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Biopharmaceutical assessment of eye drops containing aloe (Aloe arborescens Mill.) and neomycin sulphate.

The subject of the studies was eye drops made of aloe, containing the group of aloe chemical substances of anti-inflammatory use and neomycin sulphate. The aim of the studies was to evaluate the permeability of biologically active aloe substances, determined as aloenin, through synthetic lipophilic and hydrophilic membranes in a standard perfusion apparatus and in vitro verification of the transport possibilities of these substances through the isolated cornea of pig's eye. The permeability process of biologically active aloe substances determined as aloenin, through synthetic lipophilic and hydrophilic membranes, was analyzed using the first-order kinetics. Estimated quotas of permeability rate constant show that the investigated chemical compounds of aloe, included in the eye drops, diffused through the applied membranes. The studies of permeability through isolated pig's cornea proved that biologically active aloe substances could not overcome this biological barrier. On the basis of biopharmaceutical studies it can be concluded that the eye drops containing aloe and neomycin sulphate, due to the lack of permeating abilities through the eye cornea, should be particularly useful in the treatment of inflammations and infections of external parts of the eye, such as conjuctiva, eyelid edges, lacrimal sac and cornea.

Aloe↗

Effect of magnetic field on the biosynthesis of neomycin by Streptomyces marinensis.

The effect of 30, 70, 90, 100, 110 and 150 gauss permanent magnetic field strength on the growth and neomycin titre of Streptomyces marinensis was studied. Maximum growth was attained in 120 h at all magnetic strengths. Gradual increase in neomycin titre was observed with increase of magnetic field strength up to 110 gauss.

Anti-Bacterial Agents↗

[Local use of neomycin. The histomorphological changes on the part of the neuroreceptor apparatus of the rabbit cornea].

The experimental histological studies with rabbits showed that neomycin in the form of 1 and 10 per cent solutions and ointments used for prolong periods of time affected the neuroreceptor apparatus of the animal cornea. It is not recommended to use 10 per cent solutions and ointments in the ophthalmological practice. Before using neomycin it is necessary to examine the cornea sensitivity and if it is lowered, the antibiotic should not be used.

Administration, Topical↗

Neomycin in urinary tract infections; a clinical evaluation.

Neomycin was effective in treating 31 cases of severe Gram-negative bacillary urinary tract infections sensitive to neomycin and resistant to other agents. The recommended dosage schedule of 0.5 gm. every 12 hours for five days was demonstrated to be relatively safe. However, close watch should be maintained for signs of nephrotoxicity and ototoxicity.

Gram-Negative Bacteria↗

Topical treatment of basal cell carcinoma with neomycin.

Basal cell carcinoma (BCC) is the most common skin cancer, occurring more frequently than malignancies of any other tissue or organ, either individually or in total. Medical treatment modalities of BCC offer cost reduction and clinical advantages in selected cases. Neomycin has been reported to have an important role on proliferation of endothelial cells and neoplastic cells. This finding may lead to new strategies for the therapeutic use of agents which block FGF activities in disease states associated with enhanced keratinocyte proliferation. We report here a case of BCC treated with neomycin 5% cream that induced a regression of BCC.

Administration, Topical↗

Cross-sensitivity within the neomycin group of antibiotics.

Neomycin sensitive patients were tested for hypersensitivity to kanamycin, gentamycin, tobramycin, spectinomycin and to the new, not yet registered sisomycin and netilmicin. Cross-sensitivity occured in a considerable part of the patients, except for spectinomycin, the structure of which is basically different from that of the other aminoglycosides tested. The common occurence of cross-sensitivity between neomycin and other aminoglycoside antibiotics shows that it is possible to predict cross-sensitivity between a new drug and an old sensitizing one before clinical reactions from the new drug have occured. Such an investigation should be performed before adopting new antibiotics.

Aminoglycosides↗

[Torulopsis glabrata neomycin-resistant mutant abolishes pyruvate production with enhancement of glucose consumption rate].

To further increase the rate of glucose consumption by multi-vitamin auxotrophic yeast Torulopsis glabrata. A neomycin-resistant mutant N07, with the activity of F1-ATPase decreased roughly 35% but glucose consumed per cell was increased 38% than that of parent strain, was breed based on analysis of energy metabolic pathway. The typical inhibitors of F1F0-ATPase, DCCD, NaN3 and neomycin, depressed the F1-ATPase activity of parental strain but no effect on that of mutant strain. Strain N07 was cultured in a pyruvate fermentation medium containing 100g/L of glucose using flask. It was found that the rate of glucose consumption and pyruvate production were higher by 34% and 42.9% in the mutant than in the parent, respectively. However, the rate and yield of growth (about 24%) of the mutant was lower than that of the parent. The content of intracellular ATP of the mutant also decreased 23.7% than that of the parent. The activities of key enzymes in glycolytic pathway and electron transfer chain of the mutant and the parent were determined. Enzymatic analysis revealed that, compared with the parent strain CCTCC M202019. The activities of key enzymes, phosphofructokinase, pyruvate kinase, glyceraldyde-3-phosphate dehydrogenase of the mutant N07 increased 63.7%, 28.8% and 14.4%, respectively, all the key enzymes of electron transfer chain in the mutant N07 also increased roughly 10%.

