Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C1786H2779N509O519S29
Dược Lực Học :
Drotrecogin alfa is activated human protein C that is synthesized by recombinant DNA technology. It is a glycoprotein of approximately 55 kilodalton molecular weight, consisting of a heavy chain and a light chain linked by a disulfide bond.
Drotrecogin alfa inhibits factor Va and VIIIa, thereby reducing the coagulability of blood.
Cơ Chế Tác Dụng :
Drotrecogin alfa is activated human protein C that is synthesized by recombinant DNA technology. It is a glycoprotein of approximately 55 kilodalton molecular weight, consisting of a heavy chain and a light chain linked by a disulfide bond. Drotrecogin alfa was withdrawn from the market after a major study indicated that it was not effective in improving outcomes in patients with sepsis.
Activated protein C combines with protein S on platelet surfaces and then degrades factor Va and factor VIIIa, thereby reducing blood coagulability.
Dược Động Học :
▧ Half Life :
5.5 hours (mammalian reticulocytes, in vitro).
▧ Clearance :
* 40 L/hr [severe sepsis adults]
* 30 +/- 8 L/hr [patients without sepsis undergoing hemodialysis]
* 28 +/- 9 L/hr [heathy]
Chỉ Định :
For reduction of mortality in patients with severe sepsis.
Tương Tác Thuốc :
-
Clopidogrel
Antiplatelet agents such as clopidogrel may enhance the adverse/toxic effect of Drotrecogin Alfa. Bleeding may occur. Increase monitoring for signs/symptoms of bleeding during concomitant therapy. If possible, avoid use of drotrecogin within 7 days of use of any IIb/IIIa antagonists, higher dose aspirin (more than 650 mg/day), or use of other antiplatelet agents.
-
Dalteparin
Low molecular weight heparin (LMWH) such as dalteparin may enhance the adverse/toxic effect of drotrecogin alfa. Bleeding may occur.
-
Enoxaparin
Combination should be used with caution after weighing advantages and disadvantages. Low molecular weight heparins such as enoxaparin may increase the adverse effects of drotrecogin. Monitor for bleeding if used concomitantly.
-
Fondaparinux sodium
Drotrecogin alfa may increase the adverse effects of fondaparinux, resulting in excessive bleeding. Concomitant use should be avoided.
-
Heparin
The potential benefits of drotrecogin alfa should be weighed against an increased risk of bleeding in patients receiving therapeutic doses of heparin. 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.
-
Ketoprofen
The antiplatelet effect of ketoprofen may increase the bleed risk associated with drotrecogin alfa. Consider spacing use of the two agents by at least 7 days. Increase monitoring for signs and symptoms of bleeding during concomitant therapy.
-
Nadroparin
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.
-
Tenecteplase
Increased risk of bleeding.
-
Tinzaparin
Low molecular weight heparins (LMWHs) such as tinzaparin may enhance the adverse/toxic effects of drotrecogin alfa. Bleeding may occur. The potential benefits of drotrecogin alfa should be weighed against the increased risk of bleeding in patients on therapeutic doses of LMWHs.
-
Tolmetin
Increased risk of bleeding. Monitor for increased bleeding during concomitant therapy.
-
Treprostinil
The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Drotrecogin alfa. Monitor for increased bleeding during concomitant thearpy.
-
Urokinase
Increased risk of bleeding.
-
Vilazodone
Increase monitoring for signs/symptoms of bleeding during concomitant therapy. If possible, avoid use of drotrecogin within 7 days of use of any IIb/IIIa antagonists, higher dose aspirin (more than 650 mg/day), or use of other antiplatelet agents.
-
Warfarin
Increased risk of bleeding.
Liều Lượng & Cách Dùng :
Powder, for solution - Intravenous
Tài Liệu Tham Khảo Thêm
National Drug Code Directory