Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Netilmicin”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 685 records · Page 38Linked to original sources
PubMed1980

The comparative neuromuscular blocking effects of some aminoglycoside antibiotics.

The neuromuscular blocking effects of aminoglycoside antibiotics were tested in the isolated phrenic nervediaphragm preparation of the rat. The neuromuscular blocking potencies were netilmicin equals sisomicin much greater than neomycin much greater than gentamicin much greater than tobramycin. The EC 50's (concentration resulting in 50 percent depression of the original twitch tension) were respectively 13.3 x 10(-4); 13.4 x 10(-4); 13.6 x 10(-4); 15.1 x 10(-4); and 95.3 x 10(-4) Mol/l for netilmicin, sisomicin, neomycin, gentamicin and tobramycin. When a threshold dose of pancuronium was added to the bathing fluid the EC 50's were diminished respectively by a factor of 0.4 (sisomicin and neomycin) 0.5 (tobramycin) and 0.6 (netilmicin and gentamicin). Addition of a threshold dose of Org-NC45, a new steroidal non-depolarizing muscle relaxant, diminished the EC 50's to the same extent. The neuromuscular blocking effects of pancuronium and Org-NC45 themselves were potentiated by pretreatment of the preparations with a threshold dose of the aminoglycoside. Comparison of the results demonstrated the following potentiating effects: netilmicin equals sisomicin much greater than neomycin much greater than gentamicin greater than tobramycin. Which is in the same sequence s the neuromuscular blocking potencies of these drugs.

Aminoglycosides↗
PubMed1980

Combined effect of benzylpenicillin and gentamicin/netilmicin on Streptococcus faecalis.

The 50% inhibitory concentrations (IC50) of gentamicin and netilmicin were determined for 55 clinical isolates of Streptococcus faecalis, approximately half of which were recovered by culture of blood samples from patients with endocarditis. The IC50 for gentamicin was less than 5 micrograms/ml for 22 strains and less than 40 micrograms/ml for all strains, and for netilmicin the IC50 was less than 5 micrograms/ml for 51 strains and less than 40 micrograms/ml for all strains. Eight out of the 55 strains were found to have IC50 values greater than 10(4) micrograms/ml for streptomycin (3). The bacterial effect of combinations of benzylpenicillin and gentamicin or netilmicin was studied in 19 strains of S. faecalis which represented different levels of resistance to streptomycin. Netilmicin was as effective as gentamicin in combination with benzylpenicillin against all strains.

Dose-Response Relationship, Drug↗
PubMed2000

Effects of some antibiotics on enzyme activity of glucose-6-phosphate dehydrogenase from human erythrocytes.

Inhibitory effects of some antibiotics on glucose-6-phosphate dehydrogenase from the erythrocytes of human have been investigated. For this purpose, at the beginning, erythrocyte glucose-6-phosphate dehydrogenase was purified 13.654 times in a yield of 28% by using ammonium sulphate precipitation and 2',5'-ADP Sepharose 4B affinity gel. Temperature of +4 degrees C was maintained during the purification process. Enzyme activity was determined with the Beutler method by using a spectrophotometer at 340 nm. This method was utilized for all kinetic studies. Sodium ceftizoxime, sodium ampicillin, sodium cefuroxime, sodium cefazolin, sodium cefoperazone, streptomycin sulphate, gentamicin sulphate, and netilmicin sulphate were used as antibiotics. All the antibiotics indicated the inhibitory effects on the enzyme. K(i) constants for glucose-6-phosphate dehydrogenase were found by means of Lineweaver-Burk graphs. While sodium cefoperazone, gentamicin sulphate, and netilmicin sulphate showed competitive inhibition, the others displayed non-competitive inhibition. In addition, I(50) values of the antibiotics were determined by plotting activity percent vs [I]. In addition, in vivo studies were done for sodium sefuroxime in Sprague-Dawley type rats. It was found that G6PD in erythrocyte was more inhibited by the drug in 2.5 h.

Adult↗
PubMed1978

Effect of aminoglycosides on proximal tubular membranes of the human kidney.

The effect of the aminoglycosides amikacin, gentamicin, netilmicin sisomicin and tobramycin on the proximal tubule of the human kidney was investigated in 78 healthy subjects. Fifteen adults were each given gentamicin, sisomicin or tobramycin 3 mg/kg bodyweight, 10 subjects received netilmicin 3 mg/kg or amikacin 15 mg/kg additionally seven subjects amikacin 10 mg and six subjects netilmicin 6 mg on three consecutive days. The principal enzyme of the brush border membrane of the proximal tubule, alanine aminopeptidase (AAP), was determined enzymatically and immunologically in 24-hour urines. The effects of the various aminoglycosides on the membranes were different. Less of membrane AAP was greatest after amikacin and was least after tobramycin. There was no difference between gentamicin, netilmicin, and sisomicin, which had an effect intermediate between the other two compounds. The elimination of AAP occurred at intervals which might possibly have been caused by impairment of cell cycles.

Adolescent↗
PubMed1981

Differential effect of aminoglycoside treatment on glomerular filtration and renal reabsorption of lysozyme in rats.

The aminoglycosides gentamicin, netilmicin and tobramycin were each administered (30 mg/kg/day) to male Wistar rats for 21 days. At 7, 14 and 21 days rats were anesthetized and renal clearances of inulin and egg-white lysozyme were quantified. Plasma concentration of lysozyme varied between 20 and 120 mg/liter in control and aminoglycoside treated rats. Inulin clearance (GFR) averaged 0.96 ml/min/kidney in control rats. Whereas GFR decreased to an average value of 0.47 ml/min/kidney in gentamicin treated rats, GFR did not fall in tobramycin treated rats, averaging 0.97 ml/min/kidney over the entire treatment period. In netilmicin rats GFR declined to 0.53 ml/min/kidney after 7 days of treatment and then increased to 0.78 ml/min/kidney after 14 days and 21 days of treatment. Reabsorption of lysozyme averaged about 94% of the filtered load in control rats. Reabsorption of lysozyme decreased in gentamicin treated rats to about 58% after 7 days and 14 days of treatment and increased to 79% after 21 days of treatment. After tobramycin reabsorption of lysozyme decreased to about 67% after 7 days of treatment and increased to 85% after 14 days and 21 days of treatment. Reabsorption of lysozyme remained unchanged when compared to controls over the entire treatment period in netilmicin treated rats. Thus, gentamicin reduced both GFR and renal reabsorption of lysozyme. Netilmicin reduced GFR somewhat without altering lysozyme reabsorption whereas tobramycin compromised lysozyme reabsorption without altering GFR. These differences might suggest differences in site(s) of action of various aminoglycosides.

Absorption↗
PubMed2004

Effects of some antibiotics on human erythrocyte 6-phosphogluconate dehydrogenase: an in vitro and in vivo study.

The in vitro and in vivo effects of some antibiotics on human erythrocyte 6-phosphogluconate dehydrogenase were investigated. Human erythrocyte 6-phosphogluconate dehydrogenase was purified with ammonium sulphate precipitation, 2',5' ADP-Sepharose 4B affinity and gel filtration chromatography. Some antibiotics (netilmicin sulphate, cefepime, amikacin, isepamycin, chloramphenicol, ceftazidim, teicoplanin, ampicillin, ofloxacin, levofloxacin, cefotaxime, penicillin G, gentamicin sulphate, ciprofloxacin) inhibited enzyme activity in vitro but others (cefozin, decefin, streptomycin, combisid, and meronem) were devoid of inhibitory effects. For the drugs having low IC50 values (netilmicin sulphate and cefepime), in vivo studies were performed in rats. Netilmicin sulphate at 15-mg/kg inhibited enzyme activity significantly (p < 0.001) 1 h, 2 h, and 3 h after dosing and cefepime at 200-mg/kg very significantly (p < 0.001) inhibited the enzyme 1 h and 2 h after dosing. Netilmicin sulphate and cefepime inhibited rat erythrocyte 6-phosphogluconate dehydrogenase both in vivo and in-vitro.

Animals↗
PubMed1992

Bactericidal activity of antibiotics alone and in combination against Enterococcus faecalis in a pharmacodynamic model.

