Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Pyrazolones”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 577 records · Page 32Linked to original sources
PubMedDate not supplied

Hepatic toxicity of nonsteroidal anti-inflammatory drugs.

The hepatic toxicity associated with the use of nonsteroidal anti-inflammatory drugs (NSAIDs) is reviewed. NSAIDs include agents in more than 10 classes of compounds, many of which are capable of producing hepatic injury. When NSAIDs are used to treat rheumatic disease, the hepatic effects of the disease itself may complicate the diagnosis of NSAID-induced hepatic injury. Hepatotoxicity caused by drugs may be either intrinsic or idiosyncratic in nature and may be manifested by hepatocellular injury, cholestasis, or a combination of both types of injury. Intrinsic hepatotoxins, such as salicylates, produce injury in a large percentage of exposed individuals that is often dose related and occurs after a short, fixed latent period. Idiosyncratic injury, such as that caused by sulindac, occurs in unusually susceptible persons, usually after a variable latent period. Injury is not dose related. In most cases of hepatocellular injury, the prognosis of those patients who survive the acute phase of injury is good. Fatalities rarely result from cholestatic injury. Monitoring of serum hepatic-enzyme concentrations is recommended for patients receiving NSAIDs from the indole, pyrazolone, and propionic acid classes since these agents have been associated with the greatest incidence of adverse hepatic reactions. Enzyme monitoring is advisable for high-risk individuals receiving NSAIDs from other classes. Enhance vigilance on the part of clinicians, patients, and pharmaceutical manufacturers is needed to reduce the incidence of hepatotoxicity associated with the use of NSAIDs.

Anti-Inflammatory Agents↗
PubMed1983

[Analgetic drug intolerance].

Reactions as intolerance to aspirin and food additives were diagnosed in 41 cases during November 1979 -- March 1982. Allergy to pyrazolone-drugs were observed in 20 cases during the same period. 24% of the patients with intolerance to aspirin had also an intolerance to tartrazine. There were no familial occurrence of aspirin intolerance. Four patients had mainly asthma, 37 patients urticaria. New aspects of the pathogenesis of aspirin intolerance -- modulation of arachidonate metabolism and complement activation -- are discussed.

Analgesics↗
PubMed1983

[Drug-induced Quincke's edema of the mouth mucosa - an analysis of 33 cases].

Since literature only provides us with scarce information about occurrence and etiologic conditions of oro-pharyngeal Quincke's edema, we performed a retrospective evaluation of the medical records of 4,766 in-patients between the years 1970 and 1980 with registered drug-induced cutaneous and/or mucosal side effects. Among these cases there were 187 patients (= 3.92%) showing oral side effects, 33 of them with the diagnosis of Quincke's edema on the labial, oral or pharyngeal mucosa. 30 cases revealed clinical and/or historic data about concomitant occurrence of edematous lesions also in other body sites. With all patients drug intolerance was suspected by history, yet drug testings could only prove this assumption in 24 cases. Salicylates, analgetic compounds, barbiturate, pyrazolone, and penicillin are the main etiologic factors for oral Quincke's edema.

Adult↗
PubMedDate not supplied

[Interactions of oral anti-diabetic agents and non-steroid anti-rheumatic agents].

Due to the relative increase of age-diabetes and to the different forms of rheumatic diseases, long-term medicament therapy and the question of possible interactions between oral antidiabetic drugs ( OAD ) and nonsteroidal anti-inflammatory drugs (NSAID) become more important. Unfortunately there exist studies on most of the well-known NSAID, but carried out on different conditions. The present study is intended to summarize the results at hand and to evaluate them in a certain sense. From almost all the NSAID, except from the salicylates and those connected with, as well as the pyrazolones, one may say, based on published data and long-term experience, that interactions with the OAD in use nowadays are not to be expected unless without clinical relevance.

Administration, Oral↗
PubMed1982

[Non-steroidal antirheumatics: side-effects and interactions].

Side effects of non-steroidal antirheumatic drugs (NSAD) may occur in any organ system, since the prostaglandins, the synthesis of which is inhibited by NSAD, play a role in numerous adverse cellular processes throughout the body. Besides these physiologic regulations there are adverse effects of NSAD, such as bone marrow aplasia, of unexplained etiology. The interactions of NSAD are of clinical relevance in drug types such as the salicylates, pyrazolons and fenamic acids (e.g. interactions with cumarin derivatives). The clinically relevant interactions of NSAD are discussed in detail.

Anemia, Aplastic↗
PubMed1982

Phenylbutazone and sulfinpyrazone interaction with oral anticoagulant phenprocoumon.

