Ibuprofen protects platelet cyclooxygenase from irreversible inhibition by aspirin.

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Ibuprofen protects platelet cyclooxygenase from irreversible inhibition by aspirin.

Previous investigations have shown that ibuprofen inhibits the second wave of platelet aggregation and blocks the conversion of 14C-arachidonic acid to thromboxane. However, the influence of the drug on platelet function and cyclooxygenase is transitory, lasting only 24 hours. The present study has taken advantage of the short-lived influence of ibuprofen to study its interaction with the long-...

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Mechanistic insights into cyclooxygenase irreversible inactivation by aspirin.

A mechanistic hypothesis for the acetylation of cyclooxygenase (COX) by aspirin is proposed on the basis of a QM/MM study. This mechanism is consistent with previous experimental findings by other investigators. Ser 530 appears to be acetylated under intramolecular general base catalysis provided by the carboxylate moiety of aspirin, while Tyr 385 plays a crucial role in orienting and polarizin...

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Metabolic Syndrome Suboptimal Inhibition of Platelet Cyclooxygenase-1 by Aspirin in Metabolic Syndrome

Interindividual variation in the ability of aspirin to inhibit platelet cyclooxygenase-1 (COX-1) could account for some on-treatment cardiovascular events. Here, we sought to determine whether there are clinical phenotypes that are associated with a suboptimal pharmacological effect of aspirin. In a prospective, 2-week study, we evaluated the effect of aspirin (81 mg) on platelet COX-1 in 135 p...

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Suboptimal inhibition of platelet cyclooxygenase-1 by aspirin in metabolic syndrome.

Interindividual variation in the ability of aspirin to inhibit platelet cyclooxygenase-1 (COX-1) could account for some on-treatment cardiovascular events. Here, we sought to determine whether there are clinical phenotypes that are associated with a suboptimal pharmacological effect of aspirin. In a prospective, 2-week study, we evaluated the effect of aspirin (81 mg) on platelet COX-1 in 135 p...

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Population pharmacodynamic modelling of aspirin- and Ibuprofen-induced inhibition of platelet aggregation in healthy subjects.

OBJECTIVE The objective of this study was to develop a mechanism-based pharmacodynamic model that characterizes the antiplatelet effects of aspirin (acetylsalicylic acid) and ibuprofen alone and in combination. METHODS Ten healthy volunteers were enrolled in a single-blinded, randomized, three-way crossover study. Treatments consisted of single doses of oral aspirin (325 mg) and ibuprofen (40...

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ژورنال

عنوان ژورنال: Arteriosclerosis: An Official Journal of the American Heart Association, Inc.

سال: 1983

ISSN: 0276-5047

DOI: 10.1161/01.atv.3.4.383