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At least 235 records · Page 13Linked to original sources
PubMed1977

[The value of acetylsalicylic acid for the prevention of postoperative thromboembolic complications].

All studies on the value of acetylsalicylic acid for the prevention of postoperative thromboembolic complications have been evaluated. Controlled, prospective and randomized studies have been analyzed only where the incidence of postoperative deep vein thrombosis or pulmonary emboli was proven by objective diagnostic methods such as the fibrinogen test, phlebography or autopsy. In 6 studies there is no significant reduction in the incidence of deep vein thrombosis in general surgical and orthopedic patients after acetylsalicylic acid prevention. One study, though it has definite methodological defects, does suggest a significant reduction in the number of postoperative fatal pulmonary emboli in 120 patients with fractures of the upper end of the femur. On the basis of all these data, the prevention of postoperative thromboembolic complications by means of acetylsalicylic acid cannot be recommended.

Aspirin↗
PubMed2000

[Aspirin. Acetylsalicylic acid and aspirinlike drugs. A review.].

In this review acetylsalicylic acid and aspirin with little "a" are considered as synonyms. A short acount is given of the history preceeding the synthesis of acetylsalicylic acid from salicylic acid by Felix Hoffmann in 1897 and its marketing in 1899 as Aspirin(R) by the Bayer Company. Aspirin was originally considered a prodrug to salicylic acid since it was at that time thought to have the same pharmacodynamic effects as salicylic acid and is rapidly transformed to it in vivo. Later aspirin was also found to be effective in its own right. During the years aspirin has gradually become the standard drug among an increasing number of aspirinlike drugs having similar effects as aspirin and often collectively, and somewhat misleading, named "nonsteroidal antiinflammatory drugs" (NSAIDs). The seminal work of John Vane and his colleagues in the 1970s and later has irrefutably tied the effects and side effects of aspirin and aspirinlike drugs to blocking of cyclooxigenase activity and therefore to reduced production of prostaglandins and related biogenic lipids. The anticoagulant effect, where aspirin itself is the cardinal drug, is thus due to decreased synthesis of thromboxan, whereas the antipyretic effect is due to reduced synthesis of prostaglandins in the central nervous system. The analgesic effect is obviously both related to decreased synthesis of prostaglandins in the central nervous system and outside it. On the other hand the antiinflammatory effect is seemingly mostly due to blocking inflammatory phenomena, without involvement of cyclooxigenase, in the walls of vessels although blocking the synthesis of prostaglandins also has a role. All aspirinlike drugs have until quite recently been mixed blockers of cyclooxigenases (COX 1 and COX 2) with aspirin itself being the most outstanding COX 1 blocker. New aspirinlike drugs with selective COX 2 blocking effect are apparently not any better on classical indications than the older drugs with mixed COX 1 and COX 2 blocking effect and their use might moreover be limited by some severe side effects. These drugs might, however, become of value for use on new indications.

English Abstract↗
PubMed1978

The localization and some properties of the acetylsalicylic acid O-deacetylases of Ascaris lumbricoides var suum and Moniezia expansa.

1. Enzymes hydrolysing acetylsalicylic acid were found in the cytosol of the cestode, Moniezia expansa, and in the cytosol of the intestinal epithelial cells and cytosol of the reproductive tract of the nematode, Ascaris lumbricoides var suum. 2. Enzymes hydrolysing 2-naphthyl acetate and 4-methylumbelliferyl acetate were found throughout the proglottid of the cestode and in the reproductive tract, intestine, mesenchyme fluid and cuticle of the nematode. These enzymes had mol. wt. of 30 000-300 000 whereas those hydrolysing acetylsalicylic acid in both species had mol. wt. of about 87 000. 3. The acetylsalicylic acid hydrolases from both helminths showed pH optima of about 7.0, and activity was enhanced by Ca2+ and low-mol. wt. thiols. Cu2+, Cd2+, Hg2+, Zn2+, La3+, F- and EDTA at 1 mM inhibited activity. N-Ethylmaleimide, p-chloromercuribenzoate, haloxon and paraoxon also inhibited hydrolase activity.

