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PubMed1994

Synthesis and anticonvulsant activity of some new 3-(p-sulfamoylphenyl)-4(3H)-quinazolinones.

In view of their expected anticonvulsant property, a series of 3-(p-sulfamoylphenyl)-4(3H)-quinazolinone derivatives (V) were synthesized by condensation of sulfanilamide with various 4H-3,1-benzoxazin-4-ones (III). Some 2-amido-N-(p-sulfamoylphenyl)benzamides (IV) were isolated as reaction intermediates. The structures of V were confirmed by IR, 1H-NMR, MS and elemental analyses. Some of the compounds V showed significant anticonvulsant effects against pentetrazol-induced convulsions.

Animals↗

PubMedDate not supplied

[The efficacy of antibacterial preparations against Pseudomonas mallei in in-vitro and in-vivo experiments].

In vitro antibacterial activity of 43 antibiotics and chemotherapeutics against P. mallei Ts-5 was studied. The causative agent of malleus was highly susceptible to sulfanilamides, fluoroquinolones, tetracyclines, aminoglycosides, ceftazidime and imipenem. 15 antibiotics and chemotherapeutics were tested for their therapeutic efficacy on golden hamsters with experimental malleus. Combinations with trimetoprim (sulfaton and biseptol), 3rd generation quinolones (ciprofloxacin, enoxacin and ofloxacin) as well as minocycline, novobiocin and oxolinic acid were shown to be therapeutically highly efficient.

Animals↗

PubMed1994

Antibiotics and dentistry: a brief review.

The history of dental disease has involved a variety of treatment modalities. This paper is a historical perspective of the evolution of modern antimicrobial compounds and their applications for dentistry. Many individuals have made tremendous contributions in this field, beginning more than a century ago. The two primary categories of antimicrobial agents are the naturally occurring antibacterial substances (antibiotics) and the compounds of synthetic origin. Agents of fungal origin (penicillins and cephalosporins), bacterial origin, and actinomycetes origin (aminoglycosides) comprise the former group while sulfanilamides, quinolones, and fluoroquinolones are included in the latter. The antibiotic groups of significance for dentistry are the penicillins, cephalosporins, and the aminoglycosides, including erythromycin. Due to its efficacy, low cost, and ease of administration penicillin has been the antibiotic of choice for many, if not most odontogenic infections. The agents of synthetic origin have some therapeutic value for dentistry. They are compromised by high cost, lack of effectiveness, or host toxicity.

Anti-Bacterial Agents↗

PubMedDate not supplied

Confirmatory method for sulfonamide residues in animal tissues by gas chromatography and pulsed positive ion-negative ion-chemical ionization mass spectrometry.

A confirmatory method has been developed for determination of 13 sulfonamides in edible tissues. The assay involves extraction from a solution resulting from a screening procedure by liquid chromatography and subsequent derivatization. Sulfachloropyridazine (SCP), sulfadiazine (SDA), sulfadimethoxine (SDM), sulfamethazine (SMZ), sulfamerazine (SME), sulfamethoxazole (SMX), sulfamethoxypyridazine (SMP), sulfapyridine (SPR), sulfaquinoxaline (SQX), and sulfathiazole (STA) were detected as the N1-methyl-N4-trifluoroacetyl derivatives, sulfaguanidine (SGU) as the same derivative after cyclization by hexafluoroacetylacetone, and sulfacetamide (SAC) as the methyl derivative. These sulfonamides were detected by gas chromatography and pulsed positive ion-negative ion-chemical ionization mass spectrometry with methane as the reactant gas, whereas sulfanilamide (SAA) was determined as the methyl derivative by electron-impact ionization.

Acylation↗

PubMed1976

[Beef kidney carbonic anhydrases in affinity chromatography and radial immunodiffusion].

The absence of low activity carbonic anhydrase in the parenchyma of bovine kidney is demonstrated by high specific methods such as affinity chromatography on "CH-Sepharose 4 B"-sulfanilamide and radial immunodiffusion; thus, the high activity carbonic anhydrases C I and C II seem to be the only forms in this tissue. Their identity with the carbonic anhydrases of the erythrocyte suggests that their biosynthesis must be regulated by the same structural gene working alone on these two tissues.

Animals↗

PubMed1995

Possible modes of action of nimesulide in controlling neutrophilic inflammation.

