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Query: UNIPROT:Q29983 (MIC)
 21,138 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Antibiotic-resistant pneumococci, especially penicillin-resistant strains, are being increasingly isolated. Pneumococci with intermediate penicillin-resistance (MIC 0.1-1.0 micrograms/ml) have been reported from many parts of the world over the past two decades, and highly resistant strains (penicillin MICs greater than or equal to 2 micrograms/ml) have also appeared. Infection may be acquired in the hospital or community, and nosocomial outbreaks may occur which require control measures to limit organism spread. Most infections occur in children with diminished host responses. Disease caused by pneumococci with intermediate penicillin-resistance may be treated with high doses of penicillin, but disease caused by highly resistant strains, especially meningitis, may require alternative therapy. Pneumococci resistant to sulfonamides, tetracyclines, erythromycin, lincomycin, clindamycin, chloramphenicol, aminoglycosides and rifampin have also appeared. Strains resistant to all the above-mentioned agents, including all beta-lactam antibiotics tested, have been reported from South Africa and Spain. Alternative therapy for resistant strains may include vancomycin, cefotaxime, cefoperazone, ceftriaxone and imipenem. Pneumococci isolated from sites suggestive of infection, especially blood and cerebrospinal fluid, should be routinely tested for penicillin-susceptibility.
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PMID:World-wide development of antibiotic resistance in pneumococci. 331 32

Fundamental and clinical studies were performed on a newly developed carbapenem antibiotic, imipenem/cilastatin sodium (MK-0787/MK-0791), and results were summarized as follows. The antibacterial activity of MK-0787 at an inoculum of 10(6) cells/ml against strains of S. aureus which were sensitive or resistant to cefazolin (CEZ), E. coli, P. mirabilis, K. pneumoniae, S. marcescens and P. aeruginosa were determined and compared with activities of ceftazidime (CAZ), CEZ, cefmetazole (CMZ), ceftizoxime (CZX), latamoxef (LMOX), cefamandole (CMD), cefoperazone (CPZ), cefsulodin (CFS) and piperacillin (PIPC). The peak MIC of MK-0787 was less than or equal to 0.024 micrograms/ml against S. aureus, which were sensitive or resistant to CEZ, 0.10 micrograms/ml against E. coli, P. mirabilis, or K. pneumoniae, 0.39 micrograms/ml against S. marcescens and 1.56 micrograms/ml against P. aeruginosa. The antibacterial activity of MK-0787 against these bacteria was, on the whole, superior to that of CAZ, CEZ, CMZ, CZX, LMOX, CMD, CPZ, CFS or PIPC. The pharmacokinetics of MK-0787/MK-0791 was studied in 10 children at dose levels of 10 mg/10 mg/kg and 20 mg/20 mg/kg by a 30-minute intravenous drip infusion. Maximum serum levels of MK-0787, at dose levels of 10 mg/10 mg/kg and 20 mg/20 mg/kg were 41.6 micrograms/ml and 72.9 micrograms/ml, respectively, at the end of infusion and 0.1 micrograms/ml at 6 hours, respectively, after drip infusion. The half-life of both dose levels was 0.9 hour. Mean peak serum levels of MK-0791, at dose levels of 10 mg/10 mg/kg and 20 mg/20 mg/kg, were 49.7 micrograms/ml and 87.0 micrograms/ml, respectively, with half-life of 1.1 and 0.6 hour, respectively. Urinary recovery rates of MK-0787 for 6 hours at dose levels of 10 mg/10 mg/kg and 20 mg/20 mg/kg, were 47.8-82.7% and 25.5-78.0%, respectively, and of MK-0791 for 6 hours were 51.7-93.4% and 40.3-94.4%, respectively. Twenty-four patients, including 1 with purulent meningitis, 1 with septicemia, 1 with pyothorax, 10 with bronchopneumonia, 7 with pyelonephritis and 4 with infections of cutaneous soft tissue were treated with MK-0787/MK-0791 at dose levels of over 100 mg/100 mg/kg/day with purulent meningitis and septicemia and 28.8 mg/28.8 mg-72.8 mg/72.8 mg/kg/day with other infections. The clinical response in all patients was excellent or good.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Fundamental and clinical studies on imipenem/cilastatin sodium in the pediatric field]. 346 78

