-
Developmental Pharmacology and... 1984
Topics: Audiometry; Audiometry, Evoked Response; Dibekacin; Female; Half-Life; Humans; Infant, Low Birth Weight; Infant, Newborn; Infant, Newborn, Diseases; Infant, Premature; Kanamycin; Kinetics; Male
PubMed: 6518950
DOI: 10.1159/000457239 -
La Nouvelle Presse Medicale Nov 1982The principal pharmacokinetic parameters of dibekacin were studied in five adult subjects with normal renal function after IM and IV injection of a single dose of 1...
The principal pharmacokinetic parameters of dibekacin were studied in five adult subjects with normal renal function after IM and IV injection of a single dose of 1 mg/kg. The results obtained showed that the pharmacokinetics of dibekacine were independent of the dose (T1/2: 2.1 h; distribution volume: 14-161; renal clearance: congruent to 70 ml/min; urinary excretion in 24 hours congruent to 80%) and very similar to those of other aminoglycosides of the deoxystreptamine group.
Topics: Adult; Dibekacin; Humans; Kanamycin; Kidney; Kinetics; Male
PubMed: 7155848
DOI: No ID Found -
Pathologie-biologie Jun 1984Urinary tract infections in the elderly are severe and intractable, often justifying the use of aminoglycosides. We studied the effects of dibekacin in 28 patients, with...
Urinary tract infections in the elderly are severe and intractable, often justifying the use of aminoglycosides. We studied the effects of dibekacin in 28 patients, with no vesical catheter, whose average age was 78 +/- 6.1 years. The drug was given for ten days, in an average dose of 2.1 mg/kg/day divided into two injections. Serum concentration was measured after one hour on day 1 and after eight hours on days 1 and 10. Causative pathogens, all susceptible to dibekacin, were: 18 E. coli, 3 Proteus mirabilis, 3 Klebsiella, 1 Enterobacter cloacae, 1 Citrobacter and 2 Staphylococci. MIC and MBC of dibekacin were determined for each microorganism. Dibekacin was discontinued in four cases on day three because of persistent bacteriuria. Ten days after treatment end, 19 patients were cured, 4 had a relapse and 1 was reinfected. Average serum concentration of dibekacin, measured after eight hours, increased from 0.77 +/- 0.48 micrograms/ml on day 1 to 1.78 +/- 1.22 microgram/ml on day 10 (t = 4.42; p less than 0.0005), while, over the same period, there was no significant change in serum creatinine.
Topics: Aged; Blood Bactericidal Activity; Dibekacin; Female; Humans; Injections, Intramuscular; Kanamycin; Male; Microbial Sensitivity Tests; Urinary Tract Infections
PubMed: 6462747
DOI: No ID Found -
Antimicrobial Agents and Chemotherapy Mar 1978Against sulbenicillin- and gentamicin-susceptible strains of Pseudomonas aeruginosa, SCE-129 was about 10 times more active than sulbenicillin and had a similar activity... (Comparative Study)
Comparative Study
Against sulbenicillin- and gentamicin-susceptible strains of Pseudomonas aeruginosa, SCE-129 was about 10 times more active than sulbenicillin and had a similar activity to gentamicin and dibekacin. Sulbenicillin-resistant strains of P. aeruginosa were moderately resistant to SCE-129, whether these strains were gentamicin-resistant or not. Gentamicin-resistant strains of P. aeruginosa were resistant to dibekacin but not to SCE-129. Against P. maltophilia, the minimum inhibitory concentration of SCE-129 resembled those of sulbenicillin, gentamicin, and dibekacin. Most strains of P. cepacia were moderately resistant to SCE-129 and sulbenicillin and highly resistant to gentamicin and dibekacin.
Topics: Cefsulodin; Dibekacin; Gentamicins; Kanamycin; Microbial Sensitivity Tests; Penicillin G; Penicillin Resistance; Pseudomonas aeruginosa; Sulbenicillin
PubMed: 122528
DOI: 10.1128/AAC.13.3.536 -
The Journal of Antimicrobial... May 1978
Comparative Study
Topics: Bacteria; Dibekacin; Kanamycin; Microbial Sensitivity Tests
PubMed: 670124
DOI: 10.1093/jac/4.3.286 -
Journal of Pharmacobio-dynamics May 1981The LD50 values of dibekacin to mice were determined following three different methods of administration, namely, intravenous constant infusion, intravenous bolus...
The LD50 values of dibekacin to mice were determined following three different methods of administration, namely, intravenous constant infusion, intravenous bolus injection, and intramuscular injection. The serum levels of dibekacin were pharmacokinetically analyzed. The differences in LD50 values between the methods of administration were discussed from the viewpoints of pharmacokinetics. 1) The LD50 value following the intravenous constant infusion was higher than that following the intravenous bolus injection and approached the level of that following the intramuscular injection, when the infusion rate of the drug was decreased by increasing the infusion period. 2) The biological half-life of dibekacin in mice was 24--45 min. 3) The volume of distribution increased as its dose increased, and a linear correlation was noted between log Vd and log (dose). 4) The difference among the maximum serum concentrations calculated with dibekacin following the administration of LD50 was small, which coincided with the results of the experiment that the serum concentrations of dibekacin at the death following the administration of LD100 were almost the same regardless of the method of administration.
Topics: Animals; Dibekacin; Female; Half-Life; Infusions, Parenteral; Injections, Intramuscular; Injections, Intravenous; Kanamycin; Kinetics; Lethal Dose 50; Male; Mathematics; Mice; Mice, Inbred ICR
PubMed: 7288553
DOI: 10.1248/bpb1978.4.356 -
Antimicrobial Agents and Chemotherapy Apr 1985The tubular disposition of five aminoglycosides was studied in humans to establish a possible relationship between tubular reabsorption and the nephrotoxicity that has... (Comparative Study)
Comparative Study
The tubular disposition of five aminoglycosides was studied in humans to establish a possible relationship between tubular reabsorption and the nephrotoxicity that has been described in the literature. Thirty-three healthy male volunteers received a continuous intravenous infusion of isotonic saline with inulin, followed 1 h later by inulin plus gentamicin, dibekacin, tobramycin, netilmicin, or amikacin (1 mg/kg per h) or amikacin (4 mg/kg per h) over a period of 2 h. Brain-stem-evoked response audiometry was performed both before and at the end of each infusion. The latency of wave V remained constant whichever antibiotic was considered. The glomerular filtration rate did not vary significantly during the infusion of each drug. The percent fractional excretion was 79 +/- 6, 81 +/- 22, 85 +/- 5, and 99 +/- 9 for gentamicin, dibekacin, tobramycin, and netilmicin, respectively, and 83 +/- 4 and 124 +/- 13 for amikacin at concentrations of 1 and 4 mg/kg per h, respectively. Net balance and renal clearance were similar for the five aminoglycosides when administered at a rate of 1 mg/kg per h. With gentamicin only, fractional excretion was correlated with the urinary flow rate. We can conclude that (i) gentamicin, generally considered the most nephrotoxic agent, had the highest degree of net reabsorption; (ii) netilmicin exhibited a net zero tubular balance; (iii) amikacin had different patterns of tubular disposition according to the dose, i.e., reabsorption at 1 mg/kg per h and secretion at 4 mg/kg per h, raising the hypothesis of a saturable process of reabsorption; and (iv) these differences in tubular reabsorption could account at least in part for the known different nephrotoxic potentials of these five aminoglycosides in humans.
Topics: Adult; Amikacin; Aminoglycosides; Anti-Bacterial Agents; Blood Proteins; Dibekacin; Electrolytes; Gentamicins; Glomerular Filtration Rate; Humans; Kidney Tubules; L-Lactate Dehydrogenase; Male; Netilmicin; Protein Binding; Tobramycin
PubMed: 4004192
DOI: 10.1128/AAC.27.4.520 -
Drugs Under Experimental and Clinical... 1989Seven N-alkylsulfonate derivatives of an aminoglycoside antibiotic, dibekacin, were prepared and their nephrotoxicity was examined. Using water-supplied and...
