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Results for “ACETYLSALICYLIC ACID”

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PubMed1980

Influence of tranexamic acid and acetylsalicylic acid on the thickness of the normal cornea.

In a masked cross-over study ten normal subjects were treated with tranexamic acid and acetylsalicylic acid one g three times daily for seven days. The central corneal thickness. was found to increase in response to acetylsalicylic acid and to decrease in response to tranexamic acid. This finding provides evidence for the involvement of the fibrinolytic system in the regulation of the normal corneal thickness. The endothelial morphology, as seen with the specular microscope, was unchanged during treatment with either drug.

Adult↗
PubMed1997

Serotonin and opiate involvement in the antinociceptive effect of acetylsalicylic acid.

Acetylsalicylic acid (ASA), 400 mg/kg i.p., displayed antinociceptive activity in both the hot-plate and the formalin test. ASA significantly increased brain serotonin (5-HT) content and reduced the number of 5-HT2 receptors in cortical brain membranes 30 min after drug administration. Pretreatment with naloxone abolished the antinociceptive activity of both ASA and morphine in the hot-plate and formalin tests and prevented the increase in cerebral 5-HT concentration and the reduction in 5-HT2 receptors in cortical membranes induced by ASA. The serum salicylate concentrations were not affected by pretreatment with naloxone. These data indicate a central antinociceptive activity of ASA and suggest that ASA may exert its antinociceptive action through serotonergic and opiatergic pathways.

Analgesics, Non-Narcotic↗
PubMed1969

Structural changes in human serum albumin induced by ingestion of acetylsalicylic acid.

Acetylsalicylic acid (aspirin) acetylates human serum albumin under physiologic conditions in vitro. These investigations were done to determine whether this phenomenon occurs in vivo and to delineate the site(s) of acetylation on the albumin molecule. Albumin was reacted in vitro with aspirin labeled with (14)carbon at the acetyl-1 or the carboxyl carbon. The altered albumin was hydrolyzed with trypsin and peptide mapping performed. Albumin so treated contains a unique peptide, designated "A," and shows diminution of two normal peptides, designated "B" and "C." Peptide "A" is never seen in normal albumin. Amino acid analyses indicate that peptide "A" equals the sum of peptides "B" and "C." Furthermore all three peptides contain lysine but lack arginine. Thus peptide "A" is formed by the acetylation of a lysine residue which is normally susceptible to trypsin and yields peptides "B" and "C." Radioautography of the peptide maps show most of the acetyl-1-(14)C activity in peptide "A." This indicates that one of the lysine residues in this peptide is the preferential site for the transacetylation reaction. Peptide "A," used as a marker for acetylation, is found in albumin from patients who take aspirin but is not demonstrable in albumin from one of these patients while she was taking sodium salicylate. A transacetylation reaction between aspirin and human albumin occurs in vivo and is similar to that observed in vitro.

Amino Acids↗
PubMed1982

[SKF 93479, a newly developed histamine H2-receptor antagonist. / Effect on gastric potential difference in the presence and absence of acetylsalicylic acid].

Acetylsalicylic acid (ASA) alters the gastric mucosal barrier as measured by the transmucosal potential difference (PD). The effect of the newly developed histamine H2-receptor antagonist 2-(2-(5-dimethylaminoethylfuran-2-ylmethylthio)ethylamino)-5-(6-methylpyrid-3-ylmethyl)pyrimid-4-one trihydrochloride (SKF 93479) on the ASA-induced drop in gastric PD was studied in 6 healthy volunteers. Mean basal PD was -38.5 to -39.5 mV. After 1000 mg of ASA PD decreased in 10-15 min to -25 mV. In subjects pretreated orally with 0.5 mg/kg SKF 93479, PD rose during 30-45 min to -53.5 mV. After ASA PD fell to -38.5 mV, but did not fall below normal.

Adult↗
PubMed1994

[Clarification of mechanism of acetylsalicylic acid].

Acetylsalicylic acid is probably the most widely used of all drugs. Recent data has provided new insights into its mechanism of action and documented its usefulness in cardiovascular prevention. At the same time we now understand better why plants benefit from new production of the mother compound-salicylic acid. Thus very old drugs can be quite newsworthy.

