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PubMed2004

Acetylsalicylic acid inhibits monocyte adhesion to endothelial cells by an antioxidative mechanism.

The adhesion of monocytes to vascular endothelium increases in the presence of high levels of low density lipoprotein (LDL). LDL changes oxidative status of endothelial cells leading to an increased expression of cell adhesion molecules. Acetylsalicylic acid (ASA) has been shown to exert antioxidant effects in high and very high concentrations. This study was designed to demonstrate the influence of acetylsalicylic acid and its major metabolite, salicylic acid (SA), on the adhesion of monocytes to LDL-stimulated endothelial cells. Monocyte adhesion to endothelial cells was concentration-dependently inhibited by both salicylates upon stimulation of endothelial cells with TNF-alpha, oxidized LDL (oxLDL), and native LDL (nLDL). The inhibitory effect of ASA was more potent than that of SA, whereas the cyclooxygenase inhibitor ibuprofen had no effect. F2-isoprostane release from LDL-stimulated endothelial cells was reduced by simultaneous incubation with ASA or SA, whereas ibuprofen had no effect. LDL-induced activation of the transcription factor NF-kappaB was inhibited by ASA, and ferritin protein was increased when endothelial cells were incubated with this drug. These results show that acetylsalicylic acid and-less potently-salicylic acid inhibit monocyte adhesion to LDL-stimulated endothelial cells by antioxidative effects. For ASA, the observed inhibition of monocyte adhesion was accomplished with concentrations that can be reached after single oral doses of 500 mg of ASA.

Antioxidants↗

PubMed1998

In vitro activity of acetylsalicylic acid on replication of varicella-zoster virus.

Topical application of a mixture of acetylsalicylic acid (ASA) and diethyl ether is effective in the treatment of acute herpes zoster and postherpetic neuralgia. To study whether the other-than-analgesic effects of that treatment could be due to an antiviral activity of ASA the effects of the drug on the replication of varicella zoster virus (VZV) were assessed by the fluorescent focus assay on MRC5 and Vero cells. ASA caused a marked reduction in the spread of infection in MRC5 monolayers while in growing Vero cells the effective dose proved toxic. ASA concentrations (5-10 mM) which were effective in vitro against VZV are higher than the plasma concentrations attained in the standard treatment of chronic inflammatory states, but are consistent with the skin concentration attained by topical application of ASA/diethyl ether mixture. These data support similar findings relating the antiviral activity of acetylsalicylic acid to influenza virus, CMV, and HIV.

Animals↗

PubMedDate not supplied

[Effect of ammonium succinate on pharmacological effects of acetylsalicylic acid].

Ammonia succinate potentiates the main pharmacological properties and reduces the toxic effects (ulcerogenic action and general toxicity) of acetylsalicylic acid. The new preparation astam, representing a combination of acetylsalicylic acid with ammonia succinate in a 2:1 ratio, is proposed. Astam exhibits antiexudative, capillary-reinforcing, antiproliferative, pain-relieving, antipyretic, antiaggregant, and antioxidant properties. In addition, the drug inhibits the development of structural-metabolic disorders in the case of chronic immune inflammation of joints and various internal organs.

Animals↗

PubMed1994

Investigation of the influence of acetylsalicylic acid on the steady state of long-term therapy with theophylline in elderly male patients with normal renal function.

The risk inherent in the clinical control of patients with theophylline is widely recognized. Elderly patients may present an additional risk because of altered pharmacokinetics and the use of concomitant medication. Acetylsalicylic acid has been proposed for primary and secondary prevention of myocardial infarction and possible strokes. This investigation was undertaken to determine if concomitant administration of acetylsalicylic acid in elderly patients would alter steady-state levels of theophylline. A population of smoking male patients older than 60 years of age under long-term control of chronic obstructive pulmonary disease (COPD) with theophylline were evaluated for a baseline period of 3 days. Serum levels were measured at 6:00 AM and 6:00 PM. An enteric-coated acetylsalicylic acid preparation, 650 mg by mouth, was added to the daily slow-release theophylline, 6:00 AM hour dose regimen for 4 weeks. The serum levels of theophylline and salicylates were measured at 6:00 PM after dosing and at 6:00 AM the following day, at weekly intervals for 4 weeks. Urine specimens collected before administration of medication at 6:00 AM were analyzed for salicylates to further confirm dosage compliance. All volunteers continued to be clinically controlled throughout the treatment period and no symptoms of either overdose or underdose of either medication occurred. Plateau or trough theophylline serum levels did not change significantly during the salicylate treatment period. Salicylate serum levels did show during treatment self-induced metabolism. It is concluded that in elderly male patients, a daily concomitant therapeutic salicylate regimen does not alter steady-state serum theophylline levels and therefore does not per se necessitate the assay of theophylline blood levels in elderly patients.

