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PubMed1993

[Low dose acetylsalicylic acid in secondary prevention of stroke].

Acetylsalicylic acid (ASA) as secondary prophylaxis after ischaemic cerebrovascular events is well established and its efficacy unquestioned since over 15 years. According to the results of two European studies a dose of 100 mg per day is sufficient to reduce the incidence of further stroke, myocardial infarction, and death due to cardiovascular causes. This satisfactory response to low-dose ASA applies to patients with transient ischaemic attacks, reversible ischaemic events, and minor strokes. In cases with severe cardiac disease, however, a high dosage of ASA or anticoagulation therapy may be necessary to prevent further vascular events.

Aspirin↗
PubMedDate not supplied

Interaction of dexamethasone with acetylsalicylic acid in mice.

The effect of acetylsalicylic acid (ASA, 160 mg/kg b.wt.) and dexamethasone (DEX, 15 mg/kg b.wt.) on ASA antinociception and toxicity when administered orally alone or in combination for 4 consecutive days was studied in male albino mice. ASA antinociception decreased after repeated ASA administration. Bleeding time was prolonged and the intestinal ASA esterase activity was increased, which was probably related to the increased ASA general toxicity in ASA-treated animals. There were no changes in the blood alkaline content, in the ulcerogenic or hepatotoxic effect of ASA, nor in the hepatic monooxygenase activity (ethylmorphine N-demethylase and aniline hydroxylase and the cytochrome P450 and b-5 content). DEX administered alone exerted a significant antinociceptive effect, increased both acute ASA toxicity and aniline hydroxylase activity and decreased body growth. However, DEX did not change the bleeding time, the alkaline blood content nor the intestinal esterase activity. The combination of ASA and DEX did not increase the ASA antinociceptive effect nor the general and specific toxicity of ASA. DEX in combination even abolished the effect of ASA on intestinal ASA esterase and on bleeding time. DEX also increased the hepatic cytochrome P450 content and did not change the ulcerogenic effect of ASA nor the alkaline blood content.

Administration, Oral↗
PubMed1990

Effects of pentazocine and acetylsalicylic acid on pain-rating, pain-related evoked potentials and vigilance in relationship to pharmacokinetic parameters.

Achieving objective and quantitative measurement of experimental pain in human volunteers and establishing the impact of drugs remains a difficult task. This problem may be overcome by employing a method which allows the simultaneous measurement of pain ratings elicited by standardized stimulation of the nasal mucosa by carbon dioxide, together with pain-related chemo-somatosensory evoked potentials (CSSEP) and vigilance. We assessed the effect of pentazocine and acetylsalicylic acid on these parameters in 14 human volunteers and related the effects to the pharmacokinetic parameters of the drugs measured at the same time. Pentazocine was found to reduce the pain ratings as well as the amplitudes of the pain-related evoked potentials and to increase their latencies. Vigilance (measured by EEG power spectra and performance of a tracking task) was also significantly reduced. These effects were observed during the distribution phase and the first period of the terminal elimination phase of the drug. Acetylsalicylic acid had no significant effects on pain ratings, but reduced the amplitudes of the event-related potentials when compared to placebo controls. At the same time a slight, but significant, effect on vigilance (reduced performance of the tracking task) was observed. These effects could not be related to the presence of unmetabolized acetylsalicylic acid in the plasma. They appeared at later times when only salicylic acid was left. It is concluded that chemical stimuli of sufficient intensity produce pain which may be suppressed by opioid analgesics such as pentazocine. The effect of acetylsalicylic acid on this experimental pain did not reach significance for all measured parameters under the experimental conditions chosen. The changes in vigilance and in the amplitudes of pain-related chemo-somatosensory evoked potentials indicated as yet unknown CNS-effects of this non-steroidal anti-inflammatory drug.

Adult↗
PubMed1979

[The effect of acetylsalicylic acid on some parameters of peripheral circulation in children (author's transl)].

Acetylsalicylic acid in a single dose of 10 mg/kg orally affected the skin temperature of the hand of febrile and afebrile children. In the afebrile group the rise of skin temperature after 1 hour (p less than 0,05) and 2 hours (p less than 0.01) was not accompanied by significant change of the sublingual or axillar temperature. In the febrile group the rise of the skin temperature of the 3rd finger after 1 hour (p less than 0,001) and 2 hours (p less than 0.001) was accompanied by a significant decrease of the sublingual and axillar temperature and by a decrease of pulse rate. The changes were more pronounced after 1 hour after administration of the drug. Similarly, the acetylsalicylic acid enhanced the relative blood flow through the skin of the finger of hand.

