Search PubMed⌕ Search

Biomedical subjects

A Bryskier

Publications and source records attributed to A Bryskier.

At least 109 records · Page 6Linked to original sources
PubMed1985

[Sensitivity of obligate anaerobes to ofloxacin, pefloxacin, enoxacin and norfloxacin].

The in vitro activity of four new quinolones against 355 obligate anaerobes was investigated. MICs were determined using the reference method of Sutter et al. [14]. The four fluorinated quinolones tested differ from nalidixic acid which is inactive on most anaerobes except for some Clostridium perfringens strains. All strains tested were inhibited by 64 and 16 mg/l pefloxacin and ofloxacin respectively. Except for Bacteroides, all strains were inhibited by 64 mg/l norfloxacin or enoxacin. Clostridium strains other than C. perfringens exhibited heterogeneity; C. difficile and C. ramosum had the highest MICs. Bacteroides fragilis proved less susceptible to fluorinated quinolones than the other obligate anaerobes. Ofloxacin showed the greatest activity, with 4 mg/l inhibiting 100% of C. perfringens and 83% of all anaerobes investigated.

Bacteria, Anaerobic↗
PubMed1985

Ofloxacin: antibacterial activity, induction of resistance and killing curves.

The antibacterial activity of ofloxacin was compared to that of nalidixic acid, norfloxacin and against various strains. This new quinolone was about 100 times more active than nalidixic acid, and pipemidic acid and generally 2 to 4 fold more active than norfloxacin and pefloxacin except against Pseudomonas aeruginosa. The increase of resistance to ofloxacin, norfloxacin and pefloxacin seems to plateau, usually at about 16 times the initial MIC. The bactericidal activity of ofloxacin also appeared quickly and more rapidly than that of norfloxacin.

Anti-Bacterial Agents↗
PubMed1985

[Clinical evaluation of cefmenoxime in urinary tract and prostatic infections].

Cefmenoxime, a new cephalosporin, was given to fifty patients (28 male and 22 female) aged 15 to 86 years with infection of the urinary tract or prostate. Urinary tract infections, i.e. cystitis in 20 cases and pyelonephritis in 21, were usually chronic and associated with urologic anomalies. Nine patients had infection of the prostate. Pathogens recovered from the urine were 26 E. coli, 8 Klebsiella, 16 Serratia, 5 Proteus mirabilis or indole-positive Proteus, 1 Providencia, and 4 Pseudomonas. Minimal inhibitory concentrations of cefmenoxime ranged from 0.015 to 64 micrograms/ml (mean MIC: 0.12 micrograms/ml). Cefmenoxime was given as single drug therapy in all patients but one, in a daily dosage of 2 g divided into two intramuscular injections, for 3 to 28 days (average 22 days). Follow-up after discontinuation of treatment was four weeks. Therapeutic results were as follows: 13 successes and 7 failures by relapse for the 20 cystitis patients, 13 successes and 7 failures by relapse for the 20 interpretable cases of pyelonephritis, and 4 successes and 5 failures by relapse for the 9 patients with prostate infection. Local tolerance was excellent. Skin rash in 2 patients and diarrhea in 1 required withdrawal of the drug. Three other patients with diarrhea were able to continue treatment. Intolerance to ingestion of alcoholic beverages was reported by 10 patients. Hypereosinophilia was recorded in 2 cases and a transient mononucleosic reaction in one. No renal of hepatic side effects were documented.

Adolescent↗
PubMed1985

[Cefmenoxime diffusion into cerebrospinal fluid during human purulent meningitis].

We treated 10 patients with bacterial meningitis by 150 mg/kg/day cefmenoxime divided into six intravenous infusions. CSF samples were taken one hour after an IV on the second and fifth days. CSF cefmenoxime determined by microbiologic assay was 8.3 mg/l on days 2 and 5. Every patient recovered without sequelae. In our opinion, these results may support use of cefmenoxime in bacterial meningitis.

Adult↗
PubMed1985

[In vitro antibacterial activity of cefodizime (HR 221) on 323 hospital strains of Gram negative bacilli. Comparison with cefotiam, cefoperazone, cefotetan and cefotaxime].