Aspirin↗
PubMed1983

Comparative gastric irritation by two buffered acetylsalicylic acid formulations and acetylsalicylic acid. A gastric potential difference analysis.

In a single dose clinical investigation two buffered acetylsalicylic acid formulations (Ascriptin and Ascriptin A/D) were shown to be significantly less irritating to the human gastric mucosa than acetylsalicylic acid, and no more irritating than a pharmacologically inert placebo. The measurements were taken using a minimally invasive method for recording transmural gastric potential difference changes versus time.

Adult↗
PubMed1993

Modulation of rat and human lymphocyte function by n-6 and n-3 polyunsaturated fatty acids and acetylsalicylic acid.

The effects of in vitro additions of between 10 and 100 microM n-6 and n-3 polyunsaturated fatty acids were examined on the proliferation of stimulated T lymphocytes in culture. For both phytohemagglutinin-induced human blood lymphocytes and concanavalin-A-induced rat splenic lymphocytes, the largest inhibitory effects were obtained with 22:4 n-6 and 22:6 n-3, and to a lesser extent with 20:5 n-3. Arachidonic acid 20:4 n-6, the main eicosanoid precursor, was not inhibitory, it even stimulated rat lymphocyte proliferation. Acetylsalicylic acid stimulated both human and rat lymphocyte proliferation. The effects of moderate decreases in the dietary n-6/n-3 ratio by either linseed oil or fish oil maximum eicosapentaenoic acid (MaxEPA) were determined on rat lymphocyte proliferation and natural killer (NK) cell activity in vitro. Dietary changes did not affect mitogen-induced lymphocyte proliferation in vitro, but proliferation of unstimulated lymphocytes was significantly lowered (4-fold) with the n-3-enriched diets. Dietary fish oil but not linseed oil significantly increased the NK cell activity of rat splenic lymphocytes. The n-3-enriched diets, especially the fish oil diets, reduced the stimulatory effect of in vitro added acetylsalicylic acid (aspirin) on lymphocyte proliferation.

Animals↗
PubMed1996

Thyromimetic action of the peroxisome proliferators clofibrate, perfluorooctanoic acid, and acetylsalicylic acid includes changes in mRNA levels for certain genes involved in mitochondrial biogenesis.

The effects of three peroxisome proliferators on the mRNA levels for some mitochondrial inner-membrane proteins in rat liver were investigated. Clofibrate, perfluorooctanoic acid, and acetylsalicylic acid all increased the mRNA levels for the mitochondrial-encoded respiratory-chain components cytochrome c oxidase subunit I and NADH dehydrogenase subunit I. Mitochondrial 16S rRNA was also induced by clofibrate. The mRNA levels for the nuclear-encoded mitochondrial inner-membrane proteins adenine nucleotide translocator and cytochrome c1 were selectively induced by the different peroxisome proliferators. Malic enzyme, which is induced by thyroid hormone, was also induced by the three peroxisome proliferators tested. These effects are in some ways similar to those obtained with thyroid hormone.

Animals↗
PubMed1986

Influence of gender and oral contraceptive steroids on the metabolism of salicylic acid and acetylsalicylic acid.

Salicylic acid and acetylsalicylic acid (aspirin) disposition after an oral dose of aspirin, 900 mg (equivalent to 689.7 mg of salicylic acid) was studied in eight males, eight females and eight females receiving oral contraceptive steroids (OCS). Salicylic acid clearance was 61% higher in males compared to the control female group, an effect due largely to enhanced activity of the glycine conjugation pathway (salicyluric acid formation) in males. Salicylic acid clearance was 41% higher in OCS-users compared to the control female group due to increases in both the glycine and glucuronic acid conjugation pathways in the pill users. There was no difference in any salicylic acid disposition parameter between males and OCS-users. Area under the plasma concentration-time curve (AUC) and elimination half-life of aspirin was significantly greater and aspirin plasma hydrolysis rate was significantly lower in both female groups compared to males. There was no difference between OCS-users and the control female group in any of these parameters. Aspirin AUC and elimination half-life were significantly correlated with aspirin plasma hydrolysis rate. These data confirm the importance of hormonal factors in the regulation of drug conjugation reactions in humans and suggest that sex-related differences in salicylic acid and aspirin disposition may be of clinical importance.