We evaluated the bactericidal kinetics of teicoplanin, mezlocillin, netilmicin, and ciprofloxacin alone and in dual combinations against strains of Enterococcus faecalis susceptible or resistant to ampicillin in a pharmacodynamic model reproducing in bacterial culture in active human plasma or Mueller-Hinton broth the serum kinetics of these antibiotics in humans. Killing was not different in cultures grown in plasma and those grown in broth. Antibiotics used alone had no or low bactericidal activity except for high-dose ciprofloxacin (600 mg intravenously [iv] twice daily or 750 mg orally twice daily), which achieved a 3- to 4-log reduction in colony-forming units (cfu). Netilmicin was equally active at 6 mg/kg once a day or 2 mg/kg three times daily in all combinations. No major increase in bactericidal activity was detected in any combination that included mezlocillin. Maximal synergistic killing was observed for the combination of teicoplanin plus netilmicin (both at three-times daily and once-daily dosing), which sterilized the bacterial cultures (initial inoculum, 10(6) cfu/mL). Combinations of ciprofloxacin at 600 mg iv twice daily and 750 mg orally twice daily plus either teicoplanin or netilmicin were less synergistic but equally effective in total killing as a result of the high bactericidal activity of ciprofloxacin alone.

Anti-Bacterial Agents↗
PubMed1989

The prevalence of high-level aminoglycoside resistance among enterococci isolated from blood cultures during 1980-1988.

Two hundred and eighty-one strains of enterococci isolated from blood cultures of 281 consecutive patients during 1980-1988 and 108 strains of enterococci isolated from miscellaneous clinical materials during 1988 were studied for high-level resistance (MIC greater than 2000 mg/l) to amikacin, kanamycin, streptomycin, gentamicin, tobramycin and netilmicin. Before 1985 there was no enterococcal strain with high-level resistance to amikacin, gentamicin, tobramycin or netilmicin, but 14% were resistant to kanamycin and 21% to streptomycin. For strains isolated from blood cultures during 1985-1988, the prevalence of high-level resistance was as follows: amikacin, less than 1%; kanamycin, 35%; streptomycin, 26%; gentamicin, 9%; tobramycin, 9%, netilmicin, 4%. Prevalence of high-level aminoglycoside resistance of enterococci isolated from miscellaneous sources during 1988 was higher (amikacin, 5%; kanamycin, 37%; streptomycin, 31%; gentamicin, 24%, tobramycin, 27%; netilmicin, 10%). Among strains isolated from blood cultures between 1980-1984, 24% (30 of 126 strains) and among 1985-1988 strains, 40% (62 of 155 strains) were resistant to at least one of the aminoglycosides tested. Similarly, among the miscellaneous strains, 40% (43 of 108 strains) had high-level resistance to at least one of the aminoglycosides tested.

Aminoglycosides↗
PubMed1984

Gentamicin- and methicillin-resistant, clinical isolates of Staphylococcus aureus: comparative in vitro and in vivo efficacy of alternative antimicrobial drugs.

Six representative clinical isolates of gentamicin- and methicillin-resistant (GRMR) Staphylococcus aureus, constituting phage groups II and III, were susceptible only to amikacin, cefamandole, clindamycin, fosfomycin, fusidic acid, netilmicin, nitrofurantoin, trimethoprim-sulfamethoxazole, and vancomycin (Bauer-Kirby test). With few exceptions, the minimal bactericidal concentrations of the beta-lactam and aminoglycoside antibiotics tested, fusidic acid, and irregularly those of vancomycin, but not those of fosfomycin and rifampin, exceeded minimal inhibitory concentrations values by at least 8-fold. In vitro, combinations of rifampin with cefamandole, cefazolin, cefotaxime, erythromycin, fosfomycin, fusidic acid, netilmicin, and vancomycin yielded indifferent effects. The GRMR S. aureus strains were refractory against 50, 65, and 80 vol% of fresh defibrinated blood; following reduction of viable counts at 2 h (greater than or equal to 90%), rebound growth invariably occurred within 4 h after exposure. Combined human blood (55 vol%)-antibiotic assays revealed rifampin as the most effective drug, followed by vancomycin, fusidic acid, and cefamandole, in that order. Blood plus cefotaxime, cefazolin, or netilmicin yielded indifferent effects; fosfomycin failed in vitro. In terms of speed of recovery and survival data (chi 2 test), cyclophosphamide-pretreated, i.e., leukopenic NMRI mice responded best to chemotherapy with rifampin, followed by vancomycin, cefamandole, netilmicin, and fosfomycin, in that order; cefazolin yielded variable results.

