WASHINGTON – Administration of crushed tablets of ticagrelor* may provide a way to dramatically accelerate the onset of platelet inhibition in patients with ST-elevation myocardial infarction.
In a proof-of-concept crossover study involving 36 healthy volunteers, crushing a whole 90-mg tablet of ticagrelor (Brilinta) and suspending it in 200 mL of water given orally resulted in a mean plasma ticagrelor concentration of 149 ng/mL 30 minutes post dose, compared with 34 ng/mL after a whole tablet was swallowed, Dr. Glenn F. Carlson reported at the annual meeting of the American College of Cardiology.
When the crushed tablet suspended in water was administered via nasogastric tube, the results were even more dramatic: a mean plasma ticagrelor concentration of 265 ng/mL 30 minutes post dose, or a ninefold greater mean plasma concentration compared with swallowing a whole tablet, said Dr. Carlson of AstraZeneca.
At 1 hour post dose, mean plasma concentrations of ticagrelor and its metabolite remained significantly greater with both of the crushed-tablet dosing strategies than with whole ticagrelor. However, 2 to 48 hours post dose, plasma concentrations were similar for all three drug administration strategies.
The clinical relevance of these findings lies in the well-established observation that in acute coronary syndromes – and especially in ST-elevation myocardial infarction – time is myocardium. That is, the more quickly that effective antiplatelet activity and reperfusion can be achieved, the less extensive the myocardial tissue damage, he noted.
The three modes of ticagrelor administration were found to be bioequivalent and equally safe.
The study was funded by AstraZeneca. Dr. Carlson is an employee of the company.
*CORRECTION, 4/29/2014: An earlier version of the article misstated the name of the drug ticagrelor.