Adenosine Triphosphate↗

Rifaximine versus neomycin in the treatment of portosystemic encephalopathy.

In 14 patients with cirrhosis and chronic portosystemic encephalopathy, the effectiveness of treatment with a new non-assorbable antibiotic (rifaximine) was compared to neomycin. The parameters evaluated were: bradylalia, flapping tremor, performance, visual evoked potentials and the trial making test. Both treatments were combined with lactulose. The analysis of results showed a rate of positive results in the patients treated with rifaximine greater than that with neomycin. Differences, however, were not significant.

Chronic Disease↗

Inhibition of cholesterol absorption by neomycin, benzodiazepine derivatives and ketoconazole.

Neomycin and a benzodiazepine derivative (RO16-0521) inhibit similarly cholesterol absorption in man but the serum cholesterol level is reduced only by neomycin. Reason(s) for the difference are unknown. Ketoconazole inhibits 14 alpha-demethylation of lanosterol so that cholesterol synthesis is reduced. The agent inhibits also cholesterol absorption. The serum cholesterol level is reduced by about 20%, the lowering being potentiated by a simultaneous cholestyramine treatment.

Anticholesteremic Agents↗

Purification of polyphosphoinositides by chromatography on immobilized neomycin.

The binding of polyphosphoinositides (phosphatidylinositol phosphate and phosphatidylinositol bisphosphate) to the antibiotic neomycin is utilized for the purification of these lipids. Neomycin is reductively coupled to reactive glass beads (Glycophase-CPG) and serves as the stationary phase in column chromatography. A total lipid extract is prepared from tissues with chloroform-methanol-KC1 or chloroform-methanol-HC1 and washed once with acidified methanol-water. After the addition of an equal volume of methanolic 200 mM ammonium acetate, the extract is directly applied to the column. All lipids but the polyphosphoinositides are removed from the column by rinsing with 150 mM ammonium acetate in chloroform-methanol-water. Increasing the salt concentration to 600 mM elutes phosphatidylinositol phosphate. While further increases in ionic strength are not sufficient for a quantitative removal of phosphatidylinositol bisphosphate, the lipid is completely eluted by the addition of either ammonia or HC1 to the solvent. The column can be recycled and used repeatedly.

Animals↗

Treatment of severe and mild hypercholesterolaemia with probucol and neomycin.

Administration of probucol to 23 patients with familial xanthomatotic hypercholesterolaemia reduced the serum cholesterol level during the 9-month study by 9%, while in 15 patients with less severe hypercholesterolaemia the decrease was on an average 15%. A reduction of more than 10% was obtained in 57% of the former and 80% of the latter subjects. In a double blind trial a greater reduction was obtained in serum cholesterol by probucol than by placebo. Neomycin lowered the serum cholesterol more effectively than probucol in subjects with severe type II abnormality and was at least equally effective in less severe type II patients. Probucol increased transiently the faecal bile acid and dietary cholesterol excretion, while neomycin enhanced the faecal elimination of cholesterol as neutral sterols.

Clinical Trials as Topic↗

[Clinical trial of Pulvo 47 Neomycin in the treatment of leg ulcer (author's transl)].

Pulva 47 Neomycine was tested in 30 patients suffering from a leg ulcer, 11 of those were surinfected. Half the ulcers dated back over 6 months. The would preparation included a careful cleaning with a permanganate or dakin's solution. In most of the cases, the product was applied on a once a day basis during an average period of 30 days. In 12 patients, the severity of the infection needed an additional antibiotherapy administered orally. The results were expressed in relation to the activity on the infection and wound healing. In 28 patients, the signs of infection disappeared completely. The wound healing effect was very satisfying in 22 patients (19 of them had varicose or post-phlebitis ulcers). The value of the results is independent on the date of onset and on the area of the lesions. The tolerance was good; only 4 patients suffered from itching after the application of the compound. It is mainly through his wound healing effect that Pulvo 47 Neomycine represents a progress compared to other similar specialties.

Adult↗

Retroviral vector-mediated transfer of the bacterial neomycin resistance gene into fetal and adult sheep and human hematopoietic progenitors in vitro.

