Mexiletine

Source: Wikipedia, the free encyclopedia.
Mexiletine
Clinical data
Trade namesMexitil, NaMuscla
AHFS/Drugs.comMonograph
MedlinePlusa607064
License data
Pregnancy
category
  • AU: B1
Routes of
administration		By mouth, intravenous
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability90%
Protein binding50–60%
MetabolismLiver (CYP2D6 and 1A2-mediated)
Elimination half-life10–12 hours
ExcretionKidney (10%)
Identifiers
  • (RS)-1-(2,6-dimethylphenoxy)propan-2-amine
    OR
    2-(2-aminopropoxy)-1,3-dimethylbenzene
JSmol)
ChiralityRacemic mixture
  • O(c1c(cccc1C)C)CC(N)C
  • InChI=1S/C11H17NO/c1-8-5-4-6-9(2)11(8)13-7-10(3)12/h4-6,10H,7,12H2,1-3H3 checkY
  • Key:VLPIATFUUWWMKC-UHFFFAOYSA-N checkY
  (verify)

Mexiletine (

Class IB group of anti-arrhythmic medications.[2]

Medical uses

Mexiletine has several uses including the treatment of abnormal heart rhythms or

arrhythmias, chronic pain, and myotonia
.

In general when treating arrhythmias, mexiletine is reserved for use in dangerous heart rhythm disturbances such as ventricular tachycardia.[3] It is of particular use when treating arrhythmias caused by long QT syndrome.[4] The LQT3 form of long QT syndrome is amenable to treatment with mexiletine as this form is caused by defective sodium channels that continue to release a sustained current rather than fully inactivating, however other forms of long QT syndrome can also be treated with this medication.[4]

Mexiletine has been used to treat chronic pain and may also be used to treat muscle stiffness resulting from myotonic dystrophy (Steinert's disease) or nondystrophic myotonias such as myotonia congenita (Thomsen syndrome or Becker syndrome).[5][6]

Adverse effects

Common side effects of mexiletine include abdominal pain, chest discomfort, drowsiness, headache, nausea and skin reactions.[7] Uncommon or rare side effects include seizures and liver dysfunction.[7]

Pharmacology

Mexiletine is an oral analogue of

creatinine clearance falls below 10 mL/minute.[3]

Synthesis

Mexiletine synthesis:[8]

Society and culture

Mexiletine is available for human use in the US, and has been reintroduced in the UK as a licensed product, having previously only been available as a 'named patient' import. The drug is sold under the trade name Mexitil for use in arrhythmias and NaMuscla for use in myotonia.[9][10]

Veterinary uses

Mexiletine is available to veterinarians in the US for the treatment of heart disease in dogs and cats.[

Boxer dogs in combination with sotalol.[medical citation needed
]

References

  1. ^ "Product monograph brand safety updates". Health Canada. February 2024. Retrieved 24 March 2024.
  2. ISBN 978-1-107-01021-5
    .
  3. ^
    S2CID 269453
    .
  4. ^
    S2CID 54167081
    .
  5. S2CID 52917253
    .
  6. ^
    ISBN 0-85369-499-0
    .
  7. ^ a b "Mexiletine". British National Formulary. NICE. Retrieved 2019-06-17.
  8. ^ US 3954872, Koppe R, Kummer W, "1-(2{40 ,6{40 -Dimethyl-phenoxy)-2-amino-alkanes and salts thereof", issued 1976, assigned to Boehringer Sohn Ingelheim. 
  9. ^ "Mexiletine". www.drugbank.ca. Retrieved 2019-06-17.
  10. ^ "Lupin announces launch of NaMuscla". www.biospectrumindia.com. Retrieved 2019-06-17.

Further reading

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