Even in recent years the development of new non-steroidal anti-inflammatory drugs (NSAIDs) appears to be essentially driven by the archaic idea to protect humans from pain and other symptoms of inflammation. Very few attempts have been made to understand if any of these drugs can limit the tissue injury during one or several forms of inflammatory reaction. In studying the events underlying the development of the tissue injury during neutrophilic inflammation, it was found that at least a NSAID, i.e. nimesulide (CAS 51803-78-2), has high potential to interfere efficiently with the major pathway responsible for neutrophil-dependent histotoxicity. Other chemically related drugs, not classified as NSAIDs but used in disease conditions characterized by neutrophilic inflammation, i.e. dapsone and sulfapyridine, have similar activities. Therefore, it is suggested that derivates from sulfanilamide (nimesulide, dapsone and sulfapyridine) are the major candidates for developing rational therapeutic anti-inflammatory strategies for controlling the development of tissue injury during neutrophilic inflammation. Also, these molecules might serve to drive the synthesis of new histoprotective antiinflammatory drugs.

Animals↗

PubMed1977

Collaborative study of modified AOAC method of analysis for nitrite in meat and meat products.

A modified version of the AOAC method of analysis for nitrite in meat and meat products was tested collaboratively by 23 laboratories. Results were compared with those obtained by the official AOAC method. Recommended modifications include: (a) substitution of N-(1-naphthyl) ethylenediamine and sulfanilamide for Griess reagent, (b) separate addition and 1:10 dilution of the above reagents, (c) 20 min color development and absorbance read at 540 nm, (d) substitutionstitution of NaNO2 for AgNO2 and NaCL, (e) omission of mercuric chloride, (f) screening of filter paper for nitrite contamination, (g) more precise dilution of sample aliquot, and (h) standard curve linear up to 10 microng N/50 ml. Results were statistically treated by Youden's technique for comparing 2 methods, using a matched pair sample scheme. The random error for the modified method was significantly lower than the random error for the official method. A t-test showed no difference in bias between the 2 methods.

Colorimetry↗

PubMed1996

[Use of parenteral feeding in the multimodality treatment of Crohn's disease and nonspecific ulcerative colitis].

The paper reviews publication on the use of complete parenteral feeding in the multimodality treatment of inflammatory bowel disease. Complete parenteral feeding was performed in patients with skeletization and physical retardation, in severe diseases, in inefficiency or intolerance of conventional therapy with sulfanilamides and steroids, in those who had intestinal fistulas, as well in the preparation of patients for surgical treatment. The use of complete parenteral feeding, under the above circumstances allow one to achieve persistent remission, spontaneous healing of intestinal fistulas, elimination of abnormal metabolism, nutrition, constitution, water-electrolyte balance, to reduce a surgical risk and the incidence of postoperative complications and the length of patients' hospital stay.

Colitis, Ulcerative↗

PubMed1996

[Recovery rate in chemotherapy of glanders].

It was shown that out of all the studied methods for the estimation of the recovery rate in animals with experimental malleus the solid-phase enzyme immunoassay with parallel growing of the test material and subsequent isolation of the antigens and L-forms proved to be the most efficient. In addition to the routine criteria of the recovery the malleinic test was a valuable diagnostic means for the estimation of the recovery rate and the efficacy of the antibacterial drugs in a model of guinea pigs. The immunological investigations revealed a dependence of the host sanation on the term of the animal chemotherapy. There was detected no L-transformation of Pseudomonas mallei during the treatment of the animals with experimental malleus with combinations of sulfanilamides with trimethoprim (biseptol and sulfaton) or rifampicin which was evident of their high sanation activity and safety in comparison to sulfamonomethoxin used alone.

Animals↗

PubMed1997

A history of edema and its management.

The obvious disfigurement caused by clinically evident edema has been a matter of medical concern for ages. Most of the early writings on the subject (Sumerian, Babylonian, Egyptian, Greek) center on dropsy, its causes and management. While reference to the heart is made in the ancient texts, much of the focus is on the abdominal (ascitic) accumulation of fluid. The role of the heart and "dropsy of the chest" began to be differentiated and attract attention sometime by the end of the seventeenth century, and were well appreciated by the eighteenth century. By the beginning of the nineteenth century the reports of John Blackall and Richard Bright provided new insight by differentiating dropsy into that of cardiac and renal origins. The role of salt, initially measured and thought in terms of its anion chloride, began to be appreciated by the middle to late nineteenth century. Its mobilization, however, remained problematic. The "cure de dechloruration", which gained fame by the end of the nineteenth century, was not always a successful undertaking. The treatment of dropsy, which centered on augmenting secretions (diaphoretics, purgatives) or mechanical removal of body fluids (bleeding, leeching, lancing), remained a frustrating and chancy undertaking for much of the time that medicine has had to deal with it. Although mercury had been advocated as a diuretic in the sixteenth century, even the organic mercurials that were introduced after World War II were limited in their effectiveness. The discovery of sulfanilamide-induced sodium bicarbonate diuresis in the late 1940s was to provide the first step in the new age of clinically effective diuretics, which began in the 1950s with the introduction of chlorothiazide, the first orally effective agent to mobilize sodium chloride. The subsequent introduction of more potent diuretics was made possible by concurrent advances in renal physiology and the understanding of the sodium handling by the kidney.

