Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:Q29983 (MIC)
 21,138 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The concentration of Latamoxef (LMOX) in the serum, prostatic tissue and bladder mucosal tissue of 20 patients with benign prostatic hypertrophy and bladder cancer was measured after intravenous infusion of 1 g or 2 g of LMOX. Serum, prostatic tissue and bladder mucosal tissue levels of LMOX responded satisfactorily to the dose of LMOX. The bladder mucosal tissue level was higher than the prostatic tissue levels. Judging from the inhibitory concentration of LMOX (MIC 80), the concentration was sufficiently effective against infections caused by gram-negative, gram-positive and anaerobic bacilli.
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PMID:[Study of levels of latamoxef in prostatic tissue and bladder mucosal tissue]. 243 17

The activities of cefotaxime and other aminothiazoyl oxime cephalosporins against Enterococcus faecalis were enhanced by addition of 5% sheep blood to Mueller-Hinton agar. This effect was not seen with aztreonam (aminothiazoyl oxime monobactam), cefotiam (aminothiazoyl, nonoxime), or other cephalosporins, and it was specific to the syn-configuration of the oxime moiety. Enhancement of cefotaxime activity was demonstrable against approximately 50% of 86 clinical isolates and could only be shown at low bacterial inocula. Human serum, serum alpha 1-, beta- and gamma-globulin fractions and albumin often antagonized or did not affect significantly the antimicrobial activity of cefotaxime, while the alpha 2-globulin fraction usually enhanced drug activity. The in vivo activity of cefotaxime against E. faecalis was examined in a rat peritoneal abscess model. The test organism was resistant to cefotaxime by standard methods (MIC greater than 128 micrograms/ml) but was inhibited by 1.0 microgram/ml when rat serum was presented in the medium. Cefotaxime reduced titers of bacteria within abscesses after 5 days of therapy (5.77 +/- 0.68 log10 CFU/g) in comparison with those in control animals (7.38 +/- 0.28 log10 CFU/g, p less than 0.05). Moxalactam, the in vitro activity of which was not augmented by serum, proved ineffective in the animal model. While these observations do not have direct therapeutic relevance, they offer a possible explanation for the relatively infrequent occurrence of enterococcal superinfection in patients treated with cefotaxime.
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PMID:Effect of blood product medium supplements on the activity of cefotaxime and other cephalosporins against Enterococcus faecalis. 250 57

Forty-three clinical isolates of enterobacteria were selected for the production of the new plasmid-mediated expanded-spectrum beta-lactamase CTX-1. The geometric means of MICs were ranged as follows: ticarcillin, greater than 4096 mg/l; ticarcillin + clavulanic acid (2 mg/l), 64-87 mg/l; LY 163892, 8.0-69.1 mg/l; cefotaxime, 5.7-26.4 mg/l; temocillin, 8.0-21.8 mg/l; Ro 158074, 4.0-18.7 mg/l aztreonam, 1.0-14.4 mg/l and BMY 28142, 1.4-2.8 mg/l. Moxalactam, imipenem and CM 40876 were resistant to hydrolysis and MICs were lower than 2.0 mg/l. A high protective effect on cefotaxime (MIC less than or equal to 0.5 mg/l) was obtained by sulbactam (4 mg/l). Escherichia coli transconjugants from each species showed similar levels of MICs.
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PMID:Susceptibility of new beta-lactams to the expanded-spectrum beta-lactamase CTX-1. 264 26

