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[Bacteriological, pharmacokinetic and clinical studies of cefpirome in the field of pediatrics].

Bacteriological, pharmacokinetic and clinical studies on cefpirome (CPR, HR 810), a new cephem antibiotic, were carried out in the field of pediatrics. The results obtained are summarized below. 1. Antibacterial activities of CPR against clinically isolated strains of Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Escherichia coli, Klebsiella pneumoniae, Haemophilus influenzae and Haemophilus parainfluenzae were superior to those of ceftazidime. 2. Plasma concentrations and urinary excretion rates after intravenous bolus injection of CPR at doses of 10, 20 and 40 mg/kg for 5 minutes in 2 cases each were determined. Mean peak plasma concentrations of CPR at these dose levels were 33.9, 62.9 and 96.0 micrograms/ml at 15 minutes with plasma half-lives of 1.58, 1.69, and 2.13 hours, respectively. Mean cumulative urinary excretion rates in the first 8 hours after administration were 51.2, 78.0 and 74.9%, respectively. 3. Ten patients with bacterial infections (pneumonia 5 cases, urinary tract infection 5 cases) were treated with CPR at a daily dose of 16-79 mg/kg/day. The overall clinical efficacy and bacteriological eradication rates were both 100%. 4. No adverse reactions were observed except in 1 case of mild pain in blood vessels. Abnormal laboratory test results were also mild, slight elevation of GOT, GPT and thrombocytosis in 1 case and eosinophilia in 1 case.

Adolescent↗

[Antimicrobial activity of cefpiramide to fresh clinical isolates].

In the subjects of 835 strains of 37 clinically isolated microbial strains, which were separated and identified among materials collected from patients with various infections and which were sent from medical therapeutic institutions throughout Japan in 1990, for the purpose of examining the antimicrobial activity of cefpiramide (CPM), its minimum inhibitory concentration (MIC), together with those of other cephem antibiotics, was determined, and the following conclusions were obtained. 1. Microbial strains in which no CPM-resistant strains emerged were Streptococcus pyogenes, Streptococcus pneumoniae and Anaerobic Gram-positive cocci. 2. In comparison with reports by many researchers at the former half of the 1980s, microbial stains suggesting an increase in resistance to CPM were Staphylococcus aureus, Proteus vulgaris, Pseudomonas aeruginosa, Pseudomonas cepacia, Pseudomonas putida, Acinetobacter calcoaceticus, and Haemophilus influenzae, but also in other microbial strains the resistance to CPM was observed in high ratios. 3. Among strains used in the test, methicillin-resistant S. aureus, cephamycin and oxime type cephalosporin-resistant Gram-negative bacilli of Enterobacteriaceae, and new quinolone-resistant microbes were observed in high ratios; therefore, it was considered that CPM could not exert sufficient antimicrobial activities to these strains because of many resistant strains being complicated among these "CPM-resistant strains". 4. It was discussed that "the resistance mechanism observed throughout beta-lactam drugs as a while and the study themes in the dimension including social circumstances where resistant strains emerged", as pointed out by the authors in 1989, increased the significance of these days in the evaluation of timecourse changes in microbes resistant to specific drugs including CPM. 5. There are many unfavorable conditions in the antimicrobial activities of CPM to clinically isolated strains in recent years. However, it was jointly confirmed that CPM maintained effective antimicrobial activities to the majority of clinically isolated strains. Furthermore, when it was additionally considered that CPM was one of not many cephem drugs having persistent blood levels, a conclusion was drawn that CPM was one of clincally useful cephem drugs even at present.

Anti-Bacterial Agents↗

[Susceptibilities of clinical bacterial isolates to antimicrobial agents. A study mainly focused on imipenem. Research Group for Testing Imipenem Susceptibility on Clinical Isolates].

