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At least 883 records · Page 49Linked to original sources
PubMed2000

Microbial models of mammalian metabolism: microbial transformation of naproxen.

Preparative-scale fermentation of S-naproxen, the known antiinflammatory, analgesic and antipyretic drug, with Cunninghamella elegans ATCC 9245 afforded S-demethylnaproxen, the known human active metabolite of naproxen, in a 90% yield. Demethylnaproxen was also detected as the major metabolite of naproxen using Cunninghamella blakesleeana ATCC 8688a. A review of the previous microbial metabolism studies using the fungi Cunninghamella species suggested that it could be a plausible in vitro predictor for mammalian metabolism.

Animals↗
PubMed1975

Induced bleeding changes with aspirin in various tolerant and intolerant patient groups.

The advantages of aspirin as a first stage anti-hemostatic agent, combined with its relatively low cost, ease of administration and simplicity of control, have led to its use in prophylaxis for atherosclerotic and thromboembolic disease processes, in addition to its long established employment as an analgesic and antipyretic agent. However, adverse reactions in aspirin-hypersensitive patients have led to reappraisal of the risks involved in its casual administration. A method to reduce such risks is proposed.

Aspirin↗
PubMed2001

Nonsteroidal anti-inflammatory drugs and paracetamol in children.

The cyclooxygenase enzymes produce large amounts of prostaglandins in presence of tissue injury and inflammation. Prostaglandins exert their influence on nerve membrane excitability both at the peripheral site and at the spinal dorsal horn. Their key role in peripheral tissue inflammation and central sensitization warrants their incorporation in pain management strategies for children. As the COX2 isoenzyme is the main target for controlling hyperalgesia, nonsteroidal anti-inflammatory drugs (NSAIDs) with high affinity for this enzyme will provide reliable antihyperalgesic effects. The benefits of NSAIDs for postsurgical pain therapy must be balanced against the risk of postoperative bleeding in children in whom any derangement of hemostasis could adversely affect outcome. If contraindications for NSAID use exist, paracetamol is the alternative. Paracetamol has potent antipyretic and analgesic effects, but no anti-inflammatory effect. The rectal route of administration is notoriously unreliable for eliciting an analgesic effect and the oral route is to be preferred. The dosage of paracetamol must take into account the pharmacokinetic properties of the drug in children. The maximum daily dosage should not be exceeded to avoid excessive production of a hepatotoxic metabolite.

Acetaminophen↗
PubMedDate not supplied

Acetaminophen poisoning and the use of intravenous N-acetylcysteine.

Acetaminophen (N-acetyl-p-aminophenol) is the most widely used antipyretic and analgesic in the United States. Acetaminophen, a combination agent in approximately 125 medications, has been deemed safe and effective when used within the recommended dosage. In 1998 and 1999, however, 203,930 cases of acetaminophen overingestion were reported to U.S. poison centers, making it the leading pharmacologic agent associated with toxicity.

Acetaminophen↗
PubMed1998

Aspirin---the novel antiplatelet drug.

Aspirin is a non-steroidal anti-inflammatory drug that has potent antiplatelet actions. Aspirin was initially used as an analgesic and antipyretic drug before its anti-inflammatory properties were discovered. Aspirin also has antithrombotic effects due to the inhibition of cyclo- oxygenase activity in platelets, which reduces the extent of thromboxane A2 formation and consequently the aggregability of platelets. Prophylactic low-dose aspirin therapy reduces the risk of future cardiovascular events in a variety of clinical settings. The maximum effect of aspirin in reducing risks of myocardial infarction is achieved soon after the initiation of therapy. The selective inhibition of platelet thromboxane A2 may be the pharmacological basis for the effectiveness of aspirin in treating pregnancy-induced hypertension. Aspirin can virtually abolish thromboxane A2 production in patients receiving fish oil. Thus, aspirin has been and will be the standard reference compound for long-term oral treatment of platelet hyperactivity, most notably in the secondary prevention of myocardial infarction.

Journal Article↗
PubMed1997

Decision-making in otitis media in children, Part I: epidemiologic data and definitions for a reliable cost-effectiveness analysis.

There is a gap between the medical and economic weight of acute otitis media and the imprecise knowledge and irrational attitude towards diagnosis and treatment. The wide variations among prescribers need to be analyzed. Precise definitions are proposed for acute otitis media and endpoints for outcomes being estimated. An empirical antibiotic treatment gives a greater cure rate than a conservative approach with antipyretic and analgesic drugs. The incremental efficacy expected from more extended-spectrum antibacterials is not clinically significant.

Journal Article↗
PubMedDate not supplied

[Adoerse effects by the administration of salicylates].

Two cases that illustrate one of the side-effects of salicylates are presented. Both cases manifested as non thrombocytopenic purpura. Indications and contraindications for the use of salicylates are described. Emphasis is made not to use them as analgesics or antipyretics in cases with congential or acquired defects in the coagulation mechanism. Other side-effects of salicylates are described.

Blood Coagulation Disorders↗
PubMed1975

[New aspects of inflammation prevention by means of non-steroid antiphlogistics: the effect of Voltaren].