Acetyltransferases↗
PubMed1995

Low-dose ibuprofen in self-medication of mild to moderate headache: a comparison with acetylsalicylic acid and placebo.

A double-blind, threefold crossover, double-dummy trial was performed, investigating the efficacy of 200 mg ibuprofen compared with 500 mg acetylsalicylic acid and placebo in patients who usually treated their headaches with over-the-counter drugs. Ninety-five patients suffering from mild to moderate migraine or episodic tension-type headache were included. Seventy-seven patients entered the intention-to-treat analysis and 65 completed all three treatments. For the main response criterion, a minimum 50% decrease of headache intensity on a visual analogue scale at 1 h after treatment, ibuprofen was significantly superior to acetylsalicylic acid and placebo. This was true for migraine attacks and tension-type headache episodes. Towards the end of the observation period (150 min), the differences between ibuprofen and acetylsalicylic acid were no longer significant. In conclusion, ibuprofen was at least equivalent to acetylsalicylic acid and superior to placebo.

Adult↗
PubMed1992

Intrathecal injection of acetylsalicylic acid, salicylic acid and indomethacin depresses C fibre-evoked activity in the rat thalamus and spinal cord.

It was aimed to assess if intrathecal (i.t.) injections of acetylsalicylic acid and salicylic acid depress C fibre-evoked activity in the sensory part of the nociceptive system. In rats under urethane anaesthesia, activity was elicited in single neurones in the dorsomedial part of the ventral nucleus (VDM) of the thalamus and in ascending axons of the spinal cord by supramaximal electrical stimulation of the sural nerve. Acetylsalicylic acid and salicylic acid injected i.t. significantly reduced the activity evoked in thalamic neurones. The maximum depression amounted to about 50% of the activity evoked in the controls and was produced by acetylsalicylic acid at a dose of 50 micrograms (0.28 mumol)/rat and by salicylic acid at a dose of 37.5 micrograms (0.27 mumol)/rat. Indomethacin injected i.t. also reduced C fibre-evoked activity in the thalamus in a dose-dependent fashion, 100 micrograms producing a 50% depression. Salicylic acid (37.5 micrograms/rat, i.e.) depressed C fibre-evoked activity in ascending axons but had no effect on A beta fibre-evoked activity. It is concluded that i.t. injection of acetylsalicylic acid selectively inhibits nociceptive impulse transmission in the spinal cord by an action of the salicylic acid moiety. It is possible that prostaglandins are involved in the central action of salicylic acid.

Afferent Pathways↗
PubMed1994

Acetylsalicylic acid in the prevention of early stenosis and occlusion of transjugular intrahepatic portal-systemic stent shunts: a controlled study.

Stenosis or occlusion of the transjugular intrahepatic portal-systemic stent shunt may be initiated by aggregation and activation of thrombocytes on the surface of the metallic stent material. To find effective prevention of this event, we conducted a controlled trial administering acetylsalicylic acid for 3 mo. Forty-four patients (8 women and 36 men) with portal hypertension were included in this study. The patients were randomized into a group receiving 100 mg acetylsalicylic acid/day (n = 21) or into a control group (n = 23). Treatment was started immediately after transjugular intrahepatic portal-systemic stent shunt. Three months after transjugular intrahepatic portal-systemic stent shunt, 15 patients in the acetylsalicylic acid group and 19 patients in the control group underwent clinical reevaluation, gastroscopy and recatheterization with determination of the portal-systemic pressure gradient. No variceal bleeding occurred in any patients. In four patients in the acetylsalicylic acid group, erosive gastritis was observed in gastroscopy in contrast to only one patient in the control group. Complete patency of the stent was noted in 10 of 15 patients in the acetylsalicylic acid group and in 14 of 19 patients in the control group. Transjugular intrahepatic portal-systemic stent shunt restenosis associated with a significant increase of the portal-systemic gradient occurred in five patients in the acetylsalicylic acid group, which required redilation in all and additional stent placement for expansion of the stented tract in two patients. In the control group, redilation was necessary in five patients with additional stent extension in two patients.(ABSTRACT TRUNCATED AT 250 WORDS)

Aged↗
PubMed1982

[Effect of flurbiprofen and acetylsalicylic acid on the ultrastructure of blood platelets].

Flurbiprofene or acetylsalicylic acid did not change the structure of inactivated platelets. With flurbiprofene 50% aggregation inhibition was obtained at 10(-6) to 10(-5) M concentrations. To obtain the same result with acetylsalicylic acid, 10(-4) to 10(-3) M concentrations were necessary. With both agents, shape change was inhibited. The platelets in the small aggregates did not have the normal stretched dumb-bell shape but remained globulous and emitted a broad pseudopode containing normally-repolymerized microtubules.

Aspirin↗
PubMed1975

A simultaneous determination of acetylsalicylic acid, salicylic acid and salicylamide in plasma by gas liquid chromatography.

A novel method for the simultaneous determination of acetylsalicylic acid, salicylic acid and salicylamide in biological fluids by gas liquid chromatography is described. The assay has been used to determine the plasma concentration of salicylates in 10 volunteers after oral ingestion of three commercially available aspirin-containing formulations. No difficulty was encountered in determining low concentrations of acetylsalicylic acid in the presence of higher concentrations of salicylic acid. The in vivo plasma half life of acetylsalicylic acid in man was found to be 15.5 min.

Administration, Oral↗
PubMed1979

Effects of acetylsalicylic acid on lymphocyte subpopulations in peripheral blood.

The in vitro and in vivo effects of therapeutical doses of acetylsalicylic acid on lymphocyte subpopulations in peripheral blood were investigated with the following results: Acetylsalicylic acid caused both in vitro and in vivo a reduction of complement receptor bearing lymphocytes and of lymphocytes identified with fluorescent rabbit antibody to human Ig (polyvalent) and to human IgG. Sheep red blood cell receptor bearing lymphocytes, and lymphocytes identified with antibody to human IgM and IgD were unaffected by acetylsalicylic acid.

Aspirin↗
PubMed1994

[Use of acetylsalicylic acid and other antiphlogistics in hematemesis/melena].

The use of acetylsalicylic acid and other non-steroidal, anti-inflammatory drugs was studied prospectively in 207 patients admitted for suspected upper gastrointestinal bleeding. In addition to detailed drug history, plasma samples for drug analyses were obtained from the majority of the patients. 64 of the patients admitted recent intake of ulcerogenic drugs, and the plasma samples revealed another 11 users. Acetylsalicylic acid was the most prevalent substance, but all available non-steroidal, anti-inflammatory drugs were represented in the material. Gastroduodenal ulcers were found in 94 (44%) of the patients; two thirds of the users and one third of the non-users. Gastric ulcer was slightly more prevalent than duodenal ulcer in both groups. Six patients with drug-associated bleeding had previously had a verified drug-associated ulcer. Only 12 users and 16 non-users denied dyspeptic complaints before admission. The users were older, they generally had a lower Hgb on admission than non-users had, and a slightly higher transfusion requirement, but these factors did not result in significant differences as to clinical outcome. The drug analyses of plasma samples showed a discrepancy to the anamnestic data in 25% of the patients and may be a useful addition to drug history in these studies.

Adolescent↗
PubMed1995

Noninvasive assessment of the effect of xenobiotics on mitochondrial function in human beings: studies with acetylsalicylic acid and ethanol with the use of the carbon 13-labeled ketoisocaproate breath test.

