Abstract

In recent years, there has been a trend towards increased prescribing of direct-acting oral anticoagulants (DOACs) due to favourable pharmacokinetics and pharmacodynamics without the need for regular coagulation monitoring. However, recent studies have documented individual variability in plasma DOAC levels. DOAC pharmacogenetics is a relatively new area of research. There is a need to understand the role of pharmacogenetics in the adaptation of anticoagulant therapy according to a patient’s genetic characteristics. This scientific review of current data on the impact of different gene polymorphisms on apixaban pharmacokinetics broadens the understanding of the clinical relevance of genotyping for treatment efficacy and safety.

Highlights

  • 1 – Russian Medical Academy of Continuing Professional Education, Moscow, Russia 2 – S.S

  • There has been a trend towards increased prescribing of direct-acting oral anticoagulants (DOACs) due to favourable pharmacokinetics and pharmacodynamics without the need for regular coagulation monitoring

  • There is a need to understand the role of pharmacogenetics in the adaptation of anticoagulant therapy according to a patient’s genetic characteristics. This scientific review of current data on the impact of different gene polymorphisms on apixaban pharmacokinetics broadens the understanding of the clinical relevance of genotyping for treatment efficacy and safety

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Summary

Introduction

1 – Russian Medical Academy of Continuing Professional Education, Moscow, Russia 2 – S.S. Поскольку апиксабан является субстратом для P-gp и CYP3A4, приём апиксабана вместе с сильными ингибиторами P-gp или CYP3A4 может увеличить его концентрацию в плазме в среднем в 2 раза и привести к нежелательным кровотечениям, в то время как приём с индукторами P-gp или CYP3A4 может уменьшить его эффективность и концентрацию в плазме [22]. Это является фактором риска развития нежелательных реакций (в частности, кровотечений) при приёме апиксабана [24].

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