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Review
. 2021 Dec;73(6):1551-1564.
doi: 10.1007/s43440-021-00309-0. Epub 2021 Jul 20.

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

Mohammed Ahmed Akkaif  1 , Mei Li Ng  2 , Muhamad Ali Sk Abdul Kader  3 , Nur Aizati Athirah Daud  1 , Abubakar Sha'aban  1 , Baharudin Ibrahim  4
Affiliations
Review

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

Mohammed Ahmed Akkaif et al. Pharmacol Rep. 2021 Dec.

Abstract

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.

Keywords: Adenosine; Antiplatelet; ENT1; P2Y12 receptor; Ticagrelor.

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