Adult↗
PubMed2004

Comparative study of the continuous wavelet transform, derivative and partial least squares methods applied to the overlapping spectra for the simultaneous quantitative resolution of ascorbic acid and acetylsalicylic acid in effervescent tablets.

The simultaneous spectrophotometric determination of ascorbic acid (AA) and acetylsalicylic acid (ASA) in effervescent tablets in the presence of the overlapping spectra was accomplished by the continuous wavelet transform (CWT), derivative spectrophotometry (DS) and partial least squares (PLS) approaches without using any chemical pre-treatment. CWT and DS calibration equations for AA and ASA were obtained by measuring the CWT and DS amplitudes corresponding to zero-crossing points of spectra obtained by plotting continuous wavelet coefficients and first-derivative absorbance values versus the wavelengths, respectively. The PLS calibration was constructed by using the concentration set and its full absorbance data consisting of 850 points from 220 to 305 nm in the range of 210-310 nm. These three methods were tested by analyzing the synthetic mixtures of the above drugs and they were applied to the real samples containing two commercial pharmaceutical preparations of subjected drugs. A comparative study was carried out by using the experimental results obtained from three analytical methodologies and precise and accurate results were obtained.

Ascorbic Acid↗
PubMed2003

Thermodynamics of solutions I: benzoic acid and acetylsalicylic acid as models for drug substances and the prediction of solubility.

PURPOSE: To investigate the solution process of drug substances (exemplified by benzoic acid. BA. and acetylsalicylic acid, ASA), particularly the interrelation between enthalpic and entropic terms of Gibbs energy, in different solvents. To develop an approach for the estimation of standard solution enthalpies based on a self-consistent thermochemical scale. METHOD: Two independent methods, solubility experiments (concentrations of saturated solutions) and solution calorimetry (standard solution enthalpies) in aliphatic alcohols and individual organic solvents were used. Correlation between the thermodynamic functions in various solvents were analyzed by standard statistical methods. Multiple regression analysis between delta Ho(sol) values and the parameters of the solvents was run on the Koppel-Palm equation. RESULTS: Based on experimental data, a compensation effect between thermodynamic functions was observed. Correlation was found between delta Ho (sol) (BA) and delta Ho(sol) (ASA) [where the delta Ho(sol) (BA)-values were used as a self-consistent thermochemical scale]. Furthermore, delta Ho(sol) correlated with the Koppel-Palm basicity of the solvents. CONCLUSION: The model based on solubility and solution experiments might be useful for the prediction of solubility or solvation of drug substances in different media. The regression equation based on the self-consistent thermochemical scale makes it possible to approximate the ability to solvate a drug substance in comparison with structure-relative substances.

Alcohols↗
PubMed2004

Multivariate spectral calibration technique based on regression analysis for the quantitative multiresolution of a ternary mixture containing paracetamol, ascorbic acid and acetylsalicylic acid in effervescent tablets.

Multivariate spectral calibration techniques based on regression analysis were established for the quantitative multiresolution of a ternary mixture containing parecetamol (PAR) ascorbic acid (AA) and acetylsalicylic acid (ASP) having closely overlapping spectra. The mathematical algorithms of multivariate spectral calibrations as namely tri-linear regression calibration (TLRC) and multi-linear regression calibration (MLRC) are based on the use of the linear regression equations at a three-wavelength set and a ten-wavelength set in the range of 215-305 nm. These calibration techniques do not require any chemical pre-treatment and a graphical procedure of the overlapping spectra. The mathematical content of TLRC and MLRC approaches were briefly formulated for the quantitative analysis of three- or multi-component mixtures. The applicability of the formulated calibration models were tested by analysing the various synthetic ternary mixtures consisting of these active compounds and then these models were applied to real pharmaceutical formulations. It was observed that TLRC and MLRC models give a successful quantitative multiresolution. The experimental results of these techniques were compared with each other as well as with those obtained by literature methods.

Acetaminophen↗
PubMed2005

Enhanced antiplatelet effects of clopidogrel plus acetylsalicylic acid compared with acetylsalicylic acid alone or combined with extended-release dipyridamole in healthy volunteers.