We investigated susceptibilities of clinical bacterial isolates to imipenem (IPM) and other antimicrobial agents at 459 hospital laboratories throughout Japan from September to December of 1988. In this study, identification and susceptibility testing were performed at each hospital laboratory and the tests were carried out according to the 1-dilution or 3-dilution disc technique in which susceptibilities are classified into 4 grades: , ++, + and -. IPM had significantly high activity against Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Neisseria gonorrhoeae, Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter cloacae, Salmonella spp., Citrobacter freundii, Proteus mirabilis, Providencia rettgeri, Acinetobacter calcoaceticus, Moraxella catarrhalis, Alcaligenes spp., Peptococcus spp./Peptostreptococcus spp., Bacteroides fragilis and Bacteroides spp. and should slightly lower activities on coagulase-negative staphylococci (CNS), Enterococcus faecalis, Haemophilus influenzae, Serratia marcescens, Proteus vulgaris, Providencia stuartii and Pseudomonas aeruginosa than on the above mentioned bacteria. In a comparative study on activities of IPM against bacteria from different clinical sources, no remarkable differences were found due to different sources among S. pneumoniae, E. faecalis, H. influenzae, E. coli, K. pneumoniae, E. cloacae, C. freundii, P. mirabilis or A. calcoaceticus, whereas slight differences were found among Staphylococcus aureus, CNS, S. marcescens and P. aeruginosa.

Anti-Bacterial Agents↗

[Susceptibilities of clinical bacterial isolates to antimicrobial agents. A study mainly focused on imipenem. Reported by the Research Group for Testing Imipenem Susceptibility on Clinical Isolates].

This study was conducted to investigate susceptibilities of clinical bacterial isolates to imipenem (IPM) and other antibacterial agents at 64 hospital laboratories throughout Japan from September to December of 1988. In this study, identification and susceptibility testing were carried out at each laboratory and the tests were performed according to the disk dilution method recommended by NCCLS in which susceptibilities are classified into "S", "MS", "I" and "R". IPM showed markedly high in vitro activities against Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus faecalis, Haemophilus influenzae, Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter cloacae, Serratia marcescens, Salmonella spp., Citrobacter freundii, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii, Acinetobacter calcoaceticus, Moraxella (Branhamella) catarrhalis, Alcaligenes spp., Peptococcus spp./Peptostreptococcus spp., Bacteroides fragilis and Bacteroides spp. IPM also had strong activities against Achromobacter xylosoxidans and Pseudomonas aeruginosa, but less active against Flavobacterium spp., E. faecium, coagulase-negative staphylococci (CNS), Staphylococcus aureus and Pseudomonas cepacia. In a study in which activities of IPM against bacteria isolated from different clinical sources were compared, differences in susceptibilities were observed among S. aureus, CNS, A. calcoaceticus and P. aeruginosa, but such differences were not apparent among S. pneumoniae, E. faecalis, H. influenzae, E. coli, K. pneumoniae, E. cloacae, C. freundii, S. marcescens or P. mirabilis.

Bacteria↗

[Reactivity to bacterial peptidoglycans in a phagocytosis system. The range of immunological specificity of Escherichia coli peptidoglycan].

The antigenic specificity of E. coli M17 peptidoglycans (PG) was studied in the test system based on the stimulation of neutrophils with PG opsonized with the whole and exhausted IgG fraction of human serum. Within the generic taxon, the PG under study were similar in their antigenic properties. The opsonic activity of IgG exhausted with the preparations of different E. coli strains decreased by 93.2-95.8%. An essential difference of E. coli PG from similar components of other representatives of the family Enterobacteriaceae was observed: in experiments with Serratia marcescens, Klebsiella pneumoniae, Proteus mirabilis, Proteus rettgeri the decrease of opsonic activity was 47.6-79.3%. After the removal of antibodies to PG of remote taxons (Staphylococcus aureus, Micrococcus luteus, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus faecalis, Branchamella catarrhalis) the decrease of the opsonic effect was less noticeable (9.7-33.8%). The results are discussed from the viewpoint of the immunological peculiarity of PG at different taxonomic levels.

