UNIPROT:Q29983 - FACTA Search

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

The pharmacokinetics, efficacy and safety of sulbactam/ampicillin (SBT/ABPC) were evaluated in 21 children with a variety of infections. The results obtained are summarized as follows. 1. Pharmacokinetics in 4 children, each receiving a single dose of 60 mg/kg, were evaluated. The average half-life of SBT was 1.03 hours and that of ABPC was 0.83 hour. 2. In vitro antimicrobiol activity (MIC) of SBT/ABPC in which SBT and ABPC are combined at a ratio of 1:2 was stronger than ABPC alone and was quite effective against Staphylococcus aureus and Haemophilus influenzae, but activity against Escherichia coli was relatively low. Antimicrobial activity of SBT/ABPC against S. aureus was almost equal to those of piperacillin (PIPC), cefazolin (CEZ) and cefmetazole (CMZ), but against H. influenzae was stronger than those of CEZ and CMZ. Activity against E. coli was lower than those of PIPC, CEZ and CMZ. 3. A total of 21 patients including 3 with pharyngitis, 10 with bronchitis, 5 with pneumonia, 1 each with acute enteritis, pyelonephritis and suspected sepsis were treated with SBT/ABPC. The clinical efficacy rate for these patients was 95.2% (20/21). The bacteriological eradication rate was 80% (8/10). 4. There were 4 instances of side effects, 1 case each of eruption, diarrhea, thrombocytosis and eosinophilia, but all symptoms were transient.
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PMID:[Pharmacokinetic, bacteriological and clinical evaluation of sulbactam/ampicillin in pediatrics]. 274 54

The activities of ampicillin, cefaclor, cephalothin, and cefuroxime against invasive clinical isolates of Haemophilus infleunzae were studied to determine the correlation between resistance and beta-lactamase production. Approaches to in vitro susceptibility testing of cephalosporins in the clinical laboratory were also assessed. Three hundred and eight isolates of H. influenzae were tested for ampicillin susceptibility, and those which required for inhibition greater than or equal to 1.0 micrograms/ml of ampicillin were tested for beta-lactamase production with a chromogenic cephalosporin. Twenty-two percent of isolates produced beta-lactamase and 85% were serotype b. All isolates considered resistant (MIC greater than or equal to 2.0 micrograms/ml) to ampicillin produced beta-lactamase. A single beta-lactamase-producing isolate was identified, but was inhibited by 1.0 microgram/ml of ampicillin, and a zone diameter of 20 mm was produced by disk diffusion testing. One hundred and ninety-seven isolates were tested for susceptibility to cefaclor, cefuroxime, and cephalothin. Chloramphenicol susceptibility testing by disk diffusion was also performed on these isolates. General agreement and interchangeable results were found among these three cephalosporins by both agar dilution and disk diffusion methods. We conclude that ampicillin-resistant H. influenzae not producing beta-lactamase is rare among these isolates of H. influenzae responsible for invasive disease. Susceptibility testing results of cephalothin, cefaclor, or cefuroxime appear to be interchangeable, although results of cephalothin testing would tend to underestimate the activities of cefaclor or cefuroxime.
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PMID:Antimicrobial activities and susceptibility testing considerations of ampicillin, cephalothin, cefaclor, and cefuroxime against invasive isolates of Haemophilus influenzae. 278 68

The in-vitro activity of a new macrolide antibiotic CP-62,993 (Pfizer Ltd) was determined for 420 bacterial isolates, comprising 150 Haemophilus influenzae, 48 Branhamella catarrhalis, 50 Staphylococcus aureus, 50 coagulase negative staphylococci, 50 beta-haemolytic streptococci, 50 Streptococcus pneumoniae and 22 oral streptococci. CP-62,993 was compared with erythromycin and penicillin (ampicillin in the case of H. influenzae). The MICs of CP-62,993 were found to be lower than those of erythromycin for the two Gram-negative species tested: this was particularly marked in the case of H. influenzae where a ten-fold difference in the MIC50 was observed (CP-62,993, 0.25 mg/l, erythromycin 2 mg/l). In general MICs of CP-62,993 were two-fold higher than those of erythromycin for the Gram-positive species studied, with the exception of the oral streptococci which were equally susceptible (MIC50 0.03 mg/l) to both macrolides. Activity similar to that of erythromycin was observed against Str. pneumoniae (MIC values 0.015-0.12 mg/l), Staph. aureus (MIC 0.12-1 mg/l) and beta-haemolytic streptococci (MIC 0.06-4 mg/l). Incubation in a CO2 enriched atmosphere decreased activity of both erythromycin and CP-62,993. The effect was more marked for CP-62,993, the MIC50s of all groups of organisms being increased four-fold when they were incubated in the presence of 5 or 10% CO2.
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PMID:The in-vitro activity of CP-62,993 against Haemophilus influenzae, Branhamella catarrhalis, staphylococci and streptococci. 283 51

