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At least 343 records · Page 19Linked to original sources
PubMed1999

Inhibition of platelet aggregation after intake of acetylsalicylic acid detected by a platelet function analyzer (PFA-100).

OBJECTIVE: The aim of the investigation was to determine the inhibition of platelet aggregation detected by the platelet function analyzer PFA-100 in patients with coronary artery disease who routinely take 100 mg acetylsalicylic acid once daily. METHOD: The PFA-100 (Dade International Inc., Miami, USA) is a new device for in vitro measurement of platelet function in citrated whole blood. The time needed to form a platelet plug occluding the aperture cut into a collagen/epinephrine- or collagen/ADP-coated membrane is determined under high shear conditions. Typically, acetylsalicylic acid-induced inhibition of platelet aggregation is detected by prolonged closure time in collagen/epinephrine or and normal values for collagen/ADP. Blood samples of 48 patients were investigated, the control group consisted of 10 healthy volunteers without intake of acetylsalicylic acid. The upper limits of normal values of the control group were 137 sec closure time for collagen/epinephrine and 150 sec for collagen/ADP (mean + 2 SD). RESULTS: Statistical analysis (Wilcoxon test) did not show a significant difference (p = 0.46) between the patient group (129 +/- 11 sec) and the control group (92 +/- 7 sec) for collagen/epinephrine (mean +/- SEM). Only 31% of patients had closure time values above those upper limits defined above. CONCLUSION: The effect of 100 mg acetylsalicylic acid daily appears to be too small and too variable to detect a sufficient inhibition of platelet aggregation by the PFA-100 in all patients with coronary artery disease.

Adult↗
PubMed2003

Metabolic interactions between acetylsalicylic acid and benzene.

The aim of the study was to evaluate cytochrome P-450 dependent hepatic monooxygenases system and urinary excretions of phenol and muconic acid in animals subjected to acetylsalicylic acid (ASA) orally and benzene by inhalations. ASA increased urinary excretion of muconic acid although it did not affect the urinary level of phenol. Benzene decreased concentrations of P-450 and b(5) cytochromes and the activities of NADPH-cytochrome P-450 and NADH-cytochrome b(5) reductases. In rats exposed to ASA and benzene simultaneously the concentration of both cytochromes and the activity of the cytochrome dependent reductases was higher than in the rats exposed only to benzene and sometimes exceeded the control group values.

Administration, Inhalation↗
PubMed1981

Increased serum salicylate metabolites with age in patients receiving chronic acetylsalicylic acid therapy.

A high pressure liquid chromatographic method was used to measure the serum concentrations of salicylic, salicyluric and gentisic acids in patients receiving chronic acetylsalicylic acid therapy. There was good correlation between this method and the established colorimetric assay for salicylic acid. The concentration of gentisic and salicyluric acids were increased in patients older than 60 years. No correlation was found with sex, concomitant ingestion of other drugs, serum creatinine or serum albumin.

Adult↗
PubMed1980

Double blind cross-over trial comparing fenbufen and acetylsalicylic acid in rheumatoid arthritis.

25 out-patients with active classical or definite adult-onset rheumatoid arthritis were enrolled in a 4-week randomized, two-period double-blind cross-over study comparing gamma-oxo(1,1'-biphenyl)-4-butanoic acid (fenbufen) (1000 mg/d) and acetylsalicylic acid (ASA) (3600 mg/d). Only patients with active, flaring disease, off antiinflammatory drugs, were admitted into this study. Significant mean improvement from baseline was seen with both fenbufen and ASA after two weeks of treatment. There were no statistically significant differences between the degree of improvement from baseline between fenbufen and ASA. However, there were significant differences in patient tolerance of the two medications with more patients reporting adverse experiences with ASA than with fenbufen. The differences between treatments were statistically significant for side effects graded as moderate or severe with 6 patients experiencing drug-related side effects on ASA compared to none on fenbufen.

Adult↗
PubMed1993

Protection by acetylsalicylic acid against hyperglycemia-induced glycation and neural tube defects in cultured early somite mouse embryos.

The embryopathic effects of hyperglycemia have been established in rodent embryos maintained in whole embryo culture during neurulation. This study addressed the possibility that the hyperglycemia-mediated teratogenic effects are associated with increased concentrations of glycated embryonic protein. Early somite mouse embryos were cultured in 50 mmol/l glucose for 48 h and subsequently demonstrated growth retardation and severe neural malformations. Incubation with 0.005 mmol/l acetylsalicylic acid, an effective anti-glycation agent, was partially protective against hyperglycemia-induced growth retardation, neural tube defects as well as the deleterious effects on the morphological development of specific tissues. Furosine measurements indicated that acetylsalicylic acid reduced individual embryonic concentrations of glycated protein in both hyperglycemic and normoglycemic embryos. Also, the total morphological score, somite number, head length and the forebrain morphological rating of individual embryos were negatively correlated with their tissue furosine content. The results indicate the possibility that hyperglycemia during embryo culture causes dysmorphogenesis via enhanced production of glycated embryonic proteins and that the protective action of acetylsalicylic acid could be mediated by its anti-glycation properties.

