Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Flufenamic Acid”

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 55 records · Page 3Linked to original sources
PubMed1992

Interaction of flufenamic acid on ethanol metabolism in rat.

Flufenamic acid (FA) is a widely used non-steroidal anti-inflammatory drug. It is also known to be an uncoupling agent of oxidative phosphorylation in mitochondria. The interaction of FA and ethanol has been of concern in the occupational health field, since alcohol consumption is a common habit among members of the working population. Thus, we investigated the effects of FA on ethanol metabolism in the rat. In the first experiment, FA and ethanol were administered intragastrically to male Wistar rats. Ethanol and acetaldehyde were measured in blood samples collected from the tail vein by head-space gas chromatography. In the second experiment, the interaction of FA and ethanol was observed in the perfused rat liver. The following items were monitored in perfused livers from both fed and fastd rats: uptake rate of ethanol, production rate of acetaldehyde, level of reduced pyridine nucleotides, and oxygen consumption rate. In the first experiment, the rats with FA showed significantly higher concentrations of both ethanol and acetaldehyde in blood after ethanol intake than the rats without FA. In the perfused liver, FA suppressed ethanol uptake, and increased acetaldehyde concentration in the effluent. FA decreased the level of intracellular reduced pyridine nucleotides which had been elevated by ethanol. FA caused an increase in the oxygen consumption rate, which was not altered by the coexistence of ethanol. It was concluded that FA suppressed ethanol metabolism due to suppression of acetaldehyde oxidation in the liver, despite its uncoupling effect on oxidative phosphorylation in mitochondria.

Acetaldehyde↗
PubMed1981

Flufenamic acid and placebo compared in rheumatoid arthritis and osteoarthritis.

Forty patients in general practice with rheumatoid arthritis or osteoarthritis were identified as suffering from moderate pain and tenderness and moderate stiffness in excess of 30 minutes. After discontinuation of non-steroidal anti-inflammatory drugs for 2 weeks, a crossover study was conducted comparing the benefits of flufenamic acid, 100 mg, four times daily with placebo. At the same time, paracetamol at a dose up to 8 x 500 mg daily, could be used for pain which the patient judged to be unrelieved. Thirty-four patients completed the two 3-week test periods and twenty-one patients were improved in relation to morning stiffness and pain by flufenamic acid and twelve patients by placebo--a difference greater than would have occurred by chance (p = 0.05). At the same time, paracetamol consumption was reduced significantly fron a mean of 91.29 tablets to 60.68 tablets for each 3-week period. Side-effects occurred in ten patients on placebo and fifteen patients on flufenamic acid. One patient on each medication had to discontinue for multiple side-effects. Diarrhoea occurred in two patients on flufenamic acid and in one patient on placebo. Flufenamic acid is clearly effective and side-effects do not occur more often than would be expected by chance when compared with placebo.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1988

Action of the nonsteroidal anti-inflammatory agent, flufenamic acid, on calcium movements in isolated mitochondria.

The anti-inflammatory agent flufenamic acid was found to inhibit calcium uptake in isolated mitochondria at low concentrations (IC50 = 7.2 microM). Similar concentrations were required to promote the release of calcium from mitochondria preloaded with the cation (EC50 = 3.5 microM). Identical actions were found with diflunisal, mefenanamic acid and 2,4-dinitrophenol. It was concluded that flufenamic acid was affecting calcium movements across the mitochondrial membrane by virtue of its ability to uncouple oxidative phosphorylation.

2,4-Dinitrophenol↗
PubMed1986

[Detection of cutaneously administered flufenamic acid in the inner space of the knee joint].

Ten patients who were scheduled for surgery due to an internal damage of the knee joint, were treated 2 days before operation 3 times daily with an ointment containing flufenamic acid (Mobilisin spezial). At the time of operation, plasma and synovial fluid, tissue samples from the synovial membrane, Hoffa's fat pad and-- as far as possible--meniscus and articular cartilage were taken. Until 72 h after the operation, urine samples were collected. The flufenamic acid level was determined by means of high pressure liquid chromatography associated with fluorometric detection. Flufenamic acid was detected in all tissues of the knee joint and in the synovial fluid. The highest concentration of flufenamic acid was found in the synovial membrane.