Diuretics↗

PubMed1976

[On the development of oral preparations of the combination sulfamoxole/trimethoprim (CN 3123) (author's transl)].

Within the broad range of activities in pharmaceutical research, the technological development and analytical evaluation of a new drug formulation represent only one step. The pharmaceutical development of three oral formulations of a combination product containing N1-(4,5-dimethyl-2-oxazolyl)-sulfanilamide (sulfamoxole) and 2,4-diamino-5-(3,4,5-trimethoxy-benzyl)-pyrimidine (trimethoprim) in a 5:1 ratio (investigational drug CN 3123; Nevin; Supristol), which was based on the physico-chemical characteristics of the 2 active substances, is presented. The various chemical and physical tests conducted with the drug formulations are described. The pharmaceutical or in-vitro availabilities (dissolution rate) of the active ingredients were determined by way of release-rate profiles, both of the active ingredients alone and in their final formulations. Also presented are the results of plasma level determinations following oral administration of film-coated tablets and a suspension. Finally, preliminary results of extensive stability tests with the three drug formulations are discussed.

Administration, Oral↗

PubMed1976

[Antimicrobial action of the combined preparation sulfamoxole/trimethoprim in vitro (author's transl)].

A number of different methods were used to test the in vitro antimicrobial activity of the combination of N1-(4,5-dimethyl-2-oxazolyl)-sulfanilamide (sulfamoxole) and 2,4-diamino-5-(3,4,5-trimethoxy-benzyl)-pyrimidine (trimethoprim). 1. The minimum bacteriostatic inhibitory concentratiions of the sulfamoxole/trimethoprim combination (5 + 1) (CN 3123; Nevin; Supristol) were determined for 131 gram-positive and gram-negative strains of bacteria. More than 88% of the strains tested were found to be highly sensitive to the combination (M1C 0.1-3.75 mug/ml). 2. Comparative studies with the combinations sulfamoxole/trimethoprim and sulfamethoxazole/trimethoprim revealed no relevant differences of the M1C-values. 3. The synergistic effects of sulfamoxole and trimethoprim can be demonstrated with the aid of the agar dilution and agar diffusion tests using various types of bacteria and different ratios of sulfamoxole and trimethoprim. 4. Results obtained by studies on growth kinetics also demonstrate the synergistic and potentiating effect of combining sulfamoxole with trimethoprim and bactericidal properties are achieved.

Bacteria↗

PubMed1976

[Experimental studies on the effect of the combination sulfamoxole/trimethoprim on the Toxoplasma infection of the mouse (author's transl)].

Albino mice infected with Toxoplasma gondii (virulent strain BK) were treated for 20 days with a combination of N1-[4,5-dimethyl-2-oxazolyl]-sulfanilamide (sulfamoxole) and 2,4-diamino-5-(3,4,5-trimethoxy-benzyl)-pyrimidine (trimethoprim) in the ratio of 5:1 (trial preparation CN 3123; Nevin, Supristol). By the suitable dosage the mortality rate could be reduced considerably. In contrast to the untreated controls no antibodies were formed. No cysts could be detected in the brains of treated animals. Compared with the combination of trimethoprim/sulfamethoxazole the combination of trimethoprim/sulfamoxole showed a slightly better effect.

Animals↗

PubMed1976

[Pharmacological investigations with the combination sulfamoxole/trimethoprim, a new broadspectrum chemotherapeutic agent (author's transl)].

