A review of the effects of ticagrelor on adenosine concentration and its clinical significance

Akkaif, Mohammed Ahmed and Ng, Mei Li and Kader, Muhamad Ali Sk Abdul and Daud, Nur Aizati Athirah and Sha'aban, Abubakar and Ibrahim, Baharudin (2021) A review of the effects of ticagrelor on adenosine concentration and its clinical significance. Pharmacological Reports, 73 (6). pp. 1551-1564. ISSN 1734-1140, DOI https://doi.org/10.1007/s43440-021-00309-0.

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Background Ticagrelor is an oral antiplatelet drug that can reversibly bind to the platelet P2Y12 receptor. Ticagrelor is metabolized mainly by CYP3A4 and produces a rapid blood concentration-dependent platelet inhibitory effect. Unlike other P2Y12 receptor antagonists, many clinical features of ticagrelor are not related to P2Y12 receptor antagonism. Purpose This review aims to gather existing literature on the clinical effects of ticagrelor after inhibiting adenosine uptake. Methodology The current study reviewed literature related to the effects of ticagrelor on adenosine metabolism. The review also examined the drug's biological effects and clinical characteristics to see how it could be used in a clinical setting. Results Many studies have shown that ticagrelor can inhibit equilibrative nucleoside transporter 1 (ENT1). This inhibition leads to intracellular adenosine uptake, increased adenosine half-life and plasma concentration levels and an enhanced adenosine-mediated biological effect. Conclusions Based on the studies reviewed, it was found that ticagrelor essentially inhibits adenosine absorption of adenosine into cells through ENT1, which increases the concentration in the blood and subsequently increases the protection of the heart muscle by adenosine. It also prevents platelet aggregation, and extends the biological effects of coronary arteries. Moreover, it leads to a lower mortality rate in acute coronary syndrome (ACS) patients.

Item Type: Article
Uncontrolled Keywords: Ticagrelor; Antiplatelet; Adenosine; ENT1
Subjects: R Medicine
R Medicine > RM Therapeutics. Pharmacology
R Medicine > RS Pharmacy and materia medica
Divisions: Faculty of Pharmacy > Department of Clinical Pharmacy and Pharmacy Practice
Depositing User: Ms Zaharah Ramly
Date Deposited: 29 Jul 2022 07:12
Last Modified: 29 Jul 2022 07:12
URI: http://eprints.um.edu.my/id/eprint/28207

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