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Levocetirizine (as levocetirizine dihydrochloride) is a third-generation non-sedative^{[citation needed]} antihistamine, developed from the second-generation antihistamine cetirizine. Chemically, levocetirizine is the active enantiomer of cetirizine. It is the R-enantiomer of the cetirizine racemate. Levocetirizine is an inverse agonist that decreases activity at histamine H1 receptors. This in turn prevents the release of other allergy chemicals and increased blood supply to the area, and provides relief from the typical symptoms of hay fever. It does not prevent the actual release of histamine from mast cells.

The manufacturers claim it to be more effective with fewer side effects than the second-generation drugs; however, there have been no published studies supporting this assertion. A study part-funded by the manufacturer UCB concluded it may be more effective than some other second- and third-generation anti-histamines, but didn't compare it to cetirizine.^[1]

History

Levocetirizine was first launched in 2001 by Belgian pharmaceutical company UCB.

Brand names

It is sold under the brand names:

Xyzal /ˈzaɪzæl/ in Australia, Austria, Croatia, Czech Republic, Finland, France, India, Ireland (also Rinozal), Lithuania, Netherlands, Portugal, Romania, Taiwan, Turkey, The Philippines, Serbia, Slovakia, Slovenia, South Africa and UK. On May 25, 2007, the United States Food and Drug Administration approved Xyzal, where it is co-marketed by Sanofi-Aventis.
Xusal in Germany;
Xozal in Greece;
Cezera in Poland;
Xazal in Spain;
Xuzal in Mexico;
In Hungary it is marketed as Zilola (made by Richter Gedeon) and Histisynt (Actavis).
In India, levocetirizine is marketed by GlaxoSmithKline under the brand name Vozet. Torrent Pharma launched UVNIL for the rural market.
In Pakistan levocetirizine was first launched in a liquid formulation by Novartis Consumer Health Division under the name of T-Day Syrup.
In Nepal levocetirizine is available in tablet with brand name Curin manufactured by Beximco Pharma.^[2]
In Chile, it is marketed as Zival and made by Laboratorio Saval.
In Sweden, Xyzal was not granted subventions, and was withdrawn from the market.^[3]

Side effects

Levocetirizine is called a non-sedating antihistamine as it does not enter the brain in significant amounts, and is therefore unlikely to cause drowsiness. However, some people may experience some slight sleepiness, headache, mouth dryness, lightheadedness, vision problems (mainly blurred vision), palpitations and fatigue.^[4]

Research

Latest research shows levocetirizine reduces asthma attacks by 70% in children.^[5]

Availability

The drug is currently available by prescription in the United States. Although the drug was only authorized by the FDA on 25 May 2007, it was already available in most European countries. Like many new drugs it entered the market at a higher price than currently available third and second generation antihistamines. In India, one form of the drug is available as Crohist MK tablets and syrup, a formulation of levocetirizine hydrochloride and montelukast. In India, Crohist MK is a Schedule 'H' drug and may only be prescribed by a registered medical practitioner. In Finland, Hungary, China, and Kuwait^[6] the drug is sold over-the-counter.

Different brands (Actavis, Glenmark, UCB) Levocetirizine tablets and oral solution.

References

^ Grant, JA; Riethuisen, JM; Moulaert, B; DeVos, C; Gamalero, C.; Descalzi, D.; Folli, C.; Passalacqua, G.; Canonica, G.W. (February 2002). "A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjects". Ann Allergy Asthma Immunol 88 (2): 190–197. doi:10.1016/S1081-1206(10)61995-3. PMID 11868924.
^ http://web.archive.org/web/20121022184859/http://beximco-pharma.com/allergic-disorders/147-curin.html. Archived from the original on October 22, 2012. Retrieved August 29, 2012. Missing or empty |title= (help)
^ http://www.fass.se/LIF/substance?substanceId=ID11EHWRUFGBA53CSR
^ XOZAL technical specifications booklet.
^ Pasquali, M; Baiardini, I; Rogkakou, A; Riccio, AM; Gamalero, C; Descalzi, D; Folli, C; Passalacqua, G; Canonica, GW (September 2006). "Levocetirizine in persistent allergic rhinitis and asthma: effects on symptoms, quality of life and inflammatory parameters". Clinical & Experimental Allergy 36 (9): 1161–7. doi:10.1111/j.1365-2222.2006.02548.x. PMID 16961716.
^ On different names: http://www.hazipatika.com/gyogyszerkereso/termek/sefaller_5_mg_filmtabletta/54120