The in vitro and in vivo antibacterial activity of A-56268 (TE-031), the 6-O-methyl derivative of erythromycin, was compared with those of erythromycin and other reference drugs. A-56268 had the same spectrum of antibacterial activity as erythromycin. A-56268 was generally 1 log2 dilution more potent or equal to erythromycin against all organisms except haemophilus influenzae and Propionibacterium acnes, for which A-56268 was 1 log2 dilution and 3 log2 dilutions, respectively, less potent. The MBC of A-56268 and erythromycin was not significantly different from the MIC against Streptococcus pyogenes, Streptococcus pneumoniae, Staphylococcus epidermidis, and H. influenzae but was more than 2 log2 dilutions higher than the MICs for some Staphylococcus aureus strains. Human serum at a concentration of 50% did not change the in vitro potency of A-56268 or erythromycin. A-56268 was similar to erythromycin in being more active at pH 8.0 than at the physiologic pH of 7.3. The activity of A-56268 was synergistic with sulfamethoxazole against 4 of 12 strains of H. influenzae. In mouse protection tests, when administered orally A-56268 was more potent than erythromycin against H. influenzae, S. pyogenes, S. pneumoniae, and S. aureus. After subcutaneous administration the potencies of A-56268 and erythromycin were not statistically different from each other. A-56268 was more potent than erythromycin against Legionella infection in guinea pigs. The concentration of A-56268 in the serum and lung was higher than that of erythromycin after intraperitoneal administration. In A-56268 in the serum and lung was higher than that of erythromycin after intraperitoneal administration. In mice, the peak levels in serum of A-56268 and erythromycin were similar after subcutaneous administration and seven times higher for A-56268 after oral administration. The serum half-life of A-56268 was approximately twice that of erythromycin after administration by both routes.
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PMID:In vitro and in vivo evaluation of A-56268 (TE-031), a new macrolide. 294 95

There is poor correlation between the MICs and zone sizes obtained for erythromycin against Haemophilus influenzae. The effect of two media, Mueller-Hinton medium supplemented with 3% lysed horse blood and 10 micrograms of NAD per ml (MHA + LYHB) and Mueller-Hinton agar supplemented with 1% bovine hemoglobin and 1% IsoVitaleX (MHA + HGB), on the MICs and zone sizes of erythromycin against H. influenzae was determined. The effect of three different methods for inoculum preparation on the susceptibility of H. influenzae was also determined. The MICs were independent of the method of inoculum preparation, but the zone sizes were smaller if the inoculum was carefully adjusted to contain approximately 10(8) CFU/ml. MICs were higher and zone sizes were smaller when MHA + HGB was used instead of MHA + LYHB. Good correlation was found when MHA + LYHB was used for determining the MIC and MHA + HGB was used for determining susceptibility by the disk method. When the inoculum was adjusted to match a McFarland 0.5 standard, the viable counts had to be approximately 10(8) CFU/ml for good correlation between MICs and zone sizes. A-56268, a new macrolide antibiotic, was tested against H. influenzae, and its MICs and tentative breakpoints against this organism were determined. The MICs obtained by various methods were correlated with in vivo efficacy by using a mouse septicemia model. MICs obtained on MHA + HGB or MHA + LYHB incubated without a 5% CO2 atmosphere showed the best correlation with in vivo efficacy.
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PMID:Susceptibility testing of macrolide antibiotics against Haemophilus influenzae and correlation of in vitro results with in vivo efficacy in a mouse septicemia model. 295 54