Adolescent↗
PubMed1978

A quantitative study of the effects of acetylsalicylic acid on spermatogenesis and organs of the rat.

Although the occurrence of prostaglandins in the male reproductive organs is consistent, their physiological role in fertility and reproduction is not known. The influence of acetylsalicylic acid, an inhibitor of prostaglandin synthesis, on the male reproductive tract was investigated in Sprague-Dawley rats of proven fertility. Acetylsalicylic acid dissolved in phosphate buffer was administered once a day at two dosages (300 mg/kg body weight and 150 mg/kg body weight) over a period of 12 days and a period of 6 days. The animals were killed 24 hours after the final treatment and the testes, epididymides, ductus deferens, seminal vesicles, kidneys, and adrenal glands were removed and placed in Bouin's solution. Subsequently, the tissues were cleaned and weighed and the testes were prepared for quantitative study under the light microscope. Organ weights were not significantly altered in the animals that were treated with acetylsalicylic acid. Cell counts indicated that there was a significant increase in the mean number of preleptotene spermatocytes and spermatids in those animals treated with the drug for 6 days at a dose of 150 mg/kg body weight. Treatment at the same dosage for a period of 12 days produced a significant decrease in the mean numbers of preleptotene and pachytene spermatocytes and spermatids. The mean diameter of the seminiferous tubules was also significantly decreased in the latter group of animals. In the group of animals treated with ASA for 12 days at a dose of 300 mg/kg body weight the mean diameter of the seminiferous tubules was significantly increased. No clear conclusion as to the effect of the drug on spermatogenesis or the various organs could be drawn.

Animals↗
PubMed1991

[Effect of pentoxyl, ibuprofen and acetylsalicylic acid on the thymus, spleen and adrenals in an experiment].

The effect of acetylsalicylic acid, ibuprofen and pentoxyl on the histological and morphometric pattern of the thymus and the weight of the thymus and spleen was studied in rats. There was decreased function of the thymus and its atrophy with acetylsalicylic acid and ibuprofen. Pentoxyl increased the secretory activity of the thymus. The effect of the drugs on the thymus and spleen was unidirectional.

Adrenal Glands↗
PubMed1997

[Coumarin combined with low-dose acetylsalicylic acid in the prevention of thromboembolic complications in patients with mitral and aortic valve prostheses].

Authors studied the effect of coumarin, and its combination with low-dose (125 mg/day) acetylsalicylic acid in the prevention of thromboembolic complication during a 10-year period (average 4.7 years) in a randomized trial of 296 patients aged 18-60 year with tilting disc type prosthetic heart valve (159 mitral and 137 aortic) in sinus rhythm. In the group treated with coumarin (152 patients, 743.4 patient-years) 4 cases (2 of them fatal) of valve thrombosis, 12 cases of peripheral embolism and 9 cases (3 intracranial, 3 among them fatal) of major bleeding were observed; in the group treated with coumarin plus acetylsalicylic acid (144 patients, 638.7 patient-years) 2 cases (1 of them fatal) of valve thrombosis, 4 cases of peripheral embolism and 14 cases (3 of them fatal) of major bleeding were observed. In the case of valve thromboses the difference between the two groups was non-significant but still clinically remarkable; peripheral embolism occurred in significantly higher number (p < 0.05). There was no statistically significant difference of bleeding complications between the two groups. The results suggest that the combination of coumarin plus low-dose acetylsalicylic acid is more effective in the prevention of thromboembolic complications in patients with mitral and aortic prosthetic heart valve than coumarin alone; the danger of bleeding complications seems to be acceptable with adequate control.

Adolescent↗
PubMed1981

Spectrofluorometric determination of acetylsalicylic acid, salicylamide, and salicyclic acid as an impurity in pharmaceutical preparations.

