Fondaparinux sodium: A selective inhibitor of factor Xa

被引:54
作者
Bauer, KA
机构
[1] VA Boston Healthcare Syst, Hematol Sect, Boston, MA 02215 USA
[2] Beth Israel Deaconess Med Ctr, Boston, MA 02215 USA
关键词
anticoagulants; duration of action; mechanism of action; Org-31540; pharmacokinetics; SR-90107A; thromboembolism; toxicity;
D O I
10.1093/ajhp/58.suppl_2.S14
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The pharmacology and mechanism of action of fondaparinux sodium are described. Fondaparinux sodium is the first agent of a new class of anticoagulants that selectively target factor Xa. It has a linear, dose-dependent pharmacokinetic profile, which provides a highly predictable response. It is 100% bioavailable, has a rapid onset of action, and has a half-life of 14 to 16 hours, allowing for sustained antithrombotic activity over a 24-hour period. The drug does not affect prothrombin time or activated partial thromboplastin time, nor does it affect platelet function or aggregation. Studies in patients with confirmed heparin-induced thrombocytopenia demonstrate that the drug is not associated with in vitro cross-reactivity to heparin antibodies. Fondaparinux sodium appears to meet the criteria for an ideal antithrombotic agent: equal or better effectiveness than currently available agents, a low bleeding risk, no need for laboratory monitoring, and once-daily administration.
引用
收藏
页码:S14 / S17
页数:4
相关论文
共 15 条
  • [1] Absence of cross-reactivity of SR90107A/ORG31540 pentasaccharide with antibodies to heparin-PF4 complexes developed in heparin-induced thrombocytopenia
    Amiral, J
    Lormeau, JC
    MarfaingKoka, A
    Vissac, AM
    Wolf, M
    BoyerNeumann, C
    Tardy, B
    Herbert, JM
    Meyer, D
    [J]. BLOOD COAGULATION & FIBRINOLYSIS, 1997, 8 (02) : 114 - 117
  • [2] Boneu B, 1995, THROMB HAEMOSTASIS, V74, P1468
  • [3] STRUCTURE-ACTIVITY RELATIONSHIP IN HEPARIN - A SYNTHETIC PENTASACCHARIDE WITH HIGH-AFFINITY FOR ANTI-THROMBIN-III AND ELICITING HIGH ANTI-FACTOR-XA ACTIVITY
    CHOAY, J
    PETITOU, M
    LORMEAU, JC
    SINAY, P
    CASU, B
    GATTI, G
    [J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1983, 116 (02) : 492 - 499
  • [4] ELALAMY I, 1995, THROMB HAEMOSTASIS, V74, P1384
  • [5] SR 90107A Org 31540, a novel anti-factor Xa antithrombotic agent
    Herbert, JM
    Petitou, M
    Lormeau, JC
    Cariou, R
    Necciari, J
    Magnani, HN
    Zandberg, P
    vanAmsterdam, RGM
    vanBoeckel, CAA
    Meuleman, DG
    [J]. CARDIOVASCULAR DRUG REVIEWS, 1997, 15 (01): : 1 - 26
  • [6] Oral anticoagulants: Mechanism of action, clinical effectiveness, and optimal therapeutic range
    Hirsh, J
    Dalen, JE
    Anderson, DR
    Poller, L
    Bussey, H
    Ansell, J
    Deykin, D
    [J]. CHEST, 2001, 119 (01) : 8S - 21S
  • [7] Heparin and low-molecular-weight heparin - Mechanisms of action, pharmacokinetics, dosing, monitoring, efficacy, and safety
    Hirsh, J
    Warkentin, TE
    Shaughnessy, SG
    Anand, SS
    Halperin, JL
    Raschke, R
    Granger, C
    Ohman, EM
    Dalen, JE
    [J]. CHEST, 2001, 119 (01) : 64S - 94S
  • [8] Lormeau JC, 1995, THROMB HAEMOSTASIS, V74, P1474
  • [9] OLSON ST, 1992, J BIOL CHEM, V267, P12528
  • [10] PETITOU M, 1991, NATURE, V350, P30