10. Bivalirudin Trifluoroacetate
12. Bg 8967
13. Bivalirudin [usan:ban:inn]
18. Phe-pro-arg-pro-(gly)4 Desulfato-tyr63'-hirugen
20. L-leucine, D-phenylalanyl-l-prolyl-l-arginyl-l-prolylglycylglycylglycylglycyl-l-asparaginylglycyl-l-alpha-aspartyl-l-phenylalanyl-l-alpha-glutamyl-l-alpha-glutamyl-l-isoleucyl-l-prolyl-l-alpha-glutamyl-l-alpha-glutamyl-l-tyrosyl-
22. Bivalirudin [usan:inn:ban]
23. Angiomax (tn)
25. Bivalirudin Trifluoacetate
43. The Medicines Company Brand Of Bivalirudin
49. (r,r)-2,6-bis(4,5-dihydro-4-phenyl-2-oxazolyl)pyridine; (r,r)-2,6-bis(4-phenyl-2-oxazolinyl)pyridine; (+)-2,6-bis[(4r)-4-phenyl-2-oxazolin-2-yl]pyridine
|Molecular Weight||2180.317 g/mol|
|Hydrogen Bond Donor Count||28|
|Hydrogen Bond Acceptor Count||35|
|Rotatable Bond Count||67|
|Exact Mass||2179.989 g/mol|
|Monoisotopic Mass||2178.986 g/mol|
|Topological Polar Surface Area||902 A^2|
|Heavy Atom Count||155|
|Isotope Atom Count||0|
|Defined Atom Stereocenter Count||16|
|Undefined Atom Stereocenter Count||0|
|Defined Bond Stereocenter Count||0|
|Undefined Bond Stereocenter Count||0|
|Covalently Bonded Unit Count||1|
|1 of 3|
|Company||THE MEDICINES CO (Application Number: N020873. Patents: 7582727, 7582727*PED, 7598343, 7598343*PED)|
|2 of 3|
|Drug Name||BIVALIRUDIN IN 0.9% SODIUM CHLORIDE|
|Company||BAXTER HLTHCARE CORP (Application Number: N208374)|
|3 of 3|
|Company||ACCORD HLTHCARE (Application Number: A206551); APOTEX INC (Application Number: A204876); DR REDDYS LABS LTD (Application Number: A201577); FRESENIUS KABI USA (Application Number: A090189); HOSPIRA INC (Application Number: A090811); HOSPIRA INC (Application Number: A090816)|
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.
Angiox is indicated as an anticoagulant in adult patients undergoing percutaneous coronary intervention (PCI), including patients with ST-segment elevation myocardial infarction (STEMI) undergoing primary PCI.Angiox is also indicated for the treatment of adult patients with unstable angina/non-ST segment elevation myocardial infarction (UA/NSTEMI) planned for urgent or early intervention.Angiox should be administered with aspirin and clopidogrel.
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.
Bivalirudin is a 20 amino acid long synthetic peptide with thrombin-specific anticoagulant properties. Bivalirudin reversibly binds thrombin, free as well as clot bound, at the catalytic site and the anion-binding exosite, thereby preventing the formation and activation of fibrin, factor XIIIa, and other coagulation factors. This drug is primarily used during coronary angioplasty procedures, in combination with aspirin, in patients with unstable angina.
Endogenous factors and drugs that directly inhibit the action of THROMBIN, usually by blocking its enzymatic activity. They are distinguished from INDIRECT THROMBIN INHIBITORS, such as HEPARIN, which act by enhancing the inhibitory effects of antithrombins.
Anatomical main group: B - Blood and blood forming organs
Therapeutic subgroup: B01 - Antithrombotic agents
Pharmacological subgroup: B01A - Antithrombotic agents
Chemical subgroup: B01AE - Direct thrombin inhibitors
Chemical substance: B01AE06 - bivalirudin
B - Blood and blood forming organs
B01 - Antithrombotic agents
B01A - Antithrombotic agents
B01AE - Direct thrombin inhibitors
B01AE06 - Bivalirudin
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.
Route of Elimination
Bivalirudin is cleared from plasma by a combination of renal mechanisms (20%) and proteolytic cleavage.
Volume of Distribution
80% proteolytic cleavage
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.