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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/03/27 14:12:07」(JST)

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"Aleva" redirects here. For the pepper called "aleva", see Cayenne pepper.

Ebastine (trade names Evastin, Kestine, Ebastel, Aleva, Ebatrol) is a H₁ antihistamine with low potential for causing drowsiness.

It does not penetrate the blood–brain barrier to a significant amount and thus combines an effective block of the H₁ receptor in peripheral tissue with a low incidence of central side effects, i.e. seldom causing sedation or drowsiness.^[1]^[2]^[3]

The patent in which the structure of ebastine is first mentioned is EP 134124 in Europe and US 4550116 in the US. The substance is often provided in micronised form due to poor water solubility.

Uses and availability[edit]

Ebastine is a second-generation H1 receptor antagonist that is indicated mainly for allergic rhinitis and chronic idiopathic urticaria.^[4] It is available in 10 and 20 mg tablets^[5] and as fast-dissolving tablets,^[6] as well as in pediatric syrup. It has a recommended flexible daily dose of 10 or 20 mg, depending on disease severity.

Ebastine is available in different formulations (tablets, fast dissolving tablets and syrup) and commercialized under different brand names around the world, Ebet, Ebastel FLAS, Kestine, KestineLIO, KestinLYO, EstivanLYO, Evastel Z, Ebatrol, etc.

Pharmacokinetic profile[edit]

After oral administration, ebastine undergoes extensive first-pass metabolism by hepatic cytochrome P450 3A4 into its active carboxylic acid metabolite, carebastine. This conversion is practically complete.

Carebastine, the active metabolite

Efficacy[edit]

Data from over 8,000 patients in more than 40 clinical trials^{[not in citation given]} and studies^[4]^[5]^[7]^[8]^[3]^[9] suggest efficacy of ebastine in the treatment of intermittent allergic rhinitis, persistent allergic rhinitis and other indications.

Safety[edit]

Ebastine has shown overall safety and tolerability profile with no cognitive/psychomotor impairment^[5] and no sedation^[5] worse than placebo^[2], and cardiac safety, that is, no QT prolongation.^[5] The incidence of most commonly reported adverse events was comparable between the ebastine and placebo groups, which confirms that ebastine has a favourable safety profile.

While experiments in pregnant animals showed no risk for the unborn, no such data are available in humans. It is not known whether ebastine passes into the breast milk.^[2]

References[edit]

^ Tagawa, M; Kano, M; Okamura, N (2001). "Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)-clorphrniramine, a classical antihistamine". Br J Clin Pharmacl 52 (5): 501–509. PMC 2014616. PMID 11736858.
^ ^a ^b ^c Dinnendahl, V, Fricke, U, ed. (2010). Arzneistoff-Profile (in German) 4 (23 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-98-46-3.
^ ^a ^b Bousquet, J; Gaudaño, EM; Palama Carlos, AG (1999). "A 12-week, placebo-controlled study of the efficacy and safety of ebastine, 10 and 20 mg once daily, in the treatment of perennial allergic rhinitis". Allergy 54 (6): 562–568. PMID 10435469.
^ ^a ^b Van Cauwenberge, P; de Belder, T; Sys, L (2004). "A review of the second-generation antihistamine ebastine for the treatment of allergic disorders". Exp Rew Pharmacother 5 (8): 1807–13. PMID 15264995.
^ ^a ^b ^c ^d ^e Sastre, J (2008). "Ebastine in allergic rhinitis and chronic idiopathic urticaria". Allergy 63 (Suppl 89): 1–20. doi:10.1111/j.1398-9995.2008.01897.x. PMID 19032340.
^ Antonijoan, R; García-Gea, C; Puntes, M (2007). "Comparison of inhibition of cutaneous histamine reaction of ebastine fast-dissolving tablet (20 mg) versus desloratadine capsules (5 mg): a randomized, double-blind, double-dummy, placebo-controlled, three period crossover study in healthy, nonatopic adults". Clin Ther 29 (5): 814–22. PMID 17697901.
^ Ratner, P; Falqués, M; Chuecos, F (2005). "Meta-analysis of the efficacy of ebastine 20 mg compared to loratadine 10 mg and placebo in the symptomatic treatment of seasonal allergic rhinitis". Int Arch Allergy Immunol 138 (4): 312–8. PMID 16224195.
^ Antonijoan; García-Gea, C; Puntes, M (2007). "A comparison of ebastine 10 mg fast-dissolving tablet with oral desloratadine and placebo in inhibiting the cutaneous reaction to histamine in healthy adults". Clin Drug Invest 27 (7): 453–61. PMID 17563125.
^ Gehanno, P; Bremard-Oury, C; Zeisser, P (1996). "Comparison of ebastine to cetirizine in seasonal allergic rhinitis in adults". Annals of Allergy, Asthma and Immunol 76 (6): 507–12. PMID 8673684.

