About: Bivalirudin     Goto   Sponge   NotDistinct   Permalink

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http://linked.open...gbank/description
  • 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. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Seybert AL, Coons JC, Zerumsky K: Treatment of heparin-induced thrombocytopenia: is there a role for bivalirudin? Pharmacotherapy. 2006 Feb;26(2):229-41. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16466327 # Dager WE, Dougherty JA, Nguyen PH, Militello MA, Smythe MA: Heparin-induced thrombocytopenia: treatment options and special considerations. Pharmacotherapy. 2007 Apr;27(4):564-87. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17381384 # Dang CH, Durkalski VL, Nappi JM: Evaluation of treatment with direct thrombin inhibitors in patients with heparin-induced thrombocytopenia. Pharmacotherapy. 2006 Apr;26(4):461-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16553503 # Robson R: The use of bivalirudin in patients with renal impairment. J Invasive Cardiol. 2000 Dec;12 Suppl F:33F-6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11156732 # Van De Car DA, Rao SV, Ohman EM: Bivalirudin: a review of the pharmacology and clinical application. Expert Rev Cardiovasc Ther. 2010 Dec;8(12):1673-81. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21108549 # Shammas NW: Bivalirudin: pharmacology and clinical applications. Cardiovasc Drug Rev. 2005 Winter;23(4):345-60. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16614733 # Gleason TG, Chengelis CP, Jackson CB, Lindstrom P: A 24-hour continuous infusion study of bivalirudin in the rat. Int J Toxicol. 2003 May-Jun;22(3):195-206. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12851152 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • investigational (en)
http://linked.open...drugbank/halfLife
  • * Normal renal function: 25 min (in normal conditions) * Creatinine clearance 10-29mL/min: 57min * Dialysis-dependant patients: 3.5h (en)
http://linked.open...ugbank/indication
  • 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. (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Bivalirudin (en)
adms:identifier
http://linked.open...mechanismOfAction
  • 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. (en)
http://linked.open...drugbank/packager
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Bivalirudin is cleared from plasma by a combination of renal mechanisms (20%) and proteolytic cleavage. (en)
http://linked.open...drugbank/toxicity
  • 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. (en)
http://linked.open...umeOfDistribution
  • 0.2L/kg (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • Echinacea (en)
  • Dan shen, dong quai, evening primrose oil, gingko, policosanol, willow bark (en)
http://linked.open...nk/proteinBinding
  • Other than thrombin and red blood cells, bivalirudin does not bind to plasma proteins. (en)
http://linked.open...ynthesisReference
  • Avi Tovi, Chaim Eidelman, Shimon Shushan, Alon Hagi, Alexander Ivchenko, Gabriel-Marcus Butilca, Leah Bar-Oz, Tehila Gadi, Gil Zaovi, "Process for production of Bivalirudin." U.S. Patent US20070093423, issued April 26, 2007. (en)
foaf:page
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...l/drug/hasATCCode
http://linked.open...ugbank/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. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 128270-60-0 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...rugbank/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] (en)
http://linked.open...gbank/containedIn
http://linked.open...nk/Hydrophobicity
http://linked.open...Isoelectric-Point
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