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PubMed1978

[Promoting and inhibitory influences of tribenoside and acetylsalicylic acid on spontaneous arthrosis in the mouse (author's transl)].

Tribenoside administered in moderate doses over periods of three or ten months, inhibited the development of spontaneous arthrosis in mice of the C 57 black strain. Acetylsalicylic acid administered once daily in oral doses of 50 and 150 mg/kg for five months, had a distinctly promoting effect on the development of the same arthrosis. Attention is drawn to certain common features in the activity spectra of the two drugs, but especially also to their opposite effects on mucopolysaccharide metabolism and on regenerative processes which are promoted by tribenoside but inhibited by acetylsalicylic acid.

Administration, Oral↗
PubMed2002

[Acetylsalicylic acid (ASA)--is everything clear?].

The authors summarize results of trials with acetysalicyl acid (ASA) in patients with ischaemic heart disease and in particular with chronic cardiac failure. They draw attention to the relatively frequent use this drug in common practice, although so far not a single trial was completed which would prove the effect of acetylsalicyl acid on long-term mortality. The authors discuss also possible interactions of acetylsalicyl acid and ACE inhibitors which in retrospective analyses indicate possible veakening of the ACE-I when administered concurrently with ASA in cardiac failure. The authors mention also other antiaggregation drugs, which similarly as ASA, significantly reduce the mortality in acute coronary syndrome. Their long-term administration is however not associated with further improvement of the diagnosis. Trials are mentioned which compare antiaggregation and anticolagulation treatment in patients with ischaemic heart disease. They analyze also the effect of dosage (benefit vs. risk). After ASA > 300 mg there are more frequent complications, and without a proved effect on total mortality, while doses < or = 100 mg seem to be safer but there is evidence that they are effective in reducing the total mortality of patients with IHD and/or cardiac failure.

Angiotensin-Converting Enzyme Inhibitors↗
PubMed1980

Lysosomal hydrolases in tears and the lacrimal gland: effect of acetylsalicylic acid on the release from the lacrimal gland.

Free and lysosomal activities of 10 acid hydrolases have been determined in human lacrimal gland tissue. The enzyme activities appeared mainly in the lysosomal fraction, and the proportions correspond very well with those found in the tear fluid. Acetylsalicylic acid at blood levelsof about 1 mM produced a significant lowering of the beta-hexosaminidase concentration in tears. It is suggested that acetylsalicylic acid may have a stabilizing effect on lacrimal lysosomes, resulting in a diminished release of lysosomal enzyme from the lacrimal gland.

Aspirin↗
PubMed2004

The effect of acetylsalicylic acid on the release rates of leukotrienes B4 and C4 from cultured skin melanocytes of active vitiligo.

OBJECTIVE: The aim of this study is to investigate the effect of the non-steroidal anti-inflammatory agent, acetylsalicylic acid (ASA), otherwise known as aspirin, at different concentrations on the release rates of the pro-inflammatory mediators, leukotriene B4 (LTB4) and leukotriene C4 (LTC4) from in vitro cultured melanocytes obtained from normal pigmented skin of patients with active vitiligo. METHODS: This study was carried out between April, 2000 and September, 2001, at The Vitiligo Unit, King Abdul-Aziz University Medical Center, Jeddah, Kingdom of Saudi Arabia. Skin biopsies were obtained from patients with active vitiligo (n=7) of different extent and duration, and normal healthy age-matched individuals (n=7) serving as control were recruited to the study. The release rates of LTB4 and LTC4 were determined before and after the addition of the ASA at 3 different concentrations (15, 75, 150 microg/ml) in the primary skin melanocytes culture medium using a commercially available kit based on radioimmunoassay method. RESULTS: Following the ASA treatment at 3 different concentrations (15, 75 and 150 microg/ml), the release rates of LTB4 and LTC4 were increased from melanocytes of the normal individuals (13%, 7.5% and 30%; 7.2%, 51.4% and 60.7%, p<0.001). However, in patients with active vitiligo, the release rate of LTB4 from melanocytes was decreased (2.9%, 14.4% and 7.4%, p<0.05), whereas that of LTC4 was increased (3.9%, 93.8% and 101.4%, p<0.001). CONCLUSION: Acetylsalicylic acid at therapeutic concentrations can regulate the release rates of LTB4 and LTC4 from cultured skin melanocytes of normal and active vitiligo subjects.

