Tìm theo
Moricizine
Các tên gọi khác (11 ) :
  • [10-(3-Morpholin-4-yl-propionyl)-10H-phenothiazin-2-yl]-carbamic acid ethyl ester
  • EN-313
  • Ethmozin
  • Ethyl 10-(3-morpholinopropionyl)phenothiazine-2-carbamate
  • Ethyl 10-(beta-N-morpholinylpropionyl)phenothiazine-2-carbamate
  • Etmozin
  • Moracizin
  • Moracizina
  • Moracizine
  • Moracizinum
  • Moricizine
Thuốc chống loạn nhịp
Thuốc Gốc
Small Molecule
CAS: 31883-05-3
ATC: C01BG01
ĐG : Bristol-Myers Squibb Co. , http://www.bms.com
CTHH: C22H25N3O4S
PTK: 427.517
An antiarrhythmia agent used primarily for ventricular rhythm disturbances. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H25N3O4S
Phân tử khối
427.517
Monoisotopic mass
427.156576993
InChI
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)
InChI Key
InChIKey=FUBVWMNBEHXPSU-UHFFFAOYSA-N
IUPAC Name
ethyl N-{10-[3-(morpholin-4-yl)propanoyl]-10H-phenothiazin-2-yl}carbamate
Traditional IUPAC Name
moricizine
SMILES
CCOC(=O)NC1=CC2=C(SC3=CC=CC=C3N2C(=O)CCN2CCOCC2)C=C1
Độ tan chảy
156-157 °C
Độ hòa tan
0.457 mg/L
logP
2.98
logS
-4.1
pKa (strongest acidic)
12.9
pKa (Strongest Basic)
6.73
PSA
71.11 Å2
Refractivity
118.88 m3·mol-1
Polarizability
45.27 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : An antiarrhythmia agent used primarily for ventricular rhythm disturbances. [PubChem] Moricizine works by inhibiting the rapid inward sodium current across myocardial cell membranes.
Dược Động Học :
▧ 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.
▧ Volume of Distribution :
* 300 L
▧ Protein binding :
Approximately 95%.
▧ Metabolism :
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).
Độc Tính : Symptoms of overdose include vomiting, unconsciousness, and severe low blood pressure.
Chỉ Định : Used to treat irregular heartbeats (arrhythmias) and maintain a normal heart rate.
Tương Tác Thuốc :
  • Diltiazem Increased effect/toxicity of moricizine
  • Ranolazine Possible additive effect on QT prolongation
  • Telithromycin Telithromycin 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.
  • Voriconazole Voriconazole, 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.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Ethmozine
  • Công ty : Olainfarm
    Sản phẩm biệt dược : Etmozins
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00680
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=34633
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509072
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07743
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05077
ChemSpider
http://www.chemspider.com/Chemical-Structure.31872.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/54092-046-01
PharmGKB
http://www.pharmgkb.org/drug/PA164747738
Wikipedia
http://en.wikipedia.org/wiki/Moricizine
Drugs.com
http://www.drugs.com/cdi/moricizine.html
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