The interaction of ampicillin and chloramphenicol on three ampicillin-susceptible, chloramphenicol-resistant strains of Haemophilus influenzae was studied by checkerboard testing with subcultures, time-kill experiments, and a disk method. In all three strains there was inhibition of the bactericidal action of ampicillin by chloramphenicol at concentrations close to the MIC (10 micrograms/ml). This chloramphenicol concentration was close to that which might be achieved in cerebrospinal fluid during treatment for meningitis and was in the bactericidal range for chloramphenicol-susceptible organisms. It is suggested however that in the initial treatment of meningitis caused by ampicillin-susceptible, chloramphenicol-resistant strains, inhibition of the action of ampicillin by chloramphenicol may represent a clinical risk.
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PMID:Combined action of chloramphenicol and ampicillin on chloramphenicol-resistant Haemophilus influenzae. 348 29

Thirty patients (17 male, 13 female; age 17 to 84 years; normal renal function in 23 cases) with severe bacterial infections were treated with ceftriaxone. The infections was septicemia in 20 cases, a septicemia-like condition in 2 and a focal infection in 8 (2 abscesses of the lung, 2 pyelonephritis, 1 abscess of the liver, 1 subphrenic abscess, 1 meningitis developed from an abscess of the brain and 1 acute intestinal infection). 25 infections were bacteriologically documented, with recovery of the following pathogens: 20 Gram negative rods (including 10 E. coli) that were all susceptible to ceftriaxone (MIC = 0.02 to 0.5 mg/l) except 2 (1 Pseudomonas and 1 E. cloacae), 5 susceptible Gram positive cocci (3 Pneumococcus, 1 Streptococcus and 1 Staphylococcus epidermidis) and 3 susceptible anaerobes (2 B. fragilis and 1 B. melaninogenicus). Ceftriaxone was given alone in 15 cases and in association with another antibiotic in 15 cases (aminoglycoside in 10 cases, nitroimidazole in 4 and fosfomycin in 1). The dose of ceftriaxone was 1 to 2 g per day in 28 cases, 3 g per day in 1 case (meningitis with abscess of the brain) and 1 g every other day in 1 case (chronic renal failure under hemodialysis). Duration of treatment ranged from 10 to 62 days (average 17 days). The usual routes of administration were IV and IM; the SC route was used on 4 occasions. Pharmacokinetic studies of serum levels were carried out in several patients including two who had ceftriaxone subcutaneously; results were consistent with those previously reported in the literature.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Clinical evaluation of ceftriaxone in severe infections in adults]. 353 20

Studies were carried out on the penetration of cefuzonam (L-105, CZON), a new synthetic cephalosporin antibiotic, into cerebrospinal fluid, and on the clinical efficacy against bacterial infections. The results are summarized as follows: Concentrations of CZON in cerebrospinal fluid at 1 hour after intravenous administration of 100 mg/kg in cases of furunculosis of the external canal, encephalitis and mumps meningitis were 0.56 micrograms/ml, 1.44 micrograms/ml and 0.33 micrograms/ml, respectively. Concentrations of CZON in cerebrospinal fluid at 1 hour after intravenous administration of 100 mg/kg in 3 cases of purulent meningitis were 2.80-6.40 micrograms/ml at the acute stage and 0.56-1.45 micrograms/ml even at the recovering stage. Sensitivities of clinically isolated strains to CZON were determined and expressed as MIC. MICs of CZON on Haemophilus influenzae, Escherichia coli, Proteus mirabilis and Klebsiella pneumoniae were similar to MIC's of cefmenoxime (CMX), and lower than those of cefoperazone (CPZ), cefmetazole (CMZ), cefatiam (CTM) and Cefazolin (CEZ). The MIC of CZON on Staphylococcus aureus was similar to those of CEZ, CMZ and CTM, and lower than those of CMX and CPZ. Clinical responses of CZON were good in 2 cases of purulent meningitis, good in 2 cases of pyothorax, excellent in 1 case of septicemia, excellent in 3 cases of urinary tract infections, excellent in 7 cases and good in 3 cases out of 10 cases of pneumonia. Clinical responses of other diseases were excellent in 4 cases of bronchitis, good in 1 case of furunculosis of the external canal, excellent in 1 case of tonsillitis. No side effects nor abnormal laboratory findings were observed except 2 cases of mild diarrhea out of 24 cases.
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PMID:[Clinical evaluation of cefuzonam in pediatrics and a study on the penetration into cerebrospinal fluid]. 361 85