Animals↗
PubMedDate not supplied

Effects of some drugs on rat erythrocyte 6-phosphogluconate dehydrogenase: an in vitro and in vivo study.

The in vitro and in vivo effects of some drugs on rat erythrocytes 6-phosphogluconate dehydrogenase were investigated in this study. Rat erythrocyte 6-phosphogluconate dehydrogenase was partially purified with ammonium sulfate precipitation. The enzyme activity was determined by Beutler's method. Some drugs such as ampicillin, amikacin sulfate, and netilmicin sulfate inhibited the enzyme activity in in vitro conditions, while metamizole activated it. The I50 values of the inhibiting drugs were 66.2, 5.836, and 0.963 mM, respectively. For the drugs having low I50 values (drug concentrations which produce 50% inhibition) (amikacin sulfate and netilmicin sulfate), in vivo studies were performed in rats (Sprague-Dawley). Amikacin sulfate at 64 mg/kg inhibited the enzyme activity significantly (p < 0.05) 2 h after dosing. Netilmicin sulfate at 6.4 mg/kg also inhibited the enzyme significantly (p < 0.05) 4 h after dosing. Amikacin sulfate and netilmicin sulfate inhibited rat erythrocyte 6-phospogluconate dehydrogenase both in vivo and in vitro. The enzyme was inhibited in vitro by ampicillin and activated in vitro by metamizole.

Animals↗
PubMed2004

[Aminoglycoside resistance of Acinetobacter baumannii hospital strains in the Czech Republic].

OBJECTIVE: To investigate the nature of aminoglycoside resistance of clinically important multidrug-resistant (MDR) Acinetobacter baumannii strains from the Czech Republic. MATERIAL AND METHODS: Seventy MDR hospital strains from 1991-2001 classified into pan-European clones I (n = 41) and II (n = 21) and a group of other MDR strains (n = 8) were studied. Fifteen other strains wild-type susceptible to aminoglycosides were used as controls. Susceptibility to aminoglycosides was determined by the disk diffusion and agar dilution tests. The presence of six genes encoding different aminoglycoside-modifying enzymes (AME) and of the adeB gene encoding a component of the AdeABC efflux pump was detected using PCR. RESULTS: MDR strains showed the following pattern of resistance to aminoglycosides: kanamycin (93 %; inhibition zone diameters < or =13 mm), gentamicin (87 %; MICs > or =16 mg/l), amikacin (47 %; MICs > or =64 mg/l), tobramycin (31 %; MICs > or = 16 mg/l) and netilmicin (17 %; MICs ? 32 mg/l). Forty-six (66 %) MDR strains had netilmicin MICs of 8-16 mg/l in contrast to 0.5-1.0 mg/l found for control susceptible strains. The presence of at least one of the following AME genes was detected in 66 (94 %) MDR strains: aphA1 (n = 56), aacC1 (n = 52), aphA6 (n = 39) and aadB (n = 20). The presence of these genes and phenotypes of resistance to kanamycin, gentamicin, tobramycin and amikacin were in good agreement. The genes encoding netilmicin-modifying enzymes (aacC2, aacA4) were not detected in any strain. Fifty-six (80 %) MDR strains comprised two to four different AME genes in eight combinations. Clones I and II shared all of the genes studied (with the exception of aadB not detected in clone I). The gene adeB was found in all MDR strains and eight of 15 control susceptible strains. CONCLUSION: Clinically relevant aminoglycoside resistance of Czech A. baumannii strains is significantly associated with the genes encoding enzymatic modification of kanamycin, gentamicin, amikacin and tobramycin. These genes can spread horizontally and emerge in different combinations leading to high-level resistance to multiple aminoglycosides. The AdeABC pump is likely to play a role in the intermediate susceptibility to netilmicin but further study is needed in this regard.

