Tìm theo
Dipyridamole
Các tên gọi khác (9 ) :
  • Cardoxin
  • Cleridium 150
  • Curantyl
  • Dipiridamol
  • Dipyridamine
  • Dipyridamolum
  • Dipyudamine
  • Dypyridamol
  • Persantin
platelet aggregation inhibitors, phosphodiesterase inhibitors, vasodilator agents
Thuốc Gốc
Small Molecule
CAS: 58-32-2
ATC: B01AC07
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C24H40N8O4
PTK: 504.6256
A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H40N8O4
Phân tử khối
504.6256
Monoisotopic mass
504.317251808
InChI
InChI=1S/C24H40N8O4/c33-15-11-31(12-16-34)23-26-20-19(21(27-23)29-7-3-1-4-8-29)25-24(32(13-17-35)14-18-36)28-22(20)30-9-5-2-6-10-30/h33-36H,1-18H2
InChI Key
InChIKey=IZEKFCXSFNUWAM-UHFFFAOYSA-N
IUPAC Name
2-({6-[bis(2-hydroxyethyl)amino]-4,8-bis(piperidin-1-yl)pyrimido[5,4-d][1,3]diazin-2-yl}(2-hydroxyethyl)amino)ethan-1-ol
Traditional IUPAC Name
dipyridamole
SMILES
OCCN(CCO)C1=NC2=C(N=C(N=C2N2CCCCC2)N(CCO)CCO)C(=N1)N1CCCCC1
Độ tan chảy
163 °C
Độ hòa tan
Slightly
logP
1.5
logS
-2.7
pKa (strongest acidic)
14.97
pKa (Strongest Basic)
6.59
PSA
145.44 Å2
Refractivity
142.78 m3·mol-1
Polarizability
56.94 Å3
Rotatable Bond Count
12
H Bond Acceptor Count
12
H Bond Donor Count
4
Physiological Charge
0
Number of Rings
4
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Dipyridamole, a non-nitrate coronary vasodilator that also inhibits platelet aggregation, is combined with other anticoagulant drugs, such as warfarin, to prevent thrombosis in patients with valvular or vascular disorders. Dipyridamole is also used in myocardial perfusion imaging, as an antiplatelet agent, and in combination with aspirin for stroke prophylaxis.
Cơ Chế Tác Dụng : A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752) Dipyridamole likely inhibits both adenosine deaminase and phosphodiesterase, preventing the degradation of cAMP, an inhibitor of platelet function. This elevation in cAMP blocks the release of arachidonic acid from membrane phospholipids and reduces thromboxane A2 activity. Dipyridamole also directly stimulates the release of prostacyclin, which induces adenylate cyclase activity, thereby raising the intraplatelet concentration of cAMP and further inhibiting platelet aggregation.
Dược Động Học :
▧ Absorption :
70%
▧ Volume of Distribution :
* 1 to 2.5 L/kg
▧ Protein binding :
99%
▧ Metabolism :
hepatic
▧ Route of Elimination :
Dipyridamole is metabolized in the liver to the glucuronic acid conjugate and excreted with the bile.
▧ Half Life :
40 minutes
▧ Clearance :
* 2.3-3.5 mL/min/kg
Độc Tính : Hypotension, if it occurs, is likely to be of short duration, but a vasopressor drug may be used if necessary. The oral LD50 in rats is greater than 6,000 mg/kg while in the dogs, the oral LD50 is approximately 400 mg/kg. LD50=8.4g/kg (orally in rat)
Chỉ Định : For as an adjunct to coumarin anticoagulants in the prevention of postoperative thromboembolic complications of cardiac valve replacement and also used in prevention of angina.
Tương Tác Thuốc :
  • Adenosine Dipyridamole may increase the effect/toxicity of adenosine.
  • Fludarabine Dipyridamole may decrease the effect of fludarabine.
  • Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
  • Regadenoson Dipyridamole may change the effects of regadenoson. When possible, withhold dipyridamole for at least two days prior to regadenoson administration.
  • Topotecan The p-glycoprotein inhibitor, Dipyridamole, may increase the bioavailability of oral Topotecan. A clinically significant effect is also expected with IV Topotecan. Concomitant therapy should be avoided.
  • Treprostinil The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Dipyridamole. Monitor for increased bleeding during concomitant thearpy. Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Liều Lượng & Cách Dùng : Liquid - Intravenous
Solution - Intravenous
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : lsei
    Sản phẩm biệt dược : Agilease
  • Công ty : Rafa
    Sản phẩm biệt dược : Cardoxin
  • Công ty : Millot
    Sản phẩm biệt dược : Cleridium 150
  • Công ty : Arzneimittelwerk
    Sản phẩm biệt dược : Curantyl
  • Công ty :
    Sản phẩm biệt dược : Persantin
  • Sản phẩm biệt dược : Persantine
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00975
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3108
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506292
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00302
ChemSpider
http://www.chemspider.com/Chemical-Structure.2997.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=23620
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/55390-555-10
PharmGKB
http://www.pharmgkb.org/drug/PA449367
Wikipedia
http://en.wikipedia.org/wiki/Dipyridamole
RxList
http://www.rxlist.com/cgi/generic2/dipyrid.htm
Drugs.com
http://www.drugs.com/cdi/dipyridamole.html
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