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Ticagrelor Pharmacokinetics and Pharmacodynamics in Chinese Patients with STEMI and NSTEMI Without Opioid Administration

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Abstract

Introduction

The pharmacodynamics (PD) and pharmacokinetics (PK) study of ticagrelor loading dose (LD) in Chinese patients with acute coronary syndrome (ACS) without opioid administration has never been investigated. Therefore, the aim of this study was to evaluate the antiplatelet effects and the PK parameters of ticagrelor in Chinese patients with ACS without opioid administration.

Methods

A sample size of 30 eligible patients with ACS were enrolled in this study. Blood samples were obtained predose and 1, 2, 4, 8, and 12 h after 180 mg LD of ticagrelor. P2Y12 reactivity units (PRU) and plasma concentrations of ticagrelor and its two metabolites were measured.

Results

In total, 15 patients were admitted to ST segment elevation myocardial infarction (STEMI) and non-ST segment elevation myocardial infarction (NSTEMI) groups, respectively. For patients with NSTEMI, PRU declined significantly during the first 4 h and maintained a relatively stable antiplatelet effect from 4 to 12 h after LD. A similar trend was found in the STEMI group without significant differences of PRU in each designed time compared with patients with NSTEMI (P > 0.05). Tmax of metabolite AR-C124910XX was 4 h after LD for both groups. There were no significant differences for drug concentration, Cmax, or AUC of ticagrelor and AR-C124910XX between patients with STEMI and NSTEMI (P > 0.05).

Conclusions

For Chinese patients with ACS, at least 4 h was needed to achieve an adequate antiplatelet effect for ticagrelor LD. There were no differences in PK or PD between Chinese patients with STEMI and NSTEMI.

Clinical Trial Registration

ChiCTR1800014764.

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Acknowledgements

The authors would like to thank all study participants.

Funding

No funding or sponsorship was received for this study or publication of this article. The Rapid Service Fee was funded by the authors.

Authorship

All named authors meet the International Committee of Medical Journal Editors (ICMJE) criteria for authorship for this article, take responsibility for the integrity of the work as a whole, and have given their approval for this version to be published.

Author contributions

Juying Qian and Junbo Ge designed research; Yinman Wang, Yaolin Chen, Qibing Wang, and Hongyi Wu performed research; Yinman Wang, Yaolin Chen, Juying Qian, and Qibing Wang analyzed data; Yinman Wang and Hongyi Wu wrote the paper.

Disclosures

Yinman Wang, Hongyi Wu, Yaolin Chen, Qibing Wang, Juying Qian, and Junbo Ge have nothing to disclose.

Compliance with Ethics Guidelines

This study (ChiCTR1800014764) was conducted in accordance with the Declaration of Helsinki and was approved by the Ethics Committee of Zhongshan Hospital, Fudan University (SFDA,2013B00564;H20120486). All patients signed informed consent to participate in the study.

Data Availability

The datasets generated during and analyzed during the current study are available from the corresponding author on reasonable request.

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Author notes

  1. Yinman Wang, Hongyi Wu, and Yaolin Chen contributed equally to this work and should be considered co-first authors.

Authors and Affiliations

  1. Department of Cardiology, Zhongshan Hospital, Fudan University. Shanghai Institute of Cardiovascular Diseases, Shanghai, China

    Yinman Wang, Hongyi Wu, Qibing Wang, Juying Qian & Junbo Ge

  2. Department of Cardiology, Xiamen Branch, Zhongshan Hospital, Fudan University, Xiamen, Fujian Province, China

    Yaolin Chen

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  1. Yinman Wang
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  2. Hongyi Wu
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  6. Junbo Ge
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Corresponding author

Correspondence to Juying Qian.

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Wang, Y., Wu, H., Chen, Y. et al. Ticagrelor Pharmacokinetics and Pharmacodynamics in Chinese Patients with STEMI and NSTEMI Without Opioid Administration. Adv Ther 37, 4220–4232 (2020). https://doi.org/10.1007/s12325-020-01423-w

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  • DOI: https://doi.org/10.1007/s12325-020-01423-w

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