Acinetobacter baumannii↗
PubMed1989

[Yersinia enterocolitica infections and thalassemia major in children].

We report two cases of severe Yersinia enterocolitica infection in children with homozygous thalassemia. One patient had septicemia and the other had mesenteric adenitis. Two factors can enhance the infectivity of Yersinia enterocolitica in children with thalassemia: iron overload and deferoxamine therapy. Laparotomy and cefotaxime-netilmicin therapy were successful in the patient with mesenteric adenitis. In the patient with septicemia, cefotaxime-netilmicin, then doxycycline-netilmicin failed, and recovery was finally achieved under rifampicin-netilmicin. Because of the possibility of septicemic dissemination secondary to digestive Yersinia enterocolitica infection in children with thalassemia, we advocate immediate discontinuation of deferoxamine and prescription of oral antimicrobial therapy (trimethoprim-sulfamethoxazole for instance) in every thalassemic patient with febrile diarrhea.

Adolescent↗
PubMed1987

Enterococci and aminoglycosides: evaluation of susceptibility and synergism of their combination with piperacillin.

Some clinical isolates of enterococci were tested for susceptibility to gentamicin, tobramycin, amikacin and netilmicin. Five percent of Streptococcus faecalis tested demonstrated high level resistance (minimum inhibitory concentration (MIC) greater than 2024 micrograms/ml) to gentamicin, tobramycin and netilmicin, while amikacin had MICs greater than 128 micrograms/ml for all strains tested. Since a combination of a beta-lactam and streptomycin does not produce synergism against all strains of enterococci for an increase in the number of highly resistant strains, the effect of piperacillin plus gentamicin, tobramycin, and netilmicin was examined. The combination piperacillin + netilmicin seemed to be very effective against all enterococci tested.

Aminoglycosides↗
PubMed1986

In vivo uptake kinetics of aminoglycosides in the kidney cortex of rats.

The renal cortical uptake kinetics of four aminoglycosides were studied in vivo. Gentamicin, netilmicin, tobramycin or amikacin were administered to rats by continuous infusion over 6 hr achieving constant serum levels ranging from 0.2 to 100 micrograms/ml. Renal cortical concentrations at the end of the infusion were plotted against the steady-state serum levels. Steady-state elevations of serum gentamicin and netilmicin were associated with nonlinear increases in cortical levels, suggesting saturable uptake. Analysis of the data using Michaelis-Menten kinetics indicates that the apparent Km for gentamicin and netilmicin were 15.01 and 23.84 micrograms/ml and Vmax 149.83 and 178.36 micrograms/g of cortex per hr, respectively. The "initial" rate of uptake (at serum levels below 15 micrograms/ml) was highest for gentamicin. The cortical uptake of tobramycin was linearly related to elevations in serum levels [cortex concentration (conc) = 9.24 + 1.40 serum conc]. The initial rate of tobramycin uptake was considerably lower than that for gentamicin and netilmicin. For amikacin, the initial rate of uptake followed Michaelis Menten kinetics and the second phase of the titration curve was linear. The equation for total amikacin uptake was: cortex conc = 12.98 + 1.71 serum conc. Aminoglycosides exhibit differing kinetics for renal cortical uptake in the rat during constant infusions. These results indicate that more than one mechanism probably mediates the uptake of each aminoglycoside. Depending on which mechanism predominates, the kinetic pattern may be saturable, linear or mixed.

Aminoglycosides↗
PubMed1984

Preclinical comparative evaluation of aminoglycosides.

Five aminoglycoside antibiotics including gentamicin, sisomicin, tobramycin, amikacin and netilmicin were comparatively tested in vitro against 283 clinical isolates of Pseudomonas, Enterobacteriaceae and Gram-positive cocci, using the agar dilution technique according to I.C.S. recommendations. In respect to potency by weight, netilmicin proved the most active aminoglycoside against E. coli, K. pneumoniae, Enterobacter, Serratia spp. and Staphylococcus aureus, followed by sisomicin or tobramycin in relation to various bacterial species. Against Pseudomonas aeruginosa, sisomicin and tobramycin had the lowest MICs (minimum inhibitory concentrations). Amikacin had overall less activity but the widest spectrum. Rate of killing curves showed few differences among the aminoglycosides tested. Against gentamicin-resistant strains (MIC greater than or equal to 16 micrograms/ml) the activity of netilmicin was comparable to or higher than that of amikacin, except for P. aeruginosa, P. cepacia and indole-positive Proteus, which were inhibited by amikacin only. Netilmicin also showed the highest "therapeutical index" calculated as the ratio between MIC and blood levels for each aminoglycoside against each most important bacterial specie.

