Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Dược Lực Học :
Bivalirudin directly and reversibly inhibits thrombin by specifically binding both to the catalytic site and to the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible because thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Cơ Chế Tác Dụng :
Bivalirudin is a synthetic 20 residue peptide (thrombin inhibitor) which reversibly inhibits thrombin. Once bound to the active site, thrombin cannot activate fibrinogen into fibrin, the crucial step in the formation of thrombus. It is administered intravenously. Because it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure.
Inhibits the action of thrombin by binding both to its catalytic site and to its anion-binding exosite. Thrombin is a serine proteinase that plays a central role in the thrombotic process, acting to cleave fibrinogen into fibrin monomers and to activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Dược Động Học :
▧ Absorption :
Following intravenous administration, bivalirudin exhibits linear
pharmacokinetics . The mean steady state concentration is 12.3 +/-
1.7mcg/mL after administration of an intravenous bolus of 1mg/kg
followd by a 2.5mg/kg/hr intravenous infusion given over 4 hours.
▧ Volume of Distribution :
▧ Protein binding :
Other than thrombin and red blood cells, bivalirudin does not bind to
▧ Metabolism :
80% proteolytic cleavage
▧ Route of Elimination :
Bivalirudin is cleared from plasma by a combination of renal mechanisms (20%) and proteolytic cleavage.
▧ Half Life :
* Normal renal function: 25 min (in normal conditions)
* Creatinine clearance 10-29mL/min: 57min
* Dialysis-dependant patients: 3.5h
▧ Clearance :
* 3.4 mL/min/kg [Normal renal function]
* 3.4 mL/min/kg [mild renal function]
* 2.7 mL/min/kg [moderate renal function]
* 2.8 mL/min/kg [severe renal function]
* 1 mL/min/kg [Dialysis-dependent patients]
Độc Tính :
Based on a study by Gleason et al., the no-observed-adverse-effect level (NOAEL) for bivalirudin, administered to rats via intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Chỉ Định :
For treatment of heparin-induced thrombocytopenia and for the
prevention of thrombosis. Bivalirudin is indicated for use in
patients undergoing percutaneous coronary intervention (PCI), in
patients at moderate to high risk acute coronary syndromes due to
unstable angina or non-ST segment elevation in whom a PCI is planned.
Tương Tác Thuốc :
Anticoagulants increase the risk for gastrointestinal ulceration/irritation and/or GI bleeding. If these two agents must be used, patients need to be closely monitored for signs and symptoms of GI toxicity.
Gemcitabine may enhance the adverse/toxic effect of Bleomycin. The risk of pulmonary toxicity may be increased. Use extreme caution if using gemcitabine and bleomycin in combination. Monitor for the development of pulmonary toxicity.
Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
Anticoagulants may enhance the anticoagulant effect of rivaroxaban. Avoid concurrent use of rivaroxaban with other anticoagulants whenever possible, other than during transition periods, due to the possible increased for bleeding.
The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Bivalirudin. Monitor for increased bleeding during concomitant thearpy.
Liều Lượng & Cách Dùng :
Powder, for solution - Intravenous - 250mg
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