Cases with infections of urinary tracts were divided into 3 groups of the simple infections, and complicated infections without indwelling of catheter, and complicated infections with indwelling of catheter. Susceptibilities to antimicrobial agents of Escherichia coli, Klebsiella spp., Proteus spp., Citrobacter spp., Enterobacter spp., Pseudomonas aeruginosa and Serratia marcescens which were isolated from patients with these infections were determined. There was no tendency of decline in the susceptibilities of E. coli isolated from the patients with simple urinary tract infections (UTI). Susceptibilities of E. coli isolated from the patients with complicated UTI without and with indwelling of catheter to cephem antibiotics of the third generation were examined. The susceptibility of E. coli strains isolated from patients with complicated UTI without and with indwelling of catheter remained the same. More specifically, cefmenoxime (CMX) at a concentration of less than 0.10 microgram/ml inhibited the growth of E. coli isolated from cases without: with catheter at 74.1%: 78.3% in 1982, 75.4%: 73.3% in 1983, and 81.3%: 84.8% in 1984. Also, ceftizoxime (CZX) at a concentration of less than 0.10 microgram/ml inhibited the growth at 83.3%: 95.7% in 1982, 89.2%: 86.7% in 1983, and 91.7%: 97.0% in 1984. Latamoxef (LMOX) at less than 0.10 microgram/ml inhibited the growth at 59.3%: 43.5% in 1982, 47.7%: 40.0% in 1983, and 47.9%: 42.4% in 1984. The antibacterial effect of penicillin against Klebsiella spp. was found to be poor, while those of oral cephem antibiotics, cephalexin (CEX), cefaclor (CCL), and cefazolin (CEZ) which is the cephem antibiotics of the so-called first generation and cefotiam (CTM) among other cephem antibiotics of the so-called second generation were relatively good. A study of susceptibilities of Klebsiella spp. isolated from patients with complicated UTI without and with indwelling of catheter revealed inhibition of growth by CTM at a concentration of 0.39 microgram/ml at 84.0%: 75.9% in 1982, 70.6%: 75.0% in 1983, and 95.8%: 77.8% in 1984. Cefmetazole (CMZ) at a concentration of 0.39 microgram/ml showed a relatively lower rate of growth inhibition of Klebsiella spp., while at 0.78 microgram/ml it inhibited the growth at 88.0%: 72.4% in 1982, 52.9%: 50.0% in 1983, and 70.8%: 66.7% in 1984. The antibacterial effects of both CTM and CMZ against Klebsiella spp. isolated from patients with indwelling of catheter were found to be poor, and some of the bacterial strains showed a MIC over than 100 micrograms/ml.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Comparative studies of antimicrobial agents against causative organisms isolated from urinary tract infections (1984). III. Secular changes in susceptibility]. 310 9

Antimicrobial activities of sulbactam/cefoperazone (SBT/CPZ) against 50 fresh clinical isolates of Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Citrobacter freundii, Enterobacter spp., Serratia marcescens, Proteus mirabilis, Proteus vulgaris and Pseudomonas aeruginosa were compared to those of CPZ, Cefotiam (CTM), Cefotaxime (CTX) and Latamoxef (LMOX). Minimal inhibitory concentrations (MIC's) of SBT and CPZ mixed in a ratio of 1:1 were determined by the dilution method using Mueller-Hinton agar and expressed by absolute concentrations of CPZ. Antimicrobial activities of SBT/CPZ against principally penicillinase (PCase) producing bacteria, i.e., S. aureus, E. coli, K. pneumoniae, P. mirabilis, were superior to those of CPZ alone. The presence of SBT in concentrations around 0.39 approximately 1.56 micrograms/ml clearly enhanced CPZ's antimicrobial activities against these PCase producing strains. The synergistic antimicrobial effects of SBT in combination with CPZ were less pronounced against principally cephalosporinase (CEPase) producing bacteria, i.e., C. freundii, Enterobacter spp., S. marcescens, P. vulgaris, and P. aeruginosa, and exerted with SBT at concentrations around 3.13 approximately 12.5 micrograms/ml. Comparative antimicrobial activities indicated by MIC80's of tested agents showed that SBT/CPZ had more stable activities against bacteria ranging from Gram-positive to Gram-negative bacteria than CTM, CTX and LMOX. MIC's of SBT/CPZ were higher than 25 micrograms/ml against 8% of S. aureus, 18% of C. freundii, 10% of Enterobacter spp., 26% of S. marcescens, 2% of P. vulgaris, and 18% of P. aeruginosa. These resistant strains against which the addition of SBT showed no synergism, may possess other mechanism of resistance than beta-lactamase production. It is concluded that the presence of CPZ resistant strains is an actual current problem and not an imaginary future problem, and that the number of resistant strains against other new cephems which have different chemical structure from CPZ is increasing. When these present bacteriological environments are considered, the appearance of SBT/CPZ in the clinical practice is timely and meaningful.
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PMID:[Antimicrobial activity of sulbactam/cefoperazone. Comparison with other new cephems]. 344 15

We administered 1 g of imipenem along with equal amounts of cilastatin (a dehydropeptidase I inhibitor) or 2 g of moxalactam intravenously over a period of 30 min to six volunteers in a crossover manner 1 week apart. The antibiotic concentrations and pharmacokinetics for each drug were determined and integrated with the microbiologic activity by measuring the duration of time that the free drug concentrations remained above the MICs for 90% of 581 clinical isolates and by measuring serum bactericidal activities against organisms which commonly infect granulocytopenic cancer patients. Moxalactam produced serum levels at 1 h after infusion of 99.9 micrograms/ml; these levels were four times greater than the plasma levels of imipenem (22.8 micrograms/ml). The trough (5.5-h) moxalactam serum levels were 10 times greater than those of imipenem (18.5 and 1.7 micrograms/ml, respectively). Essentially all of the imipenem was unbound to protein, whereas 36 to 42% of the moxalactam was unbound. Moxalactam produced free antibiotic concentrations that were above the MIC for 90% of the strains tested for more than 6 h against all of the species tested except Staphylococcus aureus (5.3 h), Enterobacter hafnia (1.6 h), and Pseudomonas aeruginosa (0 h). The imipenem concentrations were above the MIC for 90% of the strains tested for 5.6 h or more against all of the bacteria tested except Proteus spp. and Pseudomonas aeruginosa (4.5 h). The geometric mean peak bactericidal titers from volunteers receiving imipenem were more than 1:8 against all bacteria and were significantly higher than the titers from volunteers receiving moxalactam against S. aureus (1:7.3) and Pseudomonas aeruginosa (1:4.5). These data, in addition to information obtained from animal models, indicate that imipenem is a promising new candidate for carefully controlled clinical trials as a single agent for therapy of serious infections, including empiric therapy for fever in granulocytopenic cancer patients.
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PMID:Imipenem coadministered with cilastatin compared with moxalactam: integration of serum pharmacokinetics and microbiologic activity following single-dose administration to normal volunteers. 345 90