Epitopes↗

[Pharmacokinetic, bacteriological and clinical studies on imipenem/cilastatin sodium in neonates].

Pharmacokinetic, bacteriological and clinical studies on imipenem/cilastatin sodium (IPM/CS) were performed in neonates. The results obtained are summarized as follows. 1. Plasma levels and urinary excretion of IPM and CS sodium were determined in 7 neonates with ages between 7 and 26 days (gestation periods were 37 to 41 weeks and birth weights were 2,410 to 3,890 g) upon 1 hour drip intravenous infusion of IPM/CS at 10 mg/10 mg/kg, or 20 mg/20 mg/kg. Mean plasma concentrations of IPM reached their peaks at the end of infusion with levels of 12.7 +/- 3.0 micrograms/ml for the group given 10 mg/10 mg/kg, and 19.1 +/- 4.1 micrograms/ml for 20 mg/20 mg/kg. The concentration of IPM in plasma showed a dose-response to the 10 mg/10 mg/kg and 20 mg/20 mg/kg dosages. Concentrations decreased with half-lives of 1.87 +/- 0.71 hours and 1.97 +/- 0.21 hours for the low and the high dosages, and plasma levels at 8 hours after administration were 0.3 +/- 0.1 microgram/ml and 0.8 +/- 0.3 microgram/ml, respectively. Mean urinary recovery rates in 8 hours after administration were 37.6 +/- 11.8% and 26.8 +/- 17.2% for the low and the high dosages. While, mean plasma concentrations and mean urinary recovery rates of CS were higher than those of IPM, mean plasma half-lives of CS were similar to IPM. 2. IPM/CS was administered to 11 neonatal patients (with ages between 1 and 26 days) of various bacterial infections, and clinical effectiveness, bacteriological efficacy and adverse reactions were evaluated. Clinical efficacies in cases including 7 with acute pneumonia and 1 each with suspected septicemia, intrauterine infection, acute urinary tract infection and periproctal abscess were judged excellent in 10 and good in 1 case, and the efficacy rate was 100%. Causative organisms isolated from these patients included 3 strains of Escherichia coli and 1 strain each of Streptococcus pyogenes, Streptococcus agalactiae Enterococcus faecalis and Haemophilus influenzae. All the organisms were eradicated by IPM/CS, thus the bacteriological eradication rate was 100%. No adverse reactions were observed, but decreased platelet in 1 patient and increased GOT in 2 patients were found as abnormal laboratory test values. These changes, however were transient, and returned to normal after discontinuation of IPM/CS. It was concluded that the clinical results of IPM/CS are indicative of excellent efficacy, safety and usefulness of the drug in the treatment of infections in neonates.

Anti-Bacterial Agents↗

[Laboratory and clinical studies on cefteram pivoxil in pediatric field].

Pharmacokinetic and clinical studies of cefteram pivoxil (CFTM-PI, T-2588) fine granules in children were performed and the following results were obtained. 1. Peak serum concentrations in 4 children given orally a dose of 3 mg/kg and 2 children given orally a dose of 6 mg/kg after meal were reached in 3 to 4 hours and the concentration curves were dependent on dosage levels. The urinary recovery rates up to 8 hours were 29.7% in children given a dose of 3 mg/kg and 29.7% in children given a dose of 6 mg/kg. 2. Clinical efficacies were evaluated in 38 patients with bacterial infections. Twenty seven patients were given each doses of 3 mg/kg in 3 times a day and other 11 patients each doses of 6 mg/kg in 3 times. Clinical effects of CFTM-PI were excellent in 18, good in 19, fair in 1 case, hence the overall clinical efficacy rate was 97.4%. 3. Bacteriologically, 24 strains of causative organisms were isolated. The overall bacteriological eradication rate was 81.8%. Antimicrobial activities were excellent especially against Streptococcus pyogenes, Streptococcus pneumoniae, and Haemophilus influenzae. 4. As for the side effects, slight loose stools were observed in 2 cases, and in laboratory tests, elevations of GOT and GPT were observed in 1 case and an elevation of eosinophil was observed in 1 case. But no one needed any treatment. 5. CFTM-PI is a useful and safe oral antibiotic for the treatment of bacterial infections in pediatrics.

