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Antimicrobial Agents and Chemotherapy Mar 1981The in vitro activities of four new beta-lactam antibiotics and dibekacin against aerobic bacteria were compared. The new cephalosporins were more broadly active against... (Comparative Study)
Comparative Study
The in vitro activities of four new beta-lactam antibiotics and dibekacin against aerobic bacteria were compared. The new cephalosporins were more broadly active against gram-negative bacteria than were presently available cephalosporins, but were less active against staphylococci.
Topics: Aminoglycosides; Anti-Bacterial Agents; Bacteria; Cephalosporins; Dibekacin; Kanamycin; Microbial Sensitivity Tests; Penicillins; Piperacillin
PubMed: 6454384
DOI: 10.1128/AAC.19.3.490 -
Nihon Rinsho. Japanese Journal of... Nov 2001
Review
Topics: Aminoglycosides; Animals; Anti-Bacterial Agents; Anti-Infective Agents, Local; Bacterial Proteins; Bacterial Toxins; Dibekacin; Enterotoxins; Gentian Violet; Humans; Immunoglobulins, Intravenous; Methicillin Resistance; Repressor Proteins; Staphylococcal Infections; Staphylococcus aureus; Superantigens; Teicoplanin; Vancomycin
PubMed: 11808124
DOI: No ID Found -
Archives of Medical Research 1993In spontaneously beating sinus venosus of the frog Caudiverbera caudiverbera the effects of bekanamycin and dibekacin, two aminoglycoside antibiotics, on action...
In spontaneously beating sinus venosus of the frog Caudiverbera caudiverbera the effects of bekanamycin and dibekacin, two aminoglycoside antibiotics, on action potentials of cardiac primary pacemaker cells were studied by intracellular recording. Bekanamycin and dibekacin induced a concentration-dependent decrease of the amplitude, overshoot and the rate of rise of the action potential. Both also flattened the slow diastolic depolarization leading to a marked decrease in beat rate. At the highest concentration used (1 x 10(-3) M), the aminoglycosides produced a complete inhibition of primary cells action potentials. It was preceded by the appearance of subthreshold oscillations of the membrane potential which were observed for a few minutes until the electrical activity of pacemaker cell ceased. During absence of impulse initiation a stable membrane potential about -40 mV was observed. Aminoglycoside effects, excepting those on SCL, were completely suppressed when external calcium was increased to 3.6 mM. The results support the conclusion that bekanamycin and dibekacin depress the electrical activity of pacemaker cells. It is suggested that this effect is induced by aminoglycosides blockade of the slow calcium current involved in both upstroke and slow diastolic depolarization and through modification of potassium outward current. Bekanamycin at a lower concentration than that needed to induce electrophysiological effects potentiated verapamil 1 x 10(-8) effects on cardiac pacemaker cells.
Topics: Action Potentials; Animals; Anura; Calcium; Dibekacin; Heart Conduction System; In Vitro Techniques; Kanamycin; Verapamil
PubMed: 8118157
DOI: No ID Found -
Nucleic Acids Research Jul 2021How aminoglycoside antibiotics limit bacterial growth and viability is not clearly understood. Here we employ fast kinetics to reveal the molecular mechanism of action...
How aminoglycoside antibiotics limit bacterial growth and viability is not clearly understood. Here we employ fast kinetics to reveal the molecular mechanism of action of a clinically used, new-generation, semisynthetic aminoglycoside Arbekacin (ABK), which is designed to avoid enzyme-mediated deactivation common to other aminoglycosides. Our results portray complete picture of ABK inhibition of bacterial translation with precise quantitative characterizations. We find that ABK inhibits different steps of translation in nanomolar to micromolar concentrations by imparting pleotropic effects. ABK binding stalls elongating ribosomes to a state, which is unfavorable for EF-G binding. This prolongs individual translocation step from ∼50 ms to at least 2 s; the mean time of translocation increases inversely with EF-G concentration. ABK also inhibits translation termination by obstructing RF1/RF2 binding to the ribosome. Furthermore, ABK decreases accuracy of mRNA decoding (UUC vs. CUC) by ∼80 000 fold, causing aberrant protein production. Importantly, translocation and termination events cannot be completely stopped even with high ABK concentration. Extrapolating our kinetic model of ABK action, we postulate that aminoglycosides impose bacteriostatic effect mainly by inhibiting translocation, while they become bactericidal in combination with decoding errors.