Investigations were conducted with the combination of N1-(4,5-dimethyl-2-oxazolyl)-sulfanilamide (sulfamoxole) and 2,4-diamino-5-(3,4,5-trimethoxy-benzyl)-pyrimidine (trimethoprim) (CN 3123, Nevin, Supristol) in a dose ratio of 5:1, with respect to pharmacological activity and possible side effects. The effects obtained with the combination CN 3123 were compared with those of the single substances. In a dose range comparable to that as used in clinical treatment, there were no effects on cardiovascular or respiratory functions, on functions of autonomic and central nervous system, on contractility of smooth muscles and on data of clinical chemistry such as urine and electrolyte excretion, blood sugar, blood coagulation and liver function tests. Doses which are 5 to 10 times higher than the initial dose or 10 to 20 times higher than the maintenance dose used in man caused an increase of urine and sodium excretion without influencing potassium and chloride output. There were no signs of sedation as alteration of motility or EEG patterns, but in mice and rats there was an increase in both duration and depth of anaesthesia caused by barbiturates or ether. Only in a dose range 30 to 40 times higher than the initial dose for man there were some slight alterations with respect to cardiovascular system and liver function tests. In vitro, with high concentrations of CN 3123 there was a weak, unspecific spasmolytic effect on the isolated ureter and an increase in the refractory period of the guinea pig atrium. There were no hints that the side effects seen with separate administration of high or very high doses of sulfamoxole or trimethoprim were increased or poteniated by their simultaneous administration. Slight side effects in animals were only observed with doses exceeding the tenfold of the doses for therapeutic use in men. Therefore, the therapeutic range of CN 3123 seems to be more than adequate.

Animals↗

PubMed1976

[Toxicological investigations of the combination sulfamoxole/trimethoprim, a new broad-spectrum chemotherapeutic (author's transl)].

The chemotherapeutically effective 5:1 combination N1-(4,5-dimethyl-2-oxazolyl)-sulfanilamide (sulfamoxole) and 2,4-diamino-5-(3,4,5-trimethoxy-benzyl)-pyrimidine (trimethoprim) (CN 3123, Nevin, Supristol) was investigated to determine any evidence of toxicological potentiation or new toxic signs. It was found that CN 3123 had a very low acute toxicity when administered orally to mice, rats and dogs (oral LD50: mouse greater than 12 000 mg/kg; rat greater than 14 000 mg/kg; dog greater than 1000 mg/kg body weight). The combination was also tolerated by rats and dogs in repeated doses administered over a period of 4 or 26 weeks, that greatly exceeded the therapeutic dose. The only change observed occurred in the thyroid, which in all doses administered exhibited a dose-related increase in weight accompanied by histological changes indicating an activation of thyroid function and a hypersecretion of basophilic thyrotropic cells in the anterior lobe of the pituitary. Six weeks after discontinuation of treatment this condition showed a tendency to reversibility or had already returned to normal. In dogs there was a dose-related increase in iodine uptake by the thyroid and a decrease in serum thyroxine over a period of 6 months under the highest dosage of CN 3123 administered. Whereas the thyroid changes observed under the combination could be reproduced with sulfamoxole, no effect on thyroid weight was observed in rats and dogs in the subacute toxicity phase of a comparative investigation with trimethoprim. Moreover, trimethoprim did not increase the effect of sulfamoxole on the thyroid gland. The effect of sulfamoxole on the thyroid is discussed in detail with a review of the literature. It can be characterized as species-specific for sulfonamides in mice, rats, rabbits and dogs but not in monkeys or in man and appears to be caused by the inhibition of the organic binding of iodine in the thyroid, whereby the predisposing factors must vary considerably from species to species. The thyroid hypertrophy observed is due to the activation of the regulatory cycle via the anterior lobe of the pituitary. The following systemic changes occurred after 600 mg CN 3123/kg, a lethal-toxic dosage and the highest administered in the study: reduced body weight, decreased food consumption leading to cachexia, slightly increased SGPT and alkaline phosphatase, slight thrombocyte depression, enlargement and increased fatty degeneration of the liver, occurrence of necrotic areas in the liver, hemosiderin accumulation in Kupffer's cells, and an increase of reticular cells in the spleen. The acute toxicity of CN 3123 and all major functional and histological changes under repeated administration were due exclusively to sulfamoxole. The combination sulfamoxole/trimethoprim gives no indication of toxicological potentiation or new toxic signs.

Animals↗

PubMed1976

[Investigations on the effect of the combination sulfamoxole/trimethoprim on fertility and fetal development in rats and rabbits (author's tranls)].

