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Mexiletine


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	C₁₁H₁₇N O
Mol. mass	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.

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

Mexiletine may also be of use in patients experiencing refractory pain. (Sweetman, 2002) and is also effective for treating muscle stiffness resulting from myotonia congenita (Thomsen disease)

References

Peck T; Hill S, Williams M (eds.) (2004). Pharmacology for Anaesthesia and Intensive Care, 2nd ed., Cambridge University Press. ISBN 0-521-68794-2.
Sweetman S (ed.) (2002). Martindale: The complete drug reference, 33rd ed., London: Pharmaceutical Press. ISBN 0-85369-499-0.

v • d • e Antiarrhythmic agents (C01B)
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 see Beta blockers (C07)
class III	Amiodarone • Bretylium tosylate • Bunaftine • Dofetilide • Ibutilide • Sotalol
class IV	Verapamil • Diltiazem see Calcium channel blockers (C08)
class V	Adenosine • Atropine • Digoxin