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QuickView for Moricizine (compound)

Name: Moricizine
PubChem Compound ID: 34632
Description: An antiarrhythmia agent used primarily for ventricular rhythm disturbances.
Molecular formula: C22H26ClN3O4S
Molecular weight: 463.978 g/mol
Moricizine; EN 313; E-350; Ethyl 10-(3-morpholinopropionyl)phenothiazine-2-carbamate hydrochloride; (10-(3-(4-Morpholinyl)-1-oxopropyl)-10H-phenothiazin-2-yl)carbamic acid, ethyl ester, monohydrochloride; Ethyl ether of 10-(beta-morpholylpropionyl)phenthiazinecarbamino acid hydrochloride; E-313; D02087; SMR000036736; 29560-58-5.
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Name: Moricizine
Name (isomeric): DB00680
Drug Type: small molecule
Description: An antiarrhythmia agent used primarily for ventricular rhythm disturbances.
Moracizina [INN-Spanish]; Moracizine; Moracizinum [INN-Latin]
Brand: Ethmozine
Category: Anti-Arrhythmia Agents
CAS number: 31883-05-3
Indication: Used to treat irregular heartbeats (arrhythmias) and maintain a normal heart rate.
Moricizine is used to treat irregular heartbeats (arrhythmias) and to maintain a normal heart rate. It acts on the heart muscle to improve the heart's rhythm. Moricizine has potent local anesthetic activity and membrane stabilizing effect. Decreases excitability, conduction velocity, and automaticity as a result of slowed atrioventricular (AV) noda...
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Mechanism of Action: Moricizine works by inhibiting the rapid inward sodium current across myocardial cell membranes.
Absorption: Well absorbed, absorption is complete within 2 to 3 hours. Significant first-pass metabolism results in an absolute bioavailability of approximately 38%. Administration within 30 minutes after a meal slows the rate, but does not affect the extent of absorption, although peak plasma concentrations are reduced.
Protein binding: Approximately 95%.
Biotransformation: Hepatic and extensive, to at least 26 metabolites, none accounting for as much as 1% of the administered dose. Two metabolites may be pharmacologically active but are present in extremely small quantities. Moricizine induces its own metabolism (it induces hepatic cytochrome P-450 activity).
Route of elimination: Less than 1% of orally administered Ethmozine® is excreted unchanged in the urine. Approximately 56% of the administered dose is excreted in the feces and 39% is excreted in the urine.
Half Life: 2 hours (range 1.5-3.5 hours).
Toxicity: Symptoms of overdose include vomiting, unconsciousness, and severe low blood pressure.
Affected organisms: Humans and other mammals
Drug interaction:
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of moricizine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of moricizine if voriconazole is initiated, discontinued or dose changed.
DiltiazemIncreased effect/toxicity of moricizine
TelithromycinTelithromycin may reduce clearance of Moricizine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Moricizine if Telithromycin is initiated, discontinued or dose changed.
RanolazinePossible additive effect on QT prolongation