Adolescent↗
PubMed2001

The inhibition of oxygen radical release from human neutrophils by resting platelets is reversed by administration of acetylsalicylic acid or clopidogrel.

Resting platelets inhibit oxygen radical release from neutrophils. Antiplatelet therapy may support this function by preventing platelet activation. Whether antiplatelet agents affect the antioxidative action of resting platelets in the absence of platelet activation is unknown. The effect of acetylsalicylic acid or clopidogrel administration on the antioxidative action of resting platelets was therefore studied in ten healthy volunteers. Preparations of resting platelets were obtained from 5 subjects each - before, during and after an eight-day course of daily treatment with 100 mg of acetylsalicylic acid or 75 mg of the thienopyridine clopidogrel. Human peripheral blood neutrophils were pretreated with the platelets at a ratio of (1/5)0 for 45 min; then formyl-Met-Leu-Phe-triggered oxygen radical release was measured fluorometrically. The inhibitory effect of platelets on oxygen radical release from neutrophils which was seen before treatment was abolished by antiplatelet therapy with either of the drugs, and inhibition was restored gradually after discontinuing acetlsalicylic acid/ clopidogrel intake. Results suggest that the protective role of resting platelets in controlling oxygen radical release from neutrophils in the absence of platelet activation may be impaired by antiplatelet therapy.

Adult↗
PubMed1984

Effect of acetylsalicylic acid on glutathione consumption and hexose monophosphate shunt during arachidonic acid induced stimulation of human blood platelets.

Aggregation of human blood platelets by exogenous arachidonic acid is accompanied by a powerful increase in the net flux through the hexose monophosphate shunt and a decrease of the level of reduced glutathione. When platelet cyclooxygenase is inhibited by acetylsalicylic acid diminution by about 60% of arachidonic acid induced flux through the hexose monophosphate shunt as well as lower initial decrease of the glutathione level are found. Investigations with other glutathione oxidizing agents as diamide or tertiary butyl hydroperoxide reveal that acetylsalicylic acid influences neither the activities of glutathione providing enzymes nor that of glutathione peroxidase which catalyzes glutathione consuming reactions in the arachidonic acid metabolism. Together with literature data the results point to a consumption of reduced coenzymes in both cyclooxygenase and lipoxygenase pathways in platelets.

Arachidonic Acid↗
PubMed2001

A validated HPLC method for the determination of pyridostigmine bromide, acetaminophen, acetylsalicylic acid and caffeine in rat plasma and urine.

A method was developed for the separation and quantification of the anti-nerve agent pyridostigmine bromide (PB; 3-dimethylaminocarbonyloxy-N-methyl pyridinium bromide), the analgesic drugs acetaminophen and acetylsalicylic acid, and the stimulant caffeine (3,7-dihydro-1,3,7-trimethyl-1-H-purine-2,6-dione) in rat plasma and urine. The compounds were extracted using C(18) Sep-Pak(R) cartridges then analyzed by high performance liquid chromatography (HPLC) with reversed phase C18 column, and UV detection at 280 nm. The compounds were separated using gradient of 1-85% acetonitrile in water (pH 3.0) at a flow rate ranging between 1 and 1.5 ml/min in a period of 14 min. The retention times ranged from 8.8 to 11.5 min. The limits of detection were ranged between 100 and 200 ng/ml, while limits of quantitation were 150-200 ng/ml. Average percentage recovery of five spiked plasma samples were 70.9+/-9.5, 73.7+/-9.8, 88.6+/-9.3, 83.9+/-7.8, and from urine 69.1+/-8.5, 74.5+/-8.7, 85.9+/-9.8, 83.2+/-9.3, for pyridostigmine bromide, acetaminophen, acetylsalicylic acid and caffeine, respectively. The relationship between peak areas and concentration was linear over range between 100 and 1000 ng/ml. The resulting chromatograms showed no interfering peaks from endogenous plasma or urine components. This method was applied to analyze these compounds following oral administration in rats.

