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[Stomach tolerance of buffered and unbuffered low-dose acetylsalicylic acid: an endoscopy controlled double-blind study in volunteers].

In this randomised double-blind cross-over study the gastroduodenal tolerability of buffered acetylsalicylic acid (ASS) (Aspalox = 325 mg ASS plus 300 mg magnesium aluminium hydroxide) daily has been compared with unbuffered ASS (325 mg) daily in 12 healthy volunteers using upper Gl-endoscopy. The treatment period lasted 14 days: endoscopic controls were performed at entry and repeated at day 14. At day 0 the mean endoscopic score averaged 0.8 +/- 0.1 in both groups (MW +/- SEM). One tablet Aspalox daily induced marked gastroduodenal damage at day 14 (6.5 +/- 1.5). The median lesion score rose from 1.0 (day 0) to 7.0 at day 14. Unbuffered ASS evoked almost identical gastroduodenal injuries at day 14 (7.5 +/- 1.8). The corresponding median values were 1.0 (day 0) and 7.0 at day 14. Our data suggest, that the amount of buffering in the Aspalox preparation is not sufficient enough to protect human gastroduodenal mucosa against low dose acetylsalicylic acid.

Adult↗

The effect of acetylsalicylic acid on the development of the skeletal system in rats.

The authors wished to clarify the cause of micro- and phocomelia developing in rat fetuses following administration of acetylsalicylic acid. It has been proved by histological examinations that the positive ground substance of the epiphyseal cartilage, detected by Rivanol reaction, became disarranged or negative. The sulphation of glycosaminoglycans was diminished or inhibited by acetylsalicylic acid in the chondrocytes depending on the dose applied. The conclusion has been drawn that the malformation developed is due to the reduced production of sulphated mucopolysaccharides.

Animals↗

The effect of acetylsalicylic acid on TSH and PRL secretion after TRH stimulation in the human.

In order to study the effect of prostaglandins on TSH release in the human, Acetylsalicylic Acid was given to 9 normal subjects at doses necessary to obtain a salicylate level of 20 mg/dl. TRH, 400 mug was injected prior to and after the medication. Thyroid hormone parameters were measured at time 0, and TSH and PRL at time 10, 20, 30, 45 minutes after the injection. The free fraction of thyroid hormones remained constant during treatment but a significant decrease of TSH concentration (30%) was noted after TRH injection on Acetylsalicylic Acid treatment whereas no changes were noted for PRL. As noted in the animal, this study indicates that in the human, prostaglandins potentiate the effect of TRH on TSH liberation by the pituitary where it has no effect on PRL.

Adult↗

[Experimental study of the interaction of nonsteroidal anti-inflammatory agents--voltaren and acetylsalicylic acid--with beta-adrenoblockers].

It has been demonstrated in rat experiments that the beta-adrenoblockers propranolol and pindolol differ in the influence on the therapeutic and toxic effects of voltaren and acetylsalicylic acid. Propranolol has an analgetic action of its own, reducing the analgetic and antiinflammatory effects of voltaren and acetylsalicylic acid. It potentiates the antipyretic effect of voltaren and ulcerogenic action of both nonsteroidal antiinflammatory drugs. Pindolol exerts both analgetic and antiinflammatory action and does not affect the antipyretic effect of voltaren and ulcerogenic action of nonsteroidal antiinflammatory drugs. The difference in the action of the beta-adrenoblockers under study is likely to be linked with the characteristics of their pharmacological action spectrum.

Adrenergic beta-Antagonists↗

[Acetylsalicylic acid in self-medication of migraine. A pharmacy-based observational study].

BACKGROUND: The aim of the study was to investigate the efficacy and tolerability of acetylsalicylic acid in the treatment of acute migraine attacks by self-medication under daily life conditions when bought in a pharmacy and also the ability of patients to self-diagnose correctly. METHODS: A total of 296 patients were recruited from 156 pharmacies and recorded up to 3 migraine attacks. Following an advisory discussion the pharmacists gave a questionnaire to persons who had purchased acetylsalicylic acid (Aspirin Migraine) in the pharmacy to treat migraine. A total of 578 questionnaires containing 36 questions about demographic details, headache phenotype, medical history, efficacy over 2 h and tolerability of the preparation were analyzed. RESULTS: The IHS criteria (1988) for migraine were identified correctly by 92.7% of the patients. In 66.3% of the attacks, the intensity of the headache was reported as severe. In 60% of the documented attacks, a decrease from severe or moderate to mild or no headache was recorded after medication, and freedom from headache was achieved in 35.8%. The effect was reproducible over 3 migraine attacks. Nausea, photophobia and phonophobia were reduced by 71-86% compared to the baseline level. Side-effects were reported twice as often by the participants in response to closed questions than to open questions (16.6 vs. 8.3%). CONCLUSION: A high percentage of migraine patients are capable of diagnosing their condition themselves when they seek advice in a pharmacy. The data on efficacy confirm the results from controlled clinical studies. The same parameters as those used in controlled clinical studies can also be recorded in pharmacy-based observational studies, therefore, the safety and tolerability of the medication can be recorded under real conditions.

