Tìm theo
Tocainide
Các tên gọi khác (6 ) :
  • 2-Amino-2',6'-propionoxylidide
  • 2-amino-N-(2,6-Dimethylphenyl)propanamide
  • 2-Amino-N-(2,6-dimethylphenyl)propionamid
  • Alanyl-2,6-xylidide
  • Tocainida
  • Tocainidum
Thuốc chống loạn nhịp
Thuốc Gốc
Small Molecule
CAS: 41708-72-9
ATC: C01BB03
CTHH: C11H16N2O
PTK: 192.2575
An antiarrhythmic agent which exerts a potential- and frequency-dependent block of sodium channels. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C11H16N2O
Phân tử khối
192.2575
Monoisotopic mass
192.126263144
InChI
InChI=1S/C11H16N2O/c1-7-5-4-6-8(2)10(7)13-11(14)9(3)12/h4-6,9H,12H2,1-3H3,(H,13,14)
InChI Key
InChIKey=BUJAGSGYPOAWEI-UHFFFAOYSA-N
IUPAC Name
2-amino-N-(2,6-dimethylphenyl)propanamide
Traditional IUPAC Name
tocainide
SMILES
CC(N)C(=O)NC1=C(C)C=CC=C1C
Độ tan chảy
246-266 °C
Độ hòa tan
1.07E+004 mg/L
logP
0.76
logS
-2.1
pKa (strongest acidic)
13.65
pKa (Strongest Basic)
8.23
PSA
55.12 Å2
Refractivity
58.86 m3·mol-1
Polarizability
21.59 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Tocainide is a primary amine analog of lidocaine with antiarrhythmic properties useful in the treatment of ventricular arrhythmias. Tocainide, like lidocaine, produces dose dependent decreases in sodium and potassium conductance, thereby decreasing the excitability of myocardial cells. In experimental animal models, the dose-related depression of sodium current is more pronounced in ischemic tissue than in normal tissue. Tocainide is a Class I antiarrhythmic compound with electrophysiologic properties in man similar to those of lidocaine, but dissimilar from quinidine, procainamide, and disopyramide.
Cơ Chế Tác Dụng : An antiarrhythmic agent which exerts a potential- and frequency-dependent block of sodium channels. [PubChem] Tocainide acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. Tocainide binds preferentially to the inactive state of the sodium channels.The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers.
Dược Động Học :
▧ Absorption :
Following oral administration, the bioavailability approaches 100 percent, and is unaffected by food.
▧ Protein binding :
Approximately 10 percent bound to plasma protein.
▧ Metabolism :
Negligible first pass hepatic degradation. No active metabolites have been found.
▧ Half Life :
The average plasma half-life in patients is approximately 15 hours. May be prolonged up to 35 hours in patients with severe renal function impairment (creatinine clearance less than 30 mL per min per 1.73 square meters of body surface area.
Độc Tính : The oral LD50 of tocainide was calculated to be about 800 mg/kg in mice, 1000 mg/kg in rats, and 230 mg/kg in guinea pigs; deaths were usually preceded by convulsions.
Chỉ Định : For the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that, in the judgment of the physician, are life-threatening.
Tương Tác Thuốc :
  • Rifampicin Rifampin lowers tocainide levels/effects
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Tonocard
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01056
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=38945
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505385
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07142
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D06172
ChemSpider
http://www.chemspider.com/Chemical-Structure.35632.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50092595
PharmGKB
http://www.pharmgkb.org/drug/PA451706
Wikipedia
http://en.wikipedia.org/wiki/Tocainide
RxList
http://www.rxlist.com/cgi/generic3/tocainide.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ton1451.shtml
Drugs.com
http://www.drugs.com/mtm/tocainide.html
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