Topics: Anti-Bacterial Agents; Dibekacin; Kinetics; Peptide Elongation Factor G; Peptide Termination Factors; Peptides; Protein Biosynthesis; Protein Synthesis Inhibitors; RNA, Messenger; RNA, Transfer, Amino Acyl; Ribosomes
PubMed: 34125898
DOI: 10.1093/nar/gkab495 -
The Japanese Journal of Antibiotics Mar 1982The pharmacokinetic behavior of dibekacin was studied in 8 elderly subjects. These subjects had not apparent renal failure, although they were diagnosed as having...
The pharmacokinetic behavior of dibekacin was studied in 8 elderly subjects. These subjects had not apparent renal failure, although they were diagnosed as having various diseases such as arteriosclerosis, essential hypertension, etc. Dibekacin, 50 mg/subject, was infused intravenously for 1 hour. Serum and urine concentrations of dibekacin were measured by the bioassay and radioimmunoassay methods. The peak serum concentration of dibekacin ranged from 3.55 to 5.35 micrograms/ml when measured by bioassay, and from 3.19 to 8.9 micrograms/ml by radioimmunoassay. The biological half-life of dibekacin ranged from 2.13 to 3.45 hours, and from 1.57 to 3.55 hours, with these 2 methods. The area under the curve (AUC) ranged from 14.8 to 25.6 micrograms/ml-hr and from 11.3 to 18.0 microgram/ml . hr, respectively. Creatinine clearance showed a positive correlation with the elimination rate constant and a negative correlation with the distribution volume of dibekacin. These relationships were more pronounced when determined by radioimmunoassay. These data suggest that the peak serum concentration of dibekacin decreases with creatinine clearance. The serum and urine concentrations of dibekacin measured by the radioimmunoassay method correlated well with those measured by the bioassay method. Therefore, it was concluded that the radioimmunoassay method is a useful technique for monitoring the serum concentration of dibekacin.
Topics: Aged; Anti-Bacterial Agents; Biological Assay; Dibekacin; Female; Humans; Infusions, Parenteral; Kanamycin; Kinetics; Male; Middle Aged; Models, Biological; Radioimmunoassay
PubMed: 7097979
DOI: No ID Found -
Arzneimittel-Forschung 1979Dibekacin (Orbicin) is a new aminoglycoside antibiotic which chemically differs from tobramycin only by lack of an OH-group. The activity of dibekacin against E. coli,...
Dibekacin (Orbicin) is a new aminoglycoside antibiotic which chemically differs from tobramycin only by lack of an OH-group. The activity of dibekacin against E. coli, Klebsiella, Enterobacter, Serratia, Proteus indol-negative and indol-positive and Pseudomonas aeruginosa was compared with that of gentamicin, sisomicin, tobramycin and amikacin by tube dilution procedure. Dibekacin showed a high activity against P. aeruginosa including gentamicin-resistant strains. The development of resistance and cross-resistance in vitro in E. coli, Klebsiella, Proteus and P. aeruginosa to the five aminoglycosides was investigated. The experimentally produced resistance under increasing aminoglycoside concentrations was developing by multiple-step mutation. The frequency of cross-resistance is of great importance for the first choice of an aminoglycoside antibiotic in the hospitals. These in vitro studies have yielded that dibekacin and gentamicin are well suited for the first choice of an aminoglycoside in P. aeruginosa infection.