Animals↗
PubMed1978

Effect of acetylsalicylic acid, paracetamol, and placebo on pain and blood loss in dysmenorrhoeic women.

The analgesic effect of paracetamol, acetylsalicylic acid, and placebo on dysmenorrhoea were compared in a double-blind crossover study of 30 women. There was a moderate placebo effect, but no significant difference was found between the three treatments. Blood loss was also measured and it did not vary with the type of drug ingested. It is concluded that paracetamol and acetylsalicylic acid in the doses used (0.5 g X 4 for 3 days) were not effective against heavy dysmenorrhoea, and that none of the drugs influenced the amount of blood lost.

Acetaminophen↗
PubMed1989

Indomethacin and acetylsalicylic acid block neurogenic plasma protein extravasation in rat dura mater.

Leakage of 125I-bovine serum albumin was measured in rat dura mater, conjunctiva, eyelid and lip, after unilateral electrical stimulation of the trigeminal ganglion. In one animal, 99Tc-human serum albumin leakage was imaged in ipsilateral facial tissues. Pretreatment with indomethacin 1 mg/kg i.p. decreased leakage in dura mater but not in extracranial tissues. When extravasation was expressed as a ratio of stimulated to unstimulated sides, indomethacin 1 mg/kg, or acetylsalicylic acid 50 mg/kg decreased this ratio from 1.80 to 1.27 (P less than 0.01) or from 1.84 to 1.21 (P less than 0.01), respectively. Dexamethasone (1 mg/kg i.p. tid X 1 day) caused only a very small decrease. Only large doses of indomethacin (10 mg/kg) or acetylsalicylic acid (50 mg/kg) reduced substance P (SP)-induced leakage in the dura. The latter results suggest that both drugs block plasma extravasation by acting on neuropeptides-induced changes in vascular permeability and/or smooth muscle contractility. However, inhibition of SP release from sensory axons cannot be excluded at concentrations which block neurogenic plasma extravasation but not SP-induced plasma leakage. Together, these results provide a possible mechanism for the therapeutic effects of indomethacin and acetylsalicylic acid in headache.

Animals↗
PubMed1982

[Comparative pharmacokinetics and relative bioavailability of the active principles diazepam, acetylsalicylic acid, caffeine, and dihydroergotamine tartrate in a combination product].

Following application of Silentan coated tablets (a combination of acetylsalicylic acid, caffeine, diazepam and dihydroergotamine (DHE) tartrate) in six healthy male volunteers serum concentrations were determined. The estimated relative bioavailabilities of these substances in the commercially available drug were compared to the encapsulated single substances. For acetylsalicylic acid and caffeine there were nearly no differences to be observed. Significant differences of the relative bioavailabilities are shown by Silentan-diazepam (= 118%) and Silentan-DHE-tartrate (= 310%) in comparison with the standard encapsulated preparations.

Adult↗
PubMed2004

Sequential injection chromatographic determination of paracetamol, caffeine, and acetylsalicylic acid in pharmaceutical tablets.

In this contribution, a new separation method for simultaneous determination of paracetamol, caffeine, acetylsalicylic acid, and internal standard benzoic acid was developed based on a novel reversed-phase sequential injection chromatography (SIC) technique with UV detection. A Chromolith Flash RP-18e, 25-4.6mm column (Merck, Germany) and a FIAlab 3000 system (USA) with an 8-port selection valve and a 5 mL syringe were used for sequential injection chromatographic separations in our study. The mobile phase used was acetonitrile-(0.01 M) phosphate buffer (10:90, v/v) pH 4.05, flow rate 0.6 mL min(-1). UV detection was at 210 and 230 nm. The validation parameters showed good results: linearity (r >0.999) for all compounds, detection limits in the range 0.3-0.8 microg mL(-1), repeatability (RSD) of peak heights between runs in the range 1.10-4.30% at three concentration levels and intra-day repeatability of the retention times in the range 0.28-0.43%. The analysis time was <6 min. The method was found to be applicable for the routine analysis of the active compounds paracetamol, caffeine, and acetylsalicylic acid in pharmaceutical tablets.

Acetaminophen↗
PubMed1983

Faecal blood loss during administration of acetylsalicylic acid, ketoprofen and two new ketoprofen sustained-release compounds.

