临床药物手册( 英文原版)7.pdf

Hematologic Drugs Coagulants and Anticoagulants ABCIXIMAB ReoPro Pharmacology. Abciximab is a chimeric human-murine monoclonal antibody Fab fragment that binds to and irreversibly inhibits the platelet glycoprotein IIb/IIIa receptor. Blockade of the glycoprotein IIb/IIIa receptor prevents fibrino- gen from binding, thereby inhibiting platelet aggregation. Abciximab also binds to the vitronectin receptor found on platelets, endothelial cells, monocytes, and smooth muscle cells; the clinical relevance of this is unknown. Abciximab inhibits platelet aggregation and prolongs bleeding time in a dose-dependent manner.1,2 Administration and Adult Dosage. IV for percutaneous coronary intervention 0.25 mg/kg as a bolus 10–60 min before starting percutaneous coronary interven- tion and then 0.125 µg/kg/min (up to 10 µg/min) by continuous infusion for 12 hr. IV for unstable angina and planned percutaneous intervention within 24 hr 0.25 mg/kg as a bolus and then 0.125 µg/kg/min (up to 10 µg/min) by continuous infusion for 18–24 hr, concluding 1 hr after the percutaneous coronary interven- tion. (See Parameters to Monitor and Notes.) Special Populations. Geriatric Dosage. Same as adult dosage. Dosage Forms. Inj 2 mg/mL. Pharmacokinetics. Onset and Duration. Rapid inhibition of platelet function after IV administration. Platelet function gradually recovers after discontinuation of the IV infusion; bleeding time approaches baseline values within 24 hr and ex vivo platelet aggregation approaches baseline levels within 48 hr. Low levels of glyco- protein IIb/IIIa inhibition are detectable for up to 14 days after administration.1 Fate. Abciximab is rapidly cleared from the plasma after administration by rapid binding to the glycoprotein IIb/IIIa recept