To compare the marked hypoprothrombinemic augmentation in man of racemic warfarin sodium by the pyrazolons phenylbutazone and sulfinpyrazone with that of the coumarin anticoagulant phenprocoumon, these interactions were studied prospectively in six normal subjects. Large single doses of racemic phenprocoumon, 0.6 mg/kg orally, were administered with and without daily phenylbutazone, 300 mg, or sulfinpyrazone, 400 mg, beginning three days before phenprocoumon and continuing for 14 days. Daily blood samples were drawn for phenprocoumon content and one-stage prothrombin time. Phenylbutazone markedly increased both the phenprocoumon concentrations and prothrombin times, whereas sulfinpyrazone did not.

4-Hydroxycoumarins↗
PubMed1982

A study of package inserts of potentially toxic drugs.

Information contained in the package inserts of drugs chosen as potential causes of blood dyscrasia, renal toxicity, hepatotoxicity, and cardiac toxicity has been studied. Chloramphenicol and pyrazolones were chosen as representatives of drugs that could produce blood dyscrasia, aminoglycosides and cephaloridine as potential nephrotoxic agents, isoniazid and monoamine oxidase inhibitors as possible hepatotoxic drugs, and tricyclic antidepressants and digitalis as drugs of recognized cardiac toxicity. Adverse effects were clearly described in only 27.8% of the package inserts, whereas 40.3% did not mention them, and 15.7% specifically stated that the product was devoid of adverse effects. Information about the type of toxicity that led to the selection of drugs included in this study was uncommon in most cases.

Drug Labeling↗
PubMed1981

Bentonite-induced rat paw oedema as a tool for simultaneous testing of prophylactic and therapeutic effects of anti-inflammatory and other drugs.

The possibility of screening simultaneously the prophylactic and therapeutic effects of a single dose of anti-inflammatory drugs was further tested. Bentonite oedema was induced in the left paw (0.05 ml of 5% bentonite gel subcutaneously). After the measurement of its size in the 23rd h, the rats were given the test drugs (i.m. or p.o.) and 1 h thereafter, bentonite oedema was induced in the right paw. Some of the drugs suppressed the oedema both prophylactically and therapeutically (steroidal and some nonsteroidal anti-inflammatory drugs, sodium aurothiomalate etc.), some others suppressed it only prophylactically (some derivatives of pyrazolone etc.) and some of the remaining drugs tested had no effect at all on the oedema after a single administration. Advantages and limitations of this method are discussed.

Animals↗
PubMed1981

[Pseudo-(venocuran-)lupus--a minor episode in the history of medicine].

Pseudolupus is a syndrome characterized by recurrent fever arthralgia, myalgia, involvement of lung and heart, high sedimentation rate, leukocytosis and lymphopenia. The diagnosis is established by the presence of circulating antimitochondrial antibodies. In 1975 it was found that the disease was due to prolonged treatment with Venocuran, a drug against venous disorders composed of phenopyrazone (pyrazolone derivative), horse-chestnut extract, and Miroton (glycosides extracted from white squill [Urginea maritima], convallaria, oleander and adonis). The drug was then withdrawn. No new cases have come to our attention since then. 15 patients with severe pseudolupus known to us in 1975 have now been followed up. In 6 of the patients all symptoms disappeared within weeks or a few months after withdrawal of the drug. However, the other 9 patients had at least 1 and often 2--3 relapses in the following months to years. In some patients, symptoms remained as long as 4--5 years. Antimitochondrial antibodies persisted in 4 patients for more than 3 years and in 1 patient are still detectable now. The pathomechanism of pseudolupus has not been elucidated.

Autoantibodies↗
PubMed1995

Dipyrone and diclofenac do not influence creatinine-clearance, inulin-clearance or PAH-clearance in healthy male volunteers.

The effects of the non-steroidal anti-inflammatory drug diclofenac and the pyrazolone derivative dipyrone on renal function were compared with those of placebo in 12 healthy male volunteers in a randomized, controlled, triple-crossover study with a wash-out period of 4 days between each of the 3 trial periods (dipyrone, diclofenac and placebo) which lasted three days each. The volunteers received dipyrone (1 g, 3 times/day for 2 days, followed by twice 1 g on the main trial day, which was day 3 of each study period) or diclofenac (50 mg, 3 times/day for 2 days, followed by twice 50 mg on the main trial day) or placebo orally. Standardized meals (50 mEq sodium per day) were given from one week before the start until the end of the study and on the main trial days a protein-rich lunch (2 g protein/kg body weight) was taken. Renal function was assessed in each study period by measurement of creatinine-clearance, inulin-clearance and p-aminohippurate (PAH)-clearance to characterize glomerular filtration rate and renal plasma flow. High protein intake induced glomerular hyperfiltration (increased creatinine-clearance, inulin-clearance and PAH-clearance) in all 3 study periods (dipyrone, diclofenac, placebo). Dipyrone and diclofenac had no effect on renal clearance of creatinine, inulin or PAH in comparison to placebo. These results show that dipyrone and diclofenac at therapeutic dosages over 3 days do not decrease glomerular filtration and renal plasma flow in healthy individuals. Furthermore, it is unlikely that prostaglandins play a major role in protein-induced glomerular hyperfiltration.

