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Neomycin Sulfate is an aminoglycoside antibiotic. It has good antibacterial effect on Enterobacteriaceae such as Staphylococcus spp. (methicillin-sensitive strain), Corynebacterium spp., Escherichia coli, Klebsiella spp. and Aspergillus spp. It is poorly active against various groups of Streptococcus spp., Streptococcus pneumoniae and Enterococcus spp.
Pseudomonas aeruginosa, anaerobes and other resistant to the product.
Bacteria have partial or complete cross-resistance to streptomycin, neomycin and kanamycin, gentamicin. Neomycin has significant nephrotoxicity and ototoxicity when administered systemically, so it is limited to oral or topical application.
Uses and functions of Neomycin Sulfate.
Blocks voltage-sensitive Ca2+ channels without affecting the neuronal Na+/Ca2+ reverse transporter protein (antiporter).
Binds to ribosomal 30S and 50S subunits causing protein miscoding; inhibits initiation and prolongation of protein synthesis. Antimicrobial spectrum:Gram-negative and positive bacteria.
It can be used for the prevention and treatment of dysentery, diarrhoea and stunting caused by E. coli and Salmonella in pigs, chickens, cattle and other livestock and poultry. It can also be used as the treatment of enteritis in fish and shrimp among aquatic products.
It is a broad-spectrum antibiotic with good effect on Bacillus aureus, Bacillus diphtheriae and Bacillus anthracis.
Pharmacological Effect of Neomycin Sulfate.
Pharmacokinetics: Neomycin is seldom absorbed orally (about 3%), but larger doses taken orally over a long period of time can still be absorbed in considerable amounts when there is ulceration or inflammation of the intestinal mucosa, especially in renal hypoplasia when the blood concentration of the drug can be significantly increased. Most of it is excreted in the faeces without change after oral administration.
Indications: oral can be used for:
1. Intestinal infections.
2. It can also be used for bowel preparation before colon surgery or as adjunctive therapy in hepatic coma. Neomycin should not be used in the treatment of systemic infections.
In vitro studies of Bulk Neomycin Sulfate Powder.
Neomycin interacts preferentially with the nuclease-substrate complex and this interaction leads to a decrease in the cleavage rate, achieved by stabilising the ground state of the complex and destabilising the transition state of the cleavage step.
Neomycin causes conformational changes in the structure of the trans-activation region (TAR), which can be detected by circular dichroism spectroscopy.Neomycin acts as a non-competitive inhibitor that binds to the Tat-TAR complex and increases the rate constants (Koff) for RNA and peptide dissociation.
Neomycin is the most potent aminoglycoside (groove-binder) used to stabilise the triple-stranded helix of DNA.Neomycin stabilises the TAT, as well as the mixed-base DNA triple-helix, better than known DNA groove-binders (which usually disrupt the triple-helix) and polyamines.
Neomycin better stabilises the TAT triple helix, but also stabilises the CGC(+) triple helix.Neomycin concentration- and voltage-dependently induces partial inhibition of channels at the cytoplasmic and luminal surfaces.
Neomycin has a greater affinity for the lumen than the cytoplasm: the dissociation constants (Kb(0)) at zero voltage are 210.2 nM and 589.7 nM, respectively.Neomycin also exhibits voltage-dependent relief of inhibition at potentials greater than 60 mV.
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