]
アレルギ-・免疫 10(3), 387-395, 2003-03
NAID 50000765336

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リンク元	「エメダスチン」
拡張検索	「emedastine difumarate」

「エメダスチン」

Emedastine
Clinical data
Trade names	Emadine
AHFS/Drugs.com	Monograph
Routes of; administration	Topical (ophthalmic solution)
ATC code	S01GX06 (WHO);
Legal status
Legal status	In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	~50% (oral) (Tmax = 1–2 hours)
Metabolism	Hepatic
Biological half-life	3–4 hours (oral), 10 hours (topical)
Identifiers
	IUPAC name 1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-benzimidazole;
CAS Number	87233-61-2 ;
PubChem CID	3219;
IUPHAR/BPS	7174;
DrugBank	DB01084 ;
ChemSpider	3106 ;
UNII	9J1H7Y9OJV;
KEGG	D07890 ;
ChEBI	CHEBI:4779 ;
ChEMBL	CHEMBL594 ;
Chemical and physical data
Formula	C17H26N4O
Molar mass	302.415 g/mol
3D model (Jmol)	Interactive image;
	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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英: emedastine
化: フマル酸エメダスチン emedastine difumarate
商: ダレン、レミカット、エメロミン

「emedastine difumarate」

　　[★] エメダスチン。フマル酸エメダスチン

[PI-1] "Emadine (emedastine difumarate ophthalmic solution) 0.05%. Full Prescribing Information" (PDF). Alcon Laboratories, Inc. 6201 South Freeway Fort Worth, Texas 76134, USA. Retrieved 5 January 2016.

[2] 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.

v t e Antihistamines (R06)

Aminoalkyl ethers	Bromazine (bromodiphenhydramine) Carbinoxamine Clemastine Chlorphenoxamine Diphenylpyraline Diphenhydramine Doxylamine Orphenadrine Phenyltoloxamine

Substituted alkylamines	Brompheniramine Chlorphenamine Dexbrompheniramine (+pseudoephedrine) Dexchlorpheniramine (+betamethasone) Dimetindene Pheniramine Talastine

Substituted ethylenediamines	Chloropyramine Histapyrrodine Mepyramine Methapyrilene Tripelennamine (pyribenzamine)

Phenothiazine derivatives	Alimemazine Fenethazine Hydroxyethylpromethazine Isothipendyl Mequitazine Methdilazine Oxomemazine Promethazine

Piperazine derivatives	Buclizine Cetirizine Levocetirizine Chlorcyclizine Cinnarizine Cyclizine Hydroxyzine Meclizine Oxatomide

Others for systemic use	Antazoline Azanator Azatadine Bamipine Cyproheptadine Deptropine Ebastine Emedastine Epinastine Ketotifen Latrepirdine Mebhydrolin Mizolastine Olopatadine Phenindamine Pimethixene Pyrrobutamine Quifenadine Rupatadine Triprolidine selective (Acrivastine Astemizole Azelastine Bilastine Desloratadine Fexofenadine Loratadine Terfenadine)

For topical use	Bamipine Chloropyramine Chlorphenoxamine Clemastine Dimetindene Diphenhydramine Isothipendyl Mepyramine Promethazine Thenalidine

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emedastine