Mexiletine

From Wikipedia, the free encyclopedia

Mexiletine chemical structure
Mexiletine
Systematic (IUPAC) name
1-(2,6-dimethylphenoxy)propan-2-amine
Identifiers
CAS number 31828-71-4
ATC code C01BB02
PubChem 4178
DrugBank APRD00242
Chemical data
Formula C11H17NO 
Mol. weight 179.259 g/mol
Pharmacokinetic data
Bioavailability 90%
Protein binding 50-60%
Metabolism Hepatic (CYP2D6 and 1A2- mediated)
Half life 10-12 hours
Excretion Renal (10%)
Therapeutic considerations
Pregnancy cat.

B1(AU) C(US)

Legal status

POM(UK) -only(US)

Routes Oral, IV

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 nerve impulses 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 duration by shortening the repolarization phase. This is achieved by blocking sodium channels.

Mexiletine may also be of use in patients experiencing refractory pain. (Sweetman, 2002)

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Antiarrhythmic agents (C01B)edit
class Ia:

Ajmaline, Disopyramide, Prajmaline, Procainamide, Quinidine, Sparteine

class Ib:

Aprindine, Lidocaine, Mexiletine, Tocainide

class Ic:

Encainide, Flecainide, Lorcainide, Moricizine, Propafenone

class II:

Propranolol, Metoprolol, Nadolol, Atenolol, Acebutolol, Pindolol, Sotalol see Beta blockers (C07)

class III:

Amiodarone, Bretylium tosilate, Bunaftine, Dofetilide, Ibutilide

class IV:

Verapamil, Diltiazem see Calcium channel blockers (C08)

class V:

Adenosine, Atropine, Digoxin