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Pharmacokinetics and pharmacodynamics of a bolus and infusion of cangrelor: a direct, parenteral P2Y12 receptor antagonist

Academic Article
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Overview

authors

  • Akers, W. S.
  • Oh, J. J.
  • Oestreich, J. H.
  • Ferraris, S.
  • Wethington, M.
  • Steinhubl, Steven

publication date

  • January 2010

journal

  • Journal of Clinical Pharmacology  Journal

abstract

  • The purpose of this study is to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of cangrelor administered as an intravenous bolus plus a continuous infusion in healthy volunteers. Twenty-two healthy volunteers are randomized to receive 1 of 2 intravenous cangrelor dosing regimens: a 15-microg/kg bolus followed by a 2-microg/kg/min infusion or a 30-microg/kg bolus followed by a 4-microg/kg/min infusion. The infusion is continued for 60 minutes, and serial blood samples are obtained for evaluation of pharmacokinetic and pharmacodynamic parameters. Administration of an intravenous bolus followed by a continuous infusion rapidly achieves maximum concentrations of cangrelor that are associated with extensive platelet inhibition within 2 minutes. Moreover, extensive platelet inhibition is maintained throughout the infusion period with near-full recovery of platelet function within 60 to 90 minutes of terminating the infusion. The effect of high-dose cangrelor is more consistent and demonstrates a greater level of inhibition on adenosine diphosphate-induced P-selectin expression; how ever, no significant differences are observed between the 2 dosing regimens with regard to platelet aggregation or time to recovery of platelet function. Cangrelor administered as an intravenous bolus followed by a continuous infusion in healthy volunteers offers rapid and reversible inhibition of platelet function.

subject areas

  • Adenosine Monophosphate
  • Adult
  • Female
  • Humans
  • Infusions, Intravenous
  • Injections, Intraventricular
  • Male
  • P-Selectin
  • Platelet Activation
  • Platelet Aggregation Inhibitors
  • Purinergic P2 Receptor Antagonists
  • Receptors, Purinergic P2Y12
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Research

keywords

  • Cangrelor
  • P2Y(12)
  • clopidogrel
  • pharmacodynamics
  • pharmacokinetics
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Identity

International Standard Serial Number (ISSN)

  • 0091-2700

Digital Object Identifier (DOI)

  • 10.1177/0091270009344986

PubMed ID

  • 19779037
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Additional Document Info

start page

  • 27

end page

  • 35

volume

  • 50

issue

  • 1

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