Voltaren, a non-steroid antiinflammatory agent (NSA) of an entirely new chemical structure, is characterized by the high degree of antiinflammatory, antipyretic and analgesic activity it displays in animal experiments. Like other NSAs, the preparation inhibits prostaglandin synthesis, and various findings indicate that the spectrum of pharmacological activity of these agents is at least partly due to this inhibitory effect. Despite this common feature, however, there are quantitative and qualitative differences between Voltaren and other NSAs.

Analgesics↗
PubMed2002

[Nimesulide (Aulin)--the selective COX-2 inhibitor in the treatment of ENT diseases].

Nonsteroidal antiinflammatory drugs (NSAIDs) are widely used in the treatment of controlling inflammatory process and relief of pain in upper airways disorders, due to their inhibition of the cyclooxygenase (COX). After classical NSAIDs different adverse effects are observed, which limit their usage in many patients. The beginning of the nineties gave the evidences, that two cyclooxygenase isoforms existed: COX-1 and COX-2. The blockage of COX-1 in consequence cause the adverse effects of NSAIDs. And COX-2 is responsible for the most inflammatory symptoms, such as pain, oedema, fever, increase of vessel permeability. So the selective inhibitors of COX-2 would be much more safe drugs, comparing with the classical NSAIDs in the treatment of inflammatory diseases. Nimesulide belongs to the new generation of NSAIDs. It not only inhibits more selectively the activity of COX-2, but has also some other properties, that increase its antiinflammatory and analgesic function. Effectiveness of nimesulide has been demonstrated by numerous clinical studies in various inflammatory diseases of upper airways. Its anti-inflammatory, analgesic and antipyretic efficacy has been at least comparable with classical NSAIDs, but the adverse effects of nimesulide have been milder and less frequent. So all those facts suggest, that nimesulide should be taken into account in the treatment of the inflammatory diseases of the ear, nose and throat.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed2003

A general overview of the use of ibuprofen in paediatrics.

Ibuprofen is prescribed for children for the treatment of acute pain and fever, and for juvenile idiopathic arthritis. The pharmacokinetic characteristics of ibuprofen in children are similar to those in adults and the relationship between dose and response is linear over the range 5-10 mg/kg. Clinical trials of ibuprofen have shown the effective dose range to be 7.5-10 mg/kg. The maximum reduction in temperature occurs 3-4 hours after administration. In comparative clinical trials, ibuprofen has been shown to be equally as effective as or more effective than paracetamol as an analgesic and antipyretic and to have a longer duration of action; it is also as effective as aspirin. The adverse effects of ibuprofen are similar to those of other non-steroidal anti-inflammatory drugs but clinical experience suggests that ibuprofen is better tolerated by children than adults and it is safer in overdose than paracetamol and aspirin.

Acute Disease↗
PubMed2003

[New aspects of neuroprotective effects of nonsteroidal anti-inflammatory drugs].

Nonsteroidal anti-inflammatory drugs (NSAIDs) exert anti-inflammatory, analgesic and antipyretic activities and are involved in the suppression of prostaglandin synthesis by inhibiting cyclooxygenase (COX), a prostaglandin synthesizing enzyme. It has been recently revealed that NSAIDs also possess inhibitory effects on the generating system of nitric oxide radicals and modulating effects on transcription factors and nuclear receptors which are related to inflammatory reactions. Since it has been reported that inflammatory processes are associated with the pathophysiology of several neurodegenerative diseases and that NSAIDs inhibit amyloid beta-protein-induced neurotoxicity to reduce the risk for Alzheimer's disease, a number of studies have been conducted focusing on the neuroprotective effects of NSAIDs. It has been clarified that the drugs exert neuroprotective effects, which are not related to their COX-inhibiting property, on pathophysiology of various neurological disorders. In this article, new aspects of neuroprotective effects of NSAIDs have been reviewed, especially, in Alzheimer's disease and Parkinson's disease, discussing various pharmacological effects of NSAIDs other than their inhibitory action on COX.

1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine↗
PubMed1992

[A clinical study of the efficacy and tolerance of nimesulide compared to flurbiprofen and sodium diclofenac in the prevention and treatment of postoperative pain and inflammatory symptoms in dentistry].

The efficacy and tolerability of a new pharmaceutical formulation of a non-steroid anti-inflammatory drug, nimesulide were studied in a double blind study in comparison with flurbiprofen and diclofenac sodium, in 150 patients suffering from postsurgical pain-inflammatory symptoms. The three drugs, administered in a dose of one suppository twice a day for 10 days, showed marked anti-inflammatory, analgesic and antipyretic activity and produced a significant, progressive improvement in the typical symptoms of the inflammatory state. Nimesulide evidenced the greatest speed and duration of therapeutic action. Assessment on the efficacy and tolerability as expressed separately by the physician and the patients were positive in almost all cases of the three treatments.

Adolescent↗
PubMed1992

Effect of a new non-steroidal anti-inflammatory combination of a histamine H2 antagonist and indomethacin on gastroduodenal mucosal membrane in rat.

