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Open Access Articles- Top Results for Mexiletine

Mexiletine

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Mexiletine
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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
  • AU: B1
  • US: C (Risk not ruled out)
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
31828-71-4 7pxY
C01BB02
PubChem CID 4178
IUPHAR ligand 2629
DrugBank DB00379 7pxY
ChemSpider 4034 7pxY
UNII 1U511HHV4Z 7pxY
KEGG D08215 7pxY
ChEBI CHEBI:6916 7pxY
ChEMBL CHEMBL558 7pxY
Chemical data
Formula C11H17NO
179.259 g/mol
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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. Its use in arrhythmias 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).

Synthesis

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. 
  3. ^ H. Koppe, W. Kummer, U.S. Patent 3,954,872 (1976).
  4. ^ H. Koppe, W. Kummer, U.S. Patent 3,659,019 (1972).
  5. ^ C.H. Boehringer Sohns, Fr 1551055  (1968).
  6. ^ H. Koppe, W. Kummer, U.S. Patent 4,031,244 (1977).

Further reading

External links


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