Tìm theo
Tirofiban
Các tên gọi khác (4 ) :
  • (2S)-2-(Butylsulfonylamino)-3-[4-(4-piperidin-4-ylbutoxy)phenyl]propanoic acid
  • N-(Butylsulfonyl)-O-(4-(4-piperidyl)butyl)-L-tyrosine
  • Tirofiban
  • Tirofibanum
fibrinolytic agents, platelet aggregation inhibitors
Thuốc Gốc
Small Molecule
CAS: 144494-65-5
ATC: B01AC17
ĐG : Baxter International Inc. , http://www.baxter.com
CTHH: C22H36N2O5S
PTK: 440.597
Tirofiban prevents the blood from clotting during episodes of chest pain or a heart attack, or while the patient is undergoing a procedure to treat a blocked coronary artery. It is a non-peptide reversible antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor, and inhibits platelet aggregation.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H36N2O5S
Phân tử khối
440.597
Monoisotopic mass
440.234492962
InChI
InChI=1S/C22H36N2O5S/c1-2-3-16-30(27,28)24-21(22(25)26)17-19-7-9-20(10-8-19)29-15-5-4-6-18-11-13-23-14-12-18/h7-10,18,21,23-24H,2-6,11-17H2,1H3,(H,25,26)/t21-/m0/s1
InChI Key
InChIKey=COKMIXFXJJXBQG-NRFANRHFSA-N
IUPAC Name
(2S)-2-(butane-1-sulfonamido)-3-{4-[4-(piperidin-4-yl)butoxy]phenyl}propanoic acid
Traditional IUPAC Name
tirofiban
SMILES
CCCCS(=O)(=O)N[C@@H](CC1=CC=C(OCCCCC2CCNCC2)C=C1)C(O)=O
Độ hòa tan
Very slightly soluble
logP
1.4
logS
-5.1
pKa (strongest acidic)
3.17
pKa (Strongest Basic)
10.21
PSA
104.73 Å2
Refractivity
117.48 m3·mol-1
Polarizability
49.27 Å3
Rotatable Bond Count
13
H Bond Acceptor Count
6
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Tirofiban prevents the blood from clotting during episodes of chest pain or a heart attack, or while the patient is undergoing a procedure to treat a blocked coronary artery. It is a non-peptide antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor, and inhibits platelet aggregation. When administered intravenously, tirofiban inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner. When given according to the recommended regimen, >90% inhibition is attained by the end of the 30-minute infusion. Tirofiban has been recently shown in patients with unstable angina to reduce ischemic events at 48 hours following infusion when compared to standard heparin therapy.
Cơ Chế Tác Dụng : Tirofiban prevents the blood from clotting during episodes of chest pain or a heart attack, or while the patient is undergoing a procedure to treat a blocked coronary artery. It is a non-peptide reversible antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor, and inhibits platelet aggregation. Tirofiban is a reversible antagonist of fibrinogen binding to the GP IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation. Platelet aggregation inhibition is reversible following cessation of the infusion of tirofiban.
Dược Động Học :

▧ Volume of Distribution :
* 22 to 42 L
▧ Protein binding :
65%
▧ Metabolism :
Metabolism appears to be limited.
▧ Route of Elimination :
It is cleared from the plasma largely by renal excretion, with about 65% of an administered dose appearing in urine and about 25% in feces, both largely as unchanged tirofiban.
▧ Half Life :
2 hours
▧ Clearance :
* 213 - 314 mL/min [Healthy subjects] * 152 - 267 mL/min [patients with coronary artery disease]
Chỉ Định : For treatment, in combination with heparin, of acute coronary syndrome, including patients who are to be managed medically and those undergoing PTCA or atherectomy.
Tương Tác Thuốc :
  • Abciximab Additive effects. Concomitant use is contraindicated.
  • Eptifibatide Additive effects. Concomitant use is contraindicated.
  • Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
  • Treprostinil The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Tirofiban. Monitor for increased bleeding during concomitant thearpy.
Liều Lượng & Cách Dùng : Solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00775
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60947
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504678
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07965
ChemSpider
http://www.chemspider.com/Chemical-Structure.54912.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/25208-001-01
PharmGKB
http://www.pharmgkb.org/drug/PA451698
Wikipedia
http://en.wikipedia.org/wiki/Tirofiban
RxList
http://www.rxlist.com/cgi/generic/tiro.htm
Drugs.com
http://www.drugs.com/cdi/tirofiban.html
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