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

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.

Antioxidant effect of acetylsalicylic and salicylic acid in rat brain slices subjected to hypoxia

“…The beneficial effect of this treatment results from its antithrombotic effect, and possibly from its neuroprotective effect. According to several studies, it seems that ASA has an antiplatelet effect, and that SA is involved in modulation of the inhibition of vascular prostacyclin synthesis and the increased production of NO that ASA brings about (Peterson et al, 1981; De Gaetano et al, 1985; De La Cruz et al, 2002a, 2003). In experiments that compared the oral administration of ASA and SA, we aimed to evaluate the importance of this cytoprotective effect in brain tissue, and to determine the role of SA in this effect.…”

Diabetic macular edema, retinopathy and age-related macular degeneration as inflammatory conditions

“…It is noteworthy that aspirin selectively enhances PGI 2 synthesis and NO and heme oxygenase-1 activity (which leads to enhanced generation of carbon monoxide, CO) and decreases levels of plasma asymmetrical dimethylarginine (ADMA), a competitive inhibitor of NO [ 57 – 61 ]. These changes in PGI 2 , NO and CO and ADMA levels may account for some of the beneficial actions of aspirin in DME, DR and AMD.…”

Designing Safer Analgesics via μ-Opioid Receptor Pathways

“…Charles Romley Wright, an English scientist, synthesized heroin in 1874 and sold it to the Bayer Company in 1898 [49]. Salicylic acid was first isolated in 1828 by Johann Andreas Buchner, and was formulated by Frederick Bayer and Felix Hoffman in 1895 [50]. In an effort to develop less-addictive painkillers, chemists synthesized compounds such as codeine and methadone in the mid-20th century.…”