The new non-steroidal anti-inflammatory drug (NSAID), N-(3-[3-(piperidinyl-methyl) phenoxy] propyl)-carbamoyl-methylthio]ethyl 1-(p-chlorobenzoyl) 5-methoxy-2-methyl-3-indolyl-acetate (CP 331, CAS 127966-70-5), a compound with a structure of an ester combining indomethacin (IM) and a histamine H2 antagonist, has been reported to have anti-inflammatory, analgesic and antipyretic effects. However, the influence of CP-331 on the gastroduodenal mucosa was not fully investigated. Therefore this study was undertaken to investigate the effect of CP-331 on the gastroduodenal mucosa membrane in rats. After single oral drug administration, the UD50 value (50% ulcerogenic dose) of CP-331 calculated from the incidence rate of gastric ulcer was higher than 1000 mg/kg; that for IM was 5.2 mg/kg. Moreover it was examined whether CP-331 had a preventive effect on NSAID-induced gastric damage. The results showed that the co-administration of CP-331 10-30 mg/kg prevented significantly the acute gastric mucosal injury caused by IM administration (20 mg/kg). CP-331 with anti-inflammatory activity does not cause gastric injury, moreover, because of its preventing and therapeutic effects on the damage to gastric mucous membrane induced by IM, CP-331 might be useful in the treatment of gastropathy caused by NSAID in clinic.

Animals↗
PubMed2003

[Paracetamol: therapeutic action, pathogenesis and treatment of acute poisonings complicated by severe liver damage].

The biosynthesis of prostaglandins proceeds in the presence of fatty acid cycloxygenases (COX-1, COX-2). COX-1 is responsible for the synthesis of prostaglandins indispensable for normal homeostasis, while COX-2 regulates local expression of pro-inflammatory prostaglandins. Paracetamol is a selective inhibitor of COX-2 thus having an analgesic and antipyretic potential. The drug is metabolised primarily in the liver. About 5% of the dose transforms into N-acetylo-p-benzoquinoneimine (NAPQI), a highly active compound. Ingestion of a single paracetamol dose higher than 8 g leads to a depletion of hepatic glutathione reserves and a loss of the detoxifying property of the liver. As a result, hepatic necrosis develops. The specific antidote is N-acetylcysteine (NAC). If applied within 10-15 h since the poisoning it enables complete survival. The efficacy of specific treatment decreases after 24 h but blood paracetamol is an indication for NAC therapy. The surviving patients with advanced paracetamol poisoning require long-lasting conservative treatment with ornithine and phospholipids as well as a light diet.

Acetaminophen↗
PubMedDate not supplied

[Modification of liver enzymes in undernourished rats treated with acetaminophen].

Acetaminophen is used as an analgesic and antipyretic. Due to its relative safety at therapeutic dose, it is frequently used in children and in pregnant women. We evaluated the effect of a dose equivalent to the therapeutic dose of Acetaminophen in undernourished rats; 72 Wistar male rats of 18 weeks of age, with weight between 270 and 280 g, were distributed randomly in four groups: A, normal without food restriction; B, normal without food restriction treated with Acetaminophen (100 mg/kg); C; undernourished by food restriction and D, undernourished by food restriction treated with Acetaminophen (100 mg/kg). The results showed decreasing of body and hepatic weight in undernourished rats and in undernourished treated with Acetaminophen, significant decrease of serum albumin concentration (p < 0.001). It was demonstrated that activity of the enzymes alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase significantly decreased (p < 0.001) in the group of undernourished rats treated with Acetaminophen compared with the other groups. We concluded that the Acetaminophen induces hepatic lesions in undernourished rats treated with a single non toxic dose of 100 mg/kg of weight, probably as a consequence of the inherent susceptibility to malnutrition.

Acetaminophen↗
PubMed1992

[Flurbiprofen in oral surgery].

Odontic surgery necessitates the very frequent use of additional auxiliary therapy to improve the post-operative symptoms. In fact the injured tissues respond to such surgical operations generally with an infiltrative-type process which is manifested predominantly by pain, pyrexia, oedema and in the more serious cases with total functional incapacity. The therapy for such symptomatology usually consists of NSAID, steroidal anti-inflammatories and/or chemotherapy. The scope of this research was to verify the possibility of utilising, exclusively, a potent non steroidal antiinflammatory whilst evaluating its therapeutic effects on the pain, the pyrexia and the oedema sustained following odontic surgery. The drug under examination was flurbiprofen, a medication with powerful antiinflammatory, analgesic and antipyretic properties whose mode of action, typical of this type of drug, is principally explained by its inhibition of prostaglandins biosynthesis. Moreover, flurbiprofen has been shown to be a potent inhibitor of platelet aggregation and of the migration of leucocytes. It has other pharmacological mechanisms of action but so far these remain insufficiently well explained. For the above mentioned study, 50 patients who had consented to take part were to undergo odontic surgery near to our clinic. They were subdivided into two groups, each consisting of 25 subjects, and each group was assigned an exclusive therapeutic regimen based on flurbiprofen. Patients in the first group were administered a flurbiprofen dose of 300 mg/day, by mouth, commencing on the day preceding the surgery and then on the next 7 consecutive days.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