Bacterial Infections↗

Preliminary report on the in vitro antibacterial activity of Bryophyllum pinnatum leaf juice.

The juice from the leaves of Bryophyllum pinnatum S. Kurtz (Crassulaceae) was tested for antibacterial activity. The extract at 5% v/v was bactericidal to a wide spectrum of Gram-positive and Gram-negative bacteria such as Bacillus subtilis, Staphyllococcus aureus, Streptococcus pyogenes; Streptococcus faecalis; Escherichia coli; Proteus spp; Klebsiella spp; Shigella spp; Salmonella spp; Serratia marcescens; and Pseudomonas aeruginosa including the clinical isolates of these organisms possessing multiple antibiotic resistance.

Anti-Bacterial Agents↗

[Pharmacokinetic, bacteriological and clinical studies of sultamicillin fine granule in pediatric field].

Pharmacokinetic, bacteriological and clinical studies on sultamicillin (SBTPC) fine granule were carried out in the field of pediatrics. The results obtained are summarized as follows. 1. Antibacterial activities of SBTPC against clinically isolated strains of Haemophilus influenzae, Haemophilus parainfluenzae, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Staphylococcus aureus, Branhamella catarrhalis, and Escherichia coli were compared with those of ampicillin (ABPC). SBTPC was superior to ABPC especially against beta-lactamase producing H. influenzae, E. coli, S. aureus, and B. catarrhalis. 2. Serum concentrations and urinary excretion rates of sulbactam (SBT) and ABPC after administration of SBTPC fine granule at a dose level of 10 mg/kg in 2 cases were determined. Mean half-lives of SBT and ABPC in the serum following oral administration were about 1.33 and 1.61 hours respectively. Mean urinary recovery rates of SBT and ABPC in 6 hours after oral administration at a dose of 10 mg/kg were 58.7% and 49.6% respectively. 3. SBTPC fine granule was administered to 20 pediatric patients with various bacterial infections (pneumonia 8 cases, bronchitis 2, pharyngitis 2, tonsillitis 4, subcutaneous abscess 1 and urinary tract infection 3). The overall clinical efficacy rate was 100% and the overall bacteriological eradication rate was 75%. 4. No adverse reactions were observed except 1 case of loose stool. No abnormal laboratory test values were observed. These results indicate the usefulness of SBTPC fine granule in the treatment of bacterial infections in children.

Adolescent↗

Once-daily administration of ceftriaxone for the treatment of selected serious bacterial infections in children.

Ceftriaxone treatment (50 to 80 mg/kg once daily) was given to 201 children between 1 month and 18 years of age. There were 201 serious bacterial infections, including epiglottitis, pneumonia, cellulitis, osteomyelitis, septic arthritis, pyelonephritis, sepsis, and meningitis. The common pathogens responsible for pediatric infections isolated from these patients included Haemophilus influenzae, Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, and Escherichia coli. The overall clinic cure rate was 94%. Ten patients were clinically improved but not cured. There were two clinical failures. Bacteriologic failure occurred in six patients. The overall bacteriologic cure rate was 97%. Twenty patients (10%) experienced adverse effects; none required discontinuation of therapy. The efficacy, safety, spectrum, and convenience of ceftriaxone monotherapy make this antimicrobial agent a candidate for the treatment of choice of selected serious pediatric infections.

Adolescent↗

[Pharmacological evaluation of an ampicillin suppository (KS-R1) in acute respiratory tract infection in children: a comparison with an oral form of ampicillin].