Studies in experimental animals and morphologic data in patients suggest that mitochondria are a prime target of the toxicity of ethanol and acetylsalicylic acid. However, the effects of socially consumed amounts of ethanol and therapeutic doses of acetylsalicylic acid on mitochondrial function in human beings are not known. The alpha-ketoisocaproic acid (KICA) breath test noninvasively assesses a mitochondrial function, the decarboxylation of KICA, by following the exhalation of labeled carbon dioxide after the administration of labeled KICA. The decarboxylation of I-[13C]KICA was measured in two groups of eight healthy volunteers after ingestion of 0.5 gm/kg of ethanol or 30 mg/kg of acetylsalicylic acid, respectively. Breath samples were collected at intervals for the determination of [13C] carbon dioxide in breath. The ingestion of ethanol resulted in peak concentrations of ethanol in plasma of 17.3 +/- 2.4 mmol/L (mean +/- 95% confidence interval) and increased the lactate/pyruvate ratio in peripheral venous blood. Although the 13C enrichment of circulating KICA and leucine were similar in the presence and absence of ethanol, the decarboxylation KICA was significantly lower (p < 0.01) at each time point in the presence of ethanol. The fraction decarboxylated in 2 hours was 6.3% +/- 1.9% of the administered dose after administration of ethanol and 14.2% +/- 3.9% (p < 0.001) in the control period. In contrast, the ingestion of acetylsalicylic acid, which resulted in plasma concentrations of 0.9 mmol/L salicylate significantly increased the decarboxylation of KICA to 19.3% +/- 3.1% of the administered dose exhaled in 2 hours.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1995

A new salicylate ISFET for the determination of salicylic and acetylsalicylic acid in drugs.

A salicylate ISFET for the analysis of salicylic and acetylsalicylic acid in drugs is described. It is based on a salicylate ion selective membrane coated on the surface of the Si3N4 gate of the FET. The sensitive membrane consists of tetra-dodecylammonium salicylate, polyvinyl chloride and a proper plasticizer. The linearity range of the sensor is 5 x 10(-5)-1.5 x 10(-2) M for the salicylic acid, and 7 x 10(-5)-1.5 x 10(-2) M for the acetylsalicylic acid, respectively. The detection limit for the two compounds is 5 x 10(-5) M while the response time is < or = 20 s. The effect of pH and different interfering ions was also studied. The sensor was used to analyse the content of acetylsalicylic and salicylic acid in some drugs, and the accuracy of the method was evaluated through recovery tests. The results obtained with this method are well correlated either with those obtained with a classical ISE employing the same sensitive membrane or with the classical volumetric method.

Aspirin↗
PubMedDate not supplied

[Bioavailability of acetylsalicylic acid administered orally or rectally in the rabbit].

The aim of this study is to compare the bioavailability of acetylsalicylic acid administered rectally in suppositories form and orally in tablets form to the rabbit. Acetylsalicylic acid was given to 8 males rabbits rectally and orally in a balanced crossover design with 15 days of interval between each study. In blood samples, acetylsalicylic acid is determined by Trinder's method. It has been established that the rectal route has a faster absorption than the oral route however it displayed a more intense first pass effect than that of the oral route.

Administration, Oral↗
PubMed1995

Antiaggregating and vasodilatory effects of a new nitroderivative of acetylsalicylic acid.

We studied in vitro the effects on platelet aggregation and vascular tone of a new nitrocompound (nitroxy-butyl-acetylsalicylate: NO-ASA). In order to elucidate any possible activity due to the release of nitric oxide or the inhibition of platelet cyclo-oxygenase we compared NO-ASA to acetylsalicylic acid. NO-ASA 1 mM inhibited arachidonic acid-induced platelet aggregation (basal 75.4 +/- 2.35%; NO-ASA 22 +/- 3.46%; M +/- SEM; P < 0.001; n = 6), but proved less active than acetylsalicylic acid (complete inhibition at 2 x 10(-5) M). NO-ASA also significantly reduced thrombin-induced (0.04-0.08 U/ml) platelet aggregation in acetylsalicylic acid-treated platelets (basal 70.5 +/- 1.7%; NO-ASA 35.4 +/- 2.2%; P < 0.001; n = 10; IC50 7 x 10(-5) M). Methylene blue reduced the effects of NO-ASA on thrombin-induced (NO-ASA 46.7 +/- 5.25%; NO-ASA+MB 59.1 +/- 4.3%; P < 0.01; n = 8), but not arachidonic acid-induced platelet aggregation. The inhibitory effects of NO-ASA on platelet aggregation were partially removed by oxyhaemoglobin. Platelet thromboxane A2 production (TXB2 concentration in the supernatant of the aggregate 35.38 +/- 7.81 ng/ml; n = 8), was totally abolished by acetylsalicylic acid (0.17 +/- 0.04 ng/ml; P < 0.001; n = 8) and reduced by NO-ASA (8.3 +/- 4.05 ng/ml; P < 0.01; n = 8). In vitro studies on isolated rat aortic rings showed NO-ASA 10(-3) M, but not ASA up to 10(-3) M, induce a dose dependent vasorelaxation (100% of epinephrine-induced contraction) both in intact and endothelium denuded arteries (IC50 5 x 10(-5) M). Addition of methylene blue reversed this relaxation. In conclusion these data demonstrate that NO-ASA acts through a double mechanism: a) by inhibiting cyclo-oxygenase and b) by releasing NO active on guanylyn cyclase both in platelets and in vascular smooth muscle cells.