Acetaminophen↗
PubMed2002

[Study of the chemical stability of acetylsalicylic acid tablets during storage in pharmacies of Concepción, Chile].

BACKGROUND: The chemical stability of a pharmaceutical product depends, among other factors, on environmental factors during transport, storage and manipulation of the product. AIM: To study the chemical stability of acetylsalicylic acid (AAS) tablets during ten months of storage in five pharmacies of Concepción, Chile. MATERIAL AND METHODS: Tablets were randomly collected at the beginning of the study and at the third, sixth and tenth month. Quantitative analyses of AAS tablets was carried out by instrumental thin layer chromatography (HPTLC). RESULTS: AAS in tablets was between 99 and 109% at the beginning of the study, between 76 and 110% at three months, between 71% and 112% at six months and between 86 and 110% at ten months of storage. CONCLUSIONS: There was a progressive decrease in the content of acetylsalicylic acid in tables during storage, but it remained between the limits accepted by the United States Pharmacopoeia (USP) (90-110%).

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1986

Acetylsalicylic acid antagonizes the bleeding-induced changes in hemoglobin proportions in normal adult rats.

Normal adult Sprague-Dawley rats were made anemic by repeated phlebotomy. Ion-exchange chromatography of anemic blood showed newborn like hemoglobin proportions, involving the same six hemoglobin components as is found when newborn and adult blood are compared. However, acetylsalicylic acid intake during anemia failed to demonstrate the changes in hemoglobin proportions, either totally or partially, depending upon the doses. Since acetylsalicylic acid inhibits prostaglandin synthesis, the data suggest that one or more prostaglandins may be involved in the process of reverse switching of hemoglobin in adult rat erythroid cells during erythropoietic stress.

Animals↗
PubMed1976

Inhibitory effect of acetylsalicylic acid on human platelet function in normal volunteers and in women using a combined oral contraceptive regime.

Six parameters related to the release reaction were measured simultaneously in 10 human volunteers prior to the intake of one single dose of 1 g acetylsalicylic acid and 1, 4, 5, 6 and 7 days alter: deltaE5 with diluted collagen, deltaE10 with Thrombofax and the serotonin-14C release by undiluted and diluted collagen, by Thrombofax and by bovine plasma. The duration of the inhibitory effect varied according to the test used. It was the most prolonged (through the 7th day) if serotonin-14C release by diluted collagen was measured. A systematic investigation of the platelet release reaction in women taking a combined oral contraceptive was also performed. There were no statistically significant differences from a control group. No difference in acetylsalicylic acid sensitivity, measured 24 hours after intake of 1 g of aspirin, could be demonstrated.

Adult↗
PubMed1980

Acute effects of acetylsalicylic acid on blood glucose and insulin in non-insulin dependent diabetes.

Two groups of diabetic patients--one treated with diet and glipizide and the other with diet alone--volunteered in the study. After a standard meal blood glucose and insulin were followed for four hours during two separate days. On the first day the patients received their ordinary treatment, whereas on the second 1 g of acetylsalicylic acid was added before the test meal. In both groups an enhanced insulin mobilization was observed, when acetylsalicylic acid has been added. A decrease of the blood sugar level was recorded as well. The latter was however less pronounced in the group of subjects receiving only diet.

Aspirin↗
PubMed1984

Injectable ketoprofen vs. acetylsalicylic acid for the relief of severe cancer pain: a double-blind, crossover trial.

