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Stroke and Transient Ischemic Attacks of the Brain and Eye
Published in Philip B. Gorelick, Fernando D. Testai, Graeme J. Hankey, Joanna M. Wardlaw, Hankey's Clinical Neurology, 2020
The Acute Stroke or Transient Ischaemic Attack Treated with Ticagrelor and ASA (acetylsalicylic acid) for Prevention of Stroke and Death (THALES) trial recently reported that among patients with a mild-to-moderate acute noncardioembolic ischemic stroke (NIHSS score ≤ 5) or TIA who were not undergoing intravenous or endovascular thrombolysis, the risk of the composite of stroke or death within 30 days was lower with the combination of ticagrelor (180 mg loading dose followed by 90 mg twice daily) plus aspirin (300–325 mg on the first day followed by 75–100 mg daily) than with aspirin alone, but the incidence of disability did not differ significantly between the two groups. Severe bleeding was more frequent with ticagrelor.70a
Hematologic Drugs
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: It should be used with caution because the pregnancy experience in humans is limited, and the reproduction studies in animals have shown the risk of structural abnormalities associated with the use of Ticagrelor during organogenesis.
Antiplatelet therapy in interventional cardiology
Published in John Edward Boland, David W. M. Muller, Interventional Cardiology and Cardiac Catheterisation, 2019
The last decade has brought an increase in the number of P2Y12 inhibitors, and a consequent requirement to change agents on occasions. However, only the transition between clopidogrel to ticagrelor has been formally investigated.35 As a consequence of PLATO, guidelines recommend switching from clopidogrel to ticagrelor in ACS patients who have previously had clopidogrel exposure.72 Patients should be loaded with 180 mg of ticagrelor regardless of their last clopidogrel dose.72 This data contrasts with TRITON-TIMI 38, which excluded participants who had exposure of patients to a P2Y12 receptor.24 Thus, registry data provides limited information with regards to switching from clopidogrel to prasugrel.104 In addition, there is no outcome data on switching between ticagrelor and prasugrel, as well as ticagrelor/prasugrel to clopidogrel. As a result, the latest ESC guidelines discourage switching P2Y12 inhibitors due to a lack of safety/efficacy data.72 However the guidelines do recognise that agents may need to be switched for clinical reason and thus offer the guidance summarised in Figure 24.3.
Efficacy and safety of ticagrelor and clopidogrel in East Asian patients with coronary artery disease undergoing percutaneous coronary intervention
Published in Current Medical Research and Opinion, 2020
Jianan Li, Hong Qiu, Lirong Yan, Tingting Guo, Yong Wang, Yang Li, Jianfeng Zheng, Yida Tang, Bo Xu, Shubin Qiao, Yuejin Yang, Runlin Gao
In our study, compared with the clopidogrel group, the ticagrelor group had a lower incidence of MACCEs after propensity score at 1-year follow-up. Ticagrelor did show advantages over clopidogrel in patients with CAD undergoing PCI in our center, while the incidence of TIMI bleeding events was higher. The protective trend of ticagrelor was similar to that observed in the PLATO trial and other studies23–25. Patients in the ticagrelor group with the diagnose of UAP, NSTEMI and STEMI, hyperlipidemia, a previous history of MI and PCI, lower LVEF, higher LDL-C, more stents, more three-vessel, left main disease and ACC/AHA type B2 or C lesions, larger stent diameter, longer total stent length, and less radial artery approach indicated that the condition of patients was more serious and that the interventional operation was difficult compared to that in the clopidogrel group. In these conditions, the clinicians prefer to use ticagrelor for antiplatelet therapy. If clopidogrel were used for antiplatelet therapy, the clinicians would likely use other types of drugs, such as glycoprotein IIb/IIIa inhibitor, to enhance the antiplatelet effect of clopidogrel. It also showed that clinicians were more confident about the antiplatelet effect of ticagrelor and avoided the combined use of other antiplatelet drugs, thus preventing related bleeding complications.
Effects of ticagrelor on the pharmacokinetics of rivaroxaban in rats
Published in Pharmaceutical Biology, 2020
Jia Chong, Hao Chen, Dapeng Dai, Shuanghu Wang, Quan Zhou, Junpeng Liu, You Lü, Hualan Wu, Minghui Du, Feifei Chen, Hui Jiang, Yunfang Zhou, Jiefu Yang
Combination of rivaroxaban with ticagrelor may cause potent antithrombotic effects. Rivaroxaban potently inhibits prothrombinase complex-bound factor Xa on the surface of activated platelets, thus inhibits thrombin generation and thrombin-induced platelet aggregation. Ticagrelor potently inhibits platelet activation, which may provide a catalytic surface for initiating and sustaining coagulation. Recently, it has been reported that rivaroxaban powerfully inhibited tissue factor-induced platelet aggregation in a concentration dependent manner and had a synergistic effect with ticagrelor (Perzborn et al. 2015). These findings may explain that very-low-dose rivaroxaban could reduce cardiovascular events in ACS patients. Our study revealed that the pharmacokinetic effects of ticagrelor on the metabolism of rivaroxaban raised rivaroxaban plasma concentration significantly in rats. The results demonstrated in our study and the pharmacodynamic interactions between rivaroxaban and ticagrelor suggest that caution should be paid when these two agents are co-administered in clinical practice, and rivaroxaban dose may need to be adjusted to minimize bleeding risk.
Ticagrelor versus clopidogrel in the management of acute myocardial infarction
Published in Journal of Community Hospital Internal Medicine Perspectives, 2019
Candice Volney, Anthony Collins, Sarah Adams
One of the newer antiplatelet agents is ticagrelor, a reversible P2Y12 receptor antagonist that binds at an allosteric site different from the ADP binding site, and doesn’t require metabolic activation [5]. Ticagrelor enhances coronary blood flow through microvascular vasodilation by inhibiting adenosine uptake by erythrocytes [4]. Adenosine offers myocardial protection against ischemia-reperfusion injury [8]. In summary, ticagrelor can be antiplatelet, vasodilatory, and cardioprotective. Compared to clopidogrel, ticagrelor has a faster onset of action and stronger platelet inhibition [4]. The Platelet Inhibition and Patient Outcomes (PLATO) study showed that ticagrelor reduces mortality due to a cardiovascular event and has a good safety profile [3]. The same study showed non-fatal complications such as dyspnea and arrhythmias due to ventricular pauses. There seems to be conflicting research in regards to ticagrelor having excess bleeding risks [3,9]. The PLATO trial led to ticagrelor implementation into clinical practice around the world [10].