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At least 19 recordsLinked to original sources
PubMed1983

[Anti-glafenine circulating antibodies: demonstration and frequency in acute renal insufficiency following intake of glafenine in toxic doses].

From 1970 to 1981, acute glafenineeeeeeee poisoning was observed in 106 patients, including 37 with acute renal insufficiency (ARI). From 1977 to 1982, the search for anti-glafenin antibodies was carried out systematically by direct and indirect tests for antiglobulin on erythrocytes, and by leucoagglutination and complement fixation tests on platelets in the presence of glafenin. An antibody was detected in only one of the 17 ARI patients studied. This antibody, IgM, has been studied along with glafenin, floctafenin, antrafenin and their metabolites. The rareness of such an antibody confirms the direct nephrotoxic action of glafenin, a drug responsible for half of the renal insufficiencies observed in an intensive care unit specialized in toxicology.

Acute Kidney Injury↗
PubMed1993

Diclofenac potassium in the management of dental pain: a multicenter double-blind comparison with glafenine.

The analgesic efficacy and tolerability of diclofenac-potassium 50 mg were compared with those of glafenine 200 mg in 109 outpatients suffering from moderate to severe dental pain. Throughout the four-day trial period, patients (Diclofenac-potassium: n = 58, mean age = 32.84 +/- 12.0 yrs. Glafenine n = 51, mean age = 34.12 +/- 14.0 yrs.) were randomised, in a double-blind fashion, to receive one tablet of either medications three times daily, together with an antibiotic, ampicillin, 500 mg, 8 hourly. Half an hour following the administration of the first analgesic dose, both treatment groups showed highly statistically significant (P < 0.001) reductions in the mean pain level when compared with their baseline values. The mean decrease of pain level in diclofenac-potassium group after 1/2 hour was significantly (P < 0.01) greater than that in the glafenine group. Moreover, the percent of pain free patients after 1/2 hour in the diclofenac-potassium group was significantly higher (P = 0.05) compared with those in the glafenine group. The mean decreases in pain and tenderness on the second and fourth days, in relation to their initial values, were greater in the diclofenac-potassium treated patients than the glafenine treated ones. The overall evaluation of therapeutic effect was considered excellent in 72% of the diclofenac- potassium patients compared with 57% of the glafenine patients. Furthermore, 95% of the diclofenac-potassium patients, compared with 90% of the glafenine ones, expressed their willingness to use the trial medication again in similar conditions. None of the patients in both treatment groups discontinued the trial due to unwanted effects. Both therapies were well tolerated. Only one patient (1.72%) in the diclofenac-potassium treatment group experienced slight diarrhoea. It can be concluded from this study that both medications are effective and well tolerated in the management of dental pain. However, diclofenac-potassium with its fast onset of effect is particularly suitable in the management of acute painful conditions.

Adolescent↗
PubMed2003

Impact of glafenine hydrochloride on human endothelial cells and human vascular smooth muscle cells: a substance reducing proliferation, migration and extracellular matrix synthesis.

The aim of this study was to examine the effects of glafenine hydrochloride (a nonsteroidal anti-inflammatory drug) on proliferation, clonogenic activity, cell-cycle, migration, and the extracellular matrix protein tenascin of human aortic smooth muscle cells (haSMCs) and human endothelial cells (ECs) in vitro.HaSMCs and ECs were seeded in tissue culture flasks. The cells were treated for 4 days with glafenine hydrochloride (10 microM, 50 microM, 100 microM). Half of the treated groups were incubated again with glafenine hydrochloride, the other half received medium free of glafenine hydrochloride every 4 days until day 20. The growth kinetics and clonogenic activity were assessed. Cell cycle distribution was investigated by FACS, migratory ability was evaluated, and effects on extracellular matrix synthesis were assessed by immunofluorescence. Glafenine hydrochloride inhibited the proliferation and clonogenic activity of haSMCs and ECs in a dose-dependent manner. A block in the G2/M phase and a reduction in the G1 phase occurred. The migratory ability of haSMCs was impaired in a dose-dependent manner and the extracellular matrix protein tenascin was reduced. As glafenine hydrochloride has the ability to fully inhibit proliferation and to partially inhibit migration in haSMCs, it could be an interesting substance for further research in the field of restenosis therapy.

Actins↗
PubMedDate not supplied

[Shock caused by glafenine. Apropos of 7 complications].