Administration, Oral↗
PubMed1995

[Common health disorders: self-care and self-medication].

SETTING: Community level. "Santa María de Benquerencia" Health District, Toledo. PARTICIPANTS: People over 15, chosen by random sampling from the municipal census, who stated that they had suffered some health disorder over the previous fortnight. MEASUREMENTS AND MAIN RESULTS: 212 surveys were accepted as valid (average age 42.75, 51.89% male and 48.11% female). 73% had suffered one of the disorders included in the survey during the previous fortnight. The commonest response was self-medication (39.84%), especially when dealing with pain and Pyrosis. Pyrazolones and Salicylates were the most commonly used drugs. The instructions were only read in 48.64% of cases. No measure was adopted in 34.56% of the disorders. The doctor was only consulted in 6.86% of cases. Both these responses were more common in men and young people. Non-pharmacological self-care was adopted in 30.07% of cases. This was generally of a dietetic or physical nature and was commoner in women and elderly people. CONCLUSIONS: Self-care, whether pharmacological or not, is the most common response to the perception of some symptom. These practices (especially self-medication because of its possible attendant problems) should be directed and used as one tool more in health care.

Adult↗
PubMedDate not supplied

Effect of antirheumatic drugs on cathepsin B1 from bovine spleen.

The inhibitory effect on cathepsin B1 of 39 antirheumatic and other agents has been studied. The enzyme was purified from bovine spleen (specific activity 2.8 units/ml/E280 unit) and the effect of the drugs measured by determining the decrease of enzyme activity towards BANA as substrate. Analgesics, antimalarials, cytostatic agents, steroids as well as d-penicillamine, colchicine, allopurinol, chlorzoxazone and chlorpromazine either had no effect on cathepsin B1 or inhibited it to a very small extent. Typical anti-inflammatory and antirheumatic agents like gold and pyrazolone derivatives (with the exception of sulfinpyrazone) suppressed the activity of the enzyme at a concentration of 10(-6) M. Two others, indomethacin and diclofenac, suppressed it at a concentration of 10(-5) M. Two sulfonated polysaccharides, arteparon and pentosan polysulfate (SP54), were also potent inhibitors. Salicylates, however, inhibited cathepsin B1 only at much higher concentrations (10(-2) M. Higher concentrations of cysteine (2 mM) decreased the inhibitory effect of some otherwise effective drugs. Inhibition of cathepsin B1 may be one way in which some of the drugs tested exercise their therapeutic effect in rheumatic diseases.

Animals↗
PubMedDate not supplied

Sensitivity to aspirin: a new serological diagnostic method.

Certain adverse reactions to aspirin (ASA), nonsteroidal anti-inflammatory drugs (NSAIDs) and pyrazolone derivatives resemble IgE-mediated hypersensitivity. However, convincing evidence of antigen-antibody interactions or inhibition of the cyclooxygenase pathway of arachidonic acid metabolism, stimulating the production of leukotrienes (LTs) and decreasing the production of prostaglandins (PGs), has not been presented. In this study, two types of specific IgE antibodies have been found in six serum samples from eight ASA-sensitive patients with salicyloyl and O-methylsalicyloyl disks using the Radio Allergo Sorbent Test (RAST), whereas no positive result could be found with acetylsalicyloyl disks. Further investigation on the specificity of these IgE antibodies and the chemical structure of their epitopes were performed by cross-inhibition studies. The results are in favor of an IgE-dependent mechanism involved in ASA sensitivity, and suggest that determination of specific IgE antibodies would be a safe diagnostic method for ASA sensitivity in vitro.

Adult↗
PubMedDate not supplied

[Aminopyrazolone free radicals in the hydrogen peroxide oxidation reaction].

