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Impact of experimental trauma and niflumic acid administration on antimicrobials' concentration in serum and mandible of rats.

Administration of antibiotics and analgesics in surgery or trauma is of great importance for an effective treatment. Trauma, as stress stimulus, causes alterations in various functions of the organism as well as in drug pharmacokinetics. The aim of this study was to determine the effect of trauma upon the serum and bone levels of the antimicrobial ampicillin and cefapirin, with and without co-administration of a non-steroidal anti-inflammatory analgesic (NSAIDs). Fifty-six male Wistar rats were divided into two groups A (control) and B (experimental). Each group consisted of 4 subgroups (n=7) receiving ampicillin, ampicillin with niflunic acid, cefapirin, and cefapirin with niflunic acid. In group B traumatic injury was performed by incision (7 mm length) in the right cheek. The levels of the antibiotics were estimated by the inhibition zone of B. subtilis. An increase in antibiotic levels was observed in group B, being statistically significant only for cefapirin level in the mandible. Upon niflumic acid co-administration a statistically significant rise in serum ampicillin and mandible cefapirin levels was observed in both control and experimental groups (student t-test). It can be concluded that the combination of antibiotics and non-steroid antiinflammatory drugs (NSAIDs) may enhance the antibacterial drug concentration.

Ampicillin↗

[Activity of cefapirin against bacterial strains isolated from acute otitis media in children].

The antibacterial activity of cefapirin was tested against 210 strains isolated from the auricular exudate of childrens' acute otitis media. For 112 strains of Haemophilus studied (20% secreted a beta-lactamase), the MIC 50 and 90 of cefapirin were 2 and 4 mg/l respectively. Ten strains of Branhamella catarrhalis were tested (9 secreted a beta-lactamase) and the MIC ranged from 0.25 to 4 mg/l. Against Streptococcus pneumoniae, cefapirin has an extremely high activity with MIC 50 and 90 less than 0.06 mg/l. Of the strains of Staphylococcus aureus sensitive to meticillin, one had a MIC less than 0.06 mg/l, and 11 had a MIC = 0.25 mg/l. For 14 strains of Enterobacteriaceae studied, we obtained a MIC 50 of 8 mg/l and a MIC 90 of 32 mg/l. The results show that cefapirin is an antibiotic particularly suitable for the treatment of acute otitis media.

Anti-Bacterial Agents↗

A comparative study of cefotaxime sodium versus a combination of cefapirin and gentamicin in the prophylactic treatment of patients undergoing cholecystectomy.

This was a randomized open evaluation of claforan vs. combination treatment of cefapirin + gentamicin. Patients taking part in the study were randomized in 3 parallel groups: 3 x 1 g claforan given during a period of 24 h (regimen I) was compared to 1 x 1 g claforan given at the time of incision (regimen II) and to a combination of cefapirin + gentamicin given in divided doses for 5 days (regimen III). Sixty-five patients (31 males and 34 females) aged between 23 and 76 years, who underwent cholecystectomy, were included in the study. There were no significant differences between the study groups in terms of sex, age, height, weight, diagnosis, aggravating factors and clinical condition of patients. Sixty of sixty-five patients noted "cholelithiasis" as diagnosis. The majority of patients documented an acute exacerbation of chronic condition. Twenty-three patients documented concomitant diseases/conditions or aggravating factors. The most frequent were: Diabetes mellitus, jaundice and clonorchiasis. During the study no additional administration of antibiotics or other concurrent treatment was recorded. Tolerance of the test substances was noted as "good" by 63 patients and satisfactory in 2 patients. In 3 patients (one patient in each treatment group) a postoperative wound infection was documented. One patient from regimen II with wound infection, therefore, received more than 1 g claforan. Postoperative hemoglobin decreased in all 3 groups (p less than 0.05). BUN decreased in the regimen group I (p less than 0.05) and increased together with creatinine in the group of regimen III (p less than 0.05). No side effects were documented in any treatment groups. The use of a single or three doses of claforan was more convenient and simple than the combination regimen. Less laboratory adverse effects (renal function) were also noted in claforan treated patients than the combination of cefapirin + gentamicin group.

