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[Streptococci isolated from the blood after tooth extraction. Their role in subacute bacterial endocarditis].

A classification, according to the Lancefield's method, of the streptocoques isolated in the blood, after teeth extractions, as well as a determination of their sensibility to the antibiotics, are attempted in this study. It concerns to 23 adults, well supported, to whom multiple extractions, under general anesthesia have been done. We studied both biochemical and serological reactions, and a test for the antibiotic resistance is realised. We insiste in the contrindiction of streptomycine and sulfanilamides in the treatment or the prevention of bacteremia of dental origine.

Anti-Bacterial Agents↗

[Rapidly growing mycobacteria that cause mycobacteriosis in humans].

Rapidly growing mycobacteria of two species, i.e. M. fortuitum and M. chelonei caused in humans mycobacteriosis frequently similar in its manifestations to tuberculosis. The both mycobacterial species were resistant to the majority of antituberculous drugs and sensitive to amikacin, dioxycycline, sefmetazole and some sulfanilamides. It was shown that it was possible to identify the mycobacterial species with the routine tests and paper indicator systems.

Aged↗

In vitro antimicrobial activity of sulfonamides against some porcine pathogens.

The minimal inhibitory concentrations (MIC) of sulfonamides were determined against Bordetella bronchiseptica (n = 10), Pasteurella multocida (n = 10), Haemophilus pleuropneumoniae (n = 20), and Streptococcus suis (n = 10) strains isolated from pigs with atrophic rhinitis, pneumonia, or meningitis. Sulfonamides tested in an agar dilution method were sulfachloropyridazine, sulfadiazine, sulfadimethoxine, sulfamethazine, sulfadoxine, sulfisoxazole, sulfamerazine, sulfamethoxazole, sulfamethoxypyridazine, sulfanilamide, sulfatroxazole, and sulfisomidine. Results indicated that monotherapy of S suis infections with sulfonamides should not be encouraged because the MIC50 of all sulfonamides investigated was greater than 32 micrograms/ml. The MIC50 of the sulfonamides against B bronchiseptica ranged from 0.5 to 8 micrograms/ml, against P multocida from 2 to 32 micrograms/ml, and against H pleuropneumoniae from 8 to 64 micrograms/ml. The MIC50 of sulfachloropyridazine, sulfadiazine, sulfadimethoxine, sulfamerazine, and sulfamethoxazole for the gram-negative bacteria did not exceed 16 micrograms/ml. Among these compounds, sulfamethoxazole had the highest activity. The frequently prescribed sulfamethazine had an overall low antimicrobial activity.

Animals↗

[Comparative analysis of the structure of incompatibility plasmids N, P and W].

Evolutionary relationships of the IncN plasmid R15 and other broad host range plasmids (IncN plasmids N3 and R46, IncP plasmids RP4 and R906, IncW plasmids Sa and R388) were studied by Southern blot hybridization technique. The IncN plasmids were shown to harbour homologous determinants for replication and conjugation. No homology was found between the rep and tra genes in R15 and in the IncW and IncP plasmids, respectively. The second rep region of the N3 plasmid is distinctive from the corresponding determinants in the IncN plasmids. Homology was demonstrated for the plasmid genes that mediate restriction and modification in R15 and N3, mercury resistance in R15 and R906, sulfanilamide resistance in R15, N3, R46, Sa, R388, and R906, streptomycin resistance in R15, R46 and Sa. The latter genes are different from the R906 SmR gene. In addition to the three known mobile elements in the plasmid R15, the fourth one (IS46) that is a part of the transposon Tn2353 was identified in this study. Besides, the third copy of this insertion sequence was found in the N3 plasmid.

Base Sequence↗

[Genetic determinants of antibiotic resistance in bacteria of the genus Salmonella].

Distribution of genetic determinants of resistance to streptomycin, kanamycin, chloramphenicol, tetracycline, sulfanilamides and trimethoprim in strains of Salmonella isolated from studied. The majority of the resistant strains carried the genes of aminoglycoside-3"-phosphotransferase, type I aminoglycoside-3'-phosphotransferase, type I chloramphenicol acetyltransferase and type II dihydropteroate synthetase. Tetracycline resistance in the strains was often due to the class B tetracycline resistance genetic determinants. It was suggested that the resistance mechanisms controlled by these genes provided higher levels of resistance to the above drugs in Salmonella as compared to the other mechanisms. Plasmid resistance genes were detected in more than 90 per cent of the clinical strains and in 35 per cent of the sporadic strains of S. typhimurium. The antibiotic resistance of the Salmonella strains of other serovars was not as a rule controlled by the plasmid genes.

