- NEWS . 25 Sep 2020
PD and PK study of ticagrelor loading dose in Chinese ACS patients
The pharmacodynamics (PD) and pharmacokinetics (PK) of ticagrelor loading dose (LD) in Chinese patients with acute coronary syndrome (ACS) without opioid administration have not been investigated. Therefore, a study was carried out to evaluate the antiplatelet effects and the PK parameters of ticagrelor in Chinese patients with ACS without opioid administration.
In the study, a total of 30 eligible patients with ACS were enrolled. Patients were divided equally into ST segment elevation myocardial infarction (STEMI) and non-ST segment elevation myocardial infarction (NSTEMI) groups. Blood samples were obtained pre-dose and 1, 2, 4, 8 and 12 hours after 180 mg LD of ticagrelor; P2Y12-reactivity units (PRU) and plasma concentrations of ticagrelor and its two metabolites were measured.
For patients with NSTEMI, PRU declined significantly during the first 4 hours and maintained a relatively stable antiplatelet effect from 4 to 12 hours after LD. A similar trend was observed in the STEMI group without significant differences of PRU in each time point compared with patients with NSTEMI. Tmax of the active metabolite of ticagrelor (AR-C124910XX) was 4 hours after LD for both groups. There were no significant differences for drug concentration, Cmax or AUC of ticagrelor and its active metabolite between patients with STEMI and NSTEMI.
These findings suggest that at least 4 hours may be needed to achieve an adequate antiplatelet effect for ticagrelor LD in Chinese patients with ACS. There seem to be no differences in PK or PD between Chinese patients with STEMI and NSTEMI.
Wang Y, et al. Ticagrelor pharmacokinetics and pharmacodynamics in Chinese patients with STEMI and NSTEMI without opioid administration. Adv Ther. 2020. doi: 10.1007/s12325-020-01423-w. [Epub ahead of print]