Adult↗
PubMed1997

The fetoplacental pressor effects of low-dose acetylsalicylic acid and angiotensin II in the ex vivo cotyledon model.

OBJECTIVE: Our purpose was to investigate perfusion pressure changes ex vivo induced by angiotensin II on fetoplacental vasculature pretreated with low-dose acetylsalicylic acid. STUDY DESIGN: Two cotyledons from each of 12 placentas were perfused. The intervillous space of one cotyledon was infused with acetylsalicylic acid (5 x 10(-5) mol/L) similar to the serum concentration of women receiving daily low-dose aspirin therapy (60 to 81 mg). The control cotyledon was infused with an equivalent amount of normal saline solution. Two doses of angiotensin II, 1 x 10(-11.5) and 1 x 10(-10) moles, were injected as boluses into the chorionic arteries of each cotyledon. A 3 x 10(-7) mole dose of angiotensin II was also injected into the intervillous space. Statistical analysis was performed with analysis of variance, and results are expressed as mean pressure change in millimeters of mercury +/- SEM. RESULTS: Perfusion pressure response did not vary between cotyledons pretreated with acetylsalicylic acid and control cotyledons when 3 x 10(-7) moles of angiotensin II was injected into the intervillous space (8.0 +/- 1.9 mm Hg vs 9.8 +/- 1.6 mm Hg, p = 0.59). There were no differences between cotyledons in pressure response to 1 x 10(-11.5) moles of angiotensin II injected into the fetal circuit (5.9 +/- 0.8 mm Hg vs 6.7 +/- 0.9 mm Hg, p = 0.51). However, in the cotyledons pretreated with acetylsalicylic acid there was a decrease in the pressor response to 1 x 10(-10) moles of angiotensin II (14.1 +/- 1.4 mm Hg vs 21.5 +/- 3.3 mm Hg, p = 0.05). CONCLUSIONS: Low-dose aspirin infused into the intervillous space decreases vasoconstriction elicited by angiotensin II in the fetoplacental compartment. This suggests that maternal low-dose aspirin therapy has effects in the fetoplacental circulation in addition to its effects in the maternal circulation.

Angiotensin II↗
PubMed1988

Decrease in arterial blood pressure in spontaneously hypertensive rats by the TXA2 receptor antagonist BM 13177 and by acetylsalicylic acid.

The effects of the selective TXA2 receptor antagonist BM 13177 and of the cyclooxygenase inhibitor acetylsalicylic acid on blood pressure and heart rate were investigated in anaesthetized spontaneously hypertensive rats (SHR). After intravenous injection of BM 13177 (60 mg/kg) there was a strong short-lasting decrease in arterial blood pressure (BP) with a maximum reduction of 21.6% in the third minute after injection. The heart rate was only slightly decreased. The formation of TXB2 and 6-keto-PGF1 alpha in serum, aorta thoracica, renal medulla, and renal cortex, which was determined by radioimmunoassay, was not altered by BM 13177. Pretreatment with acetylsalicylic acid (100 mg/kg) attenuated the BM 13177 induced reduction of blood pressure and heart rate in male, but not in female SHR. An intravenous application of acetylsalicylic acid (ASA) (100 mg/kg) resulted in a decrease of blood pressure and heart rate only in male rats. The extent of these effects was similar to that induced by BM 13177. A possible explanation for the different reactions of male and female animals might be sex differences in the sensitivity of cyclooxygenase in the aorta thoracica to ASA and/or in the balance of prohypertensive and antihypertensive prostanoids. TXA2 and other prostanoids seems to participate in the short-time regulation of BP in SHR.

