Tìm theo
Isosorbide Dinitrate
Các tên gọi khác (21 ) :
  • 1,4:3,6-Dianhydrosorbitol 2,5-dinitrate
  • Carvasin
  • Cedocard retard
  • D-Isosorbide dinitrate
  • Dianhydrosorbitol 2,5-dinitrate
  • Dinitrate d'isosorbide
  • Dinitrato de isosorbida
  • Dinitroisosorbide
  • Dinitrosorbide
  • Flindix
  • ISDN
  • Isoket
  • Isorbid
  • Isordil
  • Isosorbide 2,5-dinitrate
  • Isosorbide dinitrate
  • Isosorbidi dinitras
  • Nitrosorbide
  • Sorbide nitrate
  • Sorbidilat
  • Sorbidnitrate
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 87-33-2
ATC: C01DA08
ĐG : Amedra Pharmaceuticals LLC
CTHH: C6H8N2O8
PTK: 236.1363
A vasodilator used in the treatment of angina pectoris. Its actions are similar to nitroglycerin but with a slower onset of action. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6H8N2O8
Phân tử khối
236.1363
Monoisotopic mass
236.028065242
InChI
InChI=1S/C6H8N2O8/c9-7(10)15-3-1-13-6-4(16-8(11)12)2-14-5(3)6/h3-6H,1-2H2/t3-,4+,5-,6-/m1/s1
InChI Key
InChIKey=MOYKHGMNXAOIAT-JGWLITMVSA-N
IUPAC Name
(3R,3aS,6S,6aS)-6-(nitrooxy)-hexahydrofuro[3,2-b]furan-3-yl nitrate
Traditional IUPAC Name
isosorbide dinitrate
SMILES
[H][C@]12OC[C@H](O[N+]([O-])=O)[C@@]1([H])OC[C@H]2O[N+]([O-])=O
Độ tan chảy
70 °C
Độ hòa tan
550 mg/L (at 25 °C)
logP
1.31
logS
-2.63
pKa (Strongest Basic)
-3.9
PSA
128.56 Å2
Refractivity
44.77 m3·mol-1
Polarizability
18.07 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
8
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Isosorbide Dinitrate is a moderate to long acting oral organic nitrate used for the relief and prophylactic management of angina pectoris. It relaxes the vascular smooth muscle and consequent dilatation of peripheral arteries and veins, especially the latter. Dilatation of the veins promotes peripheral pooling of blood and decreases venous return to the heart, thereby reducing left ventricular end- diastolic pressure and pulmonary capillary wedge pressure (preload). Arteriolar relaxation reduces systemic vascular resistance, systolic arterial pressure, and mean arterial pressure.
Cơ Chế Tác Dụng : A vasodilator used in the treatment of angina pectoris. Its actions are similar to nitroglycerin but with a slower onset of action. [PubChem] Similar to other nitrites and organic nitrates, isosorbide dinitrate is converted to nitric oxide (NO), an active intermediate compound which activates the enzyme guanylate cyclase (atrial natriuretic peptide receptor A). This stimulates the synthesis of cyclic guanosine 3',5'-monophosphate (cGMP) which then activates a series of protein kinase-dependent phosphorylations in the smooth muscle cells, eventually resulting in the dephosphorylation of the myosin light chain of the smooth muscle fiber. The subsequent release of calcium ions results in the relaxation of the smooth muscle cells and vasodilation.
Dược Động Học :
▧ Absorption :
Absorption of isosorbide dinitrate after oral dosing is nearly complete, but bioavailability is highly variable (10% to 90%), with extensive first-pass metabolism in the liver. The average bioavailability of isosorbide dinitrate is about 25%.
▧ Volume of Distribution :
* 2 to 4 L/kg
▧ Protein binding :
Very low
▧ Metabolism :
Hepatic
▧ Half Life :
1 hour
Độc Tính : Symptoms of overdose include reduced cardiac output and hypotension.
Chỉ Định : For the prevention of angina pectoris due to coronary artery disease.
Tương Tác Thuốc :
  • Avanafil Additive vasodilation. Concomitant therapy is contraindicated.
  • Dihydroergotamine Possible antagonism of action
  • Ergonovine Possible antagonism of action
  • Ergotamine Possible antagonism of action
  • Methylergometrine Possible antagonism of action
  • Methysergide Possible antagonism of action
  • Sildenafil Possible significant hypotension with this combination
  • Tadalafil The vasodilatory effects of Isosorbide dinitrate may be increased by Tadalafil. Severe hypotension may occur. Concomitant therapy is contraindicated.
  • Telithromycin Telithromycin may reduce clearance of Isosorbide Dinitrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Isosorbide Dinitrate if Telithromycin is initiated, discontinued or dose changed.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Udenafil The vasodilatory effects of Isosobide dinitrate may be increased by Udenafil. Severe hypotension may occur. Concomitant therapy is contraindicated.
  • Vardenafil The vasodilatory effects of Isosorbide dinitrate may be increased by Vardenafil. Severe hypotension may occur. Concomitant therapy is contraindicated.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of isosorbide dinitrate by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of isosorbide dinitrate if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Tablet - Sublingual
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Ayerst
    Sản phẩm biệt dược : Carvasin
  • Công ty : Schwarz
    Sản phẩm biệt dược : Dilatrate-SR
  • Công ty : Vitória
    Sản phẩm biệt dược : Flindix
  • Công ty : Schwarz
    Sản phẩm biệt dược : Isoket
  • Công ty : Armstrong
    Sản phẩm biệt dược : Isorbid
  • Công ty : Valeant
    Sản phẩm biệt dược : Isordil
  • Công ty : Lusofarmaco
    Sản phẩm biệt dược : Nitrosorbide
  • Công ty : Actavis
    Sản phẩm biệt dược : Sorbidilat
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00883
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6883
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506412
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07456
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00516
ChemSpider
http://www.chemspider.com/Chemical-Structure.6619.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0008-4139-01
PharmGKB
http://www.pharmgkb.org/drug/PA450125
RxList
http://www.rxlist.com/cgi/generic2/isodinit.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/iso1212.shtml
Drugs.com
http://www.drugs.com/cdi/isosorbide-dinitrate.html
... loading
... loading