- 関
- mexiletine
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
Wikipedia preview
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)
[Wiki en表示]
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 Y |
ATC code |
C01BB02 |
PubChem |
CID 4178 |
IUPHAR ligand |
2629 |
DrugBank |
DB00379 |
ChemSpider |
4034 Y |
UNII |
1U511HHV4Z Y |
KEGG |
D08215 Y |
ChEBI |
CHEBI:6916 Y |
ChEMBL |
CHEMBL558 Y |
Chemical data |
Formula |
C11H17NO |
Mol. mass |
179.259 g/mol |
|
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 Y
Key:VLPIATFUUWWMKC-UHFFFAOYSA-N Y
|
Y (what is this?) (verify) |
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.
Further reading[edit]
- Peck T; Hill S, Williams M (eds.) (2004). Pharmacology for Anaesthesia and Intensive Care (2nd ed.). Cambridge University Press. ISBN 0-521-68794-2.
External links[edit]
- MedlinePlus Drug Information: Mexiletine
Antiarrhythmic agents (C01B)
|
|
Channel blockers |
class I
(Na+ channel blockers)
|
class Ia (Phase 0→ and Phase 3→)
|
- Ajmaline
- Disopyramide
- Lorajmine
- Prajmaline
- Procainamide#
- Quinidine#
- Sparteine
|
|
class Ib (Phase 3←)
|
- IV (Lidocaine#)
- enteral (Aprindine
- Mexiletine
- Tocainide)
|
|
class Ic (Phase 0→)
|
- Encainide‡
- Ethacizine
- Flecainide
- Indecainide‡
- Lorcainide
- Moracizine‡
- Propafenone
|
|
|
class III
(Phase 3→, K+ channel blockers)
|
- Amiodarone
- Bretylium
- Bunaftine
- Dofetilide
- Dronedarone
- E-4031†
- Ibutilide
- Nifekalant
- Sotalol
- Tedisamil
- Vernakalant
|
|
class IV
(Phase 4→, Ca2+ channel blockers)
|
|
|
|
Receptor agonists
and antagonists |
class II
(Phase 4→, β blockers)
|
- Nadolol
- Pindolol
- Propranolol
- cardioselective (Acebutolol
- Atenolol
- Esmolol
- Metoprolol)
|
|
A1 agonist
|
- Adenosine
- Benzodiazepines
- Barbiturates
|
|
M2
|
- muscarinic antagonist: Atropine
- Disopyramide
- Quinidine
muscarinic agonist: Digoxin
|
|
α receptors
|
- Amiodarone
- Bretylium
- Quinidine
- Verapamil
|
|
|
Ion transporters |
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
|
|
noco/cong/tumr, sysi/epon, injr
|
proc, drug (C1A/1B/1C/1D), blte
|
|
|
|
UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
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
- 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
Related Pictures
★リンクテーブル★
[★]
- 英
- mexiletine
- 化
- 塩酸メキシレチン mexiletine hydrochloride
- 商
- チルミメール、トイ、ポエルテン、メキシチール、メキシバール、メキシレート、メキトライド、メルデスト、メレート、モバレーン
[★]
塩酸塩、ハイドロクロライド
[★]
メキシレチン
- 同
- Mexitil