Oxidation of amidopyrine, analgin and 4-aminoantipyrine by means of H2O2 was studied in presence of peroxidase and hemoglobin. As shown by NMR, EPR and spectrophotometry the oxidation was of single electron type accompanied by free radical formation. The radicals of amidopyrine and analgin were stable, colored, participated in chemical exchange with initial molecules and disproportionated as demonstrated by stoichiometry. Radicals of 4-aminoantipyrine were unstable and dimerized to antipyrine red. Aminopyrazolone radicals were also formed after direct oxidation by Fe3+ in acidified water containing no complexes. The Fe-complexes developed shifted the equilibrium towards reduction of radicals with formation of the initial molecules. Presence of 4-amino groups was responsible for oxidation of pyrazolones under mild conditions. Alkyl derivatives of 4-amino group protons stabilized the radicals and altered their subsequent transformation form dimerization to disproportionation. Proton catalysis of aminopyrazolone oxidation occurred.

Ampyrone↗
PubMed1993

[Hemorrhages of the upper gastrointestinal tract and nonsteroidal anti-inflammatory drugs: the results of a case-controlled surveillance].

A postmarketing surveillance case-control study was set up and applied in an Italian Hospital network to quantify the risk of upper gastrointestinal bleeding (UGB) and exposure to non steroidal anti-inflammatory drugs (NSAIDs). During the period of study 441 cases of UGB and 1323 controls were recruited. The odds ratios (OR) associated with NSAIDs use were estimated for intake occurring over two different periods of time prior to hospital admission (i.e. during the preceding week and month). A strong association emerged for aspirin intake, both in the week (ORMLR = 11.2; 95% CI 7.8-16.9) and in the month (ORMLR = 6.9; 95% CI 4.6-10.2) preceding hospital admission. [MLR = Multiple logistic regression; CI = Confidence interval]. A significant increase in the risk of UGB and use of diclofenac, phenylpropionic acid derivatives, and indomethacin was also found in the two exposure periods considered, while for piroxicam a significant association was only apparent in the analysis of 1-month exposure. As expected, paracetamol and pyrazolone derivatives were not associated with UGB. This pilot experience has shown the feasibility of setting up a multicenter post-marketing surveillance programme and of establishing a network for drug monitoring within the Italian National Health Service, capable of providing a thorough evaluation of the benefit/risk profile of drugs.

Adult↗
PubMedDate not supplied

[Treatment of experimental herpesvirus infection with nonsteroidal anti-inflammatory agents].

The therapeutic effect of nonsteroid antiinflammatory drugs (pyrazolone and salicylate derivatives) and their combinations with acyclovir was assessed in experimental herpesvirus infection in cell culture and in mice. A combination of 4-iodoantipyrine and acyclovir protected mice from herpesvirus encephalitis. This effect was associated with a decrease of the level of the virus in mouse brain and an increase of the titers of serum interferon and virus neutralizing antibodies.

Acyclovir↗
PubMed1996

Aminoazoles in heterocyclic synthesis. Synthesis of some new pyrimidobenzimidazoles and pyrazolonopyridines as well as triazolo-, tetrazolo- and pyrazolo-pyrimidines of pharmaceutical interest.

The reactivity of 3-cinnamoylindole, 3-cinnamoylantipyrine and 1-(3-methyl-1-phenyl-5-pyrazolon-4 yl)-4-antipyrin-4-yl)-prop-2-ene-1- one(la-c) towards 2-aminobenzimidazole, 3-amino-1,2,4-triazole, 5-aminotetrazole monohydrate, 5-amino-3-phenylpyrazole and 3-amino-1-phenyl-2-pyrazolin-5-one to give the fused heterocycles 2a-c, 4a,b, 5a,b, 8a,b, and 10a-c has been investigated. Structures of the synthesized compounds were confirmed by both the analytical and the spectral data (IR, UV and 1H NMR).

Anti-Bacterial Agents↗
PubMedDate not supplied

[Recall of metamizole from the market in countries with modern pharmacotherapy].

Metamizole sodium (noraminophenazon sodium) is a pyrazolone derivate with analgesic, antipyretic and antiinflammatory activity, introduced in therapy in 1921. Since then, it was widely used all over the world, even in the counter preparations. In seventies its use was connected with severe, sometimes fatal side effects (agranulocytosis), resulting in gradual withdrawal of the drug. Metamizol has been withdrawn from the market in many developed countries, its use severely restricted in some of them, or permitted only in parenteral preparations for strictly defined indications (exceptionally severe pain such as posttraumatic, postoperative, abdominal colics and high body temperature unresponsive to the other antipyretics. In contrast to that, preparations containing metamizole are still in use in many countries, in some even as over the counter drugs.

Anti-Inflammatory Agents, Non-Steroidal↗