Animals↗

[Genetic determinants of resistance to antibiotics in Pseudomonas bacteria].

Seven hundred and eighty nine drug resistant strains of Pseudomonas isolated in hospitals, from antibiotic production sewage and mine soils were studied in experiments on colony hybridization with the use of 32P-labeled plasmid DNA fragments containing various antibiotic resistance genetic determinants. The genes controlling production of aminoglycoside-3'-phosphotransferase, aminoglycoside-3'-adenilyl transferase, type I dihydropteroate synthetase (DHPS I) and DHPS II were detected in the strains of all the ecological niches. More than 90 per cent of the clinical strains hybridized with the samples containing these genes, though in the soil strains the main mechanisms of streptomycin and sulfanilamides resistance were probably controlled by the other nonhomologous genetic determinants studied. The gene controlling production of aminoglycoside-3'-phosphotransferase II was detected in the strains isolated both in the hospitals (49 per cent) and from the sewage (45 per cent), while the gene of aminoglycoside-3'-phosphotransferase I was detected only in the population of the clinical strains (52 per cent). The majority of the tetracycline resistant strains isolated in the hospitals and from the sewage hybridized with the samples containing the classes A and C tetracycline resistance genetic determinants. In the soil strains the genetic determinants of the main tetracycline resistance mechanism(s) were not homologous to those of classes A, B and C. Resistance of the strains to trimetoprine was as a rule determined by the genes of type II dihydrofolate reductase.

Anti-Bacterial Agents↗

[Clinico-immunologic characteristics of acute toxic-allergic reactions to drugs and current methods for their treatment].

The paper is concerned with clinicoimmunological and allergological characterization of 29 cases of acute toxic allergic reactions (ATAR) to drugs. Four degrees of severity of disease were identified; the most severe form was toxic epidermal necrolysis caused by the use of sulfanilamides and pyrazolones in patients with acute respiratory virus and bacterial infections. Blood analysis in patients with III-IV degree of severity showed a sharp decrease in Ctot and C3 up to 0, an increase in the level of circulating immunocomplexes and "average molecules". Cellular immunity in III degree of severity was decreased. The main principles of therapy using extracorporeal immunocorrective methods were worked out. A leukocyte natural migration inhibition test was used for specific diagnosis of intolerance to medication.

Acute Disease↗

Synthesis and characterization of new 2-(arylidenehydrazino)-4-methyl-5-(arylazo)thiazoles.

In order to test their insecticidal, fungicidal and herbicidal activities the title compounds 2-20 were prepared from the reactions of various aldehyde-thiosemicarbazones with corresponding alpha-oxo-alpha-methyl-N-(p-substituted phenyl)-ethanehydrazonoyl chloride [1], derived from the coupling of chloroacetone with the diazonium salt of ethyl p-aminobenzoate, p-iodoaniline, sulfanilamide and aniline, respectively. All the synthetized compounds were characterized by their elementary analysis, and by using IR, NMR and mass spectrometry.

Chemical Phenomena↗

[Molecular genetic organization and origin of plasmid pBS52 with a broad range of bacterial hosts].

The data are presented on the localization of genetic determinants of resistance to streptomycin, ampicillin and sulfanilamides on the physical map of conjugative R plasmid pBS52 of 38,000 bp which has a broad bacterial host range and belongs to a new incompatibility group. The plasmid has a natural "polylinker" site (less than 200 bp) containing (in the order of arrangement) the recognition sites for restriction enzymes: BamHI-EcoRI-PstI-EcoRV-BglII (PvuII). The comparative analysis shows that pBS52 contains a segment homologous to DNA of plasmid RSE1010 (IncP-4). The evolutionary origin of plasmid pBS52 is discussed. The recA-independent formation of the mini-derivatives of pBS373 and pBS374 types during the transformation of Escherichia coli with pBS52 plasmid DNA has been shown. Plasmids pBS373 and yBS374 are capable of autonomous replication in Pseudomonas putida and P. aeruginosa cells, which is provided by the rep system of IncP-4 replicon.

Bacteria↗

[Drug-induced hepato- and nephropathy].