Thirty-six patients suffering from severe pain due to bone involvement from cancer participated in an analgesic study that compared single doses of ketoprofen 100 or 400 mg iv or injectable acetylsalicylic acid 1 g. A double-blind, balanced incomplete block design was adopted, in which each patient received two of the three test treatments, with an interval of 24 hours. Ketoprofen 400 mg proved significantly superior to 100 mg of the same drug, and was superior to 1 g of the acetylsalicylic acid derivative in the patients' assessment of the overall response. This was expressed by a visual analog scale and preferences. No adverse reaction was observed with any treatment.

Adult↗
PubMed1989

Effects of atropine, acetylsalicylic acid, FPL 55712, and phentolamine on increased histamine responsiveness of cat lung strips under conditions of airway inflammation.

Our recent in vitro studies on airway smooth muscles of cats with turpentine oil inflammation showed an increase of isometric tension of the lung strips to histamine application. This communication describes the effect of atropine, acetylsalicylic acid, FPL 55712, and phentolamine on the histamine contractions of the lung strips derived from control and experimental groups of cats. Pretreatment of the lung strips with atropine and acetylsalicylic acid had no significant effect on histamine induced contraction. FPL 55712 significantly decreased the mean values of isometric contractions after the low doses of histamine in experimental groups of strips. The isometric contractions after higher doses of histamine were not affected by FPL 55712 in both groups of strips. The significant increase of histamine contractions of the lung strips induced by experimental inflammation was reduced by phentolamine. The role of alpha adrenergic receptors in the increased responsiveness of the inflamed lung tissues to histamine is discussed.

Animals↗
PubMed1979

Excitation of afferent fibres in the cardiac sympathetic nerves induced by coronary occlusion and injection of bradykinin. The influence of acetylsalicylic acid and dipyron.

Afferent impulse activity was recorded in single fibres of the inferior cardiac sympathetic nerve of the cat. When the descending branch of the left coronary artery was ligated for 60 sec an enhancement of afferent impulses was recorded. Elevations in discharge frequency were also induced by injecting bradykinin, epinephrine, and isoprenaline or by general hypoxia due to interruption of the artificial ventilation. When these procedures were after pretreatment with the analgesic agents, acetylsalicylic acid or dipyron a reduction in spike discharge was observed only with bradykinin after application of acetylsalicylic acid. No influence of these pretreatments on the effects of coronary occlusion, general hypoxia and injection of epinephrine and isoprenaline could be observed. These results suggest that bradykinin does not predominate as mediator substance in eliciting ischemic heart pain.

Aminopyrine↗
PubMed1985

Acetylsalicylic acid, paracetamol and morphine inhibit behavioral responses to intrathecally administered substance P or capsaicin.

Intrathecally administered substance P (SP) or capsaicin in mice elicited a pain-related behavioral response consisting of vigorous biting, licking and scratching of the caudal part of the body. Pretreatment of the animals with intraperitoneally injected acetylsalicylic acid (300 and 400 mg/kg), paracetamol (300 and 400 mg/kg) and morphine (2.5 and 5 mg/kg) reduced the responses in a dose-dependent manner. The analgesia is probably mediated by inhibition of a postsynaptic SP sensitive mechanism. Thus these results demonstrate central antinociceptive effects of acetylsalicylic acid and paracetamol.

Acetaminophen↗
PubMed1977

Acute effects of acetylsalicylic acid in patients with chronic renal insufficiency.