We compared the efficiency of retroviral vector (N2)-mediated transfer of the bacterial neomycin resistance gene (NeoR) into adult and fetal hematopoietic progenitors of sheep and humans by assessing their ability to form colonies in the presence of lethal doses of the neomycin analogue G418 in vitro. Fetal cells from both sheep and humans exhibited a higher degree of NeoR transfer than adult cells. The overall level of NeoR expression was significantly higher for sheep than human cells. The transfer/expression of NeoR into adult human bone marrow hematopoietic progenitors was not affected by the presence or absence of T cells and monocyte/macrophages. The efficiency of NeoR transfer into both adult and fetal human cells, however, was improved when transduction was carried out in the presence of recombinant human interleukin-3 and granulocyte-macrophage colony-stimulating factor. These results demonstrate the greater efficiency of NeoR gene transfer into fetal hematopoietic progenitors, which may provide a basis for the relatively higher efficiency of the in utero approach to gene therapy.

Animals↗

[In vitro antibacterial activity of neomycin, bacitracin and a combination of both].

Bacitracin and neomycin have been used for a long time for local intestinal antisepsis or decontamination, due to their scarce or nonexistent intestinal absorption. The aim of the present study was to determine the activity of bacitracin and neomycin against recent clinical isolates of aerobic and anaerobic microorganisms and to verify their capacity to have a synergistic effect and to prevent the emergence of bacterial resistance when in combination. The results showed that the activity of either antibiotic against recent clinical isolates (even if resistant to cephalosporins and aminoglycosides) is similar to that originally displayed at the time introduction in therapy. Generally the combination of the two antibiotics showed a synergistic or additive effect and prevented the selection of resistant strains.

Bacitracin↗

[The effect of neomycin on the contractile activity of the skeletal muscles in the frog].

Neomycin, a selective inhibitor of the phosphoinositide metabolism, depending on its concentration and the incubation time, depressed the K+-contractures and contractions of m. sartorius R. ridibunda caused by a single or a tetanic electrostimulation. In the experiments on m. rectus abdominis, neomycin inhibited the Ach- and oubaine contractures but not the K+ ones. The contractures of both muscles induced with caffeine did not change in presence of the above antibiotic. The data obtained suggest a participation of phosphoinositides contractions of skeletal muscles induced by excitation of the plasma membrane.

Acetylcholine↗

Attempt with oral immunobiotherapy (broncho-vaxom) and immunochemotherapy (broncho-vaxom + neomycin) for the elimination of bacteria in symptom-free "other Salmonella" carriers.

Forty-five symptomless "other Salmonella" carriers were treated; stool became negative for Salmonella in 22 of the 25 patients treated with Broncho-Vaxom (88%) and in 16 of the 20 patients treated with Broncho-Vaxom + Neomycin (80%) (who had discharged Salmonella for not longer than one month previously). This result is very favourable when compared to data of references of thoroughly controlled patients according to which 69% was the highest rate of bacterial negativity obtained in the treated patients who discharged "other Salmonellas" for not longer than 1 month. The stool of all 10 patients admitted as symptomless carriers of "other Salmonellas" became negative for bacteria in response to the mentioned therapy (in 6 cases of Group I, and 4 cases of Group II). Treatment was unsuccessful primarily in chronic alcohol addicts and toxicosis cases (13%). The unresponsiveness of the two patients suffering from cholelithiasis and excreting also "other Salmonella" with the bile deserves attention. In such cases the positivity of the bile for Salmonella was a reason for exclusion from the study. Further studies (completed with immunological data) are required to assess the value of Broncho-Vaxom immunobiotherapy, and Broncho-Vaxom + Neomycin immunotherapy.

Adjuvants, Immunologic↗

Furazolidone toxicity in neomycin-treated turkey poults.

Furazolidone (FZ) toxicity was evaluated in turkey poults treated with neomycin at a dose of 20 mg/kg body weight for 5, 10, or 26 days. Neomycin treatment had no effect on FZ-induced anorexia, delayed the onset of altered electrocardiographic patterns by approximately 1 week, and did not significantly affect the development of FZ-induced cardiomyopathy. Data indicated that FZ toxicity is not significantly altered by the gut microflora.

Animals↗

Effect of orally administered neomycin on uterine growth in young mice and rats.

Neomycin has been widely used as a gut antibiotic in preconditioning animals for the experimental evaluation of biomaterials and biomedical devices. As a chance observation during a routine conditioning process, it was noticed that orally administered neomycin retarded uterine growth in growing mice and rats. Body weights and the weights of liver and spleen were uneffected, although there was a marginal increase in the kidneys' weight. This finding is consistent with the theory that a change induced in intestinal flora activity mediated a uterotrophic influence of dietary fiber.

Animals↗