Netilmicin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Aminoglycosides like netilmicin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically netilmicin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes, leaving the bacterium unable to synthesize proteins vital to its growth.
Pharmacology
Netilmicin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Netilmicin is a semisynthetic, water soluble antibiotic of the aminoglycoside group, produced by the fermentation of Micromonospora inyoensis, a species of actinomycete. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. It is active at low concentrations against a wide variety of pathogenic bacteria including Escherichia coli, bacteria of the Klebsiella-Enterobacter-Serratia group, Citrobacter sp., Proteus sp. (indole-positive and indole-negative), including Proteus mirabilis, P. morganii, P. rettgrei, P. vulgaris, Pseudomonas aeruginosa and Neisseria gonorrhoea. Netilmicin is also active in vitro against isolates of Hemophilus influenzae, Salmonella sp., Shigella sp. and against penicillinase and non-penicillinase-producing Staphylococcus including methicillin-resistant strains. Some strains of Providencia sp., Acinetobacter sp. and Aeromonas sp. are also sensitive to netilmicin. Many strains of the above organisms which are found to be resistant to other aminoglycosides, such as kanamycin, gentamicin, tobramycin and sisomicin, are susceptible to netilmicin in vitro. Occasionally, strains have been identified which are resistant to amikacin but susceptible to netilmicin. The combination of netilmicin and penicillin G has a synergistic bactericidal effect against most strains of Streptococcus faecalis (enterococcus). The combined effect of netilmicin and carbenicillin or ticarcillin is synergistic for many strains of Pseudomonas aeruginosa. In addