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Details

Stereochemistry ACHIRAL
Molecular Formula C22H25N3O4S
Molecular Weight 427.517
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of MORICIZINE

SMILES

CCOC(=O)NC1=CC2=C(SC3=C(C=CC=C3)N2C(=O)CCN4CCOCC4)C=C1

InChI

InChIKey=FUBVWMNBEHXPSU-UHFFFAOYSA-N
InChI=1S/C22H25N3O4S/c1-2-29-22(27)23-16-7-8-20-18(15-16)25(17-5-3-4-6-19(17)30-20)21(26)9-10-24-11-13-28-14-12-24/h3-8,15H,2,9-14H2,1H3,(H,23,27)

HIDE SMILES / InChI

Molecular Formula C22H25N3O4S
Molecular Weight 427.517
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Moricizine is an antiarrhythmic agent previously marketed as Ethmozine. It was used for prophylaxis and treatment of serious and life-threatening ventricular arrhythmias. In 2007 it was withdrawn and discontinued for commercial reasons. Moricizine can be administered intravenously but was more commonly provided as an oral formulation.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
ETHMOZINE

Cmax

ValueDoseCo-administeredAnalytePopulation
0.597 mg/L
300 mg 3 times / day multiple, oral
MORICIZINE blood
Homo sapiens
0.607 mg/L
150 mg 3 times / day multiple, oral
MORICIZINE blood
Homo sapiens
0.6 mg/L
250 mg 3 times / day multiple, oral
MORICIZINE blood
Homo sapiens
0.666 mg/L
200 mg 3 times / day multiple, oral
MORICIZINE blood
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
0.993 mg × h/L
300 mg 3 times / day multiple, oral
MORICIZINE blood
Homo sapiens
1.138 mg × h/L
150 mg 3 times / day multiple, oral
MORICIZINE blood
Homo sapiens
1.21 mg × h/L
250 mg 3 times / day multiple, oral
MORICIZINE blood
Homo sapiens
1.21 mg × h/L
200 mg 3 times / day multiple, oral
MORICIZINE blood
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
1.4 h
300 mg 3 times / day multiple, oral
MORICIZINE blood
Homo sapiens
1.5 h
150 mg 3 times / day multiple, oral
MORICIZINE blood
Homo sapiens
1.4 h
250 mg 3 times / day multiple, oral
MORICIZINE blood
Homo sapiens
1.4 h
200 mg 3 times / day multiple, oral
MORICIZINE blood
Homo sapiens

Doses

AEs

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer








Drug as perpetrator​

PubMed

Sample Use Guides

In Vivo Use Guide
Patients with greater than or equal to 30 ventricular premature complexes (VPCs) per hour were given moricizine HCL (816 +/- 103 mg daily) as a three times oral daily dose. Moricizine suppressed 81% of VPCs alone and 87% of VPCs in combination with 120 mg of propranolol.
Route of Administration: Oral
In Vitro Use Guide
Single ventricular myocytes from guinea-pig hearts were prepared by enzymatic dissociation. Isolated single cells were transferred to a recording chamber of an inverted phase-contrast microscope which was maintained at 34 - 35 deg-C. Membrane currents were recorded by using whole-cell patch-clamp technique using an amplifier. Application of 1O micro-M moricizine was started at 7 minutes and continued up to 13 minutes after the formation of whole cell configuration. In the absence of drug, the current decayed with time and the average value of relative currents at 20 min was 0.48 ± 0.11. In the presence of 10 micro-M moricizine, the tail currents decreased progressively with time and the minimum value of 0.29 was reached at 13 min after rupture of the membrane (or 6 min after the application of moricizine).
Substance Class Chemical
Record UNII
2GT1D0TMX1
Record Status Validated (UNII)
Record Version