Review ArticleEmerging Role of Fentanyl in Antiplatelet TherapyKuczyńska, Katarzyna MSc; Boncler, Magdalena PhDAuthor Information Department of Haemostasis and Haemostatic Disorders, Chair of Biomedical Sciences, Medical University of Lodz, Lodz, Poland. Reprints: Magdalena Boncler, PhD, Department of Haemostasis and Haemostatic Disorders, Chair of Biomedical Sciences, Medical University of Lodz, ul. Mazowiecka 6/8, 92-215 Lodz, Poland (e-mail: email@example.com). The authors report no conflicts of interest. Journal of Cardiovascular Pharmacology: September 2020 - Volume 76 - Issue 3 - p 267-275 doi: 10.1097/FJC.0000000000000880 Buy Metrics Abstract Fentanyl is a potent synthetic opioid used to alleviate severe and chronic pain, as well as an adjunct to general or local anesthesia. Although fentanyl has been used for decades, its full effects are still unknown. Its analgesic and anesthetic activity arises from the stimulation of μ-opioid receptors, resulting in the inhibition of adenyl cyclase and downregulation of cyclic adenosine 3',5'-monophosphate (cAMP), as well as decreased calcium channel activity and increased potassium channel activity. The μ-opioid receptors are abundantly distributed within the central nervous system, where they mediate analgesia, and in the nerve cells of the intestines, where they regulate gastrointestinal tract motility in the secretion or transport of fluids and electrolytes. They are also expressed in blood cells, blood vessel cells, and skin. Given the widespread distribution of μ-opioid receptors, it is likely that fentanyl may also regulate the activity of many other cells, including platelets. Recent findings indicate that it may impair the action of ticagrelor: an oral P2Y12 receptor inhibitor acting as an antiplatelet drug. It could pose a risk of insufficient platelet inhibition and result in thrombotic complications in patients with coronary artery disease. This article tackles the issue of fentanyl interactions with antiplatelet drugs. The mechanism of this phenomenon is not fully understood. Similarly, the biological effects exerted by fentanyl on platelets and the presence of opioid receptors on the platelet surface remain an open question. Copyright © 2020 Wolters Kluwer Health, Inc. All rights reserved.