Glafenine-induced shock. Seven cases. Glafenine is a widely prescribed analgesic drug, and shock is one of its severe side-effects. We report six documented and one highly probable cases of such accidents. From these seven cases and a review of the literature, we have extracted the clinical characteristics of glafenine-induced shock. Shock usually occurs about 30 minutes on average after taking one single tablet. Previous use of the drug is found in more than 50 per cent of the patients, and it was often followed by a neglected side-effect. A series of cutaneous and respiratory manifestations precedes or accompanies the shock. Two physiopathological mechanisms of glafenine-induced shock have been postulated: either anaphylaxis or idiosyncratic reaction involving the prostaglandins. In vitro tests give highly variable results and therefore are of limited value. Glafenine-induced shock is rare; its incidence, probably underestimated, is about 0.7 in 10(5) treatments. Prevention is essential, cure relies on adrenaline.

Adult↗
PubMed1988

A method for comparing analgesics: glafenine and paracetamol. Multicenter cross-over approach.

A double-blind multicenter cross-over study was conducted on 166 outpatients with painful chronic osteoarthritis of the hip and of the femoro-tibial joints, to compare the effectiveness of glafenine and paracetamol. Patients were randomly assigned to receive over a period of a week, either 400 mg of glafenine or 1000 mg of paracetamol twice a day at 8 a.m. and 4 p.m. in order to fill up the physical activity period during the daytime. This interval between tablet intake was chosen according to the design of the model. At the end of the week treatment period, patients crossed over. There was no wash out period between treatments. The following measurements: pain intensity (on Huskisson's visual analogue scale), functional index for hip and knee diseases, patients' overall opinion, patient preference, were evaluated at days 0, 7, 14. The results showed that both treatments produced effective analgesia but the improvement was significantly greater and observed in a larger number of cases when using glafenine rather than paracetamol. Fifty-one per cent of the nonresponsive patients to paracetamol could benefit from the glafenine treatment and 18 per cent of patients suffering from hip or knee osteoarthritis in this study showed improvement only with glafenine. Safety and biological tolerance were satisfactory with both drugs.

Acetaminophen↗
PubMed1975

Comparison of the biological effects in rat of high doses of two 4-amino-7-chloroquinoline derivatives: chloroquine and glafenine.

When given orally in elevated but nonlethal doses (150 to 450 mg/kg, on 2 consecutive days), glafenine induces in rats (body weight 100 g) a transient nephritis with an increase in blood urea, hypertrophy of adrenals, and some changes in the serum proteinogram. These effects do not appear to be due to the 4-amino-7-chloroquinoline structure from which glafenine is derived, as they are not observed with the structural analogue chloroquine given at equimolar doses under the same conditions. Further, they do not appear to be due to glycerol, the by-product of metabolic glafenine hydrolysis. The responsible molecule appears to be either glafenine itself or its acid metabolite 4-(0-carboxyphenylamino) 7-chloroquinoline.

Adrenal Glands↗
PubMed1979

Biotransformations of glafenine in the rat and in man.

The biotransformations of a therapeutic dose of the non-narcotic analgesic, glafenine, have been studied in the rat and in man. In the rat, the ester bond is extensively hydrolysed to give glafenic acid which is the major metabolite excreted in bile and in urine. Two minor pathways have been identified one leading by hydroxylation of the benzene ring of glafenine or glafenic acid in para of the amino-substituent to the corresponding phenols, the other, by oxidation of the quinoline nitrogen of glafenic acid, to its N-oxide. In vivo this N-oxide is partly reduced into the parent compound. Hydroxyglafenic acid is the product of both direct oxidation of glafenic acid and hydrolysis of hydroxyglafenine. The glyceric esters are conjugated as glucuro-ethers and/or sulfo-esters and the carboxylic metabolites as acyl glucuronides. The conjugation rate, high for glafenine, its phenol homologue and glafenic acid, is low for hydroxyglafenic acid and the N-oxide. The analogous urinary excretion patterns in man and in the rat suggest a similarity in the biotransformation of glafenine in these two species.

Animals↗
PubMed1988

Effective high-performance liquid chromatographic determination of glafenine in plasma: pharmacokinetic application.

A high-performance liquid chromatographic method for an effective determination of glafenine and its main metabolite, glafenic acid, is described. The assay involves separate extraction procedures for glafenine and for its metabolite, but the same internal standard (floctafenine) and the same chromatographic conditions (including a 5-micron C8 column, a quaternary solvent mixture of water-acetonitrile-diethylamine-acetic acid and an ultraviolet detector set at 360 nm). For 1 ml of plasma, the detection limit is 0.05 mg/l for glafenine and 0.25 mg/l for glafenic acid. Compared with previously described techniques, this assay uses a very low glafenine linearity range, which allows the true pharmacokinetics of this drug to be described for the first time.

Chromatography, High Pressure Liquid↗
PubMed1978

Leucocyte migration test and hypersensitivity to glafenin.

