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mexiletine (Rx)Brand and Other Names:

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 150mg
  • 200mg
  • 250mg
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Ventricular Arrhythmias (Life-Threatening)

200-300 mg PO TID

May increase to 400 mg q8hr

No more than 1200 mg/day

Take with food or antacid

Therapeutic range: 0.5-2 mg/L

Organ Transplant Rejection (Orphan)

Prevention of acute and chronic rejection in patients who have received solid organ transplants

Orphan indication sponsor

  • James W Williams, MD; Rush-Presbyterian-St. Luke's Medical Ctr, Dept o, 1653 West Congress Parkway; Chicago, IL 60612-3833

Myotonia (Orphan)

Treatment of nondystrophic myotonia

Orphan indication sponsor

  • University of Rochester Medical Center; 1351 Mt. Hope Ave, Suite 203; Rochester, NY 14620

Renal Impairment

Clcr<10 mL/min: 50-75% of normal dose

Hepatic Impairment

25-30% of normal dose

Other Indications & Uses

Life-threatening ventr arrhythmias

Off-label: Prophylaxis of vent. arrhythmias in acute phase MI (no change in mortality)

Not FDA approved

Usual dose for arrhythmias: 2.5-5 mg/kg PO q8hr

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Interactions

Interaction Checker

mexiletine and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Nausea (40%)

            Vomiting (40%)

            Heartburn (40%)

            Ataxia (20%)

            Dizziness (19%)

            Lightheadedness (19%)

            Tremor (13%)

            1-10%

            Coordination difficulties (10%)

            Palpitation (4-7%)

            Hypotension (4-7%)

            Blurred vision (6%)

            Frequency Not Defined

            Angina

            Edema

            Exacerbation of CHF

            Puilmonary fibrosis

            Proarrhythmia

            Convulsions

            Rash

            Dry mouth

            Mouth sores

            Dyspnea

            Tinnitus

            Systemic lupus erythematosus

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            Warnings

            Black Box Warnings

            National Heart, Lung, and Blood Institute's Cardiac Arrhythmia Suppression Trial (CAST): Excessive mortality or nonfatal cardiac arrest (7.7%) shown with encainide or flecainide compared with placebo (3%)

            CAST was a long-term, multicenter, randomized, double-blind study in patients with asymptomatic non-life-threatening ventricular arrhythmias who had a myocardial infarction (MI) >6 days but <2 yr previously

            Average duration of treatment w/ encainide or flecainide in CAST was 10 months

            Applicability of CAST results to other populations (eg, patients without recent MI) is uncertain

            Reserve use of Class IC antiarrhythmics for life-threatening ventricular arrhythmias: Considering the known proarrhythmic properties of mexiletine & lack of evidence of improved survival for any antiarrhythmic drug in patients without life-threatening arrhythmias, mexiletine use, as well as other antiarrhythmic agents, should be reserved for patients with life-threatening ventricular arrhythmias

            Contraindications

            Hypersensitivity to mexiletine

            Cardiogenic shock, 2°/3° AV block w/o pacemaker

            Cautions

            CHF, hypotension, history of seizures

            Use in less severe arrhythmias not recommended; avoid in Tx of asymptomatic ventricular premature contractions

            Hepatic dz, seizure disorders, pregnancy

            Good for automatic and reentrant arrhythmias, not PSVT's

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: enters breast milk at concs comparable to maternal plasma (AAP Committee states compatible w/ nursing)

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Half-Life: 6-17 hr

            Peak Plasma Time: 1-4 hr (PO)

            Therapeutic range: 0.5-2 mcg/mL

            Toxicity range: >2 mcg/mL

            Other Information

            Bioavailability: 80-90%

            Protein Bound: 50-70%

            Vd: 5-9 L/kg

            Metabolism: in liver to form parahydroxymexiletine & 2-hydroxymexiletine mainly by hepatic P450 enzyme CYP2D6 & partially by CYP1A2

            Metabolites: parahydroxymexiletine & 2-hydroxymexiletine (inactive)

            Excretion: urine 8-15%

            Dialyzable: HD: no; PD: no

            Mechanism of Action

            Class 1B antidysrhythmic; combines with fast Na channels & thereby inhibits recovery after repolarization resulting in decreasing myocardial excitsbility & conduction velocity

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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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