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)

Minimal inhibitory and bactericidal concentrations (MIC and MBC) of clarithromycin were determined with 49 Mycobacterium avium strains isolated from patients with acquired immunodeficiency syndrome. The inhibitory activity depended on the pH of the medium: the drug was more active at pH 7.4 and less active at pH 5.0, with activity at pH 6.8 in an intermediate position. The broth-determined MIC found at pH 7.4 were 0.25 and 0.5 micrograms/ml for most strains. The agar-determined MIC for most strains ranged from 1.0 to 4.0 micrograms/ml. The MBC of the drug were 8- to 64-fold higher than the MIC, which indicates that the efficacy of clarithromycin can be associated with its inhibitory rather than its bactericidal activity.
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PMID:Clarithromycin minimal inhibitory and bactericidal concentrations against Mycobacterium avium. 153 86

MDL 62208, MDL 62211, and MDL 62873 are three semisynthetic amide derivatives of teicoplanin (MDL 62208 is an amide of teicoplanin aglycone, MDL 62211 is an amide of the teicoplanin A2 complex, and MDL 62873 is the corresponding derivative of peak A2-2 of the complex). The three semisynthetic glycopeptides were evaluated for in vitro antibacterial activity in comparison with the parent drug (teicoplanin) and vancomycin. A variety of gram-positive bacteria of clinical origin, whose species were carefully determined and that included 428 staphylococci (207 methicillin susceptible and 221 methicillin resistant), 41 streptococci, 82 enterococci, 43 strains of Listeria monocytogenes, 10 JK coryneform bacteria, and 67 anaerobes belonging to the genera Clostridium, Propionibacterium, Peptostreptococcus, and Eubacterium, were tested. The only resistances to MDL 62208, MDL 62211, and MDL 62873 were encountered with vancomycin- and teicoplanin-resistant enterococci. All of the other test strains, including some teicoplanin-resistant coagulase-negative staphylococci of the species Staphylococcus haemolyticus and Staphylococcus epidermidis, were highly susceptible to the three teicoplanin amides. Only minor differences in activity were observed among MDL 62208, MDL 62211, and MDL 62873, whereas the three experimental compounds were usually found to be more potent than teicoplanin or vancomycin (especially against staphylococci, with differences mostly ranging from 2- to 16-fold). The MBC-to-MIC ratios varied depending on the organisms, with the highest ratios usually observed for enterococci and listeriae. Overall, the MBC-to-MIC ratios yielded by the teicoplanin analogs were slightly greater than those yielded by teicoplanin or vancomycin.
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PMID:In vitro activities of three semisynthetic amide derivatives of teicoplanin, MDL 62208, MDL 62211, and MDL 62873. 153 77

A series of 16 antibiotics from different classes (5-nitro imidazoles, beta-lactams, cyclins, macrolids, chloramphenicol) was examined for their bacteriostatic and bactericidal activities on 45 strains of Clostridium perfringens, with determination of MIC and MBC values. Several techniques of multivariate analysis were used in order to visualize differentiations in sensitivity profiles: Principal component analysis (PCA) and preferentially Correspondence factorial analysis (CFA). This approach revealed the efficacy of antibiotics from both general and family classifications.
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PMID:Comparative sensitivity study of Clostridium perfringens towards 16 antibiotics from different classes. 161 77

The ability of brobactam to inhibit beta-lactamases and the in vitro activity of ampicillin combined with brobactam was compared with another beta-lactamase inhibitor, clavulanic acid, and other beta-lactam antibiotics. Both inhibitors showed good and similar activity against staphylococcal penicillinase and most broad-spectrum beta-lactamases found in the Enterobacteriaceae, whether plasmid or chromosomally mediated. Both inhibitors were less active against chromosomally mediated cephalosporinases in Enterobacteriaceae, but brobactam was 8-50 times more potent than clavulanic acid. The amount and type of beta-lactamase produced by a particular bacterial strain was reflected in its sensitivity to a combination of ampicillin and brobactam, and correlated well with the sensitivity of extracted beta-lactamase to inhibition by brobactam. The in-vitro activity of ampicillin/brobactam in a 3:1 ratio was compared to amoxycillin/clavulanic acid (4:1 ratio), amoxycillin, cefaclor and cefuroxime. The two inhibitor combinations were generally of similar activity, but the brobactam combination had superior activity against Proteus vulgaris, Morganella morganii, Citrobacter freundii and Yersinia enterocolitica. The cephalosporins were less effective against the Bacteroides fragilis group, Prot. vulgaris and M. morganii, but had advantages in the case of Escherichia coli, Klebsiella spp. and C. diversus. The MBC of ampicillin/brobactam was similar to the MIC. No resistant sub-populations were observed amongst the staphylococcal strains investigated. Exposure of bacteria to sub-inhibitory levels of ampicillin/brobactam did not lead generally to the development of resistance.
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PMID:In-vitro evaluation of ampicillin/brobactam and comparison with other beta-lactam antibiotics. 164 79

Four fluoroquinolones were tested for antimicrobial activity against 300 isolates of staphylococci collected from medical centres throughout the United States. No cross-resistance to methicillin or oxacillin and the fluoroquinolones was observed. All four drugs were bactericidal agents and all ciprofloxacin-susceptible strains were inhibited at recommended breakpoint concentrations. Ciprofloxacin-resistant strains showed complete cross-resistance to the other fluoroquinolones. The relative potency of the study drugs as judged by MIC/MBC determinations was: temafloxacin greater than ciprofloxacin greater than ofloxacin greater than enoxacin.
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PMID:Anti-staphylococcal activity of temafloxacin, ciprofloxacin, ofloxacin and enoxacin. 166 29

The MICs and MBCs of the new difluorinated quinolone drug sparfloxacin against type strains belonging to 21 species of mycobacteria were screened. The MICs and MBCs were within the range of 0.1 to 2.0 and 0.1 to 4.0 micrograms/ml, respectively (with an MBC/MIC ratio of 1 to 2), and against 18 of the 21 species tested, the drug showed significant bactericidal activity (at least 99% killing or more of the initial inoculum added) at concentrations well within the reported peak concentrations in serum (Cmax) in humans. MICs of sparfloxacin for 7 of 10 Mycobacterium avium complex strains were below the Cmax, with MBC/MIC ratios within the range of 2 to 4. Enhancement of its activity by ethambutol, rifampin, amikacin, and clarithromycin (which were used at sublethal concentrations) assessed by using BACTEC radiometry revealed that its activity was further enhanced in 2 of 10 strains by rifampin and in 7 of 10 strains by ethambutol. The bactericidal effects of various drugs used alone as well as two-drug combinations used at Cmax levels were also screened against four strains of M. avium complex growing intracellularly in two different macrophage systems, namely, mouse bone marrow-derived macrophages and peripheral blood monocyte-derived human macrophages. Our results showed a satisfactory correlation between the extracellular and intracellular drug activity data.
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PMID:Antimycobacterial spectrum of sparfloxacin and its activities alone and in association with other drugs against Mycobacterium avium complex growing extracellularly and intracellularly in murine and human macrophages. 166 50

Bacteria-laden skin squames, detached bacterial clumps and isolated bacteria floating in skin fluids are the major infective units in hand and skin transmission of microorganisms. These units have differing ability to colonize new surfaces and may have different susceptibility to antiseptics. MIC-MBC testing on isolated bacteria serves to confirm the expected susceptibility of particular isolates and is useful for surveillance of the evolution of antiseptic resistance; however, it is often unreliable in predicting the in-vivo effect. In-vitro tests aimed at duplicating natural conditions (including the effect of antiseptics on bacterial biofilms, or better, on the different infective units) are under evaluation. Meanwhile, tests involving natural skin surfaces, like the Story test, offer reproducible and useful data.
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PMID:Laboratory and in-vitro testing of skin antiseptics: a prediction for in-vivo activity? 167 47

