Romanian Society of Pharmaceutical Sciences
 

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TICAGRELOR – MECHANISM OF ACTION AND ITS IMPACT ON DRUG EFFICACY

LOREDANA-MARIA MARIN 1*, IULIAN SÎRBU 2, EMMA-ADRIANA OZON 3, MARCIN SKOTNICKI 4, JANINA LULEK 4, RĂZVAN DANIEL CHIVU 5, DOINA DRĂGĂNESCU 1

1“Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Physics, 020956 Bucharest, Romania
2 Zentiva S.A., 032266 Bucharest, Romania
3 “Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmacy, 020956 Bucharest, Romania
4 Poznan University of Medical Sciences, Faculty of Pharmacy, Department of Pharmaceutical Technology, Industrial Pharmacy Division, 60-806 Poznan, Poland
5 “Carol Davila” University of Medicine and Pharmacy, Faculty of Midwifery and Nursing, 050474 Bucharest, Romania

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Ticagrelor is an oral antiplatelet agent that inhibits cellular adenosine re-uptake by reversibly binding to the P2Y12 receptors on platelets, with a broad therapeutic window compared to other antiplatelet agents. By increasing the plasma level of adenosine, the coronary blood flow is increased and the platelet conglomeration is restrained, preventing major cardiovascular events. These effects positively influence clinical outcomes in patients with acute ischemic stroke or coronary syndromes, as established by the results of several large randomised trials. However, due to its effect on adenosine metabolism, its use is associated with many adverse reactions, including dyspnoea and increased serum uric acid. Ticagrelor is a substrate and modulator of the P-glycoprotein transporter and the CYP3A4 enzyme, a member of the cytochrome P450; thus, polypharmacy and co-morbidities should not be neglected during the administration of ticagrelor together with other pharmacological agents. Therefore, international treatment guidelines acknowledge the importance of ticagrelor in contemporary cardiovascular medicine.