Mohammed Ahmed Akkaif1, Mei Li Ng2, Muhamad Ali Sk Abdul Kader3, Nur Aizati Athirah Daud1, Abubakar Sha'aban1, Baharudin Ibrahim4. 1. School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800, Gelugor, Penang, Malaysia. 2. Advanced Medical and Dental Institute, Universiti Sains Malaysia, 13200, Gelugor, Penang, Malaysia. 3. Department of Cardiology, Penang General Hospital, 10990, George Town, Pulau Pinang, Malaysia. 4. Faculty of Pharmacy, University of Malaya, 50603, Kuala Lumpur, Malaysia. baharudin.ibrahim@um.edu.my.
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.
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.
Authors: Lars Wallentin; Richard C Becker; Andrzej Budaj; Christopher P Cannon; Håkan Emanuelsson; Claes Held; Jay Horrow; Steen Husted; Stefan James; Hugo Katus; Kenneth W Mahaffey; Benjamin M Scirica; Allan Skene; Philippe Gabriel Steg; Robert F Storey; Robert A Harrington; Anneli Freij; Mona Thorsén Journal: N Engl J Med Date: 2009-08-30 Impact factor: 91.245
Authors: Mohammed Ahmed Akkaif; Nur Aizati Athirah Daud; Abubakar Sha'aban; Mei Li Ng; Muhamad Ali Sk Abdul Kader; Dzul Azri Mohamed Noor; Baharudin Ibrahim Journal: Molecules Date: 2021-04-01 Impact factor: 4.411
Authors: Mohammed Ahmed Akkaif; Ahmad Naoras Bitar; Laith A I K Al-Kaif; Nur Aizati Athirah Daud; Abubakar Sha'aban; Dzul Azri Mohamed Noor; Fatimatuzzahra' Abd Aziz; Arturo Cesaro; Muhamad Ali Sk Abdul Kader; Mohamed Jahangir Abdul Wahab; Chee Sin Khaw; Baharudin Ibrahim Journal: J Cardiovasc Dev Dis Date: 2022-09-16