The leucocyte migration test (LMT) was performed on 20 patients with an intolerance to glafenin--a non-narcotic analgesic drug. LMT was found to be positive in 50% of the subjects with intolerance, a highly significant percentage as compared with the control groups. HSA-glafenin was found to be the most appropriate method for presenting the antigen, but glafenin and its hydroxylated metabolites were only found to induce a migration inhibition in the subjects intolerant to glafenin.

Adult↗
PubMed1983

Tiapride versus glafenine: a double-blind comparative study in the management of acute rheumatic pain.

A double-blind study was carried out in 42 patients suffering from acute rheumatic pain to compare the analgesic effectiveness and tolerance of tiapride with that of glafenine, a widely used analgesic in Europe. Patients were allocated at random to receive either 100 mg tiapride or 200 mg glafenine 3-times daily over a period of 14 days. Pain intensity was rated daily by the patients using a visual analogue scale and an overall assessment of response to treatment was made by both patients and physician at the end of the study. The results showed that, whilst both treatments resulted in a marked reduction in mean pain scores, pain disappeared completely in 16 (76%) of the 21 patients treated with tiapride compared with 9 (43%) of the 21 receiving glafenine. There was also a significant difference in favour of tiapride in the physician's overall assessment of response which was considered as excellent in 71% of the patients on tiapride compared with 31% receiving glafenine. Both treatments were well tolerated and few side-effects were reported. Drowsiness occurred in 6 patients on tiapride but this was only mild in 5 and moderate in the other patient.

Adult↗
PubMed1988

Comparative analgesic efficacy and tolerability of ketorolac tromethamine and glafenine in patients with post-operative pain.

In a randomized, single-dose, double-blind, parallel comparative trial of analgesic efficacy, 96 adult patients received either 10 mg ketorolac tromethamine or 400 mg glafenine orally the morning after surgery if they requested pain relief medication. Each patient provided a baseline pain assessment and then received the assigned medication. Patients assessed pain intensity and pain relief and reported any adverse events in interviews held 30 minutes after drug administration and then hourly for 6 hours. The demographic characteristics, baseline pain intensity, and surgical categories of the 47 patients who received ketorolac tromethamine and the 49 who received glafenine were similar. Both drugs provided prompt, sustained pain relief throughout the 6-hour observation period, and there were no statistically significant differences between the two groups in any of the efficacy measures analyzed. The global assessment recorded by patients suggested a slight clinical advantage for ketorolac tromethamine (32.6% of 'excellent' responses) as compared to glafenine (12.5% 'excellent'). The differences in overall response were statistically significant (p = 0.017). Fourteen (30%) patients who received ketorolac tromethamine and 17 (35%) who received glafenine reported adverse experiences that began or seemed to worsen after administration of the study drugs. The most prominent were drowsiness and sleeping, both of which are common in post-surgical patients.

Adolescent↗
PubMed1983

[Renal toxicity of glafenine in man: renal stones and acute renal failure].

The role of glafenine in certain cases of acute renal failure was described several years ago, but very little work has been done on the intratubular precipitates generally responsible for these manifestations. We have been able to study 6 cases of acute poisoning and 5 cases of glafenine renal stones which have shown that several mechanisms are likely to be involved. In 4 cases, the acute poisoning resulted in reversible oliguria which resolved after several days. In 3 of the 5 cases of renal stones, variable amounts of glafenine were found in the zone of nucleation. Infrared spectrophotometric and chromatographic examination of the first urine after the return of diuresis in the oliguric subjects and in the patients with renal stones, revealed that several metabolites of glafenine could be implicated in the development of these renal precipitates. In the different cases, free metabolites and conjugated derivatives were found to be responsible. The authors discuss the relationship between the products detected and the clinical manifestations observed.

Acute Kidney Injury↗
PubMed1991

Glafenine-associated anaphylaxis as a cause of hospital admission in The Netherlands.

In 1981 generalized anaphylaxis was registered on 166 occasions in Dutch general and academic hospitals. Clinical details of 120 of those patients revealed that in 107 anaphylaxis was either probable (n = 90) or possible (n = 17), whereas in 13 cases some other reaction than anaphylaxis had occurred. The series of confirmed cases contained 46 men and 61 women, with mean ages of 47 y and 48 y, respectively. There was a complete recovery in 102 patients and two patients died. Hypotension was present in 79 cases (74%), dyspnoea in 34 cases (32%) and a skin reaction, mainly urticaria, erythema or angioedema, was mentioned in 62 cases (58%). Most cases of anaphylaxis were drug-induced (76%), the main causes being the analgesic glafenine and contrast media. Glafenine was mentioned as the cause in 36% of all admissions for drug-induced anaphylaxis. Only 3.7% of cases had been reported to the voluntary reporting scheme of the Netherlands Centre for Monitoring of Adverse Reactions to Drugs. On the basis of reimbursement data, the risk of developing severe anaphylaxis to glafenine was estimated at 11.7-19.3-fold relative to indomethacin, and 13.4-20.2-fold relative to oral penicillins.