Adult↗

An investigation of the effect on platelet function of acetylsalicylic acid, dipyridamole and the two drugs in combination in patients with transient attacks of ischaemia.

Twenty patients suffering from transient attacks of ischaemia were studied. Seven received acetylsalicylic acid, six dipyridamole and seven a combination of the two drugs. No significant difference in platelet aggregation was shown in the acute phase between the three treatment groups using an adenosine diphosphate test method. Using Thrombofax platelet substitute, however, a significant difference was seen in all measures. On the seventh day following the ischaemic attack the Thrombofax values returned to normal but, in contrast, Platelet Factor 4 release was increased. Monthly testing of platelet activity during treatment shows that the combination of acetylsalicylic acid with dipyridamole was more effective in bringing about an early inhibition of Platelet Factor 4 release than either agent alone.

Adult↗

Effects of microgravity on the binding of acetylsalicylic acid by Rhizobium leguminosarum bv. trifolii.

Bacteroids can be induced in vitro by treating growing Rhizobium leguminosarum bv. trifolii with succinic acid or succinic acid structural analogs like acetysalicylic acid. Quantitating bacteroid induction by measuring acetylsalicylic binding under normal (1 g) conditions showed two forms of binding to occur. In one form of binding cells immediately bound comparatively high levels of acetylsalicylic acid, but the binding was quickly reversed. The second form of binding increased with time by first order kinetics and reached saturation in 40 s. Similar experiments performed in the microgravity environment aboard the NASA 930 aircraft showed only one form of binding and total acetylsalicyclic acid bound was 32% higher than at 1 g.

Aspirin↗

[Clarification on publications concerning the synthesis of acetylsalicylic acid].

Charles Frédéric Gerhardt (1816-1856) mentioned in his Traité de chimie Organique (1854) a publication, in French (realized in 1852 but published in 1853) entitled "Researches on anhydrous organic acids" in which, was reported the reaction of sodium salicylate with acetyl chloride. He thought that the reaction product was an acid anhydride, but obtained really crude acetylsalicylic acid. Later on, but also in 1853, a publication in german, by the same author related the same experiments. Surprisingly only the second publication has been mentioned in most of the historical studies on the subject. Acetyl salicylic acid was identified and synthesised in 1859 by von Gilm by another method and the product obtained by Gerhardt was identified to it in 1869.

Acids↗

Acetylsalicylic acid and blood coagulation in the horse.

Equine blood may contain salicylic acid (SA) taken up as free acid or represents the metabolite of acetylsalicylic acid (ASA). To obtain information of SA in race horses we screened blood samples of trotting-horses routinely drawn to be analyzed for doping substances. The individual values determined followed a Gaussian distribution displaying a geometric mean of 19 ng SA per ml serum. A probit analysis revealed linear relationship (r = 0.995). Additional studies examined the antithrombotic efficacy of ASA in the horse. An oral dose of 300 mg ASA considerably elevated the bleeding time for more than 2 hours with concomitant SA serum levels between 800 and 1000 ng/ml. It is concluded that salicylate levels even below 1 microgram/ml serum bring about considerable pharmacologic effects such as prolongation of bleeding time, decrease in blood viscosity and possibly dilatation of blood vessels. These effects may improve the tissue supply with blood including oxygen.

Animals↗

Topical acetylsalicylic acid in the treatment of allergic pollinosic conjunctivitis.

The pharmacological treatment of allergic conjunctivitis includes the use of topical antiinflammatory drugs, i.e. steroids and NSAIDs (nonsteroidal antiinflammatory drugs), such as acetylsalicylic acid (ASA). However, steroids are not suitable in prolonged treatment, as well as in pollinosis in the Mediterranean area, because of their side effects. The present double-blind study evaluates the topical use of acetylsalicylic acid eye drops (1% solution) compared to placebo in the treatment of patients with seasonal allergic conjunctivitis during the period June-July 1990. The patients were randomized and treated with ASA eye drops or placebo eye drops, both applied as one drop in each eye q.i.d. for 14 days. The severity of symptoms was evaluated before and after treatment by the investigator and the patient. An overall judgement of therapeutic response was expressed independently by the patient and the investigator at the end of the treatment. The ASA-treated group improved significantly compared to the placebo-treated group. No serious side effects were observed. The results confirm the clinical efficacy and safety of topical ASA in the treatment of pollen-induced allergic conjunctivitis.