Cefuzoname (CZON) one of the aminothiazolyloxyiminoacetamido cephalosporins, was studied for its antibacterial activity, absorption and excretion, concentration in the cerebrospinal fluid (CSF) and the penetration, and clinical efficacy. The following are a summary of the results: 1. Antibacterial activity; The antibacterial activity of CZON was studied on clinically isolated Staphylococcus aureus (cefazolin (CEZ)-susceptible and CEZ-tolerant strains), Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis. Compared with CZON were cefmenoxime (CMX), latamoxef (LMOX), cefoperazone, cefmetazol (CMZ), cefotiam and CEZ, but for S. aureus cefamandole (CMD) was replaced for CPZ. Activities of CZON against S. aureus, both CEZ-susceptible and CEZ-tolerant strains, were superior to those of 6 control drugs. The distribution of MICs for the CEZ-susceptible strains was 0.10-12.5 micrograms/ml, and for the CEZ-tolerant strains 0.20-greater than 100 micrograms/ml. MIC peaks were 0.39 micrograms/ml and 0.78-1.56 micrograms/ml for CEZ-susceptible and CEZ-tolerant strains, respectively. Against both susceptible and tolerant strains, CZON showed superiority to CMZ and CMD, which are used prevalently and used for Methicillin-resistant S. aureus also. Distributions of MICs of CZON (and the peak of MICs) on E. coli, K. pneumoniae, and P. mirabilis were less than or equal to 0.025-1.56 (less than or equal to 0.025), less than or equal to 0.025-25 (less than or equal to 0.025-0.05), less than or equal to 0.025-25 (less than or equal to 0.025) micrograms/ml, respectively, showing CZON's similar antibacterial activity to those of cephalosporins, CMX and LMOX, which are 5th group. 2. Absorption and excretion: Eight patients, aged 10 months to 15 years, were administered with CZON 20 mg/kg, one shot intravenously. Serum concentrations somewhat varied from patient to patient, but the mean value was 48.7 micrograms/ml after 30 minutes of administration which decreased rapidly to 13.3 micrograms/ml after 1 hour, to 3.4 micrograms/ml after 2 hours, to 1.14 micrograms/ml after 4 hours, and to 0.15 microgram/ml after 6 hours. Half-lives were 0.67-1.47 hours, with the mean of 0.87 hour. Urinary recovery rates were 24.7-55.9%, with the mean of 45.1%, in 6 hours after administration. 3. CSF concentration and penetration rate: To 4 pediatric patients with purulent meningitis, CZON 25 mg/kg or 50 mg/kg was administered and the concentration in CSF was measured.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Fundamental and clinical studies on cefuzoname in the pediatric field]. 361 94

