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Pronunciation |
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(mor
I siz
een) |
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U.S. Brand
Names |
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Ethmozine® |
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Generic
Available |
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No |
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Synonyms |
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Moricizine Hydrochloride |
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Pharmacological Index |
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Antiarrhythmic Agent, Class I |
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Use |
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For treatment of ventricular tachycardia and life-threatening ventricular
arrhythmias |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to moricizine or any component; pre-existing second- or
third-degree AV block (except in patients with a functioning artificial
pacemaker); right bundle branch block when associated with left hemiblock or
bifascicular block (unless functional pacemaker in place); cardiogenic
shock |
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Warnings/Precautions |
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Can be proarrhythmic; watch for new rhythm disturbances or existing
arrhythmias that worsen. Use cautiously in CAD, previous history of MI, CHF, and
cardiomegaly. The CAST II trial demonstrated a decreased trend in survival for
patients receiving moricizine. Dose-related increases in PR and QRS intervals
occur. Use cautiously in patients with pre-existing conduction abnormalities,
and significant hepatic impairment. Safety and efficacy have not been
established in pediatric patients. |
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Adverse
Reactions |
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>10%: Central nervous system: Dizziness
1% to 10%:
Cardiovascular: Proarrhythmia, palpitations, cardiac death, EKG
abnormalities, congestive heart failure
Central nervous system: Headache, fatigue, insomnia
Endocrine & metabolic: Decreased libido
Gastrointestinal: Nausea, diarrhea, ileus
Ocular: Blurred vision, periorbital edema
Respiratory: Dyspnea
<1% (Limited to important or life-threatening symptoms): Ventricular
tachycardia, cardiac chest pain, hypotension or hypertension, syncope,
supraventricular arrhythmias, myocardial infarction, apnea |
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Overdosage/Toxicology |
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Has a narrow therapeutic index and severe toxicity may occur slightly above
the therapeutic range, especially if combined with other antiarrhythmic drugs.
(Acute single ingestion of twice the daily therapeutic dose is
life-threatening). Symptoms of overdose include increases in P-R, QRS, Q-T
intervals and amplitude of the T wave, A-V block, bradycardia, hypotension,
ventricular arrhythmias (monomorphic or polymorphic ventricular tachycardia),
and asystole; other symptoms include dizziness, blurred vision, headache, and GI
upset.
Treatment is supportive, using conventional treatment (fluids, positioning,
anticonvulsants, antiarrhythmics). Note: Type Ia antiarrhythmic agents
should not be used to treat cardiotoxicity caused by type 1c drugs; sodium
bicarbonate may reverse QRS prolongation, bradycardia and hypotension;
ventricular pacing may be needed. |
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Drug
Interactions |
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Cimetidine increases moricizine levels by 50%.
Digoxin may result in additive prolongation of the PR interval when combined
with moricizine (but not rate of second- and third-degree A-V block).
Diltiazem increases moricizine levels resulting in an increased incidence of
side effects. Moricizine decreases diltiazem plasma levels and decreases its
half-life.
Drugs which may prolong QT interval (including cisapride, erythromycin,
phenothiazines, cyclic antidepressants, and some quinolones) are contraindicated
with Type Ia antiarrhythmics. Moricizine has some Type Ia activity, and caution
should be used.
Theophylline levels are decreased by 50% with moricizine due to increased
clearance. |
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Mechanism of
Action |
|
Class I antiarrhythmic agent; reduces the fast inward current carried by
sodium ions, shortens Phase I and Phase II repolarization, resulting in
decreased action potential duration and effective refractory
period |
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Pharmacodynamics/Kinetics |
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Protein binding, plasma: 95%
Metabolism: Undergoes significant first-pass metabolism absolute
Bioavailability: 38%
Half-life: Normal patients: 3-4 hours; Cardiac disease patients: 6-13 hours
Elimination: Some enterohepatic recycling occurs; 56% is excreted in feces
and 39% in urine |
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Usual Dosage |
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Adults: Oral: 200-300 mg every 8 hours, adjust dosage at 150 mg/day at 3-day
intervals.
When transferred from encainide, propafenone, tocainide, or mexiletine: Start
Ethmozine® 8-12 hours after last dose
When transferred from flecainide: Start Ethmozine®
12-24 hours after last dose
When transferred from procainamide: Start Ethmozine®
3-6 hours after last dose
When transferred from quinidine or disopyramide: Start
Ethmozine® 6-12 hours after last dose
Dosing interval in renal or hepatic impairment: Start at 600 mg/day
or less. |
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Dietary
Considerations |
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Food delays absorption; best if taken on an empty
stomach |
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Cardiovascular
Considerations |
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This Class Ic antiarrhythmic agent was associated with a trend toward
increased mortality in the CAST trial and therefore should not be used in
patients with cardiovascular disease. Although moricizine was effective in
suppressing asymptomatic ventricular arrhythmias in patients after myocardial
infarction, it was accompanied by increased mortality. Cardiotoxic arrhythmic
effects of moricizine and other Class Ic drugs should not be treated using Class
Ia antiarrhythmics. |
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Mental Health: Effects
on Mental Status |
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Dizziness is common; may cause sedation or insomnia; may rarely cause
anxiety, confusion, amnesia |
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Mental Health:
Effects on Psychiatric
Treatment |
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Use caution with TCAs may produce Q-T prolongation |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Take exactly as directed; do not take additional doses or discontinue without
consulting prescriber. You will need regular cardiac checkups and blood tests
while taking this medication. You may experience dizziness or visual changes
(use caution when driving or engaging in tasks requiring alertness until
response to drug is known); nausea or vomiting (small frequent meals, frequent
mouth care, chewing gum, or sucking lozenges may help); or headaches, sleep
disturbances, or decreased libido (usually temporary, if persistent consult
prescriber). Report chest pain, palpitation, or erratic heartbeat; increased
weight or swelling of hands or feet; blurred vision or facial swelling; acute
diarrhea; changes in bowel or bladder patterns; or difficulty breathing.
Breast-feeding precautions: Breast-feeding is not
recommended. |
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Nursing
Implications |
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Administering 30 minutes after a meal delays the rate of absorption,
resulting in lower peak plasma concentrations |
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Dosage Forms |
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Tablet, as hydrochloride: 200 mg, 250 mg, 300 mg |
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References |
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