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

Among eight cephalosporins and cephamycins tested in preliminary in vitro screening against Mycobacterium tuberculosis, the most promising for further study was found to be ceforanide, followed by ceftizoxime, cephapirin, and cefotaxime. Moxalactam, cefoxitin, cefamandole, and cephalothin were found to be not active enough against M. tuberculosis to be considered for further in vitro studies. The antibacterial activity of various ceforanide concentrations was investigated by three methods: (i) the dynamics of radiometric readings (growth index) in 7H12 broth; (ii) the number of CFU in the same medium; and (iii) the proportion method on 7H11 agar plates. There was a good correlation among the results obtained with these methods. The MIC for most strains ranged from 6.0 to 25.0 micrograms/ml. The BACTEC radiometric method is a reliable, rapid, and convenient method for preliminary screening and determination of the level of antibacterial activity of drugs not commonly used against M. tuberculosis.
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PMID:Determination of in vitro susceptibility of Mycobacterium tuberculosis to cephalosporins by radiometric and conventional methods. 392 Sep 57

We evaluated the microbiologic characteristics including MIC determinations, synergy plate assays and serum bactericidal activity for two regimens being examined as empiric antibiotic therapy for febrile granulocytopenic cancer patients. The regimens consisted of moxalactam (4 g.i.v. q12h) plus piperacillin (75 mg/kg i.v. q6h) or moxalactam (as above) plus amikacin (levels adjusted to one hour post-infusion levels of 25 mg/l and troughs of 6-8 mg/l). Detailed pharmacokinetics were ascertained for the beta lactams. All drugs were active against a panel of 11 strains each of Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus aureus. The pharmacokinetic profile showed serum levels sufficient to provide good antimicrobial activity throughout the dosing interval. Both regimens displayed synergistic or partially synergistic activity in the main for the test organisms; moxalactam plus piperacillin produced good results against S. aureus and P. aeruginosa. In the serum bactericidal assays, the moxalactam-piperacillin combination produced significantly higher mean titers at both peak and trough when compared to the moxalactam-amikacin regimen. This may be because moxalactam acts as a beta lactamase inhibitor for both staphylococcal beta lactamase, as well as the Sabath-Abraham Id type beta lactamase carried by P. aeruginosa (among others). Moxalactam-piperacillin deserves extensive evaluation as empiric therapy for the febrile neutropenic cancer patients.
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PMID:Moxalactam and piperacillin: a study of in vitro characteristics and pharmacokinetics in cancer patients. 398 51

N-Formimidoyl thienamycin (N-F-thienamycin) and moxalactam were compared with other currently available and investigational antibiotics against 100 clinical isolates of Bacteroides fragilis by an agar dilution method. N-F-thienamycin was the most active among the beta-lactam agents tested, with a minimal inhibitory concentration for 90% of isolates (MIC90) of 0.25 micrograms/ml. Moxalactam was next in activity, with an MIC90 of 4 micrograms/ml. N-F-thienamycin was somewhat more active, and moxalactam was slightly less active, than metronidazole and clindamycin. An increase in inoculum size caused an increase in the MIC of N-F-thienamycin, cefoperazone, and cefotaxime. This inoculum effect could influence the usefulness of these drugs in certain clinical conditions. The minimal bactericidal concentration was less than two times the MIC for most agents and less than four times the MIC for all beta-lactam agents at each inoculum size tested. Investigation of the mechanism of resistance to beta-lactam agents demonstrated a correlation between the level of resistance and beta-lactamase activity in each strain tested. N-F-thienamycin and cefoxitin were not hydrolyzed, and moxalactam was less susceptible to hydrolysis than the other beta-lactam antibiotics. Moxalactam and N-F-thienamycin may prove to be useful against infections with B. fragilis.
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PMID:In vitro activity of N-formimidoyl thienamycin, moxalactam, and other new beta-lactam agents against Bacteroides fragilis: contribution of beta-lactamase to resistance. 621 86


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