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mexiletine
generic
Black Box Warnings .
Increased Mortality
excessive mortality or nonfatal cardiac arrest rate (7.7% encainide/flecainide vs. 3% placebo) in asymptomatic non-life-threatening ventricular arrhythmias with MI 6 days - 2 years prior; restrict use to life-threatening ventricular arrhythmias, no survival benefit in patients without life-threatening arrhythmias
Adult Dosing .
Dosage forms: CAP: 150 mg, 200 mg, 250 mg
ventricular arrhythmias
- [200 mg PO q8h]
- Alt: 450 mg PO q12h; Info: rarely indicated, consult cardiologist
neuropathic pain, diabetic (off-label)
- [10 mg/kg/dose PO qd]
- Start: 150 mg PO qd x3 days then 300 mg PO qd x3 days then 10 mg/kg/dose PO qd; Info: not 1st-line tx
renal dosing
- [no adjustment]
- renal impairment: no adjustment
- HD: no adjustment, on dialysis days administer after dialysis; consider supplement if next maintenance dose not due right after dialysis; PD: no adjustment; no supplement
hepatic dosing
- [adjust dose amount]
- hepatic impairment: decr. usual dose, amount not defined
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- cardiogenic shock
- caution: AV block, 1st degree
- caution: hepatic impairment
- caution: seizure disorder
- caution: smoking habit change
Drug Interactions .
Overview
mexiletine
antiarrhythmic, class Ib
- CYP1A2 substrate
- CYP2D6 substrate
- CYP1A2 inhibitor, moderate
- affected by altered gastrointestinal motility
- binds to polyvalent cations
- lowers seizure threshold
- urine pH sensitive
Contraindicated
- fezolinetant
Avoid/Use Alternative
- acetazolamide
- aldesleukin
- alosetron
- aluminum hydroxide
- amifampridine
- ascorbic acid (vitamin C)
- bendamustine
- benzoic acid
- calcium carbonate
- dichlorphenamide
- flecainide
- iohexol
- magnesium carbonate
- magnesium hydroxide
- methazolamide
- metolazone
- pirfenidone
- potassium acid phosphate
- potassium citrate
- rose hip
- sodium acid phosphate
- sodium bicarbonate
- sodium citrate
- sotalol
- tizanidine
- topiramate
- viloxazine
- vorasidenib
- zonisamide
Monitor/Modify Tx
- aminophylline
- bupropion
- caffeine citrate
- carbamazepine
- cimetidine
- ciprofloxacin
- clozapine
- cobicistat
- dacomitinib
- darunavir
- enasidenib
- epinephrine
- etravirine
- exenatide
- fluoxetine
- fluvoxamine
- fosphenytoin
- iopamidol
- leflunomide
- lidocaine
- lixisenatide
- magnesium citrate
- magnesium oxide
- magnesium supplement
- mavacamten
- mavorixafor
- paroxetine
- phenytoin
- pomalidomide
- pramlintide
- propafenone
- propranolol
- quinapril
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- rasagiline
- rifampin
- ritonavir
- ropinirole
- St. John's wort
- sucralfate
- sulfate bowel prep
- terbinafine
- teriflunomide
- theophylline
- triclabendazole
- warfarin
Caution Advised
- aclidinium inhaled
- alfentanil
- amantadine
- amitriptyline
- amoxapine
- atropine
- belladonna alkaloids
- benztropine
- bremelanotide
- brivaracetam
- brompheniramine
- buprenorphine
- busulfan
- butorphanol
- caffeine
- cannabidiol
- carbinoxamine
- cenobamate
- chlophedianol
- chlorambucil
- chlorcyclizine
- chlorpheniramine
- chlorpromazine
- cisapride
- clemastine
- clidinium
- clobazam
- clomipramine
- clonazepam
- clorazepate
- codeine
- cyclobenzaprine
- cyproheptadine
- darifenacin
- desipramine
- dexbrompheniramine
- dexchlorpheniramine
- diazepam
- dicyclomine
- difenoxin
- dihydrocodeine
- dimenhydrinate
- diphenhydramine
- diphenoxylate
- disopyramide
- domperidone
- doxepin
- doxepin topical
- doxylamine
- dulaglutide
- duloxetine
- erythromycin
- eslicarbazepine acetate
- ethosuximide
- felbamate
- fenfluramine
- fentanyl
- fesoterodine
- flavoxate
- fluphenazine
- gabapentin
- ganaxolone
- glycopyrrolate
- glycopyrronium topical
- homatropine
- hydrocodone
- hydromorphone
- hydroxychloroquine
- hydroxyzine
- hyoscyamine
- imipramine
- ipratropium inhaled
- lacosamide
- lamotrigine
- levetiracetam
- levorphanol
- lidocaine topical
- liraglutide
- loperamide
- lorazepam
- loxapine
- meclizine
- melatonin
- meperidine
- methadone
- methscopolamine
- methsuximide
- metoclopramide
- midazolam
- mirtazapine
- molindone
- morphine
- nalbuphine
- nortriptyline
- olanzapine
- oliceridine
- opium
- orforglipron
- orphenadrine
- oxcarbazepine
- oxybutynin
- oxycodone
- oxymorphone
- pentazocine
- perampanel
- perphenazine
- pheniramine
- phenobarbital
- pimozide
- polyethylene glycol
- polyethylene glycol/electrolytes
- pregabalin
- prilocaine topical
- primidone
- prochlorperazine
- promethazine
- protriptyline
- pyrilamine
- quetiapine
- ramelteon
- remifentanil
- riluzole
- roflumilast
- roflumilast topical
- rufinamide
- scopolamine
- sodium picosulfate
- sofpironium topical
- solifenacin
- stiripentol
- sufentanil
- tapentadol
- tetracaine
- thioridazine
- thiothixene
- tiagabine
- tiotropium inhaled
- tirzepatide
- tolterodine
- tramadol
- treosulfan
- trifluoperazine
- trihexyphenidyl
- trimipramine
- triprolidine
- trospium
- valproic acid
- vigabatrin
- zolmitriptan
Adverse Reactions .
Serious Reactions
- ventricular arrhythmia
Common Reactions
- dyspepsia
- dizziness
- tremor
- impaired coordination
- insomnia
- diarrhea
- palpitations
- nervousness
- headache
- tinnitus
- depression
- rash
- dyspnea
- xerostomia
- arthralgia
- fever
- anorexia
- angina
- fatigue
Safety/Monitoring .
Therapeutic Drug Levels
0.5-2 mcg/mL; Toxic Levels: >2 mcg/mL; Timing: <2h before next dose; Time to Steady State: 4-5h; Info: consider levels if hepatic impairment
Monitoring Parameters
Cr, electrolytes at baseline; ECG
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; risk of fetal harm not expected based on limited human data; no known risk of teratogenicity, though risk of fetal death based on animal data at 4x MRHD
Lactation
Clinical Summary
weigh risk/benefit while breastfeeding; no known risk of infant harm based on limited human data and drug properties; no human data available to assess effects on milk production
Pharmacology .
Metabolism: for mexiletine: liver; CYP450: 1A2, 2D6 (primary) substrate
Excretion: for mexiletine: urine (10% unchanged); Half-life: 10-12h, 15.7h (CrCl <10), 25h (severe hepatic impairment)
Subclass: Antiarrhythmics, Oral ; Neuropathy/Neuralgia
Mechanism of Action
for mexiletine: stabilizes membranes; depresses action potential phase 0 (class Ib antiarrhythmic)
Formulary .
No Formulary Selected
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