The chemotherapeutically active combination of N1-(4,5-dimethyl-2-oxazolyl)-sulfanilamide (sulfamoxole) and 2,4-diamino-5-(3,4,5-trimethoxy-benzyl)-pyrimidine (trimethoprim) in a dose ratio of 5:1 (CN 3123, Nevin, Supristol) was investigated, with respect to teratogenicity, effects on fertility and reproduction and influence on peri- and post-natal development. Experiments with the combination and partly with the single substances were done on Sprague-Dawly and Wistar rats and on rabbits (New Zealand White). With regard to the known effects of trimethoprim in this field--fetal malformations typical of those caused by folic acid antagonists--it was to clarify whether or not potentiation phenomena or new toxic effects occur with the combination. The results were as follows: 1. CN 3123 is teratogenically and fetotoxically active when given in very high doses to pregnant rats and rabbits during the critical phase of organogenesis (day 8-15 of pregnancy in rats, day 8-14 in rabbits). There were malformations, decrease in the number of pups and an increase in the number of absorption sites. Litter size and litter weight were reduced. The malformations observed were cleft palates, rarely cleft lips, micrognathies and shortening of limbs. Doses up to 180 mg/kg CN 3123, corresponding to more than tenfold the daily maintenance dose in man, were without any effects on all parameters observed. Toxic effects were observed in Sprague-Dawley rats at a dose level of 420 mg/kg and in Wistar rats with 600 mg/kg, corresponding to the effects seen following 100 mg/kg of trimethoprim alone. Sulfamoxole in the corresponding dose of 500 mg/kg caused no embryotoxic effects in the rat. In rabbits 600 mg/kg CN 3123 induced no malformations but increased fetal loss. Therefore it can be concluded, that the teratogenic and fetotoxic effects seen with high doses of CN 3123 are due to the amount of trimethoprim in the combination. The observed effects with the combination are quantitatively related to those seen with trimethoprim. 2. CN 3123 in high doses which are teratogenic also provoked a reduction of growth of the animals. Food consumption and weight gain were reduced in dams with 420 and 600 mg/kg CN 3123. In this dose range the pup weights and the weight gain of the offspring of dams with continued dosing during lactation were also reduced. Variation rate including retardations was increased. The depressing effect of CN 3123 in high doses on food consumption and weight gain is known from long-term toxicological studies previously described [7]. 3. CN 3123 even with high doses has no effects on the fertility of male and female rats. The number of corpora lutea and implantations and also the pregnancy rate were unaffected when either the female or the male rats used for mating had been treated. There was also no influence on mating activity of the male animals treated. 4. According to the results of the fertility study with treatment of the male rats for a period of ten weeks or more there were no signs of mutagenic effects due to CN 3123.

Abnormalities, Drug-Induced↗

PubMed1976

[Pharmacokinetic studies with the combination sulfamoxole/trimethoprim in animals and men (author's transl)].

The pharmacokinetics of the 5:1 combination of N1-(4,5-dimethyl-2-oxazolyl)-sulfanilamide (sulfamoxole) and 2,4-diamino-5-(3,4,5-trimethoxy-benzyl)-pyrimidine (thrimethoprim) (CN 3123, Nevin, Supristol) corresponds to the well known data of the single substances. Investigations on blood level, concentration in plasma water and excretion via urine and bile were done on experimental animals and with therapeutic dosage (single and repeated administration) on men. There were no alterations of the kinetics of the single substances due to drug interaction during simultaneous administration, neither qualitatively nor quantitatively. The dosage schedule elaborated is as follows: dosage interval=12 h, ratio initial dose: maintenance dose=2:1. For adults this regimen with a maintenance dose of 400 mg sulfamoxole and 80 mg trimethoprim results in a steady state of the minimal concentrations immediately before the following dose. These minimal concentrations in plasma water exceed the minimal inhibitory concentrations determined in vitro for most pathogens by several times.

Administration, Oral↗

PubMed1976

[Studies on the antibacterial activity of the combination sulfamoxole/trimethoprim (CN 3123) (author's transl)].

After giving a survey on the situation of antibiotic resistance in the region of Northern Bavaria during 1973/74 and comparing the activity of a sulfamethoxazole (SMZ) trimethoprim (TMP) combination to other commonly used antibiotics and chemotherapeutic agents, the results of tests with the new combination of N1-(4,5-dimethyl-2-oxazolyl)-sulfanilamide) (sulfamoxole) and 2,4-diamino-5-(3,4,5-trimethoxy-benzyl)-pyrimidine (trimethoprim) at a ratio of 5:1 (CN 3123; Nevin, Supristol) are compared to those of tests with TMP/SMZ. This was done by correlating the inhibition zone diameters and, on the other hand, by referring to a great number of sensitivity evaluations in routine diagnostic tests. According to the size of the inhibition zone, CN 3123 showed a somewhat greater activity on Enterococcus (fecal streptococci), Escherichia coli, and Klebsiella aerogenes, whereas the TPM/SMZ combination had apparently a stronger antibacterial effect in vitro against Proteus mirabilis, Staphylococcus aureus, and the Achromobacter-group. Analysis of sensitivity readings from routine diagnosis demonstrated accordance of CN 3123 with TMP/SMZ in 92.6% (first series) and 94.2% (second series), respectively. These results should be considered critically in view of the manifold factors which influence sensitivity tests in the agar diffusion method.

Anti-Bacterial Agents↗