The effect of acetylsalicylic acid (ASA) in patients with renal insufficiency has been examined. In one investigation (A), in patients with a mean GFR of 23.0 ml/min the acute effects of ASA 750 mg i.v. (lysine-ASA 7.5 ml) and 0.9% NaCl 7.5 ml on renal water and solute output and on the clearance of inulin, creatinine and PAH were compared. In another (B) the effects of simultaneous administration of ASA 750 mg or 0.9% NaCl 7.5 ml i.v. with an infusion of furosemide 250 mg were investigated in six patients (mean GFR 12.9 ml/min) in a cross-over study. In study A there was a significant fall in urinary sodium excretion within the first 15 min after ASA administration, with a maximal decrease to 21% of the control period. Urine flow fell to 35%, osmolal clearance to 41%, inulin clearance to 54% and PAH clearance reabsorption of sodium increased. The effect of ASA lasted for 2-6 h. The mean salicylic acid concentration during the first two hours after ASA administration was 60.0 mug/ml, and the mean protein bound salicylic acid (SA) was 70.4%. There was no effect of placebo (0.9% NaCl 7.5 ml) on renal function. Pretreatment with ALA 750 mg i.v. attenuated the diuretic effect of furosemide 250 mg, and reduced creatinine clearance significantly within 0-2 h after drug administration.

Aged↗
PubMed1978

Influence of food on the absorption of acetylsalicylic acid from enteric-coated dosage forms.

The absorption of acetylsalicylic acid (ASA) from two different enteric-coated dosage forms, tablets (Premaspin) and granules (Reumyl), was studied in healthy volunteers under fasting and non-fasting conditions by following the plasma concentration and urine recovery of salicylates after single doses of ASA 1 g. Conventional tablets (Aspirin) were used as the reference. Under fasting conditions the absorption of ASA from the two different enteric-coated preparations was complete. Taken with food the enteric-coated tablets gave much lower plasma concentrations than under fasting conditions, and absorption was not complete in all subjects. In contrast, absorption from the enteric-coated granules was not influenced by the intake of food. It was concluded that enteric-coated granules of ASA permit more reproducible absorption than enteric-coated tablets.

Adult↗
PubMed1985

Plasma concentrations and anti-platelet effects after low dose acetylsalicylic acid.

The present study has investigated whether low-dose acetylsalicylic acid (ASA) can inhibit platelet aggregation locally at its site of gastrointestinal absorption without concentrations in the systemic circulation high enough for inhibition of cyclooxygenase. For this purpose platelet aggregation, thromboxane formation as well as ASA plasma concentrations were measured in 8 volunteers before oral intake of 100 mg ASA as well as 20 to 300 minutes thereafter. At each time 5 ml of blood were mixed with 5 ml of blood obtained from a second, untreated volunteer. Aggregation and thromboxane formation were also determined in these mixed blood samples. The same protocol was performed with 4 volunteers after administration of 1500 mg ASA as well as after no drug intake. In a separate experiment the concentration-effect-relationship of ASA was assessed in vitro. One hundred and forty minutes after administration of 100 mg ASA aggregation and thromboxane formation were significantly decreased to 49.4 and 4.5% of the initial values, respectively, whereas in the mixed blood sample aggregation was not impaired. Inhibition of thromboxane formation was constantly 73% of the inhibition observed in the unmixed sample throughout the study period and thus most probably was caused by dilution of the platelets of the untreated volunteer by the inactivated platelets of the ASA-treated volunteer. These data suggest the absence of pharmacologically active drug concentrations in the peripheral blood. ASA plasma concentration was highest after 40 minutes (2.2 +/- 1.6 microgram/ml; n = 5). After the 1500 mg ASA dose platelet function and thromboxane formation decreased to 29.8 and 2.0% of the initial values, respectively. Furthermore, aggregation and thromboxane formation in the mixed blood sample were markedly reduced. Thus, after the high dose of ASA effective plasma concentrations were present in the peripheral circulation. Highest ASA plasma concentrations were 21.1 +/- 8.9 micrograms/ml. IC50 values were 1.00 +/- 0.36 and 0.30 +/- 0.05 microgram/ml for aggregation and thromboxane formation in vitro, respectively. It is concluded that low dose ASA can effectively inhibit platelet function without producing pharmacologically active concentrations in the peripheral circulation.

Adult↗