Cefuzoname (CZON, L-105) a newly developed cephalosporin, has broad spectrum on Gram-positive or -negative bacteria and may also be effective against Staphylococcus aureus against which third generation cephalosporins are largely ineffective. We studied the pharmacokinetics and clinical effects of CZON on infectious disease of children. The diseases we studied included 2 cases of bacterial meningitis and 1 case each of viral meningitis, enterocolitis, upper respiratory infection, pneumonia, and mycoplasmal pneumonia. CZON was administered by drip infusion. Dose levels were 20-53 mg/kg/30-60 minutes, 3 times a day. For 5 cases, was studied time course of concentrations of CZON in plasma. Median T 1/2 was 0.96 hour. Concentrations in cerebrospinal fluid (CSF) were studied in cases of pneumonia and bacterial meningitis. In the case of pneumonia the CSF concentration of CZON was 0.272 microgram/ml after 45 minutes, in the case of meningitis they were 0.155 microgram/ml after 5 hours. Both of these values were higher than MIC of 0.025 microgram/ml against Haemophilus influenzae which was isolated from a case of bacterial meningitis. This MIC was lower than that of cefotiam and cefazolin, as well as of cefmenoxime. Clinical effects were excellent on pneumonia, good on upper respiratory infection, fair on mycoplasmal pneumonia. CZON, however, was ineffective in the treatment of a case of bacterial meningitis from which a susceptible strain of H. influenzae was isolated.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Studies on cefuzoname in the field of pediatrics]. 361 97

The concentration of antibiotics in cerebrospinal fluid is of great interest in therapeutics, especially for the treatment of the central nervous system. We studied the penetration of mezlocillin (MZPC) in 3 cases with V-P shunt and 7 cases after neurosurgical operation. After intravenous injection of 4 g MZPC in the 3 cases with V-P shunt, a peak concentration (0.26-3.6 micrograms/ml) of MZPC in the cerebrospinal fluid was reached in 2-4 hours. In the 7 cases after neurosurgical operation, cerebrospinal fluid was sampled at 4 hours after the intravenous injection of 4 g MZPC by spinal tap. Concentrations of MZPC in cerebrospinal fluid ranged from 1.1 to 17.5 micrograms/ml. The mean maximum concentration of MZPC was 5.85 micrograms/ml, which exceeded 90% MIC (minimal inhibitory concentration) against S. epidermidis, E. faecalis, H. influenzae. It is concluded MZPC can be useful for the prophylaxis of meningitis.
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PMID:[A study on penetration of mezlocillin into the cerebrospinal fluid]. 376 53

The third generation cephalosporins are very active against Haemophilus influenzae, including betalactamase producing strains, Neisseria meningitidis and against gram-negative bacilli. Considering that a CSF level at least 10 times the MIC for the causative agent must be achieved, some cephalosporins are limited in their use in meningitis. Randomized controlled studies are sparse and it is difficult to compare objectively the clinical efficacy of cephalosporins with that of commonly used regimens. Moxalactam, cefotaxime, ceftazidime and ceftriaxone were revealed as being at least as effective as standard antibiotics in the treatment of meningitis. Although the outcome from bacterial meningitis has not appreciably changed in a 14-year period from 1969 to 1982, when newer generation beta-lactam drugs were available, it is obvious that these drugs will be very useful in special situations, particularly where multiply resistant pathogens are involved. Finally, the role of third-generation cephalosporins in the treatment of bacterial meningitis is best approached by analysis based on age group and clinical setting.
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PMID:Role of third-generation cephalosporins in the treatment of bacterial meningitis. 379 77

Two grams of cefmenoxime (CMX) was administered by one-shot intravenous injection to the patients in normal pressure hydrocephalus without meningitis, and the transference of CMX into the cerebrospinal fluid (CSF) from blood was investigated. After the injection of CMX, CSF and serum were serially taken, and the concentrations of CMX were measured by agar-well method using E. coli. The conclusions drawn from this study are summarized as follows: The concentrations of CMX in CSF were more slowly decreased than those in serum. The mean ratio of transference of CMX into CSF from the serum was 1.4%. After the intravenous injection of 2 g CMX, the mean maximum concentration of CMX in CSF was 0.36 microgram/ml, which exceeded 80% MIC (minimal inhibitory concentration) against several Gram-positive cocci and Gram-negative rods, and higher concentrations than the 80% MIC were kept over 4 hours in CSF. The efficacy of CMX may be kept by its injections less than 4 times a day.
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PMID:[A study on transference of cefmenoxime into the cerebrospinal fluid]. 385 62


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