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La Nouvelle Presse Medicale Nov 1982
Topics: Animals; Dibekacin; Humans; Kanamycin; Labyrinth Diseases
PubMed: 7155843
DOI: No ID Found -
Drugs Jun 1984Sisomicin is a naturally occurring aminoglycoside antibiotic produced by Micromonospora inyoensis, while dibekacin and netilmicin are both semisynthetic aminoglycosides.... (Review)
Review
Sisomicin is a naturally occurring aminoglycoside antibiotic produced by Micromonospora inyoensis, while dibekacin and netilmicin are both semisynthetic aminoglycosides. Dibekacin is 3',4'-dideoxykanamycin B and netilmicin is 1-N-ethyl sisomicin. In both cases, these modifications render the agents insusceptible to some of the enzymes found in resistant strains of bacteria which inactivate the parent compounds. Antibacterial activity: All 3 drugs show bactericidal activity against a wide range of Gram-negative bacteria (including E. coli, Enterobacter, Klebsiella and Proteus spp. and Ps. aeruginosa) and also against staphylococci; however, in common with other amino-glycosides, streptococci are usually resistant (except when beta-lactam antibiotics are used in combination) and anaerobic organisms are not sensitive. Sisomicin is closely related structurally to gentamicin Cla, but in vitro studies have shown it to have superior activity to gentamicin against Ps. aeruginosa, closely paralleling the activity of tobramycin, while still possessing the high activity of gentamicin against Serratia and other Gram-negative rods. However, sisomicin is inactivated by virtually all bacterial enzymes which inactivate gentamicin and tobramycin. Nevertheless, it retains useful activity against a number of gentamicin-resistant strains of Ps. aeruginosa which are resistant by non-enzymatic (possibly permeability barrier) mechanisms; in this respect it closely resembles tobramycin. Dibekacin closely resembles tobramycin structurally and in vitro it seems to have a very similar antibacterial spectrum, including activity against some strains of Ps. aeruginosa resistant to gentamicin. Netilmicin has a generally broader antibacterial spectrum than gentamicin, tobramycin, sisomicin or debekacin and is resistant to inactivation by phosphorylating and adenylylating enzymes; however, it is inactivated by all acetylases, apart from acetylase 3-I. Its spectrum is therefore not as wide as that of amikacin against 'gentamicin-resistant' strains. Nonetheless, it is intrinsically more active than amikacin, weight-for-weight, against sensitive strains, apart possibly from Ps. aeruginosa. In fact, its activity against species of the Enterobacteriaceae and staphylococci sensitive to gentamicin is of the same order as the latter and possibly better for Klebsiella-Enterobacter species. All 3 agents show marked antibacterial synergy with a variety of beta-lactam antibiotics against a range of bacteria. Pharmacokinetically, sisomicin, netilmicin and dibekacin all behave like gentamicin. All 3 drugs are excreted in the urine unchanged and have beta-phase elimination half-lives of around 2 to
Topics: Aging; Animals; Bacterial Infections; Dibekacin; Drug Interactions; Drug Resistance, Microbial; Drug Synergism; Gentamicins; Humans; Kanamycin; Kidney Diseases; Netilmicin; Sisomicin
PubMed: 6376062
DOI: 10.2165/00003495-198427060-00003 -
La Nouvelle Presse Medicale Nov 1982
Topics: Animals; Dibekacin; Humans; Kanamycin
PubMed: 7155842
DOI: No ID Found -
Antimicrobial Agents and Chemotherapy Feb 1984The role of the tubular reabsorption of aminoglycosides in nephrotoxicity was considered. The tubular reabsorption rate, fractional reabsorption, and net balance,...
