Mexiletine

Mexiletine
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Gerald Chi

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Black Box Warning

WARNINGS See full prescribing information for complete Boxed Warning. Mortality: In the National Heart, Lung and Blood Institute’s Cardiac Arrhythmia Suppression Trial (CAST), a long-term, multicentered, randomized, double-blind study in patients with asymptomatic non-life-threatening ventricular arrhythmias who had a myocardial infarction more than six days but less than two years previously, an excessive mortality or non-fatal cardiac arrest rate (7.7%) was seen in patients treated with encainide or flecainide compared with that seen in patients assigned to carefully matched placebo-treated groups (3.0%). The average duration of treatment with encainide or flecainide in this study was ten months. The applicability of the CAST results to other populations (e.g., those without recent myocardial infarction) is uncertain. Considering the known proarrhythmic properties of mexiletine and the lack of evidence of improved survival for any antiarrhythmic drug in patients without life-threatening arrhythmias, the use of mexiletine as well as other antiarrhythmic agents should be reserved for patients with life-threatening ventricular arrhythmia. Acute Liver Injury: In postmarketing experience abnormal liver function tests have been reported, some in the first few weeks of therapy with mexiletine hydrochloride. Most of these have been observed in the setting of congestive heart failure or ischemia and their relationship to mexiletine hydrochloride has not been established.

Overview

Mexiletine is an antiarrhythmic that is FDA approved for the {{{indicationType}}} of ventricular arrhythmias, such as sustained ventricular tachycardia. There is a Black Box Warning for this drug as shown here. Common adverse reactions include heartburn, nausea, vomiting, coordination problem, dizziness, lightheadedness, tremor, blurred vision, visual disturbance, and anxiety.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Ventricular Arrhythmia

• Dosing Information

• The dosage of mexiletine hydrochloride must be individualized on the basis of response and tolerance, both of which are dose-related. Administration with food or antacid is recommended. Initiate mexiletine therapy with 200 mg every eight hours when rapid control of arrhythmia is not essential. A minimum of two to three days between dose adjustments is recommended. Dose may be adjusted in 50 or 100 mg increments up or down.
• As with any antiarrhythmic drug, clinical and electrocardiographic evaluation (including Holter monitoring if necessary for evaluation) are needed to determine whether the desired antiarrhythmic effect has been obtained and to guide titration and dose adjustment.
• Satisfactory control can be achieved in most patients by 200 to 300 mg given every eight hours with food or antacid. If satisfactory response has not been achieved at 300 mg q8h, and the patient tolerates mexiletine well, a dose of 400 mg q8h may be tried. As the severity of CNS side effects increases with total daily dose, the dose should not exceed 1200 mg/day.
• In general, patients with renal failure will require the usual doses of mexiletine hydrochloride. Patients with severe liver disease, however, may require lower doses and must be monitored closely. Similarly, marked right-sided congestive heart failure can reduce hepatic metabolism and reduce the needed dose. Plasma level may also be affected by certain concomitant drugs

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Mexiletine in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Mexiletine in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

• Safety and effectiveness in pediatric patients have not been established.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Mexiletine in pediatric patients.

Non–Guideline-Supported Use

Premature Ventricular Contractions, Ventricular Couplets, or Ventricular Tachycardia Associated with Congenital Heart Disease

• Dosing Information

• 1.4 to 5 mg/kg (mean 3.3 mg/kg) every 8 hours

Contraindications

• Condition1

Warnings

WARNINGS See full prescribing information for complete Boxed Warning. Mortality: In the National Heart, Lung and Blood Institute’s Cardiac Arrhythmia Suppression Trial (CAST), a long-term, multicentered, randomized, double-blind study in patients with asymptomatic non-life-threatening ventricular arrhythmias who had a myocardial infarction more than six days but less than two years previously, an excessive mortality or non-fatal cardiac arrest rate (7.7%) was seen in patients treated with encainide or flecainide compared with that seen in patients assigned to carefully matched placebo-treated groups (3.0%). The average duration of treatment with encainide or flecainide in this study was ten months. The applicability of the CAST results to other populations (e.g., those without recent myocardial infarction) is uncertain. Considering the known proarrhythmic properties of mexiletine and the lack of evidence of improved survival for any antiarrhythmic drug in patients without life-threatening arrhythmias, the use of mexiletine as well as other antiarrhythmic agents should be reserved for patients with life-threatening ventricular arrhythmia. Acute Liver Injury: In postmarketing experience abnormal liver function tests have been reported, some in the first few weeks of therapy with mexiletine hydrochloride. Most of these have been observed in the setting of congestive heart failure or ischemia and their relationship to mexiletine hydrochloride has not been established.

• Description

Precautions

• Description

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Mexiletine in the drug label.

Body as a Whole

Cardiovascular

Digestive

Endocrine

Hematologic and Lymphatic

Metabolic and Nutritional

Musculoskeletal

Neurologic

Respiratory

Skin and Hypersensitivy Reactions

Special Senses

Urogenital

Miscellaneous

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Mexiletine in the drug label.

Body as a Whole

Cardiovascular

Digestive

Endocrine

Hematologic and Lymphatic

Metabolic and Nutritional

Musculoskeletal

Neurologic

Respiratory

Skin and Hypersensitivy Reactions

Special Senses

Urogenital

Miscellaneous

Drug Interactions

• Drug

• Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

• Pregnancy Category

Pregnancy Category (AUS):

• Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Mexiletine in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Mexiletine during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Mexiletine with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Mexiletine with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Mexiletine with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Mexiletine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Mexiletine with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Mexiletine in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Mexiletine in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Mexiletine in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Mexiletine in patients who are immunocompromised.

Administration and Monitoring

Administration

• Oral

• Intravenous

Monitoring

There is limited information regarding Monitoring of Mexiletine in the drug label.

Condition1

• Description

IV Compatibility

There is limited information regarding IV Compatibility of Mexiletine in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

• Description

Management

• Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Mexiletine in the drug label.

Pharmacology

1 : 1 mixture (racemate)Mexiletine
Systematic (IUPAC) name
(RS)-1-(2,6-dimethylphenoxy)propan-2-amine OR 2-(2-aminopropoxy)-1,3-dimethylbenzene
Identifiers
CAS number	31828-71-4
ATC code	C01BB02
PubChem	4178
DrugBank	DB00379
Chemical data
Formula	Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox
Mol. mass	179.259 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	90%
Protein binding	50-60%
Metabolism	Hepatic (CYP2D6 and 1A2- mediated)
Half life	10-12 hours
Excretion	Renal (10%)
Therapeutic considerations
Pregnancy cat.	B1(AU) C(US)
Legal status	POM(UK)
Routes	Oral, IV

Mechanism of Action

Structure

This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Mexiletine in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Mexiletine in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Mexiletine in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Mexiletine in the drug label.

Condition1

• Description

How Supplied

Storage

There is limited information regarding Mexiletine Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Patient Counseling Information of Mexiletine in the drug label.

Precautions with Alcohol

• Alcohol-Mexiletine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

• Mexitil®

Look-Alike Drug Names

• A® — B®

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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