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At least 721 records · Page 40Linked to original sources
PubMed1978

Drug phototoxicity in mice.

A series of agents with alleged photosensitizing properties has been studied in mice by a quantitative in vivo method for acute drug phototoxicity. The method, originally developed for phenothiazine studies, was found suitable for several drug groups with varying mechanism of action, such as tetracyclines, protoporphyrin and psoralens. In the sulfa group only sulfanilamide was active, although weakly. Phototoxicity in vivo, hitherto not demonstrated, was observed with griseofulvin, nalidixic acid, imperatorin, kynurenic acid and amiodarone.

Animals↗
PubMed1976

[Sensitivity of 30 strains of E. coli isolated from calves to chemotherapeutic agents].

Escherichia coli strains were isolated from calves and were biochemically and serologically identified in terms of their sensitivity to antibiotics. An exclusively high frequency of sensitivity was established to sulfonamides (100 per cent), tetracicline, erythromycin, oleandomycin (86.6 per cent) ampicillin, and streptomycin (70 per cent). Well expressed was their sensitivity to nitrofurans, canamycin, neomycin, and polymyxin. It was demonstrated through serial dilutions that there exists a high level of resistance to sulfanilamides, oleandomycin, erytromycin, tetracycline, streptomycin, chloramphenicol (more than 512 mug/cm3). The prevalence of such polyresistand E. coli strains in calves is the reason for concern in the district of Haskovo.

Animals↗
PubMed1976

[Biochemical identification of Salmonella and coli bacteria and their sensitivity to chemotherapeutic agents].

Strains of enterobacteria, isolated from pathologic material (dead pigs, birds, lambs, sheep fetuses, swab fecal samples from calves) were biochemically identified by the methods of Costin, Le Minor, and Eming. One-hundred forty of them proved to belong to Escherichia coli and 236 -- to Salmonella. The sensitivity of the isolated bacteria to antibiotics (ampicillin, streptomycin, tetracyclin, kanamycin, neomycin, chloramphenicol, erythromycin, oleandomycin polymyscin), sulfonamides (norsulfasol, sulfaguanidine, and sulfadimesine), and nitrofuran preparations (furazolidon and orafuran) was tested by the disk diffusion method. There was in a high per cent of the cases resistance to tetracyclin, erytromycin, oleandomycin, sulfanilamides, streptomycin, ampicillin, and comparatively well expressed susceptibility to polymyxin, furazolidon, orafuran, kanamycin, neomycin and chloramphenicol. Prevailing were the enterobacteria polyresistant to antibiotics, the observed resistance being expressed to 3, 4, 5, 6, and 7 antibiotics at the same time (out of all nine of them that were studied). The only exception were Salmonella typhimurium and Salmonella dublin which were resistant to 2 or 3 antibiotics only. In connection with the data obtained on the tolerance of enterobacteria to chemotherapeutics it is necessary to reevaluate the programmes for the prophylaxis and control of diseases in farm animals and birds caused by Escherichia coli Salmonella spp.

Animals↗
PubMedDate not supplied

[Microcirculation and blood coagulation in patients with diabetes mellitus undergoing antidiabetic therapy of different types].

A comparative study of the peculiarities of the course of diabetes and metabolic disturbances, and also of the indices of capillary permeability, biomicroscopy of the conjunctival vessels, platelet aggregation, coagulorgam and blood clot retraction was carried out in the group of patients treated with insulin and sacharreducing sulfanilamides. Marked derangements in the microcirculatory system concerning both the vascular wall proper and of the rheological properties of the blood were revealed. These derangements were more distinct in the patients over 45 years of age with prolonged affection and the presence of vascular complications but proved to be independent of the therapy carried out.

Adult↗
PubMed1977

[Pharmacokinetics of sulfaclomide in man under therapeutically relevant conditions].

Pharmacokinetic parameters of the long-term sulfanilamide Sulfaclomid (4-[4-aminobenzensulphonamido]2,6-dimethyl-5-chlorpyrimidine) were determined in 25 female subjects. Both the elimination half-life of Sulfaclomid in the serum and the maximum acetylation rate in the urine are genetically determined. They show a polymodal behavior. The half-life is unrelated to the protein binding, which shows considerable individual differences in the therapeutic relevant range of about 200 microgram/ml serum. This confirms the human pharmacological postulate according to pharmacokinetical dosage schedules including genetic factors. An individual therapy service is necessary in certain drugs and in highly endangered groups of patients.