Aged↗

PubMed2004

[Determination of three components in compound acetylsalicylic acid tablet by dual-wavelength ratio spectrometry].

The contents of three components in compound acetylsalicylic acid tablets were determined by dual-wavelength ratio spectrometry. According to the feature of the spectra, 213, 227, 245 and 265 nm were chosen as the determining wavelengths. It is shown that for the three components good linear correlations exist for acetylsalicylic acid (5-20 microg x mL(-1)), phenacetin (2-10 microg x mL(-1)), and caffeine (2-20 microg x mL(-1)). The average recoveries were 100.03%, 100.23% and 99.96% respectively. The results were consistent with those obtained by the standard method of Health Ministry(P > 0.05). The method is simple and practical with fewer determination wavelengths and powerful spectral resolution, and can be performed on a lower level instrument, as well as be easily spreaded for application.

Aspirin↗

PubMed1999

The effects of acetylsalicylic acid, interferon-alpha, and vitamin E on prevention of parenteral nutrition-associated cholestasis: an experimental study.

BACKGROUND: Cholestasis is one of the major complications of parenteral nutrition. The purpose of this experimental study was to detect the effects of acetylsalicylic acid (ASA), vitamin E (Vit E), and interferon-alpha (IFN-alpha) on prevention of parenteral nutrition-associated cholestasis. METHODS: Ten experimental groups, each consisting of 10 4-week-old Wistar albino rats, were formed: control 10- and 20-day groups (C10 and C20), parenteral nutrition-only 10- and 20-day groups (T10 and T20), ASA-supplemented parenteral nutrition 10- and 20-day groups (TA10 and TA20), Vit E-supplemented parenteral nutrition 10- and 20-day groups (TE10 and TE20), and IFN-alpha-supplemented 10- and 20-day groups (TF10 and TF20). Acetylsalicylic acid, Vit E, and IFN-alpha were administered in the parenteral nutrition solution through an intraperitoneal route. At the end of the study, serum total bile acids, serum aspartate and alanine aminotransferases, and alkaline phosphatase were measured biochemically. In addition, the histopathologic findings of cholestasis were evaluated by using a morphologic portal inflammation index. RESULTS: Although the difference in the serum levels of transferases and alkaline phosphatase was not significant among all groups (p > 0.05), it was significant in total bile acid levels (p < 0.05). There was also a significant correlation between the histopathologic changes of the liver and serum total bile acid concentrations (p < 0.05). Portal inflammation in varying degrees was seen in all experimental groups, but not in the control groups. Serum total bile acid concentrations in parenteral nutrition groups receiving ASA were significantly lower than those in the parenteral nutrition-only group (p < 0.01). Although Vit E-supplemented parenteral nutrition was effective in preventing the development of cholestasis in the 10-day group (p < 0.05), it was not effective in the 20-day group when compared with incidence of cholestasis in the parenteral nutrition-only group (p > 0.05). Conversely, IFN-alpha-supplemented parenteral nutrition had no effect on cholestasis in the 10-day group (p > 0.05) but lowered cholestasis in the 20-day group when compared with incidence the parenteral nutrition-only group (p < 0.05). CONCLUSION: Our results indicate that acetylsalicylic acid may be beneficial in preventing, and (alpha-interferon in treating, parenteral nutrition-associated cholestasis.

Alanine Transaminase↗

PubMed1991

[Platelet aggregation with SIN 1: comparison with isosorbide-5-mononitrate and acetylsalicylic acid].

SIN 1, the bioactive metabolite of molsidomine, not only appears to lack the problem of inducing nitrate tolerance, but also exerts antiaggregatory and fibrinolytic properties. These effects, which either are not or only in part shared by the drug isosorbide-5-mononitrate, might be beneficial in the prevention of thromboembolic complications in cardiovascular disease. In contrast to the effects of acetylsalicylic acid, SIN 1 already inhibits aggregation during the first phase of aggregation, and it inhibits aggregations induced by agonists that are not or only marginally influenced by acetylsalicylic acid (such as the aggregation induced by platelet activating factor). Thus, the antiaggregatory effects of molsidomine cannot replace the effects of acetylsalicylic acid, while a combination of both drugs might be of benefit in the treatment of patients with cardiovascular disease.

Aspirin↗

PubMed2006

[Bilateral hemothorax secondary to combined antiplatelet therapy with clopidogrel and acetylsalicylic acid].

Clopidogrel is a platelet aggregation inhibitor that increases the risk of bleeding complications when combined with acetylsalicylic acid. We report a rare case of a 79-year-old male treated with clopidogrel and acetylsalicylic acid after coronary angioplasty and stenting to treat unstable angina. Two months after initiation of therapy, the patient presented with symptomatic bilateral pleural effusion. Examination of both effusions confirmed the diagnosis of spontaneous bilateral hemothorax due to combined anti-platelet therapy. Serious functional sequelae were still present 18 months after diagnosis despite bilateral pleural drainage and respiratory physiotherapy.

