Tìm theo
Nadroparin
Máu, Chế phẩm máu & Dung dịch cao phân tử
Thuốc Gốc
Small Molecule
CAS: 9041-08-1
ATC: B01AB06
Nadroparin is a low molecular weight heparin (LMWH) which, when bound to antithrombin III (ATIII), accelerates the inactivation of factor II and factor Xa. Nadroparin halts the coagulation pathway by inhibiting the activation of thrombin (factor IIa) by factor Xa. The amplification of the fibrin clotting cascade is stopped once factors Xa and IIa are inactivated. It is derived from porcine sources and has a mean molecular size of 5000 daltons. Low molecular weight heparins are less effective at inactivating factor IIa due to their shorter length compared to unfractionated heparin.
Dược Lực Học : Nadroparin is a low molecular weight heparin that is composed of a heterogeneous mixture of sulfated polysaccaride glycosaminoglycan chains. Th mean molecular weight is approximately 4300 daltons. The ratio of anti-Xa activity to anti-IIa is 3.5:1 whereas it is about 1:1 for heparin. Its use should be avoided in patients with a creatinine clearance less than 40mL/min. In these patients, unfractionated heparin should only be used. As for monitoring, active partial thromboplastin time (aPTT) will only increase at high doses of low molecular weight heparins (LMWH). Therefore, monitoring aPTT is not recommended. However, anti-Xa activity can be measured to monitor the efficacy of the LMWH.
Cơ Chế Tác Dụng : Nadroparin is a low molecular weight heparin (LMWH) which, when bound to antithrombin III (ATIII), accelerates the inactivation of factor II and factor Xa. Nadroparin halts the coagulation pathway by inhibiting the activation of thrombin (factor IIa) by factor Xa. The amplification of the fibrin clotting cascade is stopped once factors Xa and IIa are inactivated. It is derived from porcine sources and has a mean molecular size of 5000 daltons. Low molecular weight heparins are less effective at inactivating factor IIa due to their shorter length compared to unfractionated heparin. The mechanism of action for nadroparin is similar to all other LMWHs. Like all LMWHs, nadroparin has a pentasaccharide sequence which binds to ATIII, which potentiates the action of ATIII. This complex greatly accelerates the inactivation of factor Xa and factor IIa. As a result, the coagulation cascade is inhibited.
Dược Động Học :
▧ Absorption :
Absorption is linear. The bioavailability of nadroparin after subcutaneous administration is about 89%.
▧ Volume of Distribution :
3.59L
▧ Protein binding :
Much lower compared to heparin, which has over 90% protein bound.
▧ Metabolism :
Nadroparin is metabolized in the liver.
▧ Route of Elimination :
Nadroparin is eliminated via the kidneys through non-saturable mechanisms.
▧ Half Life :
In healthy patients, the half life is between 3.5hrs to 11.2hrs following subcutaneous administration.
▧ Clearance :
The clearance of nadroparin is 21.4 +/- 7.0mL/min
Độc Tính : Osteopenia with extended use, skin necrosis, thrombocytosis, severe immunologically-mediated thrombocytopenia, eosinophilia (rare), calcinosis rarely occurs at the injection site, severe bleeding, transient elevation of liver transaminases.
Chỉ Định : Nadroparin is used for prophylaxis of thromboembolic disorders and general surgery in orthopedic surgery, treatment of deep vein thrombosis, prevention of clotting during hemodialysis and treatment of unstable angina and non-Q wave myocardial infarction
Tương Tác Thuốc :
  • Drotrecogin alfa The potential benefits of drotrecogin alfa should be weighed against an increased risk of bleeding in patients receiving therapeutic doses of low molecular weight heparins such as nadroparin. Monitor for bleeding during concomitant therapy, and immediately stop infusion of drotrecogin if clinically important bleeding occurs. In patients receiving prophylactic heparin doses, consider continuing this during drotrecogin.
Liều Lượng & Cách Dùng : Injection, solution - Subcutaneous - 11 400IU/0.6mL
Injection, solution - Subcutaneous - 15 200IU/0.8mL
Injection, solution - Subcutaneous - 19 000IU/mL
Injection, solution - Subcutaneous - 2850IU/0.3mL
Injection, solution - Subcutaneous - 3800IU/0.4mL
Injection, solution - Subcutaneous - 5700IU/0.6mL
Injection, solution - Subcutaneous - 7600IU/0.8mL
Injection, solution - Subcutaneous - 9500IU/mL
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08813
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