ETHMOZINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ETHMOZINE (ETHMOZINE).
Class Ic antiarrhythmic; blocks cardiac sodium channels, slowing phase 0 depolarization and reducing conduction velocity in atrial and ventricular myocardium.
| Metabolism | Hepatic via CYP3A4; active metabolites include moricizine sulfoxide. |
| Excretion | Primarily hepatic metabolism; renal excretion of unchanged drug accounts for <1% of a dose; approximately 10-20% excreted in feces via bile. |
| Half-life | 3-12 hours (mean ~6 hours); prolonged in hepatic or renal impairment. |
| Protein binding | Approximately 85% bound to albumin. |
| Volume of Distribution | 4-11 L/kg (mean ~7 L/kg); large Vd indicates extensive tissue binding. |
| Bioavailability | Oral: approximately 30-40% due to significant first-pass metabolism; IV: 100%. |
| Onset of Action | Oral: 1-2 hours; IV: within minutes. |
| Duration of Action | Oral: 6-12 hours; IV: 4-8 hours. Effect correlates with dosing interval due to active metabolites. |
200-300 mg orally every 8 hours; maximum 900 mg/day.
| Dosage form | TABLET |
| Renal impairment | GFR 30-59 mL/min: 200-250 mg every 8 hours; GFR 10-29 mL/min: 200-300 mg every 12 hours; GFR <10 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25-50%; Child-Pugh C: contraindicated. |
| Pediatric use | Not established; use not recommended in pediatric patients. |
| Geriatric use | Start at lower end of dosing range (200 mg every 8 hours); monitor for QT prolongation and bradycardia. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ETHMOZINE (ETHMOZINE).
| Breastfeeding | Excretion into human breast milk is unknown. M/P ratio not established. Due to potential for serious adverse effects in nursing infants (e.g., cardiac arrhythmias), manufacturers advise cautious use or avoid breastfeeding during therapy. |
| Teratogenic Risk | Ethmozine (moracizine) is classified as FDA Pregnancy Category C. Animal studies have not been conducted; however, it is presumed to cross the placenta. First trimester: Risk cannot be ruled out; potential for teratogenic effects based on class (antiarrhythmic). Second and third trimesters: May cause fetal bradycardia, arrhythmias, or hypoxia due to maternal hemodynamic changes. Use only if benefit outweighs risk. |
■ FDA Black Box Warning
None designated.
| Serious Effects |
["Cardiogenic shock","Pre-existing second- or third-degree AV block (unless pacemaker)","Severe sinus node dysfunction","Hypersensitivity to moricizine or related compounds"]
| Precautions | ["Proarrhythmic effects (including new or worsened ventricular arrhythmias)","Heart block","Bradycardia","Hypotension","Liver function abnormalities","CNS effects (dizziness, headache)"] |
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| Fetal Monitoring | Monitor maternal ECG, heart rate, blood pressure, and electrolyte levels. Assess fetal heart rate and rhythm via non-stress test or biophysical profile if used in third trimester. Consider periodic fetal echocardiography for signs of arrhythmia or hydrops. |
| Fertility Effects | No human data on fertility impairment. In animal studies, no adverse effects on fertility were observed. Theoretical risk due to hormonal or hemodynamic alterations, but not well-studied. |