Acetylation↗
PubMed1977

Inhibition of urease by miscellaneous ions and compounds. Implications for the therapy of infection-induced urolithiasis.

One hundred forty-eight drugs and other organic and inorganic substances were screened for their ability to inhibit the enzyme urease in an in vitro system modeled on infected urine. The reported urease-inhibiting properties of ascorbic acid, tetracyclines, and sulfanilamide were not confirmed. At least 50 per cent inhibition was observed in the presence of kanamvcin, hydroxguanidine, benzoquinone, 1,2-naphthaquinone-4-sulfonate, chloramine-T, N-bromoacetamide, copper, mercury, and fluoride. It is, however, unlikely that therapeutically effective concentrations can be attained in urine without giving dosages likely to result in toxic effects. Hydroxyurea, at the dose level used in cytotoxic therapy, may be expected to produce effective inhibition of bacterial urease in the urinary tract, providing renal function is unimpaired and providing urinary volume does not exceed 1 liter per 24 hr. Acetohydroxamic acid is potentially the most useful drug for the treatment of infection-induced urinary stone disease available at present.

Bacterial Infections↗
PubMedDate not supplied

[Study of the allergic properties of medicinal preparations in experiments].

Materials of an experimental study on allergenic properties of prolonged-action sulfanilamides and their semi-products are presented. Investigations involved the use of express-methods with intradermal administration of the substance into the ear and introduction of the agents together with the Freind adjuvant into the hind paw pad of a guinea pig. Experiments ascertained satisfactory dermal-allergic responses to the introduction of allergens differing in their strength by employing the above methods, as express ones for primary evaluation tof allergenic properties of drugs and their semi-products in conducting toxicological investigations.

Animals↗
PubMed1975

Assay of sulfacetamide sodium ophthalmic solutions by high-pressure liquid chromatography.

A high-pressure liquid chromatographic method, using an absorption column and sulfabenzamide as the internal standard, is proposed for the determination of sulfacetamide sodium and its principal hydrolysis product, sulfanilamide, in eye drops. It affords an average recovery of 100.9% of added sodium sulfacetamide with a relative standard deviation of 1.9%.

Chromatography↗
PubMed1975

Succinylsulfathiazole crystal forms. II: Effect of additives on kinetics of interconversion.

The effect of various additives on the rate of transformation of the metastable anhydrous succinylsulfathiazole Form I to the water-stable dihydrate Form II in aqueous suspensions was studied. Some structurally related compounds, viscosity-imparting agents, surfactants, and coloring agents were used as possible transformation retardants. The effect of including seeds of Form II in the presence and absence of additives is also discussed. Some additives, e.g., methylcellulose and phthalysulfathiazole, showed significant transformation-retarding effects. Other additives, e.g., sulfanilamide and glycerin, increased the rate of transformation. Coloring agents had only slight effects. Utilization of the results in the formulation of physically stable aqueous suspensions of succinylsulfathiazole is discussed.

Chemical Phenomena↗
PubMed1980

Tissue distribution and metabolism of drugs V: effect of secretin and pancreozymin on drug transport in rabbit pancreas.

The effect of secretin and pancreozymin on the tissue distribution and penetration of drugs in the rabbit pancreas was studied to clarify hormonally regulated drug distribution. Drugs with high liquid solubility were distributed easily within the pancreas even during secretin or pancreozymin treatment, and these hormones had little effect on drug distribution from the blood to the pancreas. However, secretin increased the concentration ratio of dimethadione in the pancreatic juice (J) to plasma unbound dimethadione (Pf), probably because the pancreatic juice during secretin infusion is alkaline relative to the control. Secretin had no effect on the J/Pf of isonicotinamide and sulfanilamide. Secretin decreased the J/Pf of drugs with low lipophilicity or large molecular weight because the penetration rates of these drugs from cell water to pancreatic juice were not rapid enough to reach equilibrium. Pancreozymin was unable to change the J/Pf of any drug tested. These results suggest that the barrier between the blood and the pancreas or the barrier between the pancreas and the pancreatic juice is unchanged by secretin or pancreozymin.

Animals↗
PubMed1980

Tissue distribution and metabolism of drugs VI: Effect of second drugs on pancreatic distribution and insulin-releasing activity of sulfonylureas in perfused rat pancreas.