Spectrofluorometry, either direct or in combination with a separation technique, provides a sensitive and accurate method for the determination of certain extent fluorescent analgesic drugs and the determination of impurities in many combination preparations. A critical examination of the UV spectra of common analgesics and related compounds indicates that the fluorescence inner filter effect should be negligible below 10(-5) M and that selective excitation and emission wavelengths should minimize interference from other fluorescent species. Fluorometric procedures are presented for the determination of salicylamide, acetylsalicylic acid, and salicylic acid, as an impurity, in preparations containing salicylamide, acetylsalicylic acid, acetaminophen, caffeine, and phenacetin as major constituents. Inner filtering is the limiting factor only for the direct and indirect determination of salicylamide and the direct determination of acetylsalicylic acid. Results of fluorometric determinations compare favorably with other reference methods. Salicylic acid is determined in the 10(-7) M concentration range after separation from salicylamide, acetaminophen, and caffeine.

Acetaminophen↗
PubMed2004

Kinetic method for acetylsalicylic acid determination based on its inhibitory effect upon the catalytic decomposition of H(2)O(2).

The catalytic reaction of catalase was investigated, by means of a Clark oxygen sensor, in the presence of various concentrations of acetylsalicylic acid. Michaelis-Menten kinetic parameters were determined from Lineweaver-Burk plots, obtained in the absence and in the presence of the inhibitor. The inhibition pattern, suggested by the Lineweave-Burk plots, corresponds to a fully mixed inhibition mechanism. A kinetic method, based on the indicator reaction: [Formula: see text], was developed for the quantitative determination of acetylsalicylic acid. Calibration graphs of the reciprocal value of first-order rate constant versus acetylsalicylic concentration covered the concentration range (2.99-19.98)x10(-4) mol/L, while the detection limit was 4.12x10(-4) mol/L acetylsalicylic acid with a standard deviation of 2.1x10(-5) mol/L.

Aspirin↗
PubMed2006

Relaxation in the glass former acetylsalicylic acid studied by deuteron magnetic resonance and dielectric spectroscopy.

Supercooled liquid and glassy acetylsalicylic acid was studied using dielectric spectroscopy and deuteron relaxometry in a wide temperature range. The supercooled liquid is characterized by major deviations from thermally activated behavior. In the glass the secondary relaxation exhibits the typical features of a Johari-Goldstein process. Via measurements of spin-lattice relaxation times the selectively deuterated methyl group was used as a sensitive probe of its local environments. There is a large difference in the mean activation energy in the glass with respect to that in crystalline acetylsalicylic acid. This can be understood by taking into account the broad energy barrier distribution in the glass.

Journal Article↗
PubMed1985

Availability studies on acetylsalicylic acid, salicylamide and phenacetin at different pH values.

The optimum partitioning rate of acetylsalicylic acid has been attained at pH = 4 and minimum partitioning rate was found to be at pH = 8. The maximum partitioning rate of salicylamide was observed at pH = 5 and the smallest one was found at pH = 6 or 8. At pH = 3 a maximum amount of phenacetin was found in the aqueous phase, while at pH = 6 a maximum amount was found in the octanolic layer. The maximum partitioning rate was found at pH = 6 and lowest one was observed at pH = 3. The gastrointestinal absorption of acetylsalicylic acid, salicylamide and phenacetin was significantly increased, as reflected by the urinary excretion data in presence of solid buffer components at pH values of 4,5 and 6 respectively.

Adult↗
PubMed2006

Effects of melatonin or acetylsalicylic acid on gastric oxidative stress after bile duct ligation in rats.

BACKGROUND: Antioxidant enzyme activities decrease after bile duct ligation. The aim of this study was to assess the effect of melatonin and acetylsalicylic acid on antioxidant enzyme activities in gastric oxidative stress induced by bile duct ligation. METHODS: Sixty-four animals were divided into eight groups of eight rats each. Male Sprague-Dawley rats were subjected to either a sham operation or common bile duct ligation (BDL) before treatment with melatonin (MEL) or acetylsalicylic acid (ASA). Gastric superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx) activities, and malondialdehyde (MDA) and nitric oxide (NO) levels were determined by spectrophotometers and evaluated. RESULTS: Our results indicated that BDL caused a significant increase in lipid peroxidation, whereas coadministration of MEL with ASA significantly decreased MDA and NO levels in BDL rats. Moreover, coadministration of MEL and ASA increased antioxidant enzyme activities after the BDL, and these increases were statistically significant for CAT and GPx. On the other hand, the increase in SOD activity was not significant. CONCLUSIONS: Melatonin administration, either alone or together with acetylsalicylic acid, decreases lipid peroxidation and increases antioxidant enzyme activities in gastric tissues of rats after bile duct ligation. ASA administration, however, either alone or with a vehicle, increases lipid peroxidation and decreases antioxidant enzyme activities.