The role of the tubular reabsorption of aminoglycosides in nephrotoxicity was considered. The tubular reabsorption rate, fractional reabsorption, and net balance, expressed as the excreted to infused aminoglycoside ratio, were concomitantly studied in male rabbits by continuous infusion of gentamicin, netilmicin, dibekacin, and amikacin. Aminoglycoside nephrotoxicity was evaluated by creatinine levels in serum and pathological renal damage after 14 days of a low- or high-dose regimen, comprising either eight, hourly intramuscular injections of gentamicin, netilmicin, or dibekacin (4 mg/kg) or amikacin (16 mg/kg); twelve, hourly intramuscular injections of gentamicin, netilmicin, or dibekacin (15 mg/kg) or amikacin (60 mg/kg); or injections of saline for the control group. Aminoglycosides exhibited three degrees of tubular reabsorption: gentamicin had the highest, netilmicin had the lowest, and dibekacin and amikacin had intermediate degrees of reabsorption. Nephrotoxicity associated with alteration in renal histology was observed with gentamicin and, to a lesser extent, with dibekacin in the high-dose regiment. No nephrotoxicity was noted with netilmicin or amikacin compared with the control group. Concentrations of the aminoglycosides in renal cortex and serum were not predictive of renal toxicity. Except for amikacin, which appeared to exhibit the lowest intrinsic renal toxicity, nephrotoxicity was correlated with the tubular reabsorption of each aminoglycoside. It was concluded that aminoglycoside renal toxicity can be determined by two major factors: importance of transport into tubular cells and intrinsic intracellular toxicity.
Topics: Amikacin; Aminoglycosides; Animals; Anti-Bacterial Agents; Blood Proteins; Dibekacin; Gentamicins; Kidney Diseases; Kidney Tubules; Male; Netilmicin; Protein Binding; Rabbits
PubMed: 6712201
DOI: 10.1128/AAC.25.2.168 -
Journal of Clinical Pharmacology 1980Dibekacin (3',4-dideoxykanamycin B) is a new semisynthetic aminoglycoside developed in Japan and one which has found wide clinical acceptance in that country. The... (Comparative Study)
Comparative Study
Dibekacin (3',4-dideoxykanamycin B) is a new semisynthetic aminoglycoside developed in Japan and one which has found wide clinical acceptance in that country. The antibacterial activity of this compound indicates that it is relatively similar to gentamicin. Since it appears that the intrarenal distributional characteristics and renal cortical kinetics of aminoglycosides provide some predictive information concerning the clinical incidence of nephrotoxicity, we designed a series of pharmacokinetic studies in healthy mongrel dogs which would define such kinetic information for dibekacin and would contrast the results with similar studies for gentamicin and tobramycin. The renal cortical kinetics of dibekacin, as developed in these studies, show that in a canine model the behavior of dibekacin is similar to that of gentamicin and significantly different from tobramycin. Dibekacin and gentamicin show reproducibly higher renal cortical tissue concentrations than tobramycin in both the acute infusion studies and multiple dosing studies. The results suggest that dibekacin may possess the same inherent nephrotoxic potential as that of gentamicin. In order to show any difference in clinical toxicity between gentamicin and dibekacin, a very extensive randomized, double-blind, prospective clinical trial of efficacy and toxicity will be needed.
Topics: Animals; Anti-Bacterial Agents; Dibekacin; Dogs; Female; Gentamicins; Kanamycin; Kidney; Kidney Cortex; Kinetics; Tobramycin
PubMed: 7430416
DOI: 10.1002/j.1552-4604.1980.tb02545.x -
Acta Oto-laryngologica 1987The vestibular toxicity of two aminoglycoside antibiotics, dibekacin sulfate and habekacin sulfate, and of a drug with potent antimitotic activity, cisplatin...
The vestibular toxicity of two aminoglycoside antibiotics, dibekacin sulfate and habekacin sulfate, and of a drug with potent antimitotic activity, cisplatin (cis-diamminedichloroplatinum) has been investigated in both rats and frogs. In rats, chronic intraperitoneal injection of a saline solution of dibekacin (50 mg/kg/day), habekacin (50 mg/kg/day), cisplatin (0.5 mg/kg/day) for 4 weeks and of cisplatin (1 mg/kg/day) for 5 weeks, produced no behavioral vestibular disorders and the righting reflex could be elicited at any time. In frogs, the spontaneous discharge was recorded from individual fibres of the ampullary nerve of the horizontal semicircular canal before and after acute administration of the drugs, dissolved in Ringer, into the perilymph of the inner ear near the horizontal ampulla. Following injection of 1 microliter of solutions containing 10 micrograms or 20 micrograms of dibekacin, 20 micrograms or 50 micrograms of habekacin, 0.5 micrograms, 2.5 micrograms or 10 micrograms of cisplatin, the spontaneous discharge decreased in a number of fibres and was sometimes completely abolished. The vestibular toxicity of the three drugs tested is discussed with respect to that of aminosides whose ototoxicity is well known.