In vitro activity of a new cephalosporin, cefodizime, was investigated by comparison with cefotiam, cefoperazone, cefotetan and cefotaxime. 291 Enterobacteriaceae strains belonging to 6 cephalosporin-resistance phenotypes and 32 strains of oxidative Gram negative bacilli were tested. With modal MICs of 0.25 to 4 mg/l, cefodizime is active on most phenotypes of resistance to first or second generation cephalosporins demonstrated in vitro in Enterobacteriaceae, including strains resistant to cefamandole and intermediate to cefoxitin. Cefodizime fails to inhibit strains resistant to third generation cephalosporins (E. cloacae, C. freundii, P. stuartii), except for those strains of S. marcescens belonging to this phenotype whose modal MIC is 4 mg/l. 85% of all tested Enterobacteriaceae are inhibited by 4 mg/l and 91% by 8 mg/l. Cefodizime exhibits little activity against A. calcoaceticus and P. aeruginosa. Comparison of activities of the five cephalosporins against Enterobacteriaceae shows that cefodizime out-strips cefotiam, cefoperazone and cefotetan as a result of its broader spectrum of activity against tested species. Cefotaxime, on the contrary, proves superior to cefodizime and is still the most potent drug against. A. calcoaceticus whereas cefoperazone has the greatest effectiveness against P. aeruginosa.

Cefoperazone↗
PubMed1985

[RU 28965, a new semi-synthetic macrolide. Bioavailability and pharmacokinetic profile after oral administration].

The plasma concentration of RU 28965, a new semisynthetic macrolide, was monitored for 24 h after single 400 mg oral doses in 8 healthy volunteers. Four tablet formulations were compared in a 4 X 4 latin square design, to assess the influence of micronization and enteric coating on bioavailability. Plasma samples were assayed for unchanged RU 28965 using HPLC. Extent of absorption was equivalent for all four formulations. Micronization did not significantly affect absorption characteristics, while enteric coating resulted in slower absorption. In the second part of the study, plasma concentration was monitored for 72 h after a single oral dose of two 150 mg non-coated, non-micronized tablets in another group of 12 subjects. The following pharmacokinetic parameters were found (m +/- sem) : cmax = 11.8 +/- 0.3 microgram.ml-1, AUC = 132 +/- 17 microgram.ml-1.h, t 1/2 = 12 +/- 0.5 h.

Absorption↗
PubMed1985

[Cefpirome (HR 810). A new broad spectrum cephalosporin].

HR 810 or cefpirome is a new 2-amino-thiazol cephalosporin whose salient characteristic is a bicyclic nucleus, namely cyclopenteno-pyridinium, in position 3. This nucleus imparts a broad spectrum of activity that includes Enterobacteriaceae, Staphylococcus aureus, Pseudomonas aeruginosa, Neisseria, non-D Streptococcus and Haemophilus. Cefpirome is also active, although to a lesser extent, against Streptococcus faecalis and Acinetobacter.

Bacteria↗
PubMed1985

[HR 810 (cefpirome). Experimental evaluation of the in vitro and in vivo antibiotic activity of a new amino-2-thiazole methoxy- imino cephalosporin].

HR 810 or cefpirome is a new amino thiazole cephalosporin whose specific characteristic is a cyclopentenopyridinium group in position 3 of the cephem nucleus. This structure is responsible for a broad spectrum of activity, covering Enterobacteriaceae, including cephalosporinase-producing Enterobacter spp. and Citrobacter spp., Staphylococcus aureus, Pseudomonas aeruginosa and group D Streptococci.

Animals↗
PubMed1985

[Comparative bacteriologic activity of norfloxacin, ofloxacin and pefloxacin against 320 Gram-negative bacilli resistant and non-resistant to nalidixic acid and cephalosporins].