The distribution of sulfonylureas and their insulin-releasing potency as a pharmacological response were studied in isolated perfused rat pancreas. Sulfonylurea concentrations in the perfused pancreas in the presence or absence of a second drug were determined after perfusion for 15 min. Sulfonylureas could be distributed throughout the pancreas readily, and the tissue sulfonylurea concentration was reduced by the addition of sulfaphenazole, sulfadimethoxine, and salicylic acid. The insulin secretion rate stimulated by tolbutamide also was reduced by these three drugs; sulfanilamide, which could not displace the tolbutamide distribution, did not affect the tolbutamide-mediated secretion of insulin. These results document the importance of drug concentration in the tissue or receptor site with regard to insulin secretion and show that the sulfonylurea-mediated secretion of insulin can be modified easily by concomitant perfusion of a second drug that displaces sulfonylurea in the pancreas. These findings suggest that the drug interaction at the target organ or receptor site should be understood to provide adequate drug therapy.

Animals↗
PubMed1984

Effect of systemic anaphylaxis on the absorption of salicylic acid from the rat small intestine.

Rats were immunized by intraperitoneal injection of ovalbumin (egg albumin) emulsified in Freund's incomplete adjuvant, and then the effect of an intravenous challenge with ovalbumin on salicylic acid absorption from the small intestine was examined by means of an in situ recirculation technique. The disappearance of salicylic acid from the luminal solution was significantly decreased in rats treated with ovalbumin compared with control groups treated with saline. The decreased absorption of salicylic acid in ovalbumin-immunized rats was related to the anti-ovalbumin antibody responses examined by passive cutaneous anaphylactic reactions. On the other hand, the decreased absorption of salicylic acid was not found in ovalbumin-immunized rats challenged intravenously with bovine gamma-globulin. Similar results were also noted in rats immunized via the footpads with ovalbumin. However, no significant change was observed in the intestinal absorption of salicylic acid in normal (nonimmunized) rats challenged intravenously with ovalbumin. Furthermore, intestinal absorption of sulfadimethoxine and sulfanilamide was significantly decreased during systemic anaphylaxis, whereas no change was observed in the absorption of sulfisoxazole, quinine, sulfanilic acid, and phenolsulfonphthalein. This suggests that the intestinal absorption of rapidly absorbed drugs, including salicylic acid, is more sensitive to systemic anaphylaxis than that of poorly absorbed drugs.

Anaphylaxis↗
PubMed1986

Studies on drug-milk freeze-dried formulations. I: Bioavailability of sulfamethizole and dicumarol formulations.

In this study, solid dispersion formulations of dicumarol (3,3'-methylenebis[4-hydroxycoumarin]) and sulfamethizole (N'-(5-methyl-1,3, 4-thiadiazol-2-yl)sulfanilamide) in defatted milk were prepared by freeze-drying. X-ray crystallographic data showed that both drugs were dispersed in the formulations in an amorphous state. Bioequivalency comparisons between freeze-dried formulations, after regeneration with water, and control capsules containing the pure drug substances were studied in four male volunteers. Determination of the plasma dicumarol levels indicated superiority of the dicumarol-milk formulation. Statistically significant differences were found between area under the curve, maximum plasma concentration, and apparent elimination rates. Analysis of the urine sulfamethizole data revealed that the two formulations exhibit statistically equivalent rates and extents of excretion of unchanged sulfamethizole. The binding of both drugs to casein and their solubility in the presence of casein were measured in vitro. The presence of casein caused an increase in the solubility of dicumarol, while it had no effect on the solubility of sulfamethizole. Normal protein binding cannot be responsible for the effects noted. Extrapolation of the in vitro data to the in vivo situation was attempted. Drug-milk freeze-dried formulations are promising for the enhancement of the bioavailability of sparingly water soluble drugs.

Adult↗
PubMed1988

Determination of temazepam and related compounds in capsules by high-performance liquid chromatography.

A reversed-phase, high-performance liquid chromatographic assay method is described for temazepam hard gelatin and soft gelatin capsule analysis. The method is simple, specific, accurate, fast, and stability indicating. A reversed-phase octylsilane (C8) column with a mobile phase composed of methanol:1% acetic acid and detection at 254 nm separated sulfanilamide (internal standard), temazepam, synthetic precursor, and possible degradation products. Detector responses showed linearity to temazepam concentrations over the range 0.075-0.60 mg/mL (r = 0.9999). Mean recovery of temazepam added to capsule excipients was 100.3%. Mean assay results for 15- and 30-mg hard gelatin capsules were 101.5 and 101.3%, respectively. Mean assay results for 10- and 20-mg soft elastic gelatin capsules were 101.1 and 101.5%, respectively.