Animals↗
PubMedDate not supplied

Intravenous acetylsalicylic acid inhibits central trigeminal neurons in the dorsal horn of the upper cervical spinal cord in the cat.

Acetylsalicylic acid (ASA) is one of the most commonly used substances in the treatment of headache and other pain syndromes. It is only recently that its efficacy in the treatment of acute attacks and in the prophylaxis of migraine has been proven in clinical trials. Various peripheral and central mechanisms have been proposed for the analgesic effects of acetylsalicylic acid and its mode of action in migraine. The possible actions of acetylsalicylic acid in migraine include local analgesic effects, changes in cerebral serotonin turnover, modulation of antinociceptive neurons in the hypothalamus and inhibition of the release of algogenic peptides during neurogenic inflammation. In this study trigeminal somatosensory evoked potentials and single unit activity of central trigeminal neurons in the dorsolateral C2 spinal cord were monitored during electrical stimulation of the superior sagittal sinus in the cat. Intravenous administration of the soluble acetylsalicylic salt (acetylsalicylic lysinate, 30 mg/kg) reduced the peak-to-peak amplitudes of somatosensory evoked potentials from 219 +/- 11 mV by 18% after 45 minutes and by 26% after 60 minutes. Naloxone injection (0.5 mg/kg and 1.5 mg/kg) did not reverse the inhibition caused by ASA. The probability of trigeminal cell tiring was reduced in 63% percent of the monitored single units. The effect was not mediated through naloxone-sensitive opioid receptors and was independent from ASA-induced peripheral blockade of neuropeptides during neurogenic inflammation. The non-steroidal anti-inflammatory agent ketorolac (0.4 mg/kg, IVI) a new cyclooxygenase inhibitor, also reduced the somatosensory evoked potentials by 30% following the same time course.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMedDate not supplied

Use of a complex approach for assessment of metamizole sodium and acetylsalicylic acid toxicity, genotoxicity and cytotoxicity.

A complex approach based on the use of test organisms belonging to different systematic groups (plants, invertebrates and vertebrates), as well as the nucleolar biomarker and the micronucleus test on their cells, was applied to assess the toxicity, cytotoxicity and genotoxicity of two pharmaceutical substances (metamizole sodium and acetylsalicylic acid) applied at ic(50) concentrations for mammalian cells. The compound acetylsalicylic acid was evaluated at a concentration (1.6 x 10(3) mg l(-1)) that was non-toxic for bioassays based on fish (Carassius auratus gibelio) and hydra (Hydra attenuata) and acutely toxic for bioassays with ceriodaphnia (Ceriodaphnia affinis) and onion (Allium cepa). The metamizole sodium solution (6.25%) demonstrated acute toxicity for the whole set of test organisms. Both drugs, after their 30-360 min influence on the test organisms, first changed the nucleolar size in plant and animal cells (i.e. the transcriptional activity of ribosomal genes was affected most significantly). Moreover, the metamizole sodium solution caused nucleolar structural damage in 90% of hydra cells as early as after 30 min of exposure. The acetylsalicylic acid solution inhibited essentially the rate of cell division in the meristem of onion roots (the mitotic index decreased to 9.6 per thousand, as compared 51.7 per thousand for the control). The carp incubation and the onion germination in the acetylsalicylic acid solution showed a reproducible increase in the frequency of cells with micronuclei (2 and 5.5 times, respectively) and double nuclei (3 and 1.5 times, respectively). The approach described herein may be applied for obtaining rapid, cost-efficient and useful supplementary data on different types of toxicity for marketed drugs as well as for drugs under development.

Allium↗