Topics: Aminoglycosides; Animals; Anti-Bacterial Agents; Body Weight; Cisplatin; Dibekacin; Kanamycin; Labyrinth Diseases; Rana esculenta; Rats; Vestibule, Labyrinth
PubMed: 3499743
DOI: 10.3109/00016488709107334 -
Antimicrobial Agents and Chemotherapy Dec 1980The nephrotoxicity of dibekacin was compared with those of gentamicin and amikacin in a rat model. The doses used were 3, 10, and 30 times the suggested human... (Comparative Study)
Comparative Study
The nephrotoxicity of dibekacin was compared with those of gentamicin and amikacin in a rat model. The doses used were 3, 10, and 30 times the suggested human therapeutic dose on a weight basis. Indices of glomerular and tubular function failed to clearly differentiate the drugs. Dibekacin and gentamicin produced equally severe injury to the renal tissue. Slightly less damage occurred with amikacin.
Topics: Amikacin; Animals; Dibekacin; Gentamicins; Kanamycin; Kidney; Male; Rats
PubMed: 7235685
DOI: 10.1128/AAC.18.6.983 -
The Journal of Antibiotics Mar 2018On the occasion of the 60th anniversary of the discovery (1957) of kanamycin (KM), a series of research achievements on KM and its semisynthetic derivative Arbekacin... (Review)
Review
On the occasion of the 60th anniversary of the discovery (1957) of kanamycin (KM), a series of research achievements on KM and its semisynthetic derivative Arbekacin (ABK) are outlined. KM was first used clinically in 1958 and was appreciated for its remarkable curing effect on various bacterial infections, especially tuberculosis. ABK is a KM derivative rationally semisynthesized to overcome KM resistance due to enzymatic phosphorylation and acetylation. Since its approval in 1990 as an anti-MRSA drug, ABK has been and still is effectively used in chemotherapy because MRSA rarely develops high ABK-resistance. Research that illuminated the unique features of ABK enabling it to resist the development of resistance by MRSA are also described.
Topics: Animals; Anti-Bacterial Agents; Dibekacin; Humans; Kanamycin; Methicillin-Resistant Staphylococcus aureus; Staphylococcal Infections
PubMed: 29402999
DOI: 10.1038/s41429-017-0017-8 -
Der Urologe. Ausg. A Nov 1979
Topics: Anti-Bacterial Agents; Anti-Infective Agents, Urinary; Chemical Phenomena; Chemistry; Dibekacin; Drug Interactions; Kanamycin; Microbial Sensitivity Tests
PubMed: 505693
DOI: No ID Found -
Journal of Pharmacobio-dynamics May 1981The behaviors of dibekacin after three administration methods to rabbits and dogs were pharmacokinetically analysed. 1) In both rabbits and dogs, the pharmacokinetic...
The behaviors of dibekacin after three administration methods to rabbits and dogs were pharmacokinetically analysed. 1) In both rabbits and dogs, the pharmacokinetic constants for the intravenous constant infusion and intramuscular injection were similar to each other, and the serum levels after the intravenous constant infusion for 1 hr were similar to those after the intramuscular injection except the peak time. 2) In both rabbits and dogs, Vd increased with the dose and a linear correlation was noted between log Vd and log (dose). 3) The tissue concentrations of dibekacin decreased with the decrease in the serum concentration. 4) A correlation equation, log T 1/2 = 0.194 . log B + 1.128, was obtained, where T 1/2 and B represent the biological half-life of dibekacin and the body weight of animals, respectively. It was suggested that the pharmacokinetic behaviors of dibekacin in human beings can be predicted from the results of the animal experiments.
Topics: Animals; Dibekacin; Dogs; Female; Infusions, Parenteral; Injections, Intramuscular; Injections, Intravenous; Kanamycin; Kinetics; Male; Mathematics; Rabbits; Species Specificity; Tissue Distribution
PubMed: 7288554
DOI: 10.1248/bpb1978.4.362