BACKGROUND: Previous studies have shown the potential benefit of using antiplatelet agents with complementary modes of action. METHODS: Using a crossover design, the ex vivo antiplatelet effects of 10 days' treatment with clopidogrel 75 mg + acetylsalicylic acid (ASA) 75 mg daily, ASA 75 mg/day, or extended-release dipyridamole 200 mg/low-dose ASA 25 mg twice daily were compared, using various platelet agonists. RESULTS: Clopidogrel + ASA was significantly more effective than dipyridamole + ASA in inhibiting collagen-induced platelet aggregation in whole blood (mean 44.9 +/- 5.6% inhibition vs. 16.5 +/- 6.7%; p = 0.0009). Clopidogrel + ASA was significantly more effective than ASA or dipyridamole + ASA in inhibiting ADP-induced platelet aggregation in whole blood (p < or = 0.0001) and platelet-rich plasma (PRP) (p < or = 0.0001), and in inhibiting collagen-induced aggregation in PRP (p < or = 0.0001). ASA alone and clopidogrel + ASA were significantly more effective than dipyridamole + ASA in inhibiting arachidonic acid-induced platelet aggregation in whole blood (p < or = 0.0001). CONCLUSIONS: Based on ex vivo platelet aggregometry, clopidogrel + ASA is a more potent antiplatelet regimen than either ASA alone or the marketed combination of dipyridamole + ASA. However, the clinical significance of this finding remains to be confirmed.

Adult↗
PubMed2002

The acute and short-time effect of supplementation with the combination of n-3 fatty acids and acetylsalicylic acid on platelet function and plasma lipids.

Antiplatelet therapy with acetylsalicylic acid (ASA) is commonly used to reduce the risk of cardio- and cerebrovascular events. Fish consumption has been inversely related to coronary disease, which has been partly attributed to an inhibitory effect of n-3 polyunsaturated fatty acids (n-3 PUFA) on platelet production of tromboxane A2. In this study, we investigated the acute and short-time effect of supplementation with n-3 PUFA and intravenous ASA on platelet function, platelet fatty acid composition and plasma lipids. Eighteen healthy men were randomly allocated to a daily intake of 10 g n-3 PUFA or placebo. After this supplement (14 h and 14 days), blood was sampled before and after intravenous injection of 100 mg ASA. n-3 PUFA given for 14 days caused a minor inhibition of platelet reactivity but negligible compared to 100 mg ASA. No additive effect of n-3 PUFA and ASA could be demonstrated.

Administration, Oral↗
PubMed1988

Ascorbic acid and acetylsalicylic acid (aspirin) in the diet of broilers maintained under heat stress conditions.

Male broiler chicks were grown to 21 days of age under normal conditions, then placed in environmental chambers maintained under constant (24 C) or cyclic (24 to 35 C) heat conditions. Chicks were acclimated for 1 wk on a standard grower basal diet. Standard grower basal diets were fortified with 0, 125, 250, 500, or 1,000 ppm coated ascorbic acid (AA) or 0, 125, 250, or 500 ppm acetylsalicylic acid (ASA). Test diets were fed for 14 days in two separate studies. Cyclic heat conditions reduced feed intake and significantly reduced weight gains in both trials. Feed efficiency was not significantly affected by heat stress. Neither AA or ASA had beneficial effects on broiler growth or feed efficiency.

Animals↗
PubMed1992

Effects of tiaprofenic acid and acetylsalicylic acid on human articular chondrocytes in 3-dimensional culture.

Two nonsteroidal antiinflammatory drugs (NSAID: acetylsalicylic acid, ASA, and tiaprofenic acid, TA) were tested on differentiated human chondrocytes cultivated in clusters. DNA synthesis was depressed by ASA at therapeutic concentrations. The amount of proteoglycans in culture medium was decreased by ASA, whereas type II collagen was not modified. By contrast, TA did not affect chondroformative processes in chondrocytes. Both NSAID were potent inhibitors of prostaglandin E2 (PGE2) synthesis, TA being more efficient than ASA. From these experiments, we conclude that TA and ASA inhibit PGE2 synthesis; TA did not depress chondroformative variables in human cartilage in vitro, while ASA induced a decrease of DNA and proteoglycan syntheses.

Anti-Inflammatory Agents, Non-Steroidal↗