Seventy five patients with respiratory infections, including 40 cases of acute pneumonia, 33 cases of secondary infection after chronic pulmonary diseases and 2 cases of pulmonary abscess, were treated with cefotetan (CTT, Yamatetan) by drip infusion in order to evaluate its clinical efficacy. The overall rate of effectiveness was 83.8%. CTT was examined comparatively with other beta-lactam antibiotics for antibacterial activity on clinically isolated strains of 3 major respiratory pathogens including Haemophilus influenzae, Branhamella catarrhalis and Streptococcus pneumoniae. Minimum inhibitory concentrations (MIC's) of CTT on H. influenzae were less than 3.13 micrograms/ml regardless of the production of beta-lactamase by these organisms. As to B. catarrhalis, CTT also exerted an antibacterial activity enough to control the proliferation of all the strains at a level of 1.56 micrograms/ml. Against S. pneumoniae, on the other hand, CTT exhibited the lowest activity of all the drugs tested but still showed MIC's of 3.13 micrograms/ml or less. Drip infusion of CTT at a dose of 2 g brought about an average maximum blood concentration of 342 +/- 25.7 micrograms/ml and an average half-life in blood of 2.48 +/- 0.41 hours Maximum sputum concentration of the drug, however, was variable among the cases tested, ranging from 0.40 to 1.80 micrograms/ml. Side effects of the drug were observed in 5 cases or 6.7%. Four of them had some allergic symptoms; i.e., pyrexia and eruption. One patient was especially diagnosed as possible drug-induced interstitial pneumonia during the treatment with the drug. The diagnosis was confirmed by transbronchial lung biopsy and lymphocyte blastogenesis by CTT in vitro. As to abnormal laboratory findings, blood transaminases were elevated during drug administration in 13 cases or 17.3%, but were reduced back to the normal level after the withdrawal of the drug.
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PMID:[Laboratory and clinical studies on cefotetan in respiratory tract infections]. 304 35

MIC 90 and MBC 90 of amoxicillin, cefaclor, cefadroxil and cefuroxime axetil have been determined by the microdilution method against 48 organisms responsible of acute respiratory tract infections in children: 17 E. coli, 15 K. pneumoniae, 16 H. influenzae. An inoculum effect and an inhibitory index in blood and bronchial secretions were determined. An inoculum effect was more important for amoxicillin and cefadroxil than for cefuroxime axetil and cefaclor. Against H. influenzae, cefuroxime axetil and cefaclor have a similar activity. Against Enterobacteria, cefuroxime axetil has the lowest MIC 90 and MBC 90 and the highest inhibitory index.
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PMID:[Comparison of in vitro activity of 4 oral beta-lactams on microorganisms responsible for broncho-pulmonary infections in children]. 305 59

Cefpodoxime proxetil (CS-807) is an orally active prodrug of an oxime-type cephem antibiotic. The MIC60 values of cefpodoxime (R-3746) the active form of CS-807, were 3.13, 6.25, 0.05, 0.38, 0.2, 0.1, 3.13, 3.13, 6.25, 6.25, 0.1 and 12.5 micrograms/ml against S. aureus, coagulase-negative staphylococci, S. pneumoniae, E. coli carrying R plasmids, P. vulgaris, P. rettgeri, C. freundii, S. marcescens, A. calcoaceticus, P. cepacia, ampicillin-resistant H. influenzae and B. fragilis, respectively. Its activity was stronger than that of cefaclor and ampicillin. R-3746 manifested little activity against P. aeruginosa, methicillin-resistant S. aureus, and Enterococcus spp. R-3746 showed stronger binding affinity than cefaclor with the PBP2 of S. aureus, PBPs 1a, 1bs, 2 and 3 of E. coli, PBPs 1b, 1c and 3 of P. rettgeri, and the PBP3 of P. aeruginosa than cefaclor. Synergy of the bactericidal effect between R-3746 and serum complement was moderate, although the cells of E. coli NIHJ-JC2 and S. aureus 209P were well engulfed and rapidly digested by mouse-cultured macrophages in the presence of greater than 1/8 MIC of R-3746. Good clinical efficacy can be expected of CS-807 provided its pharmacokinetics prove to be good.
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PMID:Cefpodoxime proxetil, its in vitro antibacterial activity, affinity to bacterial penicillin-binding proteins, and synergy of bactericidal activity with serum complement and mouse-cultured macrophages. 307 32

It has been more than 4 years since third-generation cephems were introduced into clinical practice. The range of our drug selection definitely tends to increase, because we today have more antibiotics with wider spectrum, antibiotics with strong activities only against Gram-negative strains, such as monobactams, and those with tremendously high activities such as quinolone carboxylic acid derivatives, in comparison to those we had in the past. Among isolates obtained mainly from sputa of 567 patients with lower respiratory tract infections at 16 institutions throughout Japan between September of 1985 and March of 1986, 741 strains were determined to be causative organisms. MIC's of various antimicrobial agents were determined against 67 strains of Staphylococcus aureus, 100 strains of Streptococcus pneumoniae, 199 strains of Haemophilus influenzae, 92 strains of non-mucoid Pseudomonas aeruginosa, 40 strains of mucoid P. aeruginosa, 29 strains of Klebsiella pneumoniae, 10 strains of Escherichia coli and for 42 strains of Branhamella catarrhalis out of the above 741 strains to determine their drug sensitivities. As for types of lower respiratory tract infections found in 1981--1983, 57.9--64.5% of the infections were chronic respiratory infections; i.e., chronic bronchitis, chronic bronchiolitis and bronchiectasis. These chronic infections, including diffuse panbronchiolitis (DPB), were found in 63.1% of lower respiratory tract infections in 1984. Their incidence dropped to 54.0% in 1985, even though DPB was included; i.e., the incidence of chronic bronchiolitis was 5.5%, that of DPB was 7.1%, and that of bronchial asthma associated with lower respiratory tract infections in 1985 was 8.8% which was twice as much as that found in 1981--1984. Although bacterial pneumonia was found in 24.8% of all the cases in 1981, its incidence was reduced to 11.0% in 1983, 15.1% in 1984, and 17.6% in 1985. This reduction seemed to have resulted from gradual decreases in the occurrence of bacterial pneumonia among the young population. As with usual years, a high incidence rate in a total lower respiratory tract infections in 1985 was found among older patients; namely, 73.5% was at the age of 50 or over (417/567). Next, we determined relationships between clinical isolates and isolates from respiratory infections, including chronic bronchitis, chronic bronchiolitis, bronchiectasis and DPB. H. influenzae was isolated from 50.5% of patients with these infections in 1981; however, the detection rate decreased by about 20% to 29.7% in 1985. P. aeruginosa was consistently isolated, between 24.1% and 30.4% every year.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Susceptibility of bacteria isolated from the patients with lower respiratory tract infections to antibiotics (1985)]. 312 87

Based on a quantitative analysis of sputum cultures, pathogenic bacteria in respiratory ailments isolated in our laboratory during 1984 to 1986 were classified and analyzed. During the study period, the most frequently isolated agent was Haemophilus influenzae followed by Pseudomonas aeruginosa, Branhamella catarrhalis and Streptococcus pneumoniae. They together consisted of 70 approximately 74% of all the respiratory pathogenic bacteria isolated in our study. Susceptibilities of above pathogens to antimicrobial agents were investigated using the agar dilution method. Results are summarized as follows. 1. Ratio of proportion of beta-lactamase producing strains among non beta-lactamase producing strains of H. influenzae markedly decreased in 1986 (6/70, 8.6%) as compared to previous years (11/73, 15.1% in 1984 and 8/49, 16.3% in 1985). In consequence, MIC90 values for penicillins reduced considerably in 1986. Among the antibiotics examined cefmenoxime (CMX) and cefotaxime (CTX) were the most active agents against H. influenzae. A development of resistance to other cephems and new quinolones (norfloxacin, ofloxacin, ciprofloxacin) was not evident during the 3-year survey. 2. Against S. pneumoniae, benzylpenicillin was still the most active agent despite gradual increase of frequency of isolation. Ampicillin (ABPC), piperacillin (PIPC), CMX and CTX were also potent against S. pneumoniae. S. pneumoniae were frequently isolated from patients treated with new quinolones or minocycline (MINO). This phenomenon may be explained by higher MIC values of these agents against S. pneumoniae. 3. Of B. catarrhalis strains isolated, more than 80% were beta-lactamase positive, although MIC90 were not so high (1.56 micrograms/ml for ABPC and 0.20 micrograms/ml for PIPC). Among the antibiotics tested, latamoxef was the most active agent against B. catarrhalis and inhibited all the strains at a concentration of 0.05 micrograms/ml or less. No resistant strains were observed against cephems, new quinolones, erythromycin or MINO. 4. P. aeruginosa appeared to be rapidly developing resistance against new quinolones in patients with chronic P. aeruginosa respiratory infections who had been treated with these agents. In treating chronic respiratory infection due to P. aeruginosa, one must be watchful of rapid development of resistance by the organism or its replacement with S. pneumoniae.
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PMID:[Recent trend of incidence of respiratory pathogenic bacteria and its susceptibility to antimicrobial agents: studies in the year 1984-1986]. 314 25

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