title: Pharmacokinetic and pharmacodynamic properties of batifiban coadministered with antithrombin agents in Chinese healthy volunteers.
abstract: The combined use of batifiban, a synthetic platelet GPII b/ IIIa receptor antagonist, and antithrombin agents is an attractive option for the treatment of patients with non-ST-segment elevation (NSTE) acute coronary syndrome (ACS) and those scheduled for percutaneous coronary intervention. To observe whether antithrombin agents affect the pharmacokinetic and pharmacodynamic properties of batifiban in combination therapy and optimize clinical administration dosage of batifiban, an open-label and parallel study was conducted. Thirty healthy subjects were randomly divided into three groups, which were sequentially treated with batifiban alone, or oral coadministration of clopidogrel, aspirin and UFH, or batifiban coadministered with these antithrombin agents. Blood samples were collected at pre-specified time points. The evaluation index included the inhibition of platelet aggregation and pharmacokinetic parameters. The pharmacokinetic parameters of batifiban and batifiban coadministered with antithrombin agents showed no significant differences. The mean inhibition rate of platelet aggregation (%) suggested that neither batifiban alone nor antithrombin agents alone could provide such potent inhibition rate (>80%) to obtain the best clinical efficacy, but they had a synergistic effect on platelet inhibition. No serious adverse effects were observed. The results in these healthy subjects suggest that batifiban coadministrated with antithrombin agents could achieve optimum clinical treatment effect for patients with NSTE ACS, and also those scheduled for percutaneous coronary intervention.
authors.affiliation: Institute of Clinical Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China.
authors.forename: Xiao-Meng
authors.initials: XM
authors.lastname: He
authors.affiliation: Institute of Clinical Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Zhou
authors.affiliation: Institute of Clinical Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Li
authors.affiliation: Institute of Clinical Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China.
authors.forename: San-Lan
authors.initials: SL
authors.lastname: Wu
authors.affiliation: Institute of Clinical Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China.
authors.forename: Meng-Meng
authors.initials: MM
authors.lastname: Jia
authors.affiliation: Institute of Clinical Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China.
authors.forename: Ming-Zhou
authors.initials: MZ
authors.lastname: Liu
authors.affiliation: Institute of Clinical Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Chen
authors.affiliation: Department of Infection Disease, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China.
authors.forename: Ke
authors.initials: K
authors.lastname: Chen
authors.affiliation: Biothera Solutions Ltd., Guangzhou, 510760, China.
authors.forename: Sheng-Feng
authors.initials: SF
authors.lastname: Li
authors.affiliation: Biothera Solutions Ltd., Guangzhou, 510760, China.
authors.forename: Yao-Hua
authors.initials: YH
authors.lastname: Wang
authors.affiliation: Institute of Clinical Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China. lweiyong2000@hotmail.com.
authors.forename: Wei-Yong
authors.initials: WY
authors.lastname: Li
mesh_terms: D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D019540:Area Under Curve; D001241:Aspirin / Q000008:administration & dosage / Q000494:pharmacology*; D002681:China; D000077144:Clopidogrel; D004334:Drug Administration Schedule; D005260:Female; D005343:Fibrinolytic Agents / Q000008:administration & dosage / Q000494:pharmacology; D006493:Heparin / Q000008:administration & dosage / Q000494:pharmacology*; D006801:Humans; D007262:Infusions, Intravenous; D007275:Injections, Intravenous; D008297:Male; D008657:Metabolic Clearance Rate / Q000187:drug effects; D010456:Peptides, Cyclic / Q000008:administration & dosage / Q000493:pharmacokinetics*; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics; D013988:Ticlopidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D013997:Time Factors; D055815:Young Adult
chemical_list: D005343:Fibrinolytic Agents; D010456:Peptides, Cyclic; D010975:Platelet Aggregation Inhibitors; C555443:batifiban; D006493:Heparin; D000077144:Clopidogrel; D013988:Ticlopidine; D001241:Aspirin