Salvà, M; Carreño, B; Pintos, M (2004). "Phase I, single dose, open label, randomized, crossover bioequivalence studies of ebastine 10 mg and 20 mg regular tablets vs 10 and 20 mg fast-dissolving tablets in healthy male volunteers". J Invest Allergol Clin Immunol 14 (4 (Suppl 1)): S5.

Peyri, J; Vidal, J; Marrón, J (1991). "Ebastine in chronic urticaria: a double-blind placebo controlled study". J Dermatol Treat 2: 51–3.

External links[edit]

"KESTINE Package Insert". South African Electronic Package Inserts. 1997-10-24. Retrieved 2007-04-01.

UpToDate Contents

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1. 寒冷蕁麻疹 cold urticaria

English Journal

Histamine Receptor H1-mediated Sensitization of TRPV1 Mediates Visceral Hypersensitivity and Symptoms in Patients With Irritable Bowel Syndrome.

Wouters MM1, Balemans D1, Van Wanrooy S1, Dooley J2, Cibert-Goton V3, Alpizar YA4, Valdez-Morales EE5, Nasser Y5, Van Veldhoven PP6, Vanbrabant W1, Van der Merwe S7, Mols R8, Ghesquière B9, Cirillo C1, Kortekaas I10, Carmeliet P9, Peetermans WE11, Vermeire S1, Rutgeerts P1, Augustijns P8, Hellings PW12, Belmans A13, Vanner S5, Bulmer DC3, Talavera K4, Vanden Berghe P1, Liston A2, Boeckxstaens GE14.
Gastroenterology.Gastroenterology.2016 Jan 2. pii: S0016-5085(15)01862-4. doi: 10.1053/j.gastro.2015.12.034. [Epub ahead of print]
BACKGROUND & AIMS: Histamine sensitizes the nociceptor TRPV1 and has been shown to contribute to visceral hypersensitivity in animals. We investigated the role of TRPV1 in irritable bowel syndrome (IBS) and evaluated if an antagonist of histamine receptor H1 (HRH1) could reduce symptoms of patie
PMID 26752109

A comparison of the intrasubject variation of drug exposure between generic and brand-name drugs: a retrospective analysis of replicate design trials.

Yu Y1,2, Teerenstra S2,3, Neef C1,4, Burger D5, Maliepaard M2.
British journal of clinical pharmacology.Br J Clin Pharmacol.2015 Nov 17. doi: 10.1111/bcp.12828. [Epub ahead of print]
AIM(S): To investigate whether differences in total and peak drug exposure upon generic substitution are due to differences between formulations or to intrasubject pharmacokinetic variability of the active substance.METHODS: This study was designed as a retrospective reanalysis of existing studies.
PMID 26574160

Determination of Some Non-sedating Antihistamines via Their Native Fluorescence and Derivation of Some Quantitative Fluorescence Intensity - Structure Relationships.

El-Kommos ME1, El-Gizawy SM1, Atia NN1, Hosny NM2.
Journal of fluorescence.J Fluoresc.2015 Nov;25(6):1695-709. doi: 10.1007/s10895-015-1656-4. Epub 2015 Oct 6.
A validated simple, novel, and rapid spectrofluorimetric method was developed for the determination of some non-sedating antihistamines (NSAs); namely cetirizine (CTZ), ebastine (EBS), fexofenadine (FXD), and loratadine (LOR). The method is based on measuring the native fluorescence of the cited dru
PMID 26439930

Japanese Journal

医薬品の定量法における粉砕方法の影響について

髙橋和長,長谷川貴志,西條雅明 [他]
医薬品医療機器レギュラトリーサイエンス 45(2), 140-146, 2014
NAID 40019975301

Experimental evaluation of ebastine, a second-generation antihistamine, as a supportive medication for alopecia areata

OHYAMA Manabu,SHIMIZU Atsushi,TANAKA Kyoko,AMAGAI Masayuki
Journal of dermatological science 58(2), 154-157, 2010-05-01
NAID 10027400950