Upon clinical and pathological analyses of the evidence obtained on drug-related lethal nephropathies (51 cases) and hepatopathies (14 cases) as well as at puncture biopsies of the livers affected by chemotherapeutic agents it was determined that the commonest variants of the disturbances were tubular nephropathies, tubular-interstitial nephritis, papillary renal necrosis, symmetric cortical renal necrosis, fulminant hepatopathies with diffuse massive necrosis of hepatocytes. For biopsies, cholestatic drug-induced hepatopathies were found most frequently. As a rule, the patients received polychemotherapy with psychotropic, cardiovascular and antidiabetic drugs, nonsteroids, antibiotics, sulfanilamides, consumed contrast diagnostic media. The attention is drawn to considerable diagnostic difficulties faced in drug-induced damage to the organs which can be diminished by comparisons between clinical and morphological findings.

Adolescent↗

Rapid and selective method for quantitation of metronidazole in pharmaceuticals.

A selective and highly sensitive assay for N-1-substituted nitroimidazoles has been modified and adapted for rapid estimation of metronidazole in pharmaceuticals. The color reaction is based on diazotization of sulfanilamide with the nitrite ions liberated by alkaline hydrolysis of metronidazole and subsequent coupling of the diazonium salt with N-1-(naphthyl)-ethylenediamine dihydrochloride. This method is applicable for the assay of benzoyl metronidazole in oral suspension. Officially recommended excipients and preservatives do not interfere.

Hydrolysis↗

Spectrophotometric determination of aminacrine hydrochloride in creams, jellies, and suppositories: interlaboratory study.

A previously reported visible spectrophotometric method for the analysis of aminacrine hydrochloride in creams, jellies, and suppositories was studied collaboratively by 8 laboratories. Aminacrine hydrochloride was extracted into acidic ethanol and its visible spectrum recorded. The amount present was calculated by determining the net absorbance between the absorbance maximum at about 402 nm and one-half the sum of the absorbance of the minima at about 389 and 412 nm. Each collaborator received 4 creams (0.2%), 1 jel (0.2%), 1 molded suppository (6 mg/3.198 g), and 2 gelatin-encapsulated suppository samples (12 mg/6.661 g and 14 mg/6.863 g). The cream samples included blind duplicates prepared to contain 0.212% aminacrine hydrochloride, 15% sulfanilamide, and 2% allantoin. Mean recovery for the authentic cream was 104.7% with a coefficient of variation (CV) of 9.22%. The commercial products contained these respective amounts (CVs): creams, 100.0% (2.48%) and 101.5% (2.16%); jel, 118.0% (9.58%); molded suppository, 102.7% (1.88%); and gelatin encapsulated suppositories, 93.1% (1.0%) and 94.3% (1.60%). Standard aminacrine hydrochloride provided for the study was 99.6% pure by nonaqueous titration. Thin layer chromatographic identification of aminacrine hydrochloride was also tested collaboratively. The method was not adopted by AOAC.

Aminacrine↗

Free fatty acids and the binding of sulfonamides in the serum of genetically obese Zucker rat.

The purpose of this study was to evaluate the serum chemistry profiles and the degree of protein binding of six sulfonamides in the sera of genetically obese Zucker rats and their lean litter mates. Free fatty acid concentrations were significantly elevated in the serum of obese rats. Obese rat serum had a mean fraction unbound for sulfanilamide, sulfadiazine, sulfapyridine, sulfamerazine, sulfisomidine, and sulfisoxazole which was significantly higher than that found in the lean rat serum. Altered serum chemistry and/or pathological states may play a significant role in altering drug protein interactions.

Animals↗

Influence of hydrogen and chloride ions on the interaction between sulfaethidole and bovine serum albumin studied by microcalorimetric and acid-base titrimetric methods.

From earlier studies it is known that bovine serum albumin has one high affinity binding site and several lower affinity sites for the sulfa drug N1-(5-ethyl-1,3,4-thiadiazol-2-yl)sulfanilamide (sulfaethidole) (Kostenbauder, H.B., Jawad, M.J., Perrin, J.H., and Averhart, V. (1971) J. Pharm. Sci. 60, 1658-1660). This binding has been further studied using equilibrium dialysis, microcalorimetry, and pH titration technique. Results of these studies show that the binding of sulfaethidole to the first (high affinity) site may be accompanied by an uptake of protons. Proton uptake is found to be zero at pH 7.4 and approximately 0.6 at pH 8.5 for each sulfaethidole molecule bound. The other binding sites for sulfaethidole are not proton linked. The first, and probably the other binding sites, are also Cl- ion linked; for example, the binding of sulfaethidole to the first binding site is accompanied by the displacement of (on average) one Cl- ion at pH 7.4 in 0.1 M NaCl. This explains the observation that the heat of binding of sulfaethidole to the high affinity site is -33.0 kJ.mol-1 in the absence of chloride ions, but only -22.8 kJ.mol-1 in the presence of 0.1 M Cl- (at pH 7.4).

