Tìm theo
Argatroban
Thuốc Gốc
Small Molecule
CAS: 74863-84-6
ATC: B01AE03
ĐG : GlaxoSmithKline Inc. , http://www.gsk.com
CTHH: C23H36N6O5S
PTK: 508.634
Argatroban is a direct, selective thrombin inhibitor. The American College of Cardiologists (ACC) recommend using bivalirudin or argatroban in patients who have had, or at risk for, heparin induced thrombocytopenia (HIT) and are undergoing percutaneous coronary intervention. Argatroban is a non-heparin anticoagulant shown to both normalize platelet count in patients with HIT and prevent the formation of thrombi. Parental anticoagulants must be stopped and a baseline activated partial thromboplastin time must be obtained prior to administering argatroban.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
508.634
Monoisotopic mass
508.246788982
InChI
InChI=1S/C23H36N6O5S/c1-14-8-10-29(18(12-14)22(31)32)21(30)17(6-4-9-26-23(24)25)28-35(33,34)19-7-3-5-16-11-15(2)13-27-20(16)19/h3,5,7,14-15,17-18,27-28H,4,6,8-13H2,1-2H3,(H,31,32)(H4,24,25,26)/t14-,15-,17+,18-/m1/s1
InChI Key
InChIKey=KXNPVXPOPUZYGB-XYVMCAHJSA-N
IUPAC Name
(2R,4R)-1-[(2S)-5-[(diaminomethylidene)amino]-2-[(3R)-3-methyl-1,2,3,4-tetrahydroquinoline-8-sulfonamido]pentanoyl]-4-methylpiperidine-2-carboxylic acid
Traditional IUPAC Name
argatroban
SMILES
C[[email protected]@H]1CCN([[email protected]](C1)C(O)=O)C(=O)[[email protected]](CCCN=C(N)N)NS(=O)(=O)C1=CC=CC2=C1NC[[email protected]](C)C2
Độ hòa tan
2.21e-01 g/l
logP
1
logS
-3.4
pKa (strongest acidic)
3.07
pKa (Strongest Basic)
10.91
PSA
180.21 Å2
Refractivity
133.54 m3·mol-1
Polarizability
53.9 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
9
H Bond Donor Count
5
Physiological Charge
0
Number of Rings
3
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Argatroban is a synthetic direct thrombin inhibitor derived from L-arginine indicated as an anticoagulant for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia. Argatroban is a direct thrombin inhibitor that reversibly binds to the thrombin active site. Argatroban does not require the co-factor antithrombin III for antithrombotic activity. Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; protein C; and platelet aggregation. Argatroban is highly selective for thrombin with an inhibitory constant (Ki) of 0.04 µM. At therapeutic concentrations, Argatroban has little or no effect on related serine proteases (trypsin, factor Xa, plasmin, and kallikrein). Argatroban is capable of inhibiting the action of both free and clot-associated thrombin.
Cơ Chế Tác Dụng : Argatroban is a direct, selective thrombin inhibitor. The American College of Cardiologists (ACC) recommend using bivalirudin or argatroban in patients who have had, or at risk for, heparin induced thrombocytopenia (HIT) and are undergoing percutaneous coronary intervention. Argatroban is a non-heparin anticoagulant shown to both normalize platelet count in patients with HIT and prevent the formation of thrombi. Parental anticoagulants must be stopped and a baseline activated partial thromboplastin time must be obtained prior to administering argatroban. Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; protein C; and platelet aggregation.
Dược Động Học :
▧ Absorption :
Bioavailability is 100% (intravenous).
▧ Volume of Distribution :
* 174 mL/kg * 12.18 L [70-kg adult]
▧ Protein binding :
54%
▧ Metabolism :
Liver via hydroxylation and aromatization of the 3-methyltetrahydroquinoline ring. Age and gender do not substantially affect the pharmacodynamic or pharmacokinetic profile of argatroban.
▧ Route of Elimination :
Argatroban is excreted primarily in the feces (65%), presumably through biliary secretion; 22% is eliminated via urine.
▧ Half Life :
39 and 51 minutes
▧ Clearance :
* 5.1 L/kg/hr [infusion doses up to 40 mcg/kg/min]
Độc Tính : Excessive bleeding
Chỉ Định : Argatroban is indicated for prevention and treatment of thrombosis caused by heparin induced thrombocytopenia (HIT). It is also indicated for use in patients with, or at risk for, HIT who are undergoing percutaneous coronary intervention.
Tương Tác Thuốc :
  • 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 anticoagulant, Argatroban. Monitor for increased bleeding during concomitant thearpy.
Liều Lượng & Cách Dùng : Solution - Intravenous - 100mg/mL
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