External links

Full US prescribing information Xyzal® (levocetirizine dihydrochloride) tablets and oral solution (provided by UCB, December 2010, pdf file)

UpToDate Contents

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1. 寒冷蕁麻疹 cold urticaria
2. アレルギー性鼻炎の薬物療法 pharmacotherapy of allergic rhinitis
3. 慢性蕁麻疹：標準的なマネージメントおよび患者教育 chronic urticaria standard management and patient education
4. アレルギー疾患の治療のためのプレバイオティクスおよびプロバイオティクス prebiotics and probiotics for treatment of allergic disease
5. 新規発症の蕁麻疹 new onset urticaria

English Journal

Night-time sedating H1 -antihistamine increases daytime somnolence but not treatment efficacy in chronic spontaneous urticaria: a randomised controlled trial.

Staevska M, Gugutkova M, Lazarova C, Kralimarkova T, Dimitrov V, Zuberbier T, Church MK, Popov TA.Author information Clinical Centre of Allergology, Medical University Sofia, Bulgaria.AbstractBACKGROUND: Many physicians believe that the most effective way to treat chronic urticaria is to take a non-sedating second-generation H1 -antihistamine in the morning and a sedating first-generation H1 -antihistamine, usually hydroxyzine, at night to enhance sleep. But is this belief well founded?
The British journal of dermatology.Br J Dermatol.2014 Jan 28. doi: 10.1111/bjd.12846. [Epub ahead of print]
BACKGROUND: Many physicians believe that the most effective way to treat chronic urticaria is to take a non-sedating second-generation H1 -antihistamine in the morning and a sedating first-generation H1 -antihistamine, usually hydroxyzine, at night to enhance sleep. But is this belief well founded O
PMID 24472058

Effect of combination of montelukast and levocetirizine on otitis media with effusion: a prospective, placebo-controlled trial.

Ertugay CK, Cingi C, Yaz A, San T, Ulusoy S, Erdogmus N, Ertugay OC.Author information Departments of Otorhinolaryngology/Head and Neck Surgery.AbstractCONCLUSION: This study demonstrated that treatment with montelukast in combination with levocetirizine may have a beneficial effect on clinical improvement of middle ear fluid in children with otitis media with effusion (OME).
Acta oto-laryngologica.Acta Otolaryngol.2013 Dec;133(12):1266-72. doi: 10.3109/00016489.2013.824113. Epub 2013 Aug 26.
CONCLUSION: This study demonstrated that treatment with montelukast in combination with levocetirizine may have a beneficial effect on clinical improvement of middle ear fluid in children with otitis media with effusion (OME).OBJECTIVE: To evaluate the effect of the combination of montelukast and le
PMID 23972320

Evaluation of the antihistamine effects of olopatadine and levocetirizine during a 24-h period: a double-blind, randomized, cross-over, placebo-controlled comparison in skin responses induced by histamine iontophoresis.

Takeo T, Kasugai C, Tanaka R, Ando T, Ogawa A, Akita Y, Watanabe D.Author information Department of Dermatology, Aichi Medical University, Nagakute, Japan.AbstractThe antihistamine effects of olopatadine and levocetirizine, in standard-dose application described in their information (5 mg twice a day for olopatadine; 5 mg once daily for levocetirizine), were examined from 11.5 to 24 h after application. The test was designed in a double-blind, randomized, cross-over, placebo-controlled study of 12 healthy volunteers on histamine-induced flare and wheal response using an iontophoresis technique. The suppressive effect of olopatadine on the wheals induced by a 0.1-mA histamine iontophoresis lasted for 24 h after dosing. Both drugs inhibited flare induced by histamine iontophoresis almost completely until 24 h after the first administration. Suppression of the 0.2-mA-induced wheal response by levocetirizine, taken once daily, decreased with time, although 0.1-mA-induced flare was almost completely suppressed by the drug. Olopatadine completely suppressed even the wheal response induced by a 0.2-mA histamine iontophoresis. Compared with the placebo, the two drugs significantly suppressed the subjective itching assessed by visual analog scale at all intervals. There were no significant differences in subjective drowsiness and objective cognitive function between drug- and placebo-treated subjects. These results demonstrate that olopatadine seems to be more potent than levocetirizine when administrated in a standard dose. In conclusion, mild to moderate urticaria could be controlled by standard application as described in their information. On the other hand, severe urticaria could be managed by a standard application of olopatadine, but levocetirizine may need an additional dose to control severe urticaria.
The Journal of dermatology.J Dermatol.2013 Dec;40(12):987-92. doi: 10.1111/1346-8138.12326. Epub 2013 Dec 4.
The antihistamine effects of olopatadine and levocetirizine, in standard-dose application described in their information (5 mg twice a day for olopatadine; 5 mg once daily for levocetirizine), were examined from 11.5 to 24 h after application. The test was designed in a double-blind, randomized,
PMID 24303975