〓痒性皮膚疾患に対するエバスチン (エバステル^【○!R】) の有効性と安全性の検討 : 追加投与による評価

古川福実,金澤伸雄,吉益隆 [他],西出武司,青木真理子
西日本皮膚科 = The Nishinihon journal of dermatology 71(6), 609-615, 2009-12-01
NAID 10026321817

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リンク元

「エバスチン」

Ebastine
Systematic (IUPAC) name
	4-(4-benzhydryloxy-1-piperidyl)-1-(4-tert-butylphenyl)butan-1-one
Clinical data
AHFS/Drugs.com	International Drug Names
Legal status	?
Routes	Oral
Pharmacokinetic data
Protein binding	Greater than 95%
Metabolism	Hepatic (CYP3A4-mediated), to carebastine
Half-life	15 to 19 hours (carebastine)
Identifiers
CAS number	90729-43-4
ATC code	R06AX22
PubChem	CID 3191
ChemSpider	3079
UNII	TQD7Q784P1
ChEMBL	CHEMBL305660
Chemical data
Formula	C32H39NO2
Mol. mass	469.658 g/mol
	SMILES O=C(c1ccc(cc1)C(C)(C)C)CCCN4CCC(OC(c2ccccc2)c3ccccc3)CC4;
	InChI InChI=1S/C32H39NO2/c1-32(2,3)28-18-16-25(17-19-28)30(34)15-10-22-33-23-20-29(21-24-33)35-31(26-11-6-4-7-12-26)27-13-8-5-9-14-27/h4-9,11-14,16-19,29,31H,10,15,20-24H2,1-3H3 ; Key:MJJALKDDGIKVBE-UHFFFAOYSA-N ;
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英: ebastine
商: エバステル, Ebastel

抗ヒスタミン薬、持続性プロドラッグ

[Tagawa_2001-1] Tagawa, M; Kano, M; Okamura, N (2001). "Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)-clorphrniramine, a classical antihistamine". Br J Clin Pharmacl 52 (5): 501–509. PMC 2014616. PMID 11736858.

[Arzneistoff-Profile-2] Dinnendahl, V, Fricke, U, ed. (2010). Arzneistoff-Profile (in German) 4 (23 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-98-46-3.

[Bousquet_1999-3] Bousquet, J; Gaudaño, EM; Palama Carlos, AG (1999). "A 12-week, placebo-controlled study of the efficacy and safety of ebastine, 10 and 20 mg once daily, in the treatment of perennial allergic rhinitis". Allergy 54 (6): 562–568. PMID 10435469.

[Van_Cauwenberge_2004-4] Van Cauwenberge, P; de Belder, T; Sys, L (2004). "A review of the second-generation antihistamine ebastine for the treatment of allergic disorders". Exp Rew Pharmacother 5 (8): 1807–13. PMID 15264995.

[Sastre_2008-5] Sastre, J (2008). "Ebastine in allergic rhinitis and chronic idiopathic urticaria". Allergy 63 (Suppl 89): 1–20. doi:10.1111/j.1398-9995.2008.01897.x. PMID 19032340.

[pmid_17697901-6] Antonijoan, R; García-Gea, C; Puntes, M (2007). "Comparison of inhibition of cutaneous histamine reaction of ebastine fast-dissolving tablet (20 mg) versus desloratadine capsules (5 mg): a randomized, double-blind, double-dummy, placebo-controlled, three period crossover study in healthy, nonatopic adults". Clin Ther 29 (5): 814–22. PMID 17697901.

[Ratner_2005-7] Ratner, P; Falqués, M; Chuecos, F (2005). "Meta-analysis of the efficacy of ebastine 20 mg compared to loratadine 10 mg and placebo in the symptomatic treatment of seasonal allergic rhinitis". Int Arch Allergy Immunol 138 (4): 312–8. PMID 16224195.

[pmid_17563125-8] Antonijoan; García-Gea, C; Puntes, M (2007). "A comparison of ebastine 10 mg fast-dissolving tablet with oral desloratadine and placebo in inhibiting the cutaneous reaction to histamine in healthy adults". Clin Drug Invest 27 (7): 453–61. PMID 17563125.

[Gehanno_1996-9] Gehanno, P; Bremard-Oury, C; Zeisser, P (1996). "Comparison of ebastine to cetirizine in seasonal allergic rhinitis in adults". Annals of Allergy, Asthma and Immunol 76 (6): 507–12. PMID 8673684.

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ebastine