We evaluated the pharmacokinetics and therapeutic efficacy of ampicillin combined with sulbactam in a rabbit model of meningitis due to a beta-lactamase-producing strain of Escherichia coli K-1. Ceftriaxone was used as a comparison drug. The MIC and MBC were 32 and greater than 64 micrograms/ml (ampicillin), greater than 256 and greater than 256 micrograms/ml (sulbactam), 2.0 and 4.0 micrograms/ml (ampicillin-sulbactam [2:1 ratio, ampicillin concentration]) and 0.125 and 0.25 micrograms/ml (ceftriaxone). All antibiotics were given by intravenous bolus injection in a number of dosing regimens. Ampicillin and sulbactam achieved high concentrations in cerebrospinal fluid (CSF) with higher dose regimens, but only moderate bactericidal activity compared with that of ceftriaxone was obtained. CSF bacterial titers were reduced by 0.6 +/- 0.3 log10 CFU/ml/h with the highest ampicillin-sulbactam dose used (500 and 500 mg/kg of body weight, two doses). This was similar to the bactericidal activity achieved by low-dose ceftriaxone (10 mg/kg), while a higher ceftriaxone dose (100 mg/kg) produced a significant increase in bactericidal activity (1.1 +/- 0.4 log10 CFU/ml/h). It appears that ampicillin-sulbactam, despite favorable CSF pharmacokinetics in animals with meningitis, may be of limited value in the treatment of difficult-to-treat beta-lactamase-producing bacteria, against which the combination shows only moderate in vitro activity.
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PMID:Use of ampicillin-sulbactam for treatment of experimental meningitis caused by a beta-lactamase-producing strain of Escherichia coli K-1. 175 24

The relative importance of pharmacokinetic and pharmacodynamic parameters for the feasibility of a single daily dose (SDD) of antibiotics remains to be established. Therefore, we studied the relationship between in vitro bacteriological parameters (MIC, MBC, and killing rate [KR], defined as the reduction in the inoculum within 3 h), pharmacokinetic parameters (t1/2 and protein binding [PB], and in vivo antibacterial effect of a single antibiotic dose in an experimental rabbit model of Escherichia coli endocarditis. Nine antibiotics were investigated: two aminoglycosides, two quinolones, and five beta-lactams. For each drug, the minimal effective dose (MED) (in milligrams per kilogram) was defined as the lowest dose able to achieve a significant difference (P less than 0.05) of CFU in the vegetations in comparison with controls 24 h after a single intravenous injection. Aminoglycosides and quinolones had the lowest MEDs, followed by beta-lactams. Univariate regression analysis showed that KR was the major determinant of MED. A stepwise regression analysis showed that t1/2 significantly improved the predictive value of KR, while PB, MIC, and MBC did not. The final equation was MED = 1,586-238 KR-297 t1/2 (r = 0.90, P = 0.01). We concluded that the pharmacodynamic parameters (especially the high KR) of aminoglycosides and quinolones explained their low MEDs and might allow SDD. In contrast, the low KR of beta-lactams emphasized the critical importance of a long t1/2, as for ceftriaxone, allowing the use of this beta-lactam alone in SDD.
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PMID:Single daily dosing of antibiotics: importance of in vitro killing rate, serum half-life, and protein binding. 175 31

MIC and MBC values of ofloxacin and ceftriaxone were investigated against Staphylococcus aureus in MHB and MHB containing additional Mg2+, Al3+, Fe3+, Ca2+, Zn2+, Cu2+. The addition of Mg2+, Al3+, Fe3+ increased the MIC and MBC of ofloxacin and the MBC of ceftriaxone. However, the addition of these cations did not change the MIC of ceftriaxone. Our findings suggest that these interactions might be due to the formation of chelates between metal ions and antibiotics. These results also indicate that some cations may have an important role in the antibacterial activity of antibiotics.
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PMID:The effects of ions on antibacterial activity of ofloxacin and ceftriaxone. 179 Jul 23


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