title: Current strategies with high-dose tirofiban.
abstract: The glycoprotein (GP) IIb/IIIa receptor is a platelet-specific adhesion receptor that mediates the formation of platelet aggregates. Pharmacologic blockade of the receptor is associated with a reduction in major cardiovascular adverse events after percutaneous coronary interventions and in the setting of acute coronary syndromes. Three intravenous GP IIb/IIIa receptor inhibitors are available: abciximab, tirofiban and eptifibatide. Tirofiban is a small, synthetic non-peptide, competitive GP IIb/IIIa antagonist with high specificity and high affinity for the GP IIb/IIIa receptor. In a head-to-head comparison, tirofiban 10-microg/kg bolus followed by a 0.15-microg/kg/min infusion was found to be inferior to standard dose of abciximab in patients undergoing percutaneous coronary intervention. Insufficient platelet inhibition with low-dose tirofiban may likely explain these results. Subsequently, a high-bolus dose of tirofiban (25 microg/kg bolus) followed by standard infusion was tested and evidence suggest that in this dosing tirofiban may be as effective as abciximab and have a comparable safety profile. Therefore, high-bolus dose tirofiban may be an appealing and cost-effective alternative to abciximab. However, further testing is warranted given the short follow up and limited statistical power of the available data.
authors.affiliation: Gill Heart Institute, University of Kentucky, 326 Wethington Bldg, 900 S. Limestone, Lexington, Kentucky 40436-0200, USA. Mukherjee@uky.edu
authors.forename: Debabrata
authors.initials: D
authors.lastname: Mukherjee
authors.forename: Marco
authors.initials: M
authors.lastname: Roffi
mesh_terms: D004305:Dose-Response Relationship, Drug; D006801:Humans; D009203:Myocardial Infarction / Q000188:drug therapy / Q000473:pathology; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000037:antagonists & inhibitors*; D016032:Randomized Controlled Trials as Topic; D000077466:Tirofiban; D016896:Treatment Outcome; D014443:Tyrosine / Q000031:analogs & derivatives* / Q000191:economics / Q000627:therapeutic use
chemical_list: D019039:Platelet Glycoprotein GPIIb-IIIa Complex; D014443:Tyrosine; D000077466:Tirofiban