The influence of one week's treatment with acetylsalicylic acid, ketoprofen, ketoprofen sustained-release capsules (Biovail capsules), and ketoprofen sustained-release tablets (IBP tablet) on gastrointestinal bleeding was investigated in 41 healthy male volunteers by means of a radiochromium assay. The physiological faecal bleeding was 0.10 to 0.90 ml/day (99% confidence limits). It appeared that faecal bleeding during treatment with acetylsalicylic acid medication was greater than bleeding during medication with ketoprofen capsules in equipotent dosage, the latter being in turn causing significantly more bleeding than during medication with the newly developed Biovail capsules. The most modest faecal bleeding (0.8 ml/day) was seen with IBP tablets.

Adult↗
PubMed1977

Effect of acetylsalicylic acid on gastric mucosa. II. Mucosal ATP and phosphocreatine content, and salicylate effects on mitochondrial metabolism.

The effects of acetylsalicylic acid on gastric mucosal ATP and phosphocreatine and mucosal O2 consumption were studied using in vitro bullfrog gastric mucosa. Electrophysiological parameters (potential difference and resistance) changed rapidly after exposure to 10 or 20 mM acetylsalicylic acid at pH 3.0, 4.0, or 6.0 in the mucosal solution. ATP and phosphocreatine content decreased rapidly after exposure. Control mucosae contained 11.8 +/- 0.98 nmoles of ATP and 11.5 +/- 0.68 nmoles of phosphocreatine per mg of protein. ATP content decreased 21% and phosphocreatine decreased 45% after 15 to 30 min of exposure. Longer durations of exposure reduced both ATP and phosphocreatine to 10 to 15% of control levels. O2 consumption was increased during the first 15 to 30 min after exposure to acetylsalicylate. Longer durations of exposure reduced O2 consumption to near control levels. Study of isolated mitochondria confirmed that acetylsalicylate itself did not significantly affect mitochondrial respiration, respiratory control ratio, or ADP:O ratio. Salicylate had a biphasic effect which was concentration dependent. Salicylate initially stimulated and later inhibited mitochondrial respiration. Using various substrates the site of inhibition appeared to be located in the segment of the respiratory chain between coenzyme Q and cytochrome c1.

Adenosine Triphosphate↗
PubMed1988

The effects of acetylsalicylic acid upon carbohydrate metabolism during exercise.

The effects of acute acetylsalicylic acid (ASA) ingestion upon carbohydrate metabolism during a 60 min treadmill moderate intensity exercise (50% VO2max) were studied in eleven normal females. A double-blind crossover design was used to compare the experimental findings with placebo. No significant differences were noted during the exercise protocol in glucose, insulin, glucagon and free fatty acid utilization between placebo/exercise and acetylsalicylic acid/exercise treatment. A significant post-exercise hypoinsulinemic and antilipolytic effect occurred with ASA/exercise treatment (p less than 0.05). In addition, post-exercise glucagon levels remained unchanged with ASA, whereas a significant plasma glucagon increase was noted with placebo (p less than 0.05). These data suggest that a prophylactic acetylsalicylic acid/exercise regimen will not adversely affect gluco-regulatory and counter-regulatory metabolism during exercise and could therefore, be safely instituted as an adjunct preventive therapy.

Adult↗
PubMed1984

Antiaggregatory efficacy and its time-course after application of acetylsalicylic acid, prostacyclin and nafazatrom in vivo.

Antiaggregatory potency and time courses of their respective efficacy were assessed for acetylsalicylic acid, prostaglandin (PGI2) and nafazatrom, a stimulator of PGI2-release from endothelial cells, and were compared in vivo. Endothelial cell damage was induced by excitation of intravascular fluoresceinisothio-cycanate-dextran. Time from onset of the noxious stimulus to aggregate appearance (TAA) was assessed and dose-dependently delayed by antithrombotic compounds. PGI2 was two orders of magnitude more effective than nafazatrom, acetylsalicylic acid was three orders of magnitude less effective than nafazatrom. Whereas the antiaggregatory potency of PGI2 decreased after 3.1 min to 50%, the antithrombotic efficacy of both, ASA and nafazatrom, further increased after a single bolus injection.

Animals↗
PubMedDate not supplied

[Treatment of acute poisoning caused by carbamazepine, digoxin, and acetylsalicylic acid, with repeated doses of activated charcoal].