A comparative well-controlled study was performed to evaluate the efficacy and tolerability of ampicillin rectal suppository (KS-R1) compared with those of oral form of ampicillin (ABPC) against acute respiratory tract infections in pediatric field. KS-R1 at the dose of 125 mg X 4/day of ABPC in potency, or the oral form at the same dosage, was given to 166 cases of patients with acute respiratory tract infection due to Streptococcus pyogenes, Streptococcus pneumoniae or Haemophilus influenzae for 7 days, as a rule. The clinical efficacy rates evaluated in 151 cases (KS-R1 group in 77 cases, oral group in 74 cases) on standard criteria of committee members were 88.3% for the KS-R1 group and 86.5% for the oral group, respectively. There was no significant difference between 2 groups. Evaluation by stratification according to the diagnosis showed that the efficacy rates for the KS-R1 group and for the oral group were 87.5% and 85.0% against pharyngitis, 90.5% and 90.0% against tonsillitis and 84.2% and 78.6% against bronchitis, respectively. None of them showed significant difference between 2 groups. The bacteriological effect was evaluated in 55 cases (KS-R1 group in 33 cases, oral group in 22 cases), and disappearance rate was 93.9% for the KS-R1 group and 95.5% for the oral group, showing no significant difference. Side effect including subjective and objective symptoms were strictly evaluated in 163 cases (KS-R1 group in 83 cases, oral group in 80 cases), but the incidence rate which was 22.9% for the KS-R1 group and 23.8% for the oral group showed no significant difference. The above results indicate that against acute respiratory tract infections in pediatric field, KS-R1 possesses clinical efficacy and safety similar to the oral form of ABPC, and that it is a useful suppository.

Acute Disease↗

[Pharmacological evaluation of an ampicillin suppository (KS-R1) in acute pneumonia in children--a comparison with a parenteral preparation of ampicillin].

A comparative well-controlled study was performed to evaluate the efficacy and tolerability of KS-R1 (ampicillin (ABPC) rectal suppository) compared with those of intravenous injection of ABPC against acute bacterial pneumonia caused by ABPC-sensitive bacteria, such as Streptococcus pyogenes, Streptococcus pneumoniae and Haemophilus influenzae in pediatric field. KS-R1 at the dose of 250 mg X 4/day of ABPC in potency, or the intravenous injection at the dose of 125 mg X 4/day of ABPC in potency, was given to 68 cases of patients with bacterial pneumonia, aged between 10 months and 8 years and 2 months, for 7 days, as a rule. The clinical efficacy rates evaluated in 61 cases (KS-R1 group in 31 cases, intravenous group in 30 cases) on standard criteria of committee members were 93.5% for the KS-R1 group and 83.3% for the intravenous group, respectively. There was no significant difference between 2 groups. Evaluation by stratification according to the age showed that KS-R1 was significantly superior, the rate being 90.5% among the children from 1 year to 3 years in the KS-R1 group and 61.5% in the intravenous group. The bacteriological effect was evaluated in 16 cases (KS-R1 group in 7 cases, intravenous group in 9 cases), the disappearance rate was 100% for the KS-R1 group and 88.9% for the intravenous group, without significant difference. With regard to side effects, 66 cases (KS-R1 group in 35 cases, intravenous group in 31 cases) were strictly evaluated in relation to subjective and objective symptoms. As a result, no significant difference was noted between 2 groups in the incidence rate which was 17.1% for the KS-R1 group and 9.7% for the intravenous group. The above results indicate that against acute bacterial pneumonia in pediatric field, the KS-R1 at the dose of 250 mg X 4/day of ABPC in potency possesses clinical efficacy and safety similar to the intravenous injection at the dose of 125 mg X 4/day of ABPC in potency, and that it is a useful suppository.

Acute Disease↗

Five cephalosporins: pharmacokinetics and their relation to antibacterial potency.

