Tìm theo
Digitoxin
Các tên gọi khác (5 ) :
  • Crystodigin (tn)
  • Digitoksin
  • Digitoxin
  • Digitoxinum
  • Digitoxoside
enzyme inhibitors, anti arrhythmia agents, cardiotonic agents
Thuốc Gốc
Small Molecule
CAS: 71-63-6
ATC: C01AA04
ĐG : Spectrum Pharmaceuticals , http://www.spectrumpharm.com
CTHH: C41H64O13
PTK: 764.9391
A cardiac glycoside sometimes used in place of digoxin. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C41H64O13
Phân tử khối
764.9391
Monoisotopic mass
764.434692134
InChI
InChI=1S/C41H64O13/c1-20-36(46)29(42)16-34(49-20)53-38-22(3)51-35(18-31(38)44)54-37-21(2)50-33(17-30(37)43)52-25-8-11-39(4)24(15-25)6-7-28-27(39)9-12-40(5)26(10-13-41(28,40)47)23-14-32(45)48-19-23/h14,20-22,24-31,33-38,42-44,46-47H,6-13,15-19H2,1-5H3/t20-,21-,22-,24-,25+,26-,27+,28-,29+,30+,31+,33+,34+,35+,36-,37-,38-,39+,40-,41+/m1/s1
InChI Key
InChIKey=WDJUZGPOPHTGOT-XUDUSOBPSA-N
IUPAC Name
4-[(1S,2S,5S,7R,10R,11S,14R,15R)-5-{[(2R,4S,5S,6R)-5-{[(2S,4S,5S,6R)-5-{[(2S,4S,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxy}-4-hydroxy-6-methyloxan-2-yl]oxy}-4-hydroxy-6-methyloxan-2-yl]oxy}-11-hydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-14-yl]-2,5-dihydrofuran-2-one
Traditional IUPAC Name
digitoxin
SMILES
[H][C@]12CC[C@]3([H])[C@]([H])(CC[C@]4(C)[C@H](CC[C@]34O)C3=CC(=O)OC3)[C@@]1(C)CC[C@@H](C2)O[C@H]1C[C@H](O)[C@H](O[C@H]2C[C@H](O)[C@H](O[C@H]3C[C@H](O)[C@H](O)[C@@H](C)O3)[C@@H](C)O2)[C@@H](C)O1
Độ tan chảy
255.5 °C
Độ hòa tan
3.9 mg/L (at 25 °C)
logP
1.85
logS
-4.4
pKa (strongest acidic)
7.18
pKa (Strongest Basic)
0.24
PSA
182.83 Å2
Refractivity
191.72 m3·mol-1
Polarizability
83.58 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
12
H Bond Donor Count
5
Physiological Charge
0
Number of Rings
8
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Digitoxin is a cardiac glycoside sometimes used in place of DIGOXIN. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting (From Martindale, The Extra Pharmacopoeia, 30th ed, p665). Unlike digoxin (which is eliminated from the body via the kidneys), it is eliminated via the liver, so could be used in patients with poor or erratic kidney function. However, it is now rarely used in current UK medical practice. While there have been several controlled trials which have shown digoxin to be effective in a proportion of patients treated for heart failure, there is not the same strong evidence base for digitoxin, although it is presumed to be similarly effective.
Cơ Chế Tác Dụng : A cardiac glycoside sometimes used in place of digoxin. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665) Digitoxin inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations. Increased intracellular concentrations of calcium may promote activation of contractile proteins (e.g., actin, myosin). Digitoxin also acts on the electrical activity of the heart, increasing the slope of phase 4 depolarization, shortening the action potential duration, and decreasing the maximal diastolic potential.
Dược Động Học :

▧ Metabolism :
Hepatic.
Độc Tính : Digitoxin exhibits similar toxic effects to the more-commonly used digoxin, namely: anorexia, nausea, vomiting, diarrhoea, confusion, visual disturbances, and cardiac arrhythmias.
Chỉ Định : For the treatment and management of congestive cardiac insufficiency, arrhythmias and heart failure.
Tương Tác Thuốc :
  • Bendroflumethiazide Possible electrolyte variations and arrhythmias
  • Bumetanide Possible electrolyte variations and arrhythmias
  • Chlorthalidone Possible electrolyte variations and arrhythmias
  • Ethacrynic acid Possible electrolyte variations and arrhythmias
  • Furosemide Possible electrolyte variations and arrhythmias
  • Hydrochlorothiazide Possible electrolyte variations and arrhythmias
  • Indapamide Possible electrolyte variations and arrhythmias
  • Metolazone Possible electrolyte variations and arrhythmias
  • Quinidine Quinine/quinidine increases the effect of digoxin
  • Quinine Quinine/quinidine increases the effect of digoxin
  • Telithromycin Telithromycin may reduce clearance of Digitoxin. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Digitoxin if Telithromycin is initiated, discontinued or dose changed.
  • Verapamil Verapamil may increase the serum concentration of Digitoxin by decreasing its metabolism and clearance. Monitor for changes in the therapeutic/adverse effects of Digitoxin if Verpamail is initiated, discontinued or dose changed.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of digitoxin by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of digitoxin if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Liquid - Oral
Liquid - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Digitoxin powder
    Giá bán buôn : USD >486.85
    Đơn vị tính : g
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Crystodigin
  • Công ty :
    Sản phẩm biệt dược : Tardigal
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01396
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=441207
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506035
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06955
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00297
ChemSpider
http://www.chemspider.com/Chemical-Structure.389987.html
PharmGKB
http://www.pharmgkb.org/drug/PA449316
Wikipedia
http://en.wikipedia.org/wiki/Digitoxin
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