Class
- Antiarrhythmic
Mexiletine
Commonly Prescribed for
(FDA approved in bold)
- Cardiac arrhythmias
- Symptomatic myotonia (myotonia congenita, myotonic dystrophy)
- Pain in peripheral neuropathy
- Intractable headache
Mexiletine
How the Drug Works
- Class 1B antiarrhythmic agent that depresses phase 0 (reduces the rate of rise of the action potential). An oral analogue of lidocaine. It has actions on surfaces and membranes of skeletal muscle and neuronal sodium-channel blocking properties. It also reduces the effective refractory period in Purkinje fibers
Mexiletine
How Long Until It Works
- Antiarrhythmic effect will occur within hours, although it may take time to find optimal dose. May take more time (days or weeks) to see relief and determine most effective dose in myotonia or pain disorders
Mexiletine
If It Works
- Continue to use with appropriate monitoring
Mexiletine
If It Doesn’t Work
- Check serum levels and if not effective change to an alternative agent
Mexiletine
Best Augmenting Combos for Partial Response or Treatment-Resistance
- Myotonia: Quinine and other anticonvulsants are occasionally used. Phenytoin is also effective but has similar antiarrhythmic properties and may interact with mexiletine
- Neuropathic pain: other anticonvulsants and antidepressants can be used
Mexiletine
Tests
- Monitor hepatic enzymes and CBC during therapy. Obtain ECG at baseline and for any new symptoms. Check a serum mexiletine level to guide therapy and for any AEs
Adverse Effects (AEs)
Mexiletine
How Drug Causes AEs
- Drug effect blocking sodium channels
Mexiletine
Notable AEs
- GI AEs (nausea, vomiting, heartburn) are most common. CNS AEs (tremor, nervousness, coordination difficulties, blurred vision, confusion) are much more common when serum levels exceed 2 mcg/mL
Mexiletine
Life-Threatening or Dangerous AEs
- New or worsening cardiac arrhythmias
- Acute hepatic injury (usually in the first few weeks of therapy)
- Blood dyscrasias, including leukopenia (rare)
Mexiletine
Weight Gain
- Unusual
Mexiletine
Sedation
- Not unusual
Mexiletine
What to Do About AEs
- Check serum level and ECG. For serious AEs, discontinue drug