Adolescent↗
PubMed2000

Spectrophotometric determination of two N-(4-quinolyl) anthranilic acid derivative (glafenine and floctafenine).

Spectrophotometric methods were developed for the determination of glafenine and floctafenine. The first method depends upon the determination of glafenine in raw material and tablets as well as in the presence of its main degradation product glafenic acid (up to 40%). Differential first derivative spectral response at 245 nm in 0.1 N hydrochloric acid, where the corresponding degradation product exhibits no contribution in 0.1 N sodium hydroxide. The method allows the determination of 2.5-30 microg ml(-1). The second method depends upon the reaction of floctafenine with 2,3-dichloro 5,6-dicyano-p-benzoquinone (DDQ) in acetonitrile to give highly colored complex that could be measured quantitatively at (about) lambda(max) 538 nm. The method permits the determination of 40-180 microg ml(-1) or by measuring the first derivative spectral response of the color at 610 nm. The method permits the determination of floctafenine in presence of thiocolchicoside. The methods mentioned both simplicity and sensitivity, having excellent precision and accuracy (100.31 +/- 0.63, 100.78 +/- 0.77 and 99.90 +/- 0.56 for glafenine and floctafenine, respectively). The results were of comparable accuracy and reproducibility with the reported methods.

Analgesics, Non-Narcotic↗
PubMed1997

Determination of glafenine in dosage forms and serum by thin layer densitometry and high performance liquid chromatography.

New thin layer densitometry and high performance liquid chromatography (HPLC) methods are described for quantitative determination of glafenine in dosage forms in the presence of its photo-degradation products and in serum in the presence of its metabolites. Mobile phases consisting of toluene-isopropyl alcohol-dimethylformamide-water (18:3:1:0.5) and methanol-water-phosphoric acid (80:120:0.5) are found to be efficient for reasonable separation and adequate resolution of glafenine from associated substances by thin layer chromatography (TLC) and HPLC techniques, respectively. The methods are used for the study of glafenine purity, stability, bioavailability, bioequivalence and tablet dissolution rate. The results obtained by TLC and HPLC techniques are in good agreement and offer the advantages of reproducibility and accuracy.

Analgesics, Non-Narcotic↗
PubMed1992

Pharmacokinetics of glafenine and glafenic acid in patients with cirrhosis, compared to healthy volunteers.

Pharmacokinetic parameters were evaluated in 12 patients with alcoholic cirrhosis and 12 healthy volunteers after a single 400 mg oral dose of glafenine. Glafenine (G) and its major active metabolite glafenic acid (GA) were measured at regular intervals using a specific high performance liquid chromatographic method. Glafenine absorption was significantly delayed in cirrhotic patients (CP) (Tmax = 2.8 +/- 1.3 hvs 1.5 +/- 0.4 h, p less than 0.01) and was dramatically reduced in 3 patients. The large hepatic 'first pass' effect observed in healthy volunteers was markedly reduced in CP (ratio Cmax GA/Cmax G = 3.6 +/- 2.9 vs 18.9 +/- 9.8, p less than 0.001; ratio areas under the curves AUC GA/AUC G = 2.3 +/- 2.3 vs 18.2 +/- 11.2, p less than 0.001). The elimination half-life of G was prolonged in the CP (13.0 +/- 13.1 h vs 1.5 +/- 0.5 h, p less than 0.01). In CP, GA elimination half-life was increased (12.0 +/- 13.4 h vs 4.3 +/- 1.3 h, NS) but the difference did not reach statistical significance because of large variability. The significant rise of G plasma concentrations (Cmax = 2.2 +/- 2.1 mg/L vs 0.7 +/- 0.2 mg/L, p less than 0.05) and its longer half-life would lead to an accumulation if the usual dosage regimen was prescribed for CP and could result in nephrotoxicity. On the other hand, lower dosage would be ineffective because only GA is active and nephrotoxic. Hence, G should be given with great caution to CP.

Administration, Oral↗
PubMed1981

Recurrent acute renal failure due to nonaccidental poisoning with glafenin in a child.

A 7-year-old boy experienced recurrent attacks of acute renal failure over an 18 month period. Each attack was accompanied by a fluorescent yellow discoloration of his urine. Laboratory data and the kidney biopsy were consistent with acute tubulo-interstitial nephritis. Repeated contacts with the boy in a play setting and thorough toxicologic examination of his urine finally led to the conclusion that the mother systematically poisoned her child with glafenin. The clinical and experimental literature on glafenin-related disease is reviewed. This is the first report of glafenin intoxication in a child. This is also the first case of kidney disease as an expression of child abuse.

Acute Kidney Injury↗