Bacteriostatic and bactericidal effects of three fluoroquinolones, norfloxacin, ofloxacin and pefloxacin, against 320 strains of Gram-negative bacilli were studied in vitro. For nalidixic acid-susceptible Enterobacteriaceae, susceptibility or resistance to second or third generation cephalosporins has no significant bearing on the MIC 90 of each of the three antibiotics. This is not so of nalidixic acid-resistant strains. All E. coli and K. pneumoniae strains are susceptible to the three quinolones (MIC 90 less than 3 mg/1); MICs 90 are higher for E. cloacae and S. marcescens; Serratia strains in particular have an MIC 90 greater than 6 mg/1. Nalidixic acid-susceptible Acinetobacter strains can be eliminated by ofloxacin or pefloxacin, whereas norfloxacin has the greatest activity against P. aeruginosa. We conclude that when multiresistant bacteria emerge, testing of susceptibility to the three quinolones studied may be useful.

Acinetobacter↗
PubMed1985

Behaviour of cefmenoxime towards beta-lactamases.

Using several well-characterized beta-lactamases isolated from Gram-negative bacteria, the interactions of cefmenoxime, a new methoxy-imino-amino-2-thiazol cephalosporin were compared with those of cefotaxime, lamoxactam, cefoperazone and ceftazidime. On-line computerized microacidimetry allowed determination of the affinity of these compounds for the enzymes, which was characterized by Ki values. Microacidimetry showed poor interactions of cefmenoxime with penicillinase TEM-1 (low Vm, poor affinity) whereas it showed a high affinity for the cephalosporinases, as is also the case for cefotaxime or lamoxactam. Both cefmenoxime and cefotaxime showed relative susceptibility in Masuda's double disc technique.

Cefmenoxime↗
PubMed1984

Affinity of cefmenoxime for beta-lactamases: an analysis.

The interactions of cefmenoxime with beta-lactamases in comparison with cefotaxime, moxalactam, cefoperazone, and ceftazidime have been determined. On-line computerized microacidimetry allowed determination of the affinity of these compounds with the enzymes, which was characterized by Km values. The beta-lactamases that were used were two cephalosporinases and one penicillinase. Within these data, the cephalosporins could be classified into three groups: (1) those with high affinity for the cephalosporinases and very poor affinity for the penicillinase (cefmenoxime, cefotaxime, and moxalactam); (2) those with moderate affinity for the cephalosporinases and very poor affinity for the penicillinase (ceftazidime); (3) those with poor affinity for all enzymes (cefoperazone). In the case of the penicillinase (TEM-1), only cefoperazone was subject to some hydrolysis.

Bacteria↗
PubMed1984

Pharmacokinetic study of cefmenoxime (SCE 1365-CMX) in healthy adults.

Cefmenoxime pharmacokinetics were investigated in six healthy volunteers after intravenous and intramuscular administration of 0.5, 1, and 2 g. Blood and urine samples were analyzed by reversed-phase high-pressure liquid chromatography using ultraviolet detection at 275 nm. The assay is precise and linear up to 200 micrograms/ml-1, with 0.02 micrograms/ml-1 as the limit of detection. Linearity of cefmenoxime kinetics was demonstrated because the area under the plasma concentrations is proportional to studied doses. Eight hours after 1 g of cefmenoxime intramuscularly, mean plasma concentrations are, respectively, 0.6 +/- 0.1 and 0.3 +/- 0.1 microgram/ml-1. Intramuscular cefmenoxime is rapidly absorbed (Ka = 7.28 hours-1) with complete bioavailability (F = 0.99); apparent volume of distribution is 0.35 liters/kg-1 and elimination half-life 1.5 hours. The fraction of cefmenoxime excreted unchanged in the urine after intramuscular administration is 0.72, indicating a major contribution of renal clearance in total clearance. Experimental data after intramuscular administration were well fitted with a two-compartment model.

Adult↗
PubMed1984

Pharmacokinetics of cefotiam administered intravenously and intramuscularly to healthy adults.

