Mexiletine

Mexiletine
Clinical data
AHFS/Drugs.com Monograph
MedlinePlus a607064
Pregnancy
category
  • AU: B1
  • US: C (Risk not ruled out)
    Routes of
    administration    		 Oral, IV
    ATC code
    Legal status
    Legal status
    • UK: POM (Prescription only)
    Pharmacokinetic data
    Bioavailability 90%
    Protein binding 50-60%
    Metabolism Hepatic (CYP2D6 and 1A2- mediated)
    Elimination half-life 10-12 hours
    Excretion Renal (10%)
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    ECHA InfoCard 100.046.190 Edit this at Wikidata
    Chemical and physical data
    Formula C11H17NO
    Molar mass 179.259 g/mol
    3D model (JSmol)
    Chirality Racemic mixture
      (verify)

    Mexiletine (INN) (sold under the trade name Mexitil) is a non-selective voltage-gated sodium channel blocker which belongs to the Class IB anti-arrhythmic group of medicines.[1] 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 depolarization phase. This is achieved by blocking sodium channels.[2]

    This drug is now no longer freely available as a licensed product in the UK, although it remains available for human use in the US. Mexiletine is available to veterinarians in the US for the treatment heart disease in dogs and cats. It can be imported to the UK as an unlicensed, 'named-patient' drug.

    Mexiletine may also be of use in patients experiencing refractory pain[3] 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

    Mexiletine synthesis:[4]

    References

    1. ↑ Sergio Canavero; Vincenzo Bonicalzi (13 October 2011). Central Pain Syndrome: Pathophysiology, Diagnosis and Management. Cambridge University Press. pp. 286–. ISBN 978-1-107-01021-5.
    2. ↑ Mexiletine, RxList.com
    3. ↑ Sweetman S (ed.) (2002). Martindale: The complete drug reference (33rd ed.). London: Pharmaceutical Press. ISBN 0-85369-499-0.
    4. ↑ H. Koppe, W. Kummer, U.S. Patent 3,954,872 (1976).

    Further reading

    • Peck T, Hill S, Williams M, eds. (2004). Pharmacology for Anaesthesia and Intensive Care (2nd ed.). Cambridge University Press. ISBN 0-521-68794-2.



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