Seven N-alkylsulfonate derivatives of an aminoglycoside antibiotic, dibekacin, were prepared and their nephrotoxicity was examined. Using water-supplied and water-depleted rats and the BUN value as a nephrotoxic measure, dibekacin-di-N-methanesulfonate, pentasodium dibekacin-penta-N-methanesulfonate, -penta-N-ethanesulfonate, disodium dibekacin-di-N-methanesulfonate sesquisulfate, disodium and dipotassium dibekacin-di-N-ethanesulfonate sesquisulfates and sodium dibekacin-mono-N-ethane-sulfonate disulfate showed low nephrotoxicity as compared to that of the original dibekacin sulfate. Notably, dibekacin-di-N-methanesulfonate caused little change in the BUN value and was bioactive in vitro but not active in vivo against a Pseudomonas aeruginosa infection model in mice. Among the bioactive N-alkylsulfonates in vivo, disodium and dipotassium dibekacin-di-N-ethanesulfonate sesquisulfates showed a lower degree of elevation of BUN, urine volume and urine protein, lower mortality and better body weight gain than those of dibekacin sulfate during consecutive treatment for 12 and 28 days.
Topics: Animals; Bacteria; Blood Urea Nitrogen; Body Weight; Chemical Phenomena; Chemistry; Dibekacin; Kanamycin; Kidney Diseases; Lethal Dose 50; Male; Mice; Mice, Inbred ICR; Microbial Sensitivity Tests; Rats; Rats, Inbred Strains; Urodynamics
PubMed: 2591296
DOI: No ID Found -
The Tohoku Journal of Experimental... Jun 1987A possible mechanism responsible for the combined effects of sulbenicillin and dibekacin on Pseudomonas aeruginosa IAM 1007 was investigated. The bactericidal activity... (Comparative Study)
Comparative Study
A possible mechanism responsible for the combined effects of sulbenicillin and dibekacin on Pseudomonas aeruginosa IAM 1007 was investigated. The bactericidal activity of the above two drugs in combination was very strong. The regrowth of test strains after removal of the drugs was suppressed markedly, even when they were exposed to sulbenicillin plus dibekacin at a subinhibitory concentration of individual drugs. Sulbenicillin caused elongation of the bacterial cells. At the early stage of elongation, no demonstrable changes of ultrastructure of the cell wall were observed. At the late stage, lysis of the peptidoglycan layer occurred and spheroplast was formed. However, most of the outer membrane of the cell wall remained intact. Sulbenicillin acts upon the peptidoglycan layer, but not on the outer membrane. Thus it is difficult for sulbenicillin alone to cause cell lysis. On the other hand, dibekacin caused destruction of ribosomes and lysis of the outer membrane of the cell wall. Both sulbenicillin and dibekacin act on the cell wall, the former on the peptidoglycan layer (the inner membrane) and the latter on the outer membrane. The combined use of sulbenicillin and dibekacin caused elongation of bacilli and severe destruction of the inner and outer membranes of the cell wall. These morphological changes occurred even when the concentration of the individual drug was lower than its minimum inhibitory concentration (MIC). Furthermore, the cells elongated by sulbenicillin were ruptured easily when treated with dibekacin subsequently. The bacilli treated with dibekacin at a concentration lower than MIC and then treated with sulbenicillin at a concentration lower than MIC showed a marked elongation of the cells, which indicated that the effects of sulbenicillin was enhanced by dibekacin. These findings suggested strongly that sulbenicillin and dibekacin act on cell wall constituents and that their effects were complementary and synergistic.
Topics: Cell Wall; Dibekacin; Drug Synergism; Kanamycin; Microscopy, Electron; Penicillin G; Pseudomonas aeruginosa; Sulbenicillin
PubMed: 3114912
DOI: 10.1620/tjem.152.119 -
Developmental Pharmacology and... 1984
Topics: Birth Weight; Dibekacin; Humans; Infant, Newborn; Infant, Newborn, Diseases; Injections, Intramuscular; Injections, Intravenous; Kanamycin; Kinetics
PubMed: 6518951
DOI: 10.1159/000457240