同: Mexitil

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antiarrhythmic drug (trade name Mexitil) used to treat ventricular arrhythmias (同)Mexitil

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/10/19 13:37:11」(JST)

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Mexiletine (INN, sold under the trade name Mexitil) belongs to the Class IB anti-arrhythmic group of medicines. It is used to treat arrhythmias within the heart, or seriously irregular heartbeats. It slows conduction in the heart and makes the heart tissue less sensitive. Dizziness, heartburn, nausea, nervousness, trembling, unsteadiness are common side effects. It is available in injection and capsule form.

Class IB antiarrhythmics decrease action potential frequency by lengthening the repolarization phase. This is achieved by blocking sodium channels.^[1]

This drug is now no longer freely available as a licensed product in either the US or the UK. It can be imported to the UK as an unlicensed, 'named-patient' drug. Its use in arrhythmias is restricted to use in life-threatening conditions only.

Mexiletine may also be of use in patients experiencing refractory pain^[2] and is also effective for treating muscle stiffness resulting from myotonic dystrophy (Steinert's disease) or nondystrophic myotonias such as myotonia congenita (Thomsen disease).

Synthesis

Mexiletine synthesis:^[3]^[4]^[5]^[6]

References

^ Mexiletine, RxList.com
^ Sweetman S (ed.) (2002). Martindale: The complete drug reference (33rd ed.). London: Pharmaceutical Press. ISBN 0-85369-499-0.
^ H. Koppe, W. Kummer, U.S. Pat. 3.954.872 (1976).
^ H. Koppe, W. Kummer, U.S. Pat. 3.659.019 (1972).
^ C.H. Boehringer Sohns, Fr. Pat. 1.551.055 (1968).
^ H. Koppe, W. Kummer, U.S, Pat. 4.031.244 (1977).

External links

MedlinePlus Drug Information: Mexiletine

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UpToDate Contents

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1. メキシレチンの主な副作用 major side effects of mexiletine
2. 先天性ＱＴ延長症候群の予後および管理 prognosis and management of congenital long qt syndrome
3. 糖尿病性神経障害の治療 treatment of diabetic neuropathy
4. 癌疼痛の管理：鎮痛補助剤（鎮痛剤） cancer pain management adjuvant analgesics coanalgesics
5. 筋強直性ジストロフィー：予後および管理 myotonic dystrophy prognosis and management

English Journal

A Case of Long QT Syndrome Type 3 Aggravated by Beta-Blockers and Alleviated by Mexiletine: The Role of Epinephrine Provocation Test.

Park J, Kim SK, Pak HN.SourceDepartment of Cardiology, Yonsei University Health System, 50 Yonsei-ro, Seodaemun-gu, Seoul 120-752, Korea. hnpak@yuhs.ac.
Yonsei medical journal.Yonsei Med J.2013 Mar 1;54(2):529-33. doi: 10.3349/ymj.2013.54.2.529.
Long QT syndrome (LQTs) is an uncommon genetic disease causing sudden cardiac death with Torsade de Pointes (TdP). The first line drug treatment has been known to be β-blocker. We encountered a 15-year-old female student with LQTs who had prolonged QTc and multiple episodes of syncope or agonal res
PMID 23364992

Molecular dissection of lubeluzole use-dependent block of voltage-gated sodium channels discloses new therapeutic potentials.

Desaphy JF, Carbonara R, Costanza T, Lentini G, Cavalluzzi MM, Bruno C, Franchini C, Camerino DC.SourceSection of Pharmacology, Department of Pharmacy, University of Bari-Aldo Moro, via Orabona 4 - campus, I-70125 Bari, Italy. jfdesaphy@farmbiol.uniba.it.
Molecular pharmacology.Mol Pharmacol.2013 Feb;83(2):406-15. doi: 10.1124/mol.112.080804. Epub 2012 Nov 21.
Lubeluzole, which acts on various targets in vitro, including voltage-gated sodium channels, was initially proposed as a neuroprotectant. The lubeluzole structure contains a benzothiazole moiety [N-methyl-1,3-benzothiazole-2-amine (R-like)] related to riluzole and a phenoxy-propranol-amine moiety [(
PMID 23175529

In vivo evaluation of antimyotonic efficacy of β-adrenergic drugs in a rat model of myotonia.