Aged↗

PubMed1995

Binding of estradiol to whole prostatic DU-145 cells in the presence and absence of tamoxifen and acetylsalicylic acid.

Conflicting results have been obtained with regard to the estradiol receptor (ER) capacity of human prostatic tissue. Human prostatic DU-145 cells have been found to be ER-negative with immunohistochemical assays. The object of this investigation was to determine if whole DU-145 cells, which had been grown in monolayer culture, have ER and, if so, to confirm the finding with antiestrogens. After cells had been lysed, a Bmax of 44.7 +/- 4.0 fmol/mg (Kd = 0.6 +/- 0.6 nM) was obtained. Subcellular localization studies showed that the estrogen receptor level in the cytoplasmic fraction was approximately 10 times higher than in the nuclear fraction. Competitive binding studies showed that tamoxifen, DES, and acetylsalicylic acid decreased estradiol binding. The dissociation constants and relative affinities for tamoxifen, DES, and acetylsalicylic acid were 0.2 nM (281.7%), 0.2 nM (224.0%), and 0.8 nM (78.43%), respectively. However, 5 alpha-dihydrotestosterone and metabolites of acetylsalicylic acid had no effect in competitive binding studies. These results may contribute to a better understanding of prostatic carcinogenesis, which may in turn lead to more effective treatment.

Aspirin↗

PubMedDate not supplied

[The effect of suloctidil and acetylsalicylic acid on eicosanoid synthesis in human platelets].

The study aimed at comparing an effect of suloctidil and acetylsalicylic acid on malonyldialdehyde levels resulting from the arachidonic acid metabolism in blood platelets. It was shown that inhibitory effect of suloctidil is more potent than that of acetylsalicylic acid. Therefore the first is more inhibitor of an enzymatic metabolism of arachidonate in blood platelets than the latter.

Adult↗

PubMed1994

Fibroblast growth-promoting activity in proliferative vitreoretinopathy: antagonism by acetylsalicylic acid.

Proliferative vitreoretinopathy is a severe reactive process which leads to the formation of cellular membranes on the surface of the retina and in the vitreous. We determined the fibroblast growth-promoting activity of intraocular fluid from patients suffering from proliferative vitreoretinopathy, retinal detachment or cataract and further evaluated the effect of acetylsalicylic acid on growth-stimulated fibroblasts. The results demonstrated a significant enhancement of growth-promoting activity of intraocular fluid in proliferative vitreoretinopathy as compared to that of control samples. We showed that the augmented growth-promoting activity of intraocular fluid in proliferative vitreoretinopathy was significantly antagonized by inhibition of cyclooxygenase with acetylsalicylic acid (ID50 approximately 5 microM). In contrast, no significant effect was seen in corresponding control experiments. The findings suggest that metabolites of the cyclooxygenase pathway are involved in the regulation of enhanced intraocular fluid-induced fibroblast proliferation in proliferative vitreoretinopathy and that acetylsalicylic acid might be useful as an antiproliferative agent in intraocular fibrogenesis.

Adult↗

PubMed1977

Absorption, and effect on gastric mucosa, of buffered and non-buffered tablets of acetylsalicylic acid.

The effect of buffered and non-buffered acetylsalicylic acid tablets on gastric mucosa and gastric distress was investigated in healthy volunteers and in patients with rheumatoid arthritis. The absorption of acetylsalicylic and salicylic acids was also measured. The absorption of salicylic acid was not affected in clinically significant amounts by buffering the tablets. Buffered tablets containing aluminum subacetate showed a slightly delayed absorption of salicylic acid. Damage to the gastric mucosa tended to be less after the preparation buffered by magnesium hydroxide. Subjective feelings to gastric distress were not affected by buffering.

Aspirin↗

PubMedDate not supplied

Inhibitory effect of acetylsalicylic acid on matrix metalloproteinase - 2 activity in human endothelial cells exposed to high glucose.

Matrix metalloproteinases play a major role in the process of angiogenesis, an important feature of diabetes complications, cancer or rheumatoid arthritis. High glucose concentrations were reported to augment metalloproteinase-2 secretion in some cell types. In the present study we investigated the influence of acetylsalicylic acid on metalloproteinase- 2 secretion and expression in endothelial cells cultured for one week in high glucose conditions (25 mM and 33 mM). Metalloproteinase-2 activity was evidenced by gel zymography, the protein was identified by Western blotting, and the gene expression was quantitated by RT-PCR. The results indicated a marked inhibitory effect of acetylsalicylic acid at gene expression level (approximately 43%) and also at secretion level in samples of conditioned media (approximately 30%) and cellular homogenates (approximately 70%). This may suggest that acetylsalicylic acid could have a beneficial effect in preventing the angiogenic process that appears in diabetes complications.