Twelve pediatric patients with acute poisonings caused by carbamazepine, digoxin and acetylsalicylic acid were treated with multiple doses of activated charcoal combined with a saline cathartic (adsorption surface of activated charcoal nearly 950 m2/g). This procedure was effective to shorten the plasmatic levels of the drugs, besides the clinical improvement of the poisoned patients. The average initial and final levels of the drugs were: carbamazepine 21.64 and 0.9 micrograms/ml (lowering 95.81%, p < 0.05), digoxin 5.14 and 1.1 ng/ml (lowering 78.6%, P < 0.05) and acetylsalicylic acid 418.5 and 57.5 micrograms/ml, respectively, (lowering 86.3%, p < 0.05). These results suggest the usefulness of activated charcoal in the clearance of the four overdosed drugs.

Acute Disease↗
PubMed1978

Synthesis and pharmacological properties of eterylate, a new derivative of acetylsalicylic acid.

A description is given of the synthesis and main physical and chemical properties of a new derivative of acetylsalicylic acid which we have called eterylate and which is 2-(p-acetamidophenyloxy)-ethyl-o-acetoxy-benzoate. The anti-inflammatory and analgesic action of the preparation was studied and found to be comparable to that of acetylsalicylic acid and benorylate. Nevertheless, eterylate is tolerated better than the latter product, as is shown by toxicity tests and studies of the digestive system.

Animals↗
PubMed1992

[Evaluation of the antithrombotic effects of pentoxifylline, acetylsalicylic acid and low molecular weight heparin in the laser model of thrombosis].

Antithrombotic effects of different agents including acetylsalicylic acid (Asprocol/Polfa PL/), pentoxifylline (Agapurin/Spofa CS/) and low molecular weight heparin (Antixarin B. Braun, Melsungen, FRG) were studied in the laser-induced rat thrombosis model. The investigations were carried out on male Wistar rats weighing 200-300 g. Thrombus formation was induced in small mesenteric arteries 25-30 microns; using argon laser. An interference contrast system based on a Leitz Orthoplan microscope for the evaluation of thrombus formation was used. The number of laser injuries needed to induce a defined thrombus proved to be a useful way to quantitate the results in this thrombosis mode. All agents showed dose dependent antithrombotic effect in our laser model. Acetylsalicylic acid (ASA) 2 hours after oral administration markedly inhibited thrombus formation in minimal dose 50 mg/kg, pentoxifylline in dose 10 mg/kg 30 min after i.v. injection and low molecular weight heparin (Antixarin) in dose 0.1 mg/kg, 2 hours, after s.c. injection. Antithrombotic effect of administration of minimal effective doses of ASA (orally) and pentoxifylline (i.v.) lasted longer than 4 hours but less then 6 hours. LMW heparin (Antixarin) in minimal effective dose 0.1 mg/kg after s.c. injection inhibited thrombus formation in small mesenteric vessels for more than 12 hours but less than 24 hours.

Animals↗
PubMed1976

Teratogenicity studies with methotrexate, aminopterin, and acetylsalicylic acid in domestic cats.

Pregnancy was timed in cats following induced ovulation. Methotrexate, (0.5 mg/kg), aminopterin, (0.1 mg/kg), and acetylsalicylic acid, (25 or 50 mg/kg) were administered orally in gelatin capsules in single daily doses on different days of gestation, methotrexate (MTX) on days 11-14, 14-17, or 17-20, aminopterin on day 12, 14, or 16, and acetylsalicylic acid (ASA) on days 10-15 or 15-20. Maternal toxicity was produced only by MTX. MTX given on days 11-14 and 14-17 produced high frequencies of malformations including umbilical hernia. Aminopterin caused no conclusive teratogenic response. An overall increased frequency of anomalies occurred after 50 mg/kg ASA but no single anomaly predominated.

Abnormalities, Drug-Induced↗
PubMed1984

Effect of dipyrone, acetylsalicylic acid and acetaminophen on human neutrophil chemotaxis.

Dipyrone metabolites 4-methylaminoantipyrine (MAA) and 4-formylaminoantipyrine (FAA) as well as acetylsalicylic acid inhibited neutrophil migration toward zymosan-activated serum. Inhibition was maximal (76.8 +/- 19.0; 79.2 +/- 12.5 and 80.0 +/- 4.4%, respectively, P less than 0.003) when suboptimal concentrations (0.3%) of the chemoattractant were used and could be demonstrated with drug concentrations comparable with plasma concentrations obtained in clinical use. Acetaminophen and other dipyrone metabolites 4-aminoantipyrine (AA) and 4-acetylaminoantipyrine (AAA) lacked chemotactic inhibitory potential. Only MAA and FAA inhibited mildly neutrophil random migration (18.1 +/- 7.8 and 11.2 +/- 3.4%, respectively). We suggest that blocking neutrophil movement plays a role in the anti-inflammatory activity of dipyrone and acetylsalicylic acid, but their mechanism of inhibition remains obscure.

Acetaminophen↗