Adult↗

On the pharmacokinetics of cephalosporin antibiotics.

A review is given on the pharmacokinetic characteristics of some cephalosporin antibiotics. The use of the pharmacokinetic parameters serum concentration, serum protein binding, serum half life, and apparent volume of distribution as a basis for the selection of the clinically most effective cephalosporin derivative is discussed. It is concluded that these parameters must be used in conjunction with data on tissue distribution to specialized sites, and with information on antibacterial activity and toxicity.

Absorption↗

[Serum and mandible alterations of antibiotics levels under increased serum FFA].

The levels of three antibiotics (Cefapirin, Doxycycline, Gentamicin) were studied in an experimental model (swimming stress) with elevated serum FFA. Sixty Wistar rats were in three groups used divided. Each group consisted of 3 subgroups. The subgroups A and B were submitted in swimming stress procedure for 10 and 20 days. The subgroup C was the control group. Since stress increases the FFA the concentration of antibiotics in blood and bone are influenced. According to the estimation of the result the following were observed: 1) Increase of FFA in stress groups 2) Weight increase of adrenals in stress groups which means that the stress procedure was effective 3) Increase of cefapirin level 4) Increase of doxycyclin 5) Increase of gentamicin 6) Increase of haematocrite.

Animals↗

[Comparative study of 7 cephalosporins on "Staphylococcus aureus" by the method of population analysis (author's transl)].

Miscellaneous Staphylococcus aureus populations were tested with seven commercialized cephalosporins. The strains were divided in five groups according to the following criteria: penicillinase production or not: sensitivity to methicillin and cephalosporins; RB type resistance to methicillin; RH and RO type resistance to every beta-lactamine (according to Chabbert and Baudens). For each cephalosporin studied, the population cell analysis performed with these different groups showed the constant heterogeneous arrangement of the individual MIC. However, whatever the staphylococcus group, cephaloridine remains the antibiotic that inhibits the largest number of cells at lower concentration than other cephalosporins. In vitro results were compared with pharmacokinetic data of the different cephalosporins.

Cefazolin↗

Activity of beta-lactamase inhibitor sulbactam plus ampicillin against animal isolates of Pasteurella, Haemophilus, and Staphylococcus.

Antibiotic susceptibilities of Pasteurella sp, Haemophilus pleuropneumoniae, and Staphylococcus aureus isolates were determined. The combination of sodium sulbactam, a beta-lactamase inhibitor, and ampicillin had a synergistic effect against all ampicillin-resistant pathogens, rendering them susceptible to ampicillin. Studies of cell-free beta-lactamase from Pasteurella and Haemophilus isolates confirmed the presence of a constitutive penicillinase. Inhibitory concentrations of sulbactam-ampicillin were bactericidal, as demonstrated by killing curves. Ampicillin-resistant Pasteurella and Haemophilus isolates did not develop resistance to sulbactam-ampicillin when passed as many as 8 times in the presence of sublethal concentrations of sulbactam-ampicillin. The in vitro synergistic activity of sulbactam-penicillin also was seen in an in vivo synergistic response in mice challenge exposed to an ampicillin-resistant P haemolytica.

Ampicillin↗

[The clinical studies about side effects of sodium cefapirin in the stomatic infective diseases (author's transl)].

The clinical effects and side effects of administrating sodium cefapirin to the stomatic infective diseases were examined in twelve cases. The following are the main results: (1) The clinical results of the treatment were noted effective in one case, effective in nine cases and slightly effective in two cases. (2) The results of renal function tests were as follows: After the administration, it was observed that the values of Ccr test decreased in two cases, the values of PSP test decreased in one case, but the BUN values remained within the normal range in all cases. However, in all cases, no significant deviations were observed in the values of each test measured before and after the test. (3) The results of hepatic function tests were as follows. The values of GOT and GPT showed slight decrease in majority cases. However, the difference between pro and post values was within the normal range and no significant deviations were observed. (4) No side effects including drug allergy were observed in every cases.

Adult↗