Calorimetry↗

On the relation between the formation of antihapten and anti-carrier protein antibodies in the immune response induced by conjugates of various haptens with homologous serum proteins.

Rabbits inoculated with conjugates of homologous serum with ortho-aminophenol (OAP), para-aminophenol (PAP), 3-hydroxy-sulfanilamide (3-HS), DOPA and alpha-methyldopa (alpha MD), 5-aminosalicylic acid (5-ASA) and 3-hydroxy-para-aminobenzoic acid (3-HPABA) give rise to both hapten specific and anti-carrier protein antibodies. By contrast, the conjugates of homologous serum with penicilloyl (P) hapten induced only antihapten antibodies. The conclusion is, therefore, drawn that the formation of anti-carrier antibodies upon inoculation with conjugates of various haptens appears to be dependent on the nature of hapten in the conjugate. The discrepancy between the behaviour of P conjugates, on the one hand, and the DOPA and alpha MD conjugates, on the other hand, is in agreement with the observation from the clinical immunology, which has signaled a high incidence of antibodies with autoantibody character in patients taking DOPA and alpha MD, but rarely, if ever, such antibodies have been found in patients treated with penicillin.

Animals↗

Normal phase liquid chromatographic determination of sulfamethoxazole in tablets: collaborative study.

A stability-indicating liquid chromatographic method is presented for determining sulfamethoxazole in tablets. The method uses a 10 micron silica column, an isooctane-methylene chloride-2-propanol-acetonitrile-glacial acetic acid (70 + 25 + 5 + 5 + 0.5) mobile phase, and photometric detection at 254 nm. Seven laboratories collaboratively studied this method on powdered composite samples prepared from commercial 500 and 1000 mg tablets and on an authentic tablet mixture containing 83.32% added sulfamethoxazole. Mean assay results for the 500 and 1000 mg tablets were 102.2 and 97.9% of declared, respectively (n = 4). The mean recovery value for the synthetic sample was 99.4% (n = 4). The pooled reproducibility standard deviation (SD) (coefficient of variation (CV)) and pooled repeatability SD (CV) were +/- 1.01 (1.01%) and +/- 0.96 (0.96%), respectively. These results were in good agreement with those obtained by the Associate Referee for the titration method of USP XX. The proposed method can also be used for monitoring the presence of sulfanilamide in sulfamethoxazole by increasing the proportions of both acetonitrile and 2-propanol in the mobile phase. The method has been adopted official first action.

Chromatography, Liquid↗

Spectrophotometric analysis of binary mixtures of sulfonamides.

Different methods for analyzing binary mixtures by using 2 wavelengths are reviewed. The absorbance ratio calculated at 2 wavelengths, not including the isoabsorptive point, was a quadratic function of relative concentration. The curve-fitting process using orthogonal polynomials was applied to obtain the quadratic equation. An absorbance ratio can be used as a rapid purity index for sulfacetamide sodium in the presence of sulfanilamide. Sulfacetamide sodium has been determined in eye drop preparations.

Ophthalmic Solutions↗

Oversaturation of urine with sulphadiazine during treatment with a small therapeutic dose.

The urinary crystallization of N1-pyrimid-2-yl-sulfanilamide (sulphadiazine, Sulfolex) during treatment with a small therapeutic dose (600 mg/day p.o.) for 6 days was evaluated in seven voluntary female subjects. In 5/7 and 3/7, respectively, of the urine supernatants obtained from samples collected 6 and 24 h after the last dose of sulphadiazine, the sulphonamide concentration exceeded the experimental solubility of the drug in 37 degrees C urine at the same pH. However, only in 3 sediments of the 6-h urine samples could a few sulphadiazine crystals be found. The findings suggest that the urine often can be oversaturated in respect to sulphadiazine, without any marked crystallization.

Adult↗