Animals↗
PubMed1999

[The effect of monotherapy with ciprofibrate and in combination with acetylsalicylic acid on the spectrum of lipids, thromboxane and fibrinogen in patients with atherosclerosis and hyperlipoproteinemia].

Ciprofibrate is one of the basic drugs used to lower risk values of lipid parameters and fibrinogen in atherosclerosis patients. Since antiaggregation treatment with acetylsalicylic acid is a complex part of obligatory therapy of these patients, the authors studied the influence of ciprofibrate on chosen lipid parameters, fibrinogen and thromboxane in monotherapy, and also in combination with acetylsalicylic acid (ASA) in patients with advanced atherosclerosis and hyperlipoproteinemia. In the first group of patients (A-C, n = 12) after one month of low-lipid diet acetylsalicylic acid in a dose of 100 mg was administered daily during a period of 2 months followed by addition of 100 mg of ciprofabrate daily during the next 2 months. In the second group of patients (C-A, n = 11) after one month of low-lipid diet the same drugs were administered but in opposite order. Ciprofibrate was most effective in lowering the levels of triacylglycerids (-41%) and VLDL-cholesterol (-34%), but effectively lowered also the values of total cholesterol and LDL-cholesterol. In both studied groups it led to mild increase of HDL-cholesterol levels. Simultaneous administration of ASA did not significantly influence its hypolipemic activity. Ciprofibrate also significantly lowered the level of fibrinogen (-17%). Increase of the total number of platelets by about 10% was not accompanied by changes of the values and production of thromboxane. Simultaneous administration of ASA caused more than 90% inhibition of thromboxane production in monotherapy and in combination with ciprofibrate. Ciprofibrate is an effective hypolipidemic agent, also lowering the level of fibrinogen. Its combination with ASA is adequate, safe and without negative interaction influencing treatment. (Tab. 6, Fig. 1, Ref. 16.)

Aged↗
PubMed1979

[Experimental model for the study of the teratogenic interaction of chemical agents and drugs (toluene and acetylsalicylic acid)].

On the 10th-13th days of pregnancy toluene (3600 mg/m3) by inhalation) and on 12th day acetylsalicylic acid (500 mg/kg of body weight per os) were administered to CFY rats and the common effect of these agents was studied. It was established that: 1. the maternal toxicity increased, i.e. increased the mortality rate, decreased the consumption of the food and the gain of weight, increased the relative weight of the liver; 2. the foetal toxicity increased, i.e. increased the mortality rate of foetuses, the rate of the loss of the body weight, the number of the anomalies of the sternum and the incidence of the supernumerary ribs. It is believed, that the non-teratogenic toluene rises the utilization of the glycine and the level of the free salicylic-acid, consequently the embryotoxic effect of the acetylsalicylic-acid. The danger of the occurrence of malformations as an effect of interaction of chemical agents and drugs taken in therapeutic doses is stressed.

Animals↗
PubMed2003

[Effect of acetylsalicylic acid on the reproductive performance and on offspring from wistar rats].

UNLABELLED: The aim of this paper was to perform a randomized, controlled and blinded study to investigate if a therapeutic dose of acetylsalicylic acid (ASA), taken by pregnant women, may also cause embryotoxic or congenital abnormalities on experimental animal. METHODS: Females were confirmed to have mated by observations of sperm in a vaginal smear. The day on which spermatozoa were found in the vaginal smear was considered as day 1 of gestation (GD1). After randomization, mated females were assigned to experimental groups and individually caged, were given 50 mg/kg/day of acetylsalicylic acid, by needle gavage once daily, during two different periods of pregnancy. One group of dams (n=11) received aspirin from day 1 to 4 of pregnancy (before embryonic implantation) for evaluation of the blastocysts, and another group received aspirin from day 6 to 15 of pregnancy (organogenic period) for fetal evaluation. Control groups (n=12) received distilled water in same volume and during same periods as their respective experimental groups. RESULTS AND CONCLUSION: The treatment of the dams with ASA, according to minimal therapeutic dose used for humans, did not cause embryotoxic or major malformations on experimental animal but was responsible for rate increased of fetuses presenting ureteric dilatation. After analysis of the data, it appears that, although direct conclusive evidence of adverse effects in humans is lacking, a potential hazard dose exists and thus the indiscriminate use of acetylsalicylic acid (aspirin) is contraindicated.