In a group of adult volunteers, pharmacokinetic profiles of five cephalosporins were correlated with their minimal inhibitory concentrations (MICs90) against Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, and Enterobacter aerogenes. Subjects received the following intravenous regimens in a randomized, crossover fashion: (1) 0.5 gm, 1 gm, or 2 gm of cefazolin; (2) 2 gm of cephalothin; (3) 1 gm of cephapirin; (4) 1 gm of cefoxitin; or (5) 0.5 gm of cefamandole. The 500-mg dose of cefazolin produced serum concentrations that exceeded those of any of the other cephalosporins at 0.5, 1, 2, 4, and 6 hours after administration. The area under the curve for this dose of cefazolin was at least twice that of any of the other antibiotics. Two hours after a 500-mg dose of cefazolin, serum levels exceeded the MIC90 for all seven groups of pathogens; at six hours, the 500-mg dose of cefazolin continued to achieve serum levels above the MIC90 against the majority of bacterial groups. In contrast, at two hours after administration none of the other cephalosporins maintained serum levels above the MIC90 for all pathogens; at six hours, the levels of cephapirin were adequate to inhibit the two streptococci, but serum levels of all other cephalosporins were inadequate to inhibit any of the pathogens. These data indicate that a 500-mg dose of cefazolin maintains serum levels above the MICs90 longer than any of the other cephalosporins tested and support the use of a 500-mg dose of cefazolin every eight hours for surgical prophylaxis and treatment of most community-acquired infections. Such a comparatively low dosage offers substantial savings to both patient and hospital.

Adult↗

The antibacterial action of vancomycin.

Vancomycin inhibits the second stage of cell wall synthesis in susceptible bacteria. Furthermore, there is evidence that vancomycin also alters the permeability of the cell membrane and selectively inhibits ribonucleic acid synthesis. Stable L-phase variants are susceptible to vancomycin, but induction of bacterial L-phase variants with vancomycin is very difficult. Vancomycin is active against a large number of species of gram-positive cocci and bacilli, such as Staphylococcus aureus (including methicillin-resistant strains), Staphylococcus epidermidis (including multiply resistant strains). Streptococcus pneumoniae (including multiply resistant strains), Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus bovis, viridans group Streptococcus, enterococcus, Clostridium species, diphtheroids, Listeria monocytogenes, Actinomyces species, and Lactobacillus species. Antimicrobial activity can be enhanced with the combination of vancomycin and an aminoglycoside against S. aureus, S. bovis, enterococcus, and viridans Streptococcus. The combination of vancomycin and rifampin also has enhanced activity against S. aureus.

Actinomyces↗

Bacterial agents causing chronic suppurative otitis media.

Ear swabs from 350 patients with chronic otitis media attending different orthorhinolaryngological clinics at different hospitals and health centres in Benin City and Ekpoma in Edo State were screened for the presence of bacterial agents of chronic otitis media. Results revealed the presence of 19 different species indicating polymicrobial infections. Species isolated comprised Staphylococcus aureus (33.6%), Pseudomonas aeruginosa (19.3%), Proteus mirabilis (17%), Alcaligenes faecalis (6.2%) and Klebsiella aerogenes (4.3%). Others included Escherichia coli (3.3%), Proteus rettgeri (2.8%), and Staphylococcus epidermidis (2.2%), Klebsiella pneumoniae, Proteus vulgaris, Acinetobacter spp, Proteus morgani, Haemophilus influenzae, Providencia spp, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus faecalis, non-haemolytic streptococci and Diphotheroids, each accounted for less than 2% of isolates. The study also showed a higher prevalence of chronic otitis media among males (55.7%) than females (44.3%). Cases of chronic otitis media were highest among the age groups (0-5 years) with a prevalence rate of 50% and least among the 6-10 year age group with a prevalence rate of 14.9%. Antibiogram of isolates revealed marked sensitivities (over 90% of the isolates) to ciproxin, tarivid, rocephin and fortum whereas over 70% were resistant to penicillin and ampicillin. Results have indicated that Staphylococcus aureus, Pseudomonas aeruginosa and Proteus mirabilis are leading bacterial agents of otitis media and highlights the high risk involved in the use of penicillin, ampicillin, streptomycin, tetracycline, chloramphenicol, erythromycin, cloxacillin and septrin in the management of chronic otitis media in our locality.

