WordNet

antiarrhythmic drug (trade name Mexitil) used to treat ventricular arrhythmias (同)Mexitil
a complex consisting of an organic base in association with hydrogen chloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/01/31 21:42:12」(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. It's use in arrhythmia's 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).

References[edit]

^ Mexiletine, RxList.com
^ Sweetman S (ed.) (2002). Martindale: The complete drug reference (33rd ed.). London: Pharmaceutical Press. ISBN 0-85369-499-0.

External links[edit]

MedlinePlus Drug Information: Mexiletine

This drug article relating to the cardiovascular system is a stub. You can help Wikipedia by expanding it.

UpToDate Contents

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1. I群抗不整脈薬の主な副作用 major side effects of class i antiarrhythmic drugs
2. 先天性ＱＴ延長症候群の予後およびマネージメント prognosis and management of congenital long qt syndrome
3. 筋強直性ジストロフィー：予後およびマネージメント myotonic dystrophy prognosis and management
4. 糖尿病性神経障害の治療 treatment of diabetic neuropathy
5. 慢性閉塞性肺疾患（COPD）における不整脈 arrhythmias in copd

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

症例ステロイドパルス療法が奏効した塩酸メキシレチンによる薬剤性過敏症症候群の1例

池澤優子,毛利忍,廣門未知子 [他]
皮膚科の臨床 52(10), 1397-1401, 2010-10
NAID 40017336938

Pharmacological Differences Between Static and Dynamic Allodynia in Mice With Herpetic or Postherpetic Pain

SASAKI Atsushi,SERIZAWA Kenichi,ANDOH Tsugunobu,SHIRAKI Kimiyasu,TAKAHATA Hiroki,KURAISHI Yasushi
Journal of pharmacological sciences 108(3), 266-273, 2008-11-20
… Mexiletine hydrochloride (30 mg/kg, p.o.) and ketamine hydrochloride (50 mg/kg, i.p.) produced a moderate attenuation of static but not dynamic allodynia. …
NAID 10024592945

塩酸メキシレチンによるDrug-induced hypersensitivity syndrome(DIHS)の1例

石川博康,島貫美和,松田暁子
山形県立病院医学雑誌 42(2), 129-132, 2008-07
NAID 40016298647

★リンクテーブル★

リンク元	「メキシレチン」
関連記事	「hydrochloride」「mexiletine」

「メキシレチン」

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.	B1 (AU) C (US)
Legal status	POM (UK)
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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