PMID- 14521034 OWN - NLM STAT- MEDLINE DCOM- 20040114 LR - 20190222 IS - 1079-2082 (Print) IS - 1079-2082 (Linking) VI - 60 IP - 18 DP - 2003 Sep 15 TI - Bivalirudin in percutaneous coronary intervention. PG - 1841-9 AB - The chemistry and pharmacology, pharmacokinetics, pharmacodynamics, adverse effects, drug interactions, dosing and administration, and pharmacoeconomics of bivalirudin are reviewed; clinical trials of bivalirudin's application in percutaneous coronary intervention (PCI) are also discussed. Bivalirudin is a direct thrombin inhibitor approved for use in PCI. It reversibly binds to thrombin's catalytic site and substrate recognition site and blocks both circulating and fibrin-bound thrombin. Peak concentrations occur in less than 5 minutes after bolus-dose administration, and its half-life is approximately 25 minutes. It is primarily eliminated renally, and dosage reduction may be required in patients with severe renal dysfunction. Two clinical trials have demonstrated that bivalirudin is at least as effective as unfractionated heparin (UFH) in preventing ischemic complications in PCI. Other trials have shown that bivalirudin has beneficial ischemic and hemorrhagic outcomes in a more modern PCI setting (i.e., intracoronary stent placement, clopidogrel, and glycoprotein IIb/IIIa-receptor inhibitors). Bivalirudin combined with provisional glycoprotein IIb/IIIa inhibitors was noninferior to UFH with planned glycoprotein IIb/IIIa inhibitors and superior to UFH alone with respect to ischemic and hemorrhagic endopoints in PCI. Major bleeding with bivalirudin has occurred in approximately 3% of patients in clinical trials, and it is not known to have any interactions with the cytochrome P-450 isoenzyme system. The acquisition cost of bivalirudin in one study was less than the combination of UFH and glycoprotein IIb/IIIa inhibitors. Bivalirudin combined with provisional glycoprotein IIb/IIIa inhibitors appears to be an acceptable alternative to the standard of care and is superior to UFH alone in PCI. FAU - Caron, Michael F AU - Caron MF AD - Department of Pharmacy Practice, University of Rhode Island College of Pharmacy, Kingston, USA. mcaron@uri.edu FAU - McKendall, George R AU - McKendall GR LA - eng PT - Journal Article PT - Review PL - England TA - Am J Health Syst Pharm JT - American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists JID - 9503023 RN - 0 (Fibrinolytic Agents) RN - 0 (Hirudins) RN - 0 (Peptide Fragments) RN - 0 (Recombinant Proteins) RN - EC 3.4.21.5 (Thrombin) RN - TN9BEX005G (bivalirudin) SB - IM MH - Acute Disease MH - *Angioplasty, Balloon, Coronary/adverse effects MH - Clinical Trials as Topic MH - Coronary Disease/therapy MH - Drug Interactions MH - Fibrinolytic Agents/economics/pharmacokinetics/*therapeutic use MH - Hirudins/*analogs & derivatives/economics/pharmacokinetics MH - Humans MH - Peptide Fragments/economics/pharmacokinetics/*therapeutic use MH - Recombinant Proteins/economics/pharmacokinetics/*therapeutic use MH - Thrombin/*antagonists & inhibitors MH - Thrombosis/etiology/prevention & control RF - 39 EDAT- 2003/10/03 05:00 MHDA- 2004/01/15 05:00 CRDT- 2003/10/03 05:00 PHST- 2003/10/03 05:00 [pubmed] PHST- 2004/01/15 05:00 [medline] PHST- 2003/10/03 05:00 [entrez] AID - 10.1093/ajhp/60.18.1841 [doi] PST - ppublish SO - Am J Health Syst Pharm. 2003 Sep 15;60(18):1841-9. doi: 10.1093/ajhp/60.18.1841.