Mexiletine

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Mexiletine
Systematic (IUPAC) name
(RS)-1-(2,6-dimethylphenoxy)propan-2-amine
OR
2-(2-aminopropoxy)-1,3-dimethylbenzene
Clinical data
AHFS/Drugs.commonograph
MedlinePlusa607064
Pregnancy cat.B1 (AU) C (US)
Legal statusPOM (UK)
RoutesOral, IV
Pharmacokinetic data
Bioavailability90%
Protein binding50-60%
MetabolismHepatic (CYP2D6 and 1A2- mediated)
Half-life10-12 hours
ExcretionRenal (10%)
Identifiers
CAS number31828-71-4 YesY
ATC codeC01BB02
PubChemCID 4178
IUPHAR ligand2629
DrugBankDB00379
ChemSpider4034 YesY
UNII1U511HHV4Z YesY
KEGGD08215 YesY
ChEBICHEBI:6916 YesY
ChEMBLCHEMBL558 YesY
Chemical data
FormulaC11H17NO 
Mol. mass179.259 g/mol
 YesY (what is this?)  (verify)
 
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Mexiletine
Systematic (IUPAC) name
(RS)-1-(2,6-dimethylphenoxy)propan-2-amine
OR
2-(2-aminopropoxy)-1,3-dimethylbenzene
Clinical data
AHFS/Drugs.commonograph
MedlinePlusa607064
Pregnancy cat.B1 (AU) C (US)
Legal statusPOM (UK)
RoutesOral, IV
Pharmacokinetic data
Bioavailability90%
Protein binding50-60%
MetabolismHepatic (CYP2D6 and 1A2- mediated)
Half-life10-12 hours
ExcretionRenal (10%)
Identifiers
CAS number31828-71-4 YesY
ATC codeC01BB02
PubChemCID 4178
IUPHAR ligand2629
DrugBankDB00379
ChemSpider4034 YesY
UNII1U511HHV4Z YesY
KEGGD08215 YesY
ChEBICHEBI:6916 YesY
ChEMBLCHEMBL558 YesY
Chemical data
FormulaC11H17NO 
Mol. mass179.259 g/mol
 YesY (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 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[2] and is also effective for treating muscle stiffness resulting from myotonia congenita (Thomsen disease) or myotonic dystrophy (Steinert's disease).

References

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

Further reading

External links