Anti-Inflammatory Agents, Non-Steroidal↗

PubMed1974

Comparison of ibuprofen and acetylsalicylic acid in the treatment of rheumatoid arthritis.

A double-blind crossover study of ibuprofen and acetylsalicylic acid was carried out in 27 patients with rheumatoid arthritis. Patients were evaluated by joint counts, grip-strength determination, erythrocyte sedimentation rate, and number of acetaminophen tablets required in addition to the test drug, as well as by various biochemical measurements. In the doses used ibuprofen and acetylsalicylic acid appeared comparable in anti-inflammatory effect, but statistically fewer side effects were observed during administration of ibuprofen.

Acetaminophen↗

PubMedDate not supplied

Reduced skin hyperemia during tap water iontophoresis after intake of acetylsalicylic acid.

Skin microcirculation and skin temperature of 10 healthy subjects (6 men and 4 women, 20-44 yr of age) without any vascular diseases were registered when a thermoindifferent tap water iontophoresis was applied. The aim of this controlled study was to evaluate the development of skin hyperemia after the intake of 500 mg of acetylsalicylic acid (ASA). The measurement was conducted by laser-Doppler flowmetry on the proximal forearm. The skin temperature was measured before and after the treatment by an infrared thermometer. In all persons there was an intense erythema on the side of the cathode and only a modest one on the side of the anode. Without ASA preliminary treatment, the cutaneous flow showed an increase of 106% at the anodal side and that of 834% at the cathodal side (P < 0.001). After ending tap water iontophoresis, the skin temperature increased more on the cathode side than on the anode side (P < 0.001). After the intake of 500 mg ASA, the increase of the flow was 78% at the anode and 88% at the cathode. The comparison of the skin microcirculation did not show any differences at the anodal side when acetylsalicylic acid was taken before, but a strong suppression of the galvanic erythema at the cathodal side was observed after the intake of ASA. There is a direct influence of acetylsalicylic acid on the induction of the neurogenic inflammation caused by a galvanic erythema. The intensity of the induced erythema correlates with the analgesic effects of constant current treatment. An attenuation of the electrotherapeutic analgesia is possible.

Adult↗

PubMed1990

[Acetylsalicylic acid in the prevention of arterial thrombosis. Dosage problems in general and in the authors' experiment].

Acetylsalicylic acid is now accepted as a clinically useful drug for secondary prophylaxis against several thromboembolic complications, but there is still much controversy about the dosage. We discuss this problem, in the light of data from newly published clinical trials and of results from a pharmacological study performed by ourselves. All in all it seems reasonable to recommend 100-150 mg acetylsalicylic acid per day for prophylaxis after acute myocardial infarction. As for cerebrovascular indications, no clinical data available so far justify a dose reduction below 300 mg.

Adult↗

PubMed1995

Pharmacokinetic interactions of alcohol and acetylsalicylic acid.

This study assessed the influence of acetylsalicylic acid (ASA, 1.0 g), ibuprofen (0.8 g) and paracetamol (1.0 g) on the single-dose kinetics of ethanol in 12 healthy volunteers ingesting the drug and a standardised 1840-kJ breakfast 1 h before intake of ethanol. It also assessed the influence of ethanol on the single-dose kinetics of 1.0 g ASA in ten fasting healthy volunteers. Plasma concentrations of ethanol were measured by gas chromatography, and those of the drugs by liquid chromatography. There was no effect of ASA, ibuprofen or paracetamol on the single-dose kinetics of ethanol, but concurrent intake of ethanol reduced the peak concentration of ASA by 25%.

Acetaminophen↗

PubMed1982

Cellular dehydration and hypovolemia: effect of acetylsalicylic acid on drinking.

Chronic oral administration of acetylsalicylic acid (ASA), an inhibitor of prostaglandin synthesis, reduces the latency with which rats begin drinking in response to hypovolemia but has no effect on the total amount of water consumed to this stimulus. When drinking is due to cellular dehydration, latency to drink is unaffected while total water intake is markedly augmented by ASA-pretreatment. Chronic, low-dose exposure to ASA or indomethacin has no effect on plasma levels of the dipsogen, angiotensin II. These data, taken in conjunction with previous work demonstrating a suppression of drinking following administration of exogenous prostaglandin E, support the contention that the E prostaglandins are involved in the physiological control of water intake, but suggest that the precise role of the prostaglandin in controlling consumption is dependent upon the stimulus eliciting the behavior.

Angiotensin II↗