Topics: Amikacin; Bacteria; Dibekacin; Drug Resistance, Microbial; Gentamicins; Kanamycin; Microbial Sensitivity Tests; Sisomicin; Tobramycin
PubMed: 582126
DOI: No ID Found -
Acta Clinica Belgica 1982
Comparative Study
Topics: Adult; Anti-Bacterial Agents; Bacteria; Biological Availability; Dibekacin; Drug Resistance, Microbial; Humans; In Vitro Techniques; Kanamycin; Kinetics; Male; Microbial Sensitivity Tests; Tobramycin
PubMed: 7124274
DOI: 10.1080/22953337.1982.11718857 -
Archives of Oto-rhino-laryngology 1986We treated groups of pigmented guinea pigs with either intramuscular netilmicin or dibekacin at 100 and 150 mg/kg per day for 3 weeks. Saline was used as the control... (Comparative Study)
Comparative Study
We treated groups of pigmented guinea pigs with either intramuscular netilmicin or dibekacin at 100 and 150 mg/kg per day for 3 weeks. Saline was used as the control solution. All animals were tested weekly for both vestibular and auditory functions. The vestibular function was evaluated by the duration of post-rotatory nystagmus (PRN) elicited by interrupting the rotation of the animal around the vertical axis; auditory function was evaluated by the threshold response for the Preyer's pinna reflex (PPR). All animals were then sacrificed and either their labyrinths or Corti organs were processed for further investigations using the scanning electron microscope (SEM). The duration of PRN decreased over the treatment period in all of the groups as a result of adaptation. However, 150 mg/kg dibekacin produced a significant decrease of the PRN responses as compared to the control and other groups. This effect also continued during the recovery period. Likewise, the PPR threshold of the animals receiving 150 mg/kg dibekacin showed a significant increase at the end of the treatments and during the recovery period, while the other dibekacin group had no significant auditory impairment. Netilmicin at both doses did not significantly affect responses following either vestibular or auditory stimulations. SEM observations demonstrated that the sensory epithelia of the labyrinths and Corti organs affected by 150 mg/kg dibekacin had great losses of stereocilia, while comparable doses of netilmicin (150 mg/kg) had only very moderate losses of stereocilia in the labyrinths but not in the Corti organs.
Topics: Animals; Dibekacin; Ear, Inner; Female; Guinea Pigs; Hair Cells, Auditory; Kanamycin; Male; Microscopy, Electron, Scanning; Netilmicin; Nystagmus, Physiologic; Organ of Corti; Reflex, Acoustic; Vestibular Function Tests; Vestibule, Labyrinth
PubMed: 3487305
DOI: 10.1007/BF00453764 -
Antimicrobial Agents and Chemotherapy Sep 1978The antimicrobial activity of kanamycin, kanendomycin, gentamicin, amikacin, sisomicin, and dibekacin against 200 strains of Pseudomonas aeruginosa was compared....
The antimicrobial activity of kanamycin, kanendomycin, gentamicin, amikacin, sisomicin, and dibekacin against 200 strains of Pseudomonas aeruginosa was compared. Dibekacin was found to be the most active against the tested organisms, whereas the other aminoglycoside antibiotics fell in the following order of diminishing antibacterial potency: amikacin, sisomicin, gentamicin, kanendomycin, and kanamycin. Seven strains showed high-level resistance to gentamicin (minimal inhibitory concentration, 400 mug/ml), and two of them were also resistant to amikacin and sisomicin (minimal inhibitory concentration, 75 mug/ml). The minimal inhibitory concentration of dibekacin for these seven strains was 0.625 mug/ml.
Topics: Dibekacin; Drug Resistance, Microbial; Gentamicins; Kanamycin; Pseudomonas aeruginosa
PubMed: 101135
DOI: 10.1128/AAC.14.3.514 -
Kansenshogaku Zasshi. the Journal of... Mar 1984
Topics: Amikacin; Dibekacin; Drug Resistance, Microbial; Humans; Kanamycin; Leptospira; Leptospirosis; Tobramycin
PubMed: 6431032
DOI: 10.11150/kansenshogakuzasshi1970.58.197