Differences in the effects of extended-release aspirin and plain-formulated aspirin on prostanoids and nitric oxide in healthy volunteers

Fundam Clin Pharmacol. 2003 Jun;17(3):363-72. doi: 10.1046/j.1472-8206.2003.00137.x.

Abstract

This study was designed to evaluate the effects of extended-release aspirin on platelet aggregation and the production of prostanoids and nitric oxide. The participants in this double blind, randomized and crossover study were 20 healthy volunteers. Interventions were 150 mg of plain-formulated aspirin (PFASA) and 150 mg of extended-release aspirin (ERASA). Blood samples were collected before and 10, 20, 60, 120, 240, 480 and 1440 min after the first dose; 3, 7 and 14 days after daily administration and 24 h after the last dose. The main measures were platelet aggregometry, thromboxane B2, 6-keto-prostaglandin (PG) F1alpha and nitric oxide in each control. Platelet aggregation was inhibited by 50% with ERASA, and by 77% with PFASA. No differences were found in chronic treatment. Thromboxane B2 was inhibited more by the latter (51-67%), but 90% inhibition was observed in both groups after 3 days. The levels of 6-keto-PGF1alpha was reduced by 20% with ERASA and by 58% with PFASA. Nitric oxide production increased in both groups, but after 24 h, and 7-14 days, elevated concentrations of nitric oxide were found only in the ERASA. The antiplatelet effects of ERASA provide pharmacological advantages (greater prostacyclin synthesis and prolonged increase in nitric oxide production) over those provided by the plain formulation.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Aspirin / administration & dosage
  • Aspirin / blood
  • Aspirin / metabolism
  • Aspirin / pharmacology*
  • Cross-Over Studies
  • Delayed-Action Preparations
  • Dinoprost / antagonists & inhibitors*
  • Dinoprost / biosynthesis
  • Double-Blind Method
  • Epoprostenol / agonists*
  • Female
  • Humans
  • Male
  • Nitric Oxide / agonists*
  • Nitric Oxide / biosynthesis
  • Platelet Aggregation Inhibitors / administration & dosage
  • Platelet Aggregation Inhibitors / metabolism
  • Platelet Aggregation Inhibitors / pharmacology*
  • Salicylic Acid / blood
  • Thromboxane B2 / antagonists & inhibitors

Substances

  • 6-keto-prostaglandin F2alpha
  • Delayed-Action Preparations
  • Platelet Aggregation Inhibitors
  • Nitric Oxide
  • Thromboxane B2
  • Dinoprost
  • Epoprostenol
  • Salicylic Acid
  • Aspirin