Aminoglycosides↗
PubMed1980

Histological evaluation of ototoxic reaction due to some aminoglycoside antibiotics.

Twenty-one days s.c. treatment with netilmicin, gentamicin, sisomicin, and kanamicin at different doses were performed in albino guinea pigs of both sexes. Block surface preparation of Corti's organ was carried out and missing OHCs and IHCs counted in selected areas of each turn. The animals treated with gentamicin and sisomicin showed a dose-depending missing of hair cells, preferably relative to the outer ones and quantitatively the same for both the antibiotics. Furthermore, a characteristic distribution of the damage progressively increasing from the apex to the basal turn of the cochlea was detected. Kanamicin at 267 and 400 mg/kg gave the complete destruction of OHCs and IHCs along the whole cochlea while at 178 mg/kg did not show any significant damage in comparison to the control group. Finally, netilmicin neither damaged Corti's organ nor statistically determined missing OHCs and IHCs at all the doses used. These histological results and the previous electrophysiological and reflexological observations obtained in the guinea pig show a higher safety of netilmicin in comparison to the other aminoglycosides used for the problem relative to ototoxicity.

Aminoglycosides↗
PubMedDate not supplied

A randomized clinical trial of ceftriaxone and teicoplanin versus ceftazidime and teicoplanin as antibiotic therapy in febrile neutropenic cancer patients and bone marrow transplant recipients.

A prospective, randomized clinical trial comparing combination therapy with ceftriaxone and teicoplanin versus ceftazidime and teicoplanin in the treatment of febrile episodes in neutropenic cancer patients and bone marrow transplant recipients was performed. One hundred and two patients were randomized, but two patients were considered unevaluable for efficacy, and three patients were withdrawn due to incorrect randomization. Of the remaining 97 patients, infection resolved without modification of therapy in 31/49 (63%) patients treated with ceftriaxone/teicoplanin versus 27/48 (56%) patients treated with ceftazidime/teicoplanin (P = 0.48). Of all 97 patients treated therapy was modified in 18/49 (36%) with ceftriaxone/teicoplanin and 21/48 (43%) with ceftazidime/teicoplanin. Nineteen patients treated with ceftriaxone/teicoplanin received netilmicin and 21 patients treated with ceftazidime/teicoplanin also received netilmicin according to the study design (escalation therapy). When netilmicin was added infection resolved in 78% of patients treated with ceftriaxone/teicoplanin versus 84% of those treated with ceftazidime/teicoplanin. It was concluded that combination therapy with ceftriaxone/teicoplanin is an alternative to combination therapy with ceftazidime/teicoplanin, and has the advantage of once daily administration.

Adolescent↗
PubMed2003

Some properties of Plesiomonas shigelloides treated with aminoglycosides.

The effect of aminoglycoside antibiotics (amikacin, gentamicin, netilmicin and tobramycin) at sublethal concentrations (sub-MICs) on some properties of Plesiomonas shigelloides strains was evaluated. All agents decreased the bacterial surface hydrophobicity. Amikacin (1/4 of the MIC) and netilmicin (1/4 and 1/8 of the MIC) changed the hydrophobic character of P. shigelloides surface to a hydrophilic one. Treatment of the strains with aminoglycosides decreased also motility, netilmicin being the most effective. No significant changes were found in lipolytic activity of antibiotic-treated strains. In the majority of cases aminoglycosides increased sensitivity of bacteria to hydrogen peroxide. The tested antibiotics did not induce production of short-chained N-acylhomoserine lactones signal molecules. Aminoglycosides at sub-MICs affected important activities of P. shigelloides potentially associated with their virulence in dependence on strain, antibiotic and concentration.

Amikacin↗