Japanese Journal

レボセチリジン塩酸塩錠(ザイザル錠5mg)の使用実態下でのアレルギー性鼻炎と皮膚疾患に対する安全性と有効性の検討 : 使用成績調査(中間報告)

久米川一郎,長谷川直美,金谷京美 [他]
アレルギー・免疫 19(5), 790-806, 2012-05
NAID 40019302564

Enantioselective determination of cetirizine in human plasma by normal-phase liquid chromatography-atmospheric pressure chemical ionization-tandem mass spectrometry

KANG Seung Woo,JANG Hae Jong,MOORE Victor S.,PARK Ji-Young,KIM Kyoung-Ah,YOUM Jeong-Rok,HAN Sang Beom
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 878(32), 3351-3357, 2010-12-15
NAID 10028044811

「レボセチリジン」

Levocetirizine
Systematic (IUPAC) name
	2-(2-{4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid
Clinical data
Trade names	Xyzal, Levazyr
AHFS/Drugs.com	Monograph
MedlinePlus	a607056
Pregnancy; category	US: B (No risk in non-human studies); ;
Routes of; administration	Oral
Legal status
Legal status	UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Bioavailability	High
Protein binding	90%
Metabolism	Hepatic 14% CYP3A4
Biological half-life	6 to 10 hours
Excretion	Renal and fecal
Identifiers
CAS Number	130018-77-8
ATC code	R06AE09 (WHO)
PubChem	CID 1549000
IUPHAR/BPS	1214
ChemSpider	1266001
UNII	6U5EA9RT2O
KEGG	D07402
ChEMBL	CHEMBL1201191
Chemical data
Formula	C21H25ClN2O3
Molar mass	388.888 g/mol
	SMILES Clc1ccc(cc1)[C@H](N2CCN(CCOCC(=O)O)CC2)c3ccccc3 ;
	InChI InChI=1S/C21H25ClN2O3/c22-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)24-12-10-23(11-13-24)14-15-27-16-20(25)26/h1-9,21H,10-16H2,(H,25,26)/t21-/m1/s1 ; Key:ZKLPARSLTMPFCP-OAQYLSRUSA-N ;
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　　[★]

英: levocetirizine
商: ザイザル
関: 抗ヒスタミン薬。その他のアレルギー用薬

抗ヒスタミン薬;ピペラジン系
成人：1回5mg 1日1回就寝前。10mgまで増量可能。

[1] Grant, JA; Riethuisen, JM; Moulaert, B; DeVos, C; Gamalero, C.; Descalzi, D.; Folli, C.; Passalacqua, G.; Canonica, G.W. (February 2002). "A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjects". Ann Allergy Asthma Immunol 88 (2): 190–197. doi:10.1016/S1081-1206(10)61995-3. PMID 11868924.

[2] ttp://web.archive.org/web/20121022184859/http://beximco-pharma.com/allergic-disorders/147-curin.html. Archived from the original on October 22, 2012. Retrieved August 29, 2012. Missing or empty |title= (help)

[3] ttp://www.fass.se/LIF/substance?substanceId=ID11EHWRUFGBA53CSR

[4] XOZAL technical specifications booklet.

[5] Pasquali, M; Baiardini, I; Rogkakou, A; Riccio, AM; Gamalero, C; Descalzi, D; Folli, C; Passalacqua, G; Canonica, GW (September 2006). "Levocetirizine in persistent allergic rhinitis and asthma: effects on symptoms, quality of life and inflammatory parameters". Clinical & Experimental Allergy 36 (9): 1161–7. doi:10.1111/j.1365-2222.2006.02548.x. PMID 16961716.

[6] On different names: http://www.hazipatika.com/gyogyszerkereso/termek/sefaller_5_mg_filmtabletta/54120

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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levocetirizine