Adolescent↗

Evaluation of minocycline and cefuzonam for antimicrobial activity against clinical isolates.

The Antibacterial activity of minocycline (MINO) and that of cefuzonam (CZON) were assessed with clinical isolates of 19 species, and compared with that of other antibiotics. MINO was highly active against methicilli-sensitive Staphylococcus aureus (MSSA), Neisseria gonorrhoeae, Moraxella (Branhamella) catarrhalis, Haemophilus influenzae, Helicobacter pylori, Flavobacterium meningosepticum, Acinetobacter calcoaceticus, Peptostreptococcus spp. and Propionibacterium acnes, but not as effective against methicillin-resistant Staphylococcus aureus (MRSA), Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas cepacia and Alcaligenes xylosoxidans. CZON was highly active against MSSA, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus pneumoniae, N. Gonorrhoeae, M(B). catarrhalis, H. influenzae, H. pylori, P. mirabilis, Peptostreptococcus spp. and P. acnes, but not effective against MRSA. It was minimally active against Gram-negative rods (E. coli, K. pneumoniae, etc.) and bacteria that do not ferment glucose.

Bacteria↗

Comparative antimicrobial activity of lomefloxacin, norfloxacin, ofloxacin, ciprofloxacin and enoxacin against > 500 bacterial isolates.

An agar dilution technique was used to compare the antimicrobial activities of lomefloxacin, norfloxacin, ofloxacin, ciprofloxacin and enoxacin against 544 strains of bacterial isolates. Among the five quinolone agents tested, ciprofloxacin was the most active. Enoxacin was the most active after ciprofloxacin against Escherichia coli, Enterobacter aerogenes, Proteus mirabilis, Shigella spp., Yersinia enterocolitica, and Haemophilus influenzae with an MIC90 of < or = 0.25 micrograms/ml. Ofloxacin was the most active agent after ciprofloxacin against Klebsiella pneumoniae, Enterobacter cloacae, Citrobacter diversus, and Legionella pneumophila with an MIC of < or = 0.25 micrograms/ml. Ciprofloxacin inhibited Staphylococcus spp. and Streptococcus spp., at < or = 0.5 micrograms/ml and 2 micrograms/ml, respectively. Norfloxacin and enoxacin had the same antimicrobial activity (MIC90) against Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus agalactiae and some other Gram-positive species, but these activities were weak when compared with ciprofloxacin. The results of this in vitro study show that ciprofloxacin is very active against Gram-negative and Gram-positive species.

Anti-Infective Agents↗

Antibiotics and bacterial resistance. A few elements of genetic basis for this relationship.

In the preantibiotic era, many people died of bacterial infections caused by such pathogens as Staphylococcus aureus and Streptococcus pyogenes, Streptococcus pneumoniae and Mycobacterium tuberculosis. Antibiotics have reduced the mortality from infectious diseases but not the prevalence of these diseases. It was not long after the clinical introduction of the first antibiotics in the 1950s that the first reports of bacterial resistance began to appear. Use, and often abuse or misuse, of antimicrobial agents has encouraged the evolution of bacteria toward resistance, resulting often in therapeutic failure. In the beginning, new antibiotics have always appeared in plenty of time to provide new cures for diseases caused by resistant bacterial pathogens. Also, some clinically important groups of bacteria showed no signs of major increases in resistance. For example, S. pneumoniae strains remained susceptible to penicillin long after other bacteria had become resistant to it. Recent developments of bacteria resistance to antibiotics are indeed disquieting.

Bacterial Infections↗