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

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.

• Authors: Yinman Wang, Hongyi Wu, Yaolin Chen, Qibing Wang, Juying Qian, Junbo Ge
• Journal: Advances in therapy (Adv Ther) Vol. 37 Issue 10 Pg. 4220-4232 (10 2020) ISSN: 1865-8652 [Electronic] United States
• PMID: 32770531 (Publication Type: Journal Article)

Chemical References

• Analgesics, Opioid
• Platelet Aggregation Inhibitors
• Purinergic P2Y Receptor Antagonists
• Ticagrelor

Topics

• Analgesics, Opioid
• China
• Humans
• Non-ST Elevated Myocardial Infarction (drug therapy)
• Percutaneous Coronary Intervention
• Platelet Aggregation Inhibitors (therapeutic use)
• Prospective Studies
• Purinergic P2Y Receptor Antagonists
• ST Elevation Myocardial Infarction (drug therapy)
• Ticagrelor