Animals↗
PubMed2002

The effects of acetylsalicylic acid on proliferation, apoptosis, and invasion of cyclooxygenase-2 negative colon cancer cells.

BACKGROUND: Acetylsalicylic acid (ASA, aspirin), the most common nonsteroidal anti-inflammatory drug (NSAID), has been shown to have a protective effect against the incidence and mortality of colorectal cancer. However, the mechanism of its anticancer function remains unclear. The aim of this study was to determine the effects of acetylsalicylic acid on proliferation, apoptosis, and invasion in human cyclooxygenase-2 (COX-2) negative colorectal cancer cell lines. MATERIALS AND METHODS: After treatment with various concentrations of ASA, cell proliferation was measured in the human colon cancer cell line SW480. Apoptotic cells were identified by transmission electron microscopy, acridine orange staining, and flow cytometry. The invasive potential of SW480 cells was detected using an in vitro invasion assay. The production of carcinoembryonic antigen was measured by microparticle enzyme immunoassay. Expression of Bcl2, Bax, CD44v6, and nm23 were evaluated by immunocytochemistry. RESULTS: ASA significantly inhibited the proliferation of SW480 cells and stimulated apoptosis. Production of carcinoembryonic antigen and the invasive potential of SW480 cells were also inhibited by ASA. After treatment with ASA, down-regulation of Bcl2 and CD44v6 expression and up-regulation of nm23 expression were observed in SW480 cells. No obvious effect of ASA was found on Bax expression. CONCLUSION: Our findings reveal that ASA inhibits the proliferation and promotes apoptosis in the human colon cancer cell line SW480. Down-regulation of Bcl2 expression might represent a potential mechanism by which ASA induces apoptosis in this COX-2 negative colon cancer cell line. Our results also suggest that ASA decreases the invasive potential of these colon cancer cells. Decreased CEA content and CD44v6 expression and elevated nm23 expression may contribute to the effect of ASA on invasive potential of SW480 colon cancer cells.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1999

Cytoskeletal organization and incorporation of beta 3 integrin in thrombin-stimulated platelets: effect of acetylsalicylic acid.

Platelet stimulation by agonists is followed by changes in cytoskeletal organization that includes actin polymerization and association of the membrane skeleton (which is connected with the integrin alpha IIb beta 3) with the underlying cytoplasmic actin filaments. The effect of orally administered acetylsalicylic acid to healthy volunteers on incorporation of contractile protein and beta 3 integrin into the cytoskeletal core of thrombin-stimulated platelets was studied. Stimulation was followed by increased contractile protein and beta 3 incorporation into the cytoskeleton. Acetylsalicylic acid intake resulted in decreased incorporation of myosin and actin (32% and 20%, respectively), and a decrease (36%) in the association of beta 3 integrin with the cytoskeletal elements was evident. In conclusion, we have shown that acetylsalicylic acid, besides the known inhibitory effect on thromboxane synthesis, promotes changes in the cytoskeletal organization of thrombin-stimulated platelets that could limit thrombus formation.

Actinin↗
PubMed1991

Radiation-protective and platelet aggregation inhibitory effects of five traditional Chinese drugs and acetylsalicylic acid following high-dose gamma-irradiation.

High doses of 60Co radiation (4.0-8.0 Gy) in mice, rats and rabbits caused increases in rate of platelet aggregation during the first 5 days after irradiation. The inhibitory effects of the extracts of five Chinese drug plants and acetylsalicylic acid on rate of platelet aggregation were observed in both in vitro and in vivo tests, averaging 23-53% in vitro and 46-69% in vivo. Antiradiation tests on mice vs. 7.5-8.0 Gy of gamma-radiation, using the plant extracts and acetylsalicylic acid as protective agents, increased survival rates by 8-50% for the plant extracts and 35% for acetylsalicylic acid.

Animals↗