|Accession Number||DB00680 (APRD01124)|
An antiarrhythmia agent used primarily for ventricular rhythm disturbances. [PubChem]
|External IDs||EN-313 / G 214|
|Approved Prescription Products||Not Available|
|Approved Generic Prescription Products||Not Available|
|Approved Over the Counter Products||Not Available|
|Unapproved/Other Products||Not Available|
|Brand mixtures||Not Available|
|Weight||Average: 427.517 |
Used to treat irregular heartbeats (arrhythmias) and maintain a normal heart rate.
|Structured Indications||Not Available|
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) nodal and His-Purkinje conduction. Decreases the action potential duration (APD) in Purkinje fibers; also decreases the effective refractory period (ERP) but to a lesser extent than the APD, so the ERP/APD ratio is increased. Decreases the maxiumum rate of Phase 0 depolarization (V max ), but does not affect action potential amplitude or maximum diastolic potential. Does not affect atrial, AV nodal, or left ventricular refractory periods and has minimal effect on ventricular repolarization (evidenced by the overall decrease in JT interval). Has no effect on sinoatrial (SA) nodal or intra-atrial conduction and only minimal effect on sinus cycle length and sinus node recovery time. In the Vaughan Williams classification of antiarrhythmics, moricizine is considered to be a class I agent. It has properties of class IA, IB, and IC agents but does not clearly belong to any of the three subclasses. It has less effect on the slope of phase 0 and a greater effect on action potential duration and effective refractory period than class IC agents.
|Mechanism of action|
Moricizine works by inhibiting the rapid inward sodium current across myocardial cell membranes.
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.
|Volume of distribution|
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.
2 hours (range 1.5-3.5 hours).
Symptoms of overdose include vomiting, unconsciousness, and severe low blood pressure.
|Pharmacogenomic Effects/ADRs||Not Available|
|Food Interactions||Not Available|
|General References||Not Available|
|ATC Codes||C01BG01 — Moracizine|
|AHFS Codes||Not Available|
|PDB Entries||Not Available|
|FDA label||Not Available|
|Dosage forms||Not Available|
|Predicted ADMET features|
|Mass Spec (NIST)||Not Available|
|Description||This compound belongs to the class of chemical entities known as phenothiazines. These are polycyclic aromatic compounds containing a phenothiazine moiety, which is a linear tricyclic system that consists of a two benzene rings joined by a para-thiazine ring.|
|Super Class||Organic compounds|
|Alternative Parents||Diarylthioethers / Beta amino acids and derivatives / 1,4-thiazines / Morpholines / Benzenoids / Tertiary carboxylic acid amides / Trialkylamines / Propargyl-type 1,3-dipolar organic compounds / Oxacyclic compounds / Azacyclic compounds / Dialkyl ethers / Carboximidic acids and derivatives / Carbonyl compounds / Hydrocarbon derivatives / Organic oxides / Organopnictogen compounds|
|Substituents||Phenothiazine / Beta amino acid or derivatives / Diarylthioether / Aryl thioether / Para-thiazine / Morpholine / Oxazinane / Benzenoid / Tertiary carboxylic acid amide / Amino acid or derivatives/ Carboxamide group / Tertiary amine / Tertiary aliphatic amine / Carboximidic acid derivative / Carboxylic acid derivative / Dialkyl ether / Ether / Oxacycle / Azacycle / Organic 1,3-dipolar compound / Propargyl-type 1,3-dipolar organic compound / Thioether / Organic oxygen compound / Hydrocarbon derivative / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Carbonyl group / Organic nitrogen compound / Organic oxide / Amine / Aromatic heteropolycyclic compound|
|Molecular Framework||Aromatic heteropolycyclic compounds|
|External Descriptors||phenothiazines, carbamate ester, morpholines (CHEBI:6997 )|
- Pharmacological action
- General Function:
- Voltage-gated sodium channel activity involved in sa node cell action potential
- Specific Function:
- This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant Na(+) channel isoform. This channel is respon...
- Gene Name:
- Uniprot ID:
- Molecular Weight:
- 226937.475 Da
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