Desaphy JF, Costanza T, Carbonara R, Conte Camerino D.SourceSection of Pharmacology, Department of Pharmacy, University of Bari-Aldo Moro, Via Orabona 4 - Campus, 70125 Bari, Italy. jfdesaphy@farmbiol.uniba.it
Neuropharmacology.Neuropharmacology.2013 Feb;65:21-7. doi: 10.1016/j.neuropharm.2012.09.006. Epub 2012 Sep 18.
The sodium channel blocker mexiletine is considered the first-line drug in myotonic syndromes, a group of muscle disorders characterized by membrane over-excitability. We previously showed that the β-adrenoceptor modulators, clenbuterol and propranolol, block voltage-gated sodium channels in a mann
PMID 23000075

Japanese Journal

Column-Switching HPLC Determination of Mexiletine Using Tris(bipyridine)ruthenium(III) Electrogenerated Chemiluminescence and Precolumn Derivatization with Divinylsulfone

KOBAYASHI Naoko,MIYAMOTO Aoi,UCHIKURA Kazuo
Analytical sciences : the international journal of the Japan Society for Analytical Chemistry 26(12), 1289-1294, 2010-12-10
NAID 10027575018

帯状疱疹後の眼症状が釣藤散で劇的に改善した二症例

福田悟,南部隆,高橋秀則,黒木佳奈子,西山比呂史,三潴忠道
日本東洋醫學雜誌 = Japanese journal of oriental medicine 61(7), 912-916, 2010-11-20
釣藤散により帯状疱疹による眼症状が劇的に改善した2症例を経験した。症例1は78歳女性で20年前の帯状疱疹による眼内異物感とひりひりする痛みを訴え，既往に高血圧があった。週1回の星状神経節ブロック，桂枝加朮附湯エキス，アミトリプチリンおよび後にメキシレチンで治療した。最初，神経ブロックの効果は劇的であったが，その効果は1カ月間で徐々に減少した。星状神経節ブロックと釣藤散の共通作用である頭蓋内血流の増 …
NAID 10026966738

Related Pictures

★リンクテーブル★

リンク元	「薬剤性過敏症症候群」「メキシレチン」
拡張検索	「mexiletine hydrochloride」

「薬剤性過敏症症候群」

Mexiletine
Systematic (IUPAC) name
	(RS)-1-(2,6-dimethylphenoxy)propan-2-amine; OR; 2-(2-aminopropoxy)-1,3-dimethylbenzene
Clinical data
AHFS/Drugs.com	monograph
MedlinePlus	a607064
Pregnancy cat.	AU: B1; US: C;
Legal status	UK: POM;
Routes	Oral, IV
Pharmacokinetic data
Bioavailability	90%
Protein binding	50-60%
Metabolism	Hepatic (CYP2D6 and 1A2- mediated)
Half-life	10-12 hours
Excretion	Renal (10%)
Identifiers
CAS number	31828-71-4
ATC code	C01BB02
PubChem	CID 4178
IUPHAR ligand	2629
DrugBank	DB00379
ChemSpider	4034
UNII	1U511HHV4Z
KEGG	D08215
ChEBI	CHEBI:6916
ChEMBL	CHEMBL558
Chemical data
Formula	C11H17NO
Mol. mass	179.259 g/mol
	SMILES O(c1c(cccc1C)C)CC(N)C;
	InChI InChI=1S/C11H17NO/c1-8-5-4-6-9(2)11(8)13-7-10(3)12/h4-6,10H,7,12H2,1-3H3 ; Key:VLPIATFUUWWMKC-UHFFFAOYSA-N ;
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