Related Experiment Video

Updated: Mar 31, 2026

Microfluidics in Assessing Platelet Function
06:47

Microfluidics in Assessing Platelet Function

Published on: November 8, 2024

1.8K

Ticagrelor Does Not Inhibit Adenosine Transport at Relevant Concentrations: A Randomized Cross-Over Study in Healthy

T N A van den Berg1, S El Messaoudi1, G A Rongen2

  • 1Department of Pharmacology-Toxicology, Radboud university medical center, Nijmegen, The Netherlands.

Plos One
|October 29, 2015
PubMed

Insights

Ticagrelor does not impact adenosine transport or formation in healthy individuals at therapeutic doses. This suggests the drug

Area of Science:

  • Pharmacology
  • Cardiovascular Medicine
  • Biochemistry

Background:

  • Ticagrelor is a medication used to reduce cardiovascular events in myocardial infarction patients.
  • Dyspnea is a known side effect of ticagrelor, potentially linked to adenosine receptor stimulation.
  • Preclinical studies suggest ticagrelor may inhibit nucleoside transporters and increase ATP release.

Purpose of the Study:

  • To investigate the in vivo effects of ticagrelor on the human adenosine system.
  • To determine if ticagrelor influences adenosine transport and formation in healthy subjects.

Main Methods:

  • A double-blinded, placebo-controlled, cross-over trial involving 14 healthy participants.
  • Assessment of ticagrelor's effect on adenosine- and dipyridamole-induced forearm vasodilation.
  • Ex vivo measurement of adenosine and uridine uptake in isolated red blood cells.

Main Results:

  • Ticagrelor did not significantly alter adenosine- or dipyridamole-induced vasodilation.
  • Ex vivo adenosine and uridine uptake in red blood cells remained unaffected by ticagrelor.
  • In vitro studies showed ticagrelor inhibited nucleoside uptake only at supra-physiological concentrations.

Conclusions:

  • Ticagrelor does not affect adenosine transport or formation at relevant plasma concentrations in healthy individuals.
  • The adenosine system is unlikely to be the mechanism behind ticagrelor's observed pleiotropic effects.
  • ClinicalTrials.gov identifier: NCT01996735.
Abstract

More Related Videos

Testing Acetylcholine Followed by Adenosine for Invasive Diagnosis of Coronary Vasomotor Disorders05:58

Testing Acetylcholine Followed by Adenosine for Invasive Diagnosis of Coronary Vasomotor Disorders

Published on: February 3, 2021

4.5K
A Research Method For Detecting Transient Myocardial Ischemia In Patients With Suspected Acute Coronary Syndrome Using Continuous ST-segment Analysis18:11

A Research Method For Detecting Transient Myocardial Ischemia In Patients With Suspected Acute Coronary Syndrome Using Continuous ST-segment Analysis

Published on: December 28, 2012

24.9K

Related Concept Videos

Bioavailability Study Design: Healthy Subjects Versus Patients01:15

Bioavailability Study Design: Healthy Subjects Versus Patients

Bioavailability studies are essential for evaluating a drug's therapeutic efficacy and understanding its absorption patterns under various physiological conditions. Conducting such studies on target patient populations provides more relevant data by simulating real-world disease states. However, practical challenges often necessitate the use of young, healthy adult volunteers as study subjects.Patients may exhibit altered drug absorption patterns due to the effects of the disease itself,...
208
Acute Coronary Syndrome III: Diagnostic Studies01:30

Acute Coronary Syndrome III: Diagnostic Studies

Diagnosing acute coronary syndrome or ACS begins with a thorough patient history. Notable symptoms include central, crushing chest pain radiating to the left arm, neck, jaw, or back, along with shortness of breath, sweating (diaphoresis), nausea, vomiting, dizziness, and palpitations.It is crucial to note any history of cardiac illnesses and assess risk factors, including age, gender, smoking, hypertension, diabetes, hyperlipidemia, and a sedentary lifestyle.During physical examination, vital...
426
Crossover Experiments01:16

Crossover Experiments

Crossover experiments, also called the repeated-measurements design, is a study design in which all experimental units are exposed to all treatments in different periods. Crossover experiments are generally used in psychology, the pharmaceutical industry, agriculture, and medicine.
Crossover designs are performed even with smaller sample sizes since the samples can act as their controls. These are better than simple randomized trials since patients are exposed to all the treatments.
4.7K
Antiarrhythmic Drugs: Class II Agents as β-Adrenergic Blockers01:24

Antiarrhythmic Drugs: Class II Agents as β-Adrenergic Blockers

Adrenergic stimulation generally impacts cardiac rate and rhythm. Specifically, stimulation of the β-adrenoceptors triggers an increase in intracellular calcium ion influx and pacemaker currents, which may cause arrhythmias. Catecholamines like adrenaline also demonstrate β2-adrenoceptor-mediated hypokalemia, impacting cardiac action potential and disrupting the normal cardiac rhythm. Class II antiarrhythmic drugs are β-adrenoceptor antagonists or β-blockers, which...
2.3K
Bioavailability Study Design: Single Versus Multiple Dose Studies01:11

Bioavailability Study Design: Single Versus Multiple Dose Studies

Bioavailability studies are essential for understanding how a drug is absorbed, distributed, metabolized, and excreted in the body. These studies assess the extent and rate at which the active pharmaceutical agent becomes available at the site of action. The design of bioavailability studies can involve single-dose or multiple-dose regimens, each with distinct advantages and limitations.Single-dose studies are the preferred approach due to their simplicity and reduced drug exposure for...
335
Acute Coronary Syndrome I: Introduction01:30

Acute Coronary Syndrome I: Introduction

Acute Coronary Syndrome (ACS) encompasses a spectrum of heart conditions caused by sudden obstruction of coronary arteries, typically resulting from the rupture of an atherosclerotic plaque and subsequent thrombus (blood clot) formation. This obstruction can lead to partial or complete blockage of blood flow, causing varying degrees of myocardial ischemia or infarction.ACS includes the following clinical entities:Unstable Angina (UA)Non-ST-Elevation Myocardial Infarction (NSTEMI)ST-Elevation...
1.7K