Administration, Topical↗
PubMed1991

Demonstration of flufenamic acid in histological sections.

A simple method is described to show the transdermal penetration of flufenamic acid (CAS 530-78-9) into the skin of laboratory animals. After topical application of gels and creams containing flufenamic acid the substance exerts a fluorescent painting in corium and subcutis of histological slides. This effect needs the chemical reaction between the test substance and sulphuric acid in synthetic resin sections.

Animals↗
PubMed1998

In vitro investigations of drug release and penetration--enhancing effect of ultrasound on transmembrane transport of flufenamic acid.

Percutaneous absorption studies are performed in various in vitro models to determine the rate of drug absorption via the skin. We designed an phonophoretic drug delivery system to investigate the influence of ultrasound on transmembrane transport of different drugs. Phonophoresis is defined as the migration of drug molecules, contained in a contact agent, through the skin under the influence of ultrasound. We investigated the absorption of flufenamic acid in a buffer medium in dependence of ultrasound energy and application time. For evaluating membrane penetration of flufenamic acid, the concentration range of buffer solution was measured. Flufenamic acid was determined by using a fluorimetric method. Ultrasound energy was supplied for between 5 and 30 min at a range of intensities (0; 0.3; 0.6; 0.9; 1.2; 1.5 W/cm2). energy levels commonly used for therapeutic purpose. The pronounced effect of ultrasound on the transmembrane absorption of the drug was observed at all ultrasound energy level studied. The time of application was found to play an important role in delivery and transport of drug. Dependent on time, we observed an arise of temperature up to 4.5 degrees. It appears that there was no difference between an intensity of 0.3 and 1.5 W/cm2 and the measured drug concentrations in solution. The highest penetration was observed at an intensity of 1.0 W/cm2 after 30 min. These results were not significantly different from concentration in measurements after 30 min and 0.5 and 1.5 W/cm2. It seems that the arise of drug concentration is caused by effects of temperature and by variation of membrane delivery in dependence of temperature.

Biological Transport↗
PubMed1990

Penetration and enrichment of flufenamic acid in calf skin from patients with stasis dermatitis.

To investigate the hypothesis that the application of medicaments to skin from the lower leg of patients with stasis dermatitis might lead to their enhanced enrichment, compared with uninvolved skin from the same region, a penetration study was performed with flufenamic acid. In 5 patients with pronounced changes of chronic venous insufficiency and in 5 control patients without chronic venous insufficiency the flufenamic acid content in skin sections parallel to the surface was determined by HPLC. In chronic venous insufficiency-skin, the flufenamic acid concentration was higher in all skin levels compared to control skin. This enrichment of the substance could lead to a prolonged and more intense contact with antigen-presenting cells in this region, thus promoting the development of contact allergies observed so frequently in this pathologic condition.

Adult↗
PubMed1996

High-performance liquid chromatography of flufenamic acid in rat plasma.

A simple high-performance liquid chromatographic (HPLC) method for the determination of flufenamic acid in rat plasma is described. After liquid-liquid extraction, the drug is separated by HPLC on a 5-microns octadecylsilica column (Nucleosil C18) with ultraviolet detection at 280 nm. Linear calibration graphs for flufenamic acid were constructed from 0.5 to 15 micrograms/ml. The method has been applied to a pharmacokinetic study in animals.

Animals↗
PubMed1998

In vitro investigations of drug release and penetration--enhancing effect of ultrasound on transmembrane transport of flufenamic acid.