Adolescent↗

Acetylsalicylate-human serum albumin interaction as studied by NMR spectroscopy--antigenicity-producing mechanism of acetylsalicylic acid.

To discover the antigenicity-producing mechanism of acetylsalicylic acid, the interaction of this drug and relevant salicylic acid with human serum albumin (HSA) has been studied by means of nuclear magnetic resonance (NMR) spectroscopy. The determination of spin-lattice relaxation rates (1/T1) of some protons have revealed that one HSA molecule can bind acetylsalicylate and salicylate up to 80 and 290 molecules, respectively. The hydrolysis rates of acetylsalicylate were greatly enhanced in the presence of HSA, especially when the drug/HSA mole ratio was small. Thus, the esterase-like activity of HSA was verified. This activity of HSA was effectively inhibited by salicylate; the effect was ascribed to the stronger binding affinity of salicylate toward HSA as compared with that of acetylsalicylate. Based on these results, the antigenicity-producing mechanism of acetylsalicylate and salicylate has been discussed.

Aspirin↗

[Evaluation of predisposing factors for mediastinal bleeding in myocardial revascularization surgery. Role of acetylsalicylic acid, other platelet adhesion inhibitors, and anticoagulants].

OBJECTIVE: To determine the main factors for perioperative mediastinal bleeding during coronary artery by-pass grafting and to establish the role of acetylsalicylic acid, other inhibitors of platelet adhesion, and anticoagulants in its occurrence. METHODS: A multivariate analysis was performed to the data obtained from 251 patients subjected to coronary artery by-pass grafting in the year 2002. RESULTS: There were no significant differences for the occurrence of perioperative bleeding induced by the preoperative administration of acetylsalicylic acid. No significant increment in the need for blood, platelet, or cryoprecipitates transfusion existed. Patients receiving non-fractionated or low molecular weight heparin had a significantly greater (p < 0.001) transoperative bleeding than patients without this drug. Administration of the other studied drugs did not increase either mediastinal bleeding or the need for blood derivatives. CONCLUSIONS: No statistical evidence was found to suspend administration of inhibitors of platelet adhesion in patients with coronary syndromes, subjected to coronary artery by-pass grafting. However, data obtained suggest the convenience of suspending administration of low molecular weight or non-fractionated heparin to patients subjected electively to coronary artery by-pass grafting.

Adolescent↗

Acetylsalicylic acid as an adjuvant therapy for schizophrenia.

BACKGROUND: Findings from both epidemiological and basic research point to the possibility that NSAIDS impede the deterioration in schizophrenia. METHODS: To study the efficacy of acetylsalicylic acid we will perform a randomized placebo controlled double-blind add-on trial of 80 inpatients and outpatients with schizophrenia, schizophreniform or schizoaffective disorder. Patients will be 1:1 randomized to either 3 months 1000 mg acetylsalicylic acid per day or 3 months placebo, in addition to their regular antipsychotic treatment. All patients will receive pantoprazole treatment for gastroprotection. The outcomes of this study are 3-month change in psychotic and negative symptom severity, cognitive function, and several immunological parameters. This trial may (1) yield a new (adjuvant) therapy for schizophrenia and (2) add to the knowledge on the pathogenesis of this major psychiatric disorder.

Journal Article↗

Prevention of heterotopic ossification after total hip replacement. A prospective, randomised study using acetylsalicylic acid, indomethacin and fractional or single-dose irradiation.

We have carried out a prospective, randomised study of prophylaxis for heterotopic ossification (HO) comparing indomethacin for 7 and 14 days, acetylsalicylic acid, and fractional (4 x 3 Gy) or single exposure of 5 or 7 Gy irradiation after operation. We initially had 723 patients (733 hip replacements), but after withdrawals there were 685 hips of which 18.4% developed HO; 14% were grade I, 2.9% grade II and 1.5% grade III of the Brooker classification. We compared the results between these groups with those of a matched control series and found that indomethacin, 2 x 50 mg for 7 and 14 days, and postoperative irradiation of 4 x 3 Gy or 1 x 7 Gy, significantly reduced the development of HO compared with the control group. Patients in the acetylsalicylic acid group and those with a single irradiation of 5 Gy after operation developed significantly more ossification than those in the indomethacin and other irradiation groups. We suggest the use of 2 x 50 mg of indomethacin with mucoprotection for seven days as prophylaxis against HO after total hip replacement for all patients. A single irradiation of 7 Gy is recommended for patients who have developed HO after previous operations or to whom administration of indomethacin is contraindicated.

Aged↗