Anti-Anxiety Agents↗
PubMed2005

Determination of pKa values by capillary zone electrophoresis with a dynamic coating procedure.

CZE allows to measure the acidic dissociation constant (pKa) of many drug substances. However, determining the EOF intensity may be time-consuming, especially at a low pH. In order to overcome this drawback, a dynamic coating procedure of the capillary was carried out to increase microEOF, and thus to reduce the analysis time. In addition, this coating procedure enhanced migration time stability. The effective mobilities of 15 compounds were measured at different pH, producing pK'a values dependent on BGE ionic strength. The latter values were corrected with the activity coefficient to obtain a "true" pKa value. The 15 investigated compounds were (i) five acids: namely, salicylic acid, benzoic acid, ketoprofen, phenobarbital, and phenol, (ii) four bases: lidocaine, propafenone, propranolol, and quinine, (iii), five ampholytes: sulfanilamide, sulfabenzamide, sulfadimethoxine, sulfadoxine, and sulfisoxazole, and (iv) one zwitterion: cetirizine. The range of determined pKa values was between 1.2 and 11.2, and close to the pKa values available from the literature.

Electrophoresis, Capillary↗
PubMed1994

Identification of a new class of ETA selective endothelin antagonists by pharmacophore directed screening.

Novel endothelin antagonists were identified through a "pharmacophore directed screening" strategy. The sulfanilamide antibacterial agent sulfisoxazole was found to be a good endothelin receptor antagonist (IC50's of 0.60 microM and 22 microM for the ETA and ETB receptors, respectively). The structurally similar sulfamethoxazole was found to be a weaker antagonist (IC50 for ETA 16 microM and for ETB 230 microM). These compounds represent a new class of low molecular weight and ETA-selective non-peptide endothelin antagonists.

Cell Line↗
PubMed1997

Improved methods to measure end products of nitric oxide in biological fluids: nitrite, nitrate, and S-nitrosothiols.

The aim of this study was to compare and improve standard methods to determine nitrite (NO2-), nitrate (NO3-) and S-nitrosothiol (RSNO) levels in cell culture supernatants, sera, and urine. We modified the conventional Griess reaction by replacing sulfanilamide with dapsone (4,4'-diamino-diphenylsulfone) and compared the NO2- levels in our study samples with a commercially available NO2- assay kit. Our modification, along with ultrafiltration of the samples, resulted in an enhanced sensitivity to measure NO2- down to 0.2 microM. The detection limit was further improved to 0.02 microM when NO2- was identified by the fluorochrome 2,3-diaminonaphthalene (DAN). To measure the stable end product NO3- by the Griess reaction or the DAN method, this anion must be reduced to NO2-. We compared the capacity of bacterial nitrate reductase with the reducing metal cadmium to convert NO3- to NO2-. After reduction, NO2- levels were determined either by the DAN method or by our modified Griess reaction. We found that there was a high correlation (r2 = 0.998) in total NO2- concentrations in the study samples using both methods for reducing NO3- to NO2-. The simultaneous determination of NO2- and NO3- was achieved by using anion-exchange chromatography (HPLC; Polyspher IC AN-1 column). The detection limit of this assay for each anion is 0.5 microM, and it can be applied equally well to sera, urine, and culture media. We also adapted the DAN method to determine RSNO levels in our study samples. Using this approach, we were able to measure RSNO levels down to 0.15 microM. As result we discovered that RSNO levels were markedly increased in urine from septic patients and in supernatants from cytokine-stimulated human tumor cell lines. L-Citrulline, a coproduct of NO biosynthesis, was measured using a colorimetric assay with a sensitivity limit of 3.0 microM. Increased L-citrulline levels in media from cultured cells, but not in sera or urine, correlated with increased NO production. Although all methods studied were suitable for quantifying end products of NO in biological fluids and media, the use of bacterial reductase and the modified Griess reaction proved successful to provide the greatest sensitivity and linear range for routine measurements of NO2- and NO3-.

Body Fluids↗