We studied the pharmacokinetics of cefotiam, a parenteral cephalosporin, at intravenous doses of 0.5, 1, and 2 g and intramuscular doses of 0.5 and 1 g in two groups of eight healthy adult volunteers. The concentrations of cefotiam in plasma were determined over a period of 5 or 6 h and in urine over 24 h, using high-pressure liquid chromatographic procedures. Plasma concentration-time data were fitted to a three-exponential equation for the intravenous administration, and after intramuscular administration, the data were analyzed by a two-compartment or a one-compartment open model. Over the above dosing range and routes of administration, cefotiam pharmacokinetics were essentially linear, with plasma clearances varying from 19.6 to 22.5 liters/h. No significant differences were observed with respect to the terminal half-life (1 h) and the area under the curve versus the dose. Intramuscularly injected cefotiam was 63 to 74% available. The fraction of dose excreted unchanged in urine (0.50 to 0.67) indicated a substantial nonrenal mechanism of elimination. The apparent volume of distribution (about 30 liters) was higher than those of other parenteral cephalosporins.

Adult↗
PubMed1984

[Evaluation of the extravascular distribution of cefotiam (SCE 963) by the skin blister technic].

Extravascular diffusion of cefotiam was studied by a suction blister technique. Maximal cefotiam concentration in blister fluid (18.4 +/- 6.4 micrograms X ml-1) was found one hour after intravenous injection of a 1 g bolus. The area under the curve (AUC) of blister fluid concentrations was 35.4 micrograms X ml-1. Apparent elimination half-life from blister fluid was 0.72 hour. The AUC plasma/AUC blister fluid ratio approximated 1.

Adult↗
PubMed1984

[Bacteriologic, clinical and kinetic evaluation of cefmenoxime (SCE 1365) in the treatment of 68 cases of septicemia. A multicenter trial].

Cefmenoxime (SCE 1365), a new broad-spectrum, third generation cephalosporin was used in the treatment of 68 patients with bacteremia. Cefmenoxime was given as monotherapy to 63 patients in a mean daily dosage of 3 g (range: 1 to 6 g). 63 successes were recorded. Results were inconclusive in the remaining five cases. General and biological tolerance of cefmenoxime was excellent.

Adult↗
PubMed1984

Combination effect of cefmenoxime with four aminoglycosides on Enterobacteriaceae susceptible and moderately susceptible to this new cephalosporin.

The inhibitory combination effect of cefmenoxime with gentamicin, tobramycin, netilmicin and amikacin against 148 Enterobacteriaceae was compared using the checkerboard agar dilution technique. On average 41% of cefmenoxime-moderately susceptible (MIC between 2 and 32 micrograms/ml) or cefmenoxime-resistant (MIC greater than 32 micrograms/ml) strains were inhibited by synergistic, and 23,5% by partial synergistic cefmenoxime-aminoglycosides combinations. Against cefmenoxime-susceptible strains, these rates of synergy or partial synergy were twofold lower, but only one isolate was not susceptible to these combinations. The amikacin-cefmenoxime interaction was the most performant.

Amikacin↗
PubMed1984

[Transplacental passage of cefmenoxime].

The broad spectrum of activity of cefmenoxime, its beta-lactamase stability and its harmlessness for the fetus, confer upon this new cephalosporin, a possible efficacy in the treatment of obstetrical infections. This study was designed to evaluate the placental transfer of cefmenoxime. The study group consisted of 21 pregnant women undergoing a cesarian section. After a single IM injection of 1 g of cefmenoxime, samples of maternal blood and umbilical cord blood samples were both taken 1, 2, 3 or 4 hours after the injection, in order to evaluate the kinetics of the drug. Amniotic fluid samples were also taken at delivery. The results of the study showed : a peak level of 16 micrograms/ml in the maternal serum with a slow decrease and a residual value of 3.08 micrograms/ml at the 4th hour ; increasing levels of the drug in the cord blood, with a peak value of 4.8 micrograms/ml ; progressive diffusion of cefmenoxime in amniotic fluid, reaching the highest value of 4.7 micrograms/ml at the 3rd hour ; parallel kinetics of the drug in amniotic fluid and in cord blood. On the whole, this study showed a significant placental transfer of cefmenoxime, achieving therapeutic concentrations required against microorganisms responsible for obstetrical infections.

Cefmenoxime↗