Although topical drugs are usually applied at a convenient site, the target for the drug interaction may be systemic. Phonophoresis is the use of ultrasound to enhance the delivery of topical applied drugs. The purposes of our study were to investigate the in vitro penetration and the in vivo transport of flufenamic acid in dependence of ultrasound. Percutaneous absorption studies are performed in various in vitro models to determine the rate of drug absorption via the skin. We designed a phonophoretic drug delivery system to investigate the influence of ultrasound on transmembrane transport of different drugs. We investigated the absorption of flufenamic acid in a buffer medium in dependence of ultrasound energy and application time. For evaluating membrane penetration of flufenamic acid, the concentration range of buffer solution was measured. Ultrasound energy was supplied for between 5 and 30 min at a range of intensities up to 1.5 W/cm2, energy levels commonly used for therapeutic purpose. The pronounced effect of ultrasound on the transmembrane absorption of the drug was observed at all ultrasound energy levels studied. The time of application was found to play an important role in delivery and transport of drug. Dependent on time, we observed a rise of temperature up to 4.5 degrees C. It appears that there was no difference between an intensity of 0.3 and 1.5 W/cm2 and the measured drug concentrations in solution. The highest penetration was observed at an intensity of 1.0 W/cm2 after 30 min. These results were not significantly different from concentration measurements after 30 min and 0.5 and 1.5 W/cm2. It seems that the arise of drug concentration is caused by effects of temperature and by variation of membrane delivery in dependence of temperature. Using this in vitro model we note it is possible to compare the transdermal penetration and absorption of commercial flufenamic ointment in volunteers.

Administration, Topical↗
PubMed1990

Flufenamic acid, mefenamic acid and niflumic acid inhibit single nonselective cation channels in the rat exocrine pancreas.

The non-steroidal anti-inflammatory drugs, flufenamic acid, mefenamic acid and niflumic acid, block Ca2(+)-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells. Half-maximal inhibition was about 10 microM for flufenamic acid and mefenamic acid, whereas niflumic acid was less potent (IC50 about 50 microM). Indomethacin, aspirin, diltiazem and ibuprofen (100 microM) had not effect. It is concluded that the inhibitory effect of flufenamate, mefenamate and niflumate is dependent on the specific structure, consisting of two phenyl rings linked by an amino bridge.

Animals↗
PubMed1978

Flufenamic acid in treatment of primary spasmodic dysmenorrhoea. A double-blind crossover study.

A double-blind cross-over trial of flufenamic acid three times a day (200 mg) was carried out in forty-four patients with primary dysmenorrhoea. While on flufenamic for 3 months 82% of patients experienced significant pain relief. Associated gastrointestinal symptoms, i.e--vomiting and diarrhoea--were relieved in 66% and 52% patients respectively while on flufenamic acid. It is concluded that the fenamates are useful and safe drugs in the treatment of primary dysmenorrhoea.

Adolescent↗
PubMed1983

Effects of aspirin, indomethacin, flufenamic acid and paracetamol on prostaglandin output from rat stomach and renal papilla in-vitro and ex-vivo.

The effects of aspirin, indomethacin, flufenamic acid and paracetamol on prostaglandin (PG) biosynthesis were studied in whole cell preparations of rat renal papilla and stomach in-vitro and ex-vivo. In the ex-vivo experiments a low dose aspirin was a potent inhibitor of PGE output from the stomach but not the renal papilla, while in-vitro renal PGE output was inhibited by aspirin to a greater extent than gastric PGE. Indomethacin and flufenamic acid inhibited both renal papillary and gastric PGE outputs in-vitro and ex-vivo. Paracetamol enhanced PGE output from the stomach more than twice ex-vivo, and to a lesser extent in-vitro. It also augmented PGE output from the papilla ex-vivo but not in-vitro. In view of the possible contribution of cellular organization and pharmacokinetic processes to the ultimate effect, it is suggested that studies on the effects of anti-inflammatory and antipyretic agents on PG biosynthesis should not be restricted to fully in-vitro systems.

Acetaminophen↗
PubMed1990

A comparative study of naproxen gel and flufenamic acid gel in the treatment of soft tissue injuries.

One hundred patients were enrolled in a single-blind, randomized, parallel group study to compare naproxen gel (10%) with flufenamic acid gel (3%) for the treatment of soft tissue injuries. Demographic variables, the distribution of diagnoses (tendinitis, bursitis/synovitis, synovitis, periarthritis, epicondylitis) and initial severity of the complaint were similar between the two groups. The gels were applied 2 to 6 times per day, as required, and conventional clinical indices were evaluated at Day 1 (on entry to the study), Day 3 and Day 7. Global assessments of efficacy were made by both physicians and patients at the end of the study. By Day 7 both treatments had produced a highly significant improvement in symptoms (p less than 0.001). The patients using naproxen gel, however, improved more rapidly. At Day 3 the number of patients rating 'swelling', 'tenderness to firm palpation' or 'limitation of use' as 'severe' or 'moderate' was significantly less (p less than 0.05) than for patients using flufenamic acid gel. At the end of the study the physician's global efficacy rating showed no significant differences between the two gels; patients, in contrast, showed a significant preference for naproxen gel (p less than 0.05). Both gels were well tolerated. The more rapid onset of effect and patient preference for naproxen gel may be important factors in the choice of medication.

Adolescent↗
PubMed1978

Effects of flufenamic acid, dexamethasone, and SP 54 (a pentosanpolysulphate) on the histological appearance of murine embryonic tibia explants cultured in vitro.

The histological investigation of cultured, embryonic tibia explants of NMRI-mice showed, after a six day period, that incubation concentrations of Flufenamic acid, SP54 (a Pentosanopolysulphate), and Dexamethasone (9alpha-Fluor-16-beta-Methyl-Prednisolone) predominantly induced resorptive and degenerative processes, in different degrees, affecting cartilage and bone matrix. In the experiments with Flufenamic acid and Dexamethasone, the degenerative processes were found to be accompanied by the inhibition of the synthesis of cartilage matrix. The investigations with SP54, on the other hand, showed a medium increase of cartilage matrix.

Animals↗
PubMed2004

Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin.

It is becoming increasingly well established that nonsteroidal anti-inflammatory drugs (NSAID) protect against tumors of the gastrointestinal tract and that they may also protect against a variety of other tumors. These activities have been widely attributed to the inhibition of cylooxygenases (COX) and, in particular, COX-2. However, several observations have indicated that other targets may be involved. Besides targeting COX, certain NSAID also inhibit enzymes belonging to the aldo-keto reductase (AKR) family, including AKR1C3. We have demonstrated previously that overexpression of AKR1C3 acts to suppress cell differentiation and promote proliferation in myeloid cells. However, this enzyme has a broad tissue distribution and therefore represents a novel candidate for the target of the COX-independent antineoplastic actions of NSAID. Here we report on the X-ray crystal structures of AKR1C3 complexed with the NSAID indomethacin (1.8 A resolution) or flufenamic acid (1.7 A resolution). One molecule of indomethacin is bound in the active site, whereas flufenamic acid binds to both the active site and the beta-hairpin loop, at the opposite end of the central beta-barrel. Two other crystal structures (1.20 and 2.1 A resolution) show acetate bound in the active site occupying the proposed oxyanion hole. The data underline AKR1C3 as a COX-independent target for NSAID and will provide a structural basis for the future development of new cancer therapies with reduced COX-dependent side effects.

Amino Acid Sequence↗
PubMed1975

The effects of HCG, indomethacin, flufenamic acid and aspirin in the immature female rat.

Immature female rats (21 to 23 days old, 35 to 45 g) were injected subcutaneously with 2-5 i. u. HCG 18 hr before autopsy. Ovaries and uteri were removed; wet weight, dry weight and uterine protein content were determined. Ovarian and uterine weights, ovarian blood volume and uterine protein content were increased after HCG treatment. When immature female rats were pretreated with indomethacin, flufenamic acid or aspirin, the ovarian effects of HCG were inhibited: only slight increases in ovarian weight and blood volume were observed. Indomethacin attenuated the increases in uterine weight, and protein content, but neither flufenamic acid nor aspirin were effective in inhibiting these responses. The possible role of prostaglandins and of oestrogen as mediators of these responses is discussed.

Animals↗
PubMed1983

The bioavailability of flufenamic acid and its dissolution rate from capsules.

The bioavailabilities of five commercially available flufenamic acid (FA) capsules were studied in humans and beagle dogs. The dissolution rates of these capsules were determined by several methods. Experiments on in vitro/in vivo and humans/dogs correlations were performed to evaluate the dissolution test methods and the values of beagle dogs as models for predicting bioavailability of weak acid drugs in humans. Significant differences in the rates and extents of bioavailability of the different capsules were observed both in humans and dogs, but results in humans differed from those in dogs. The dissolution rates, determined by dissolution methods involving pretreatment with acidic solutions, correlated significantly with bioavailabilities in humans and dogs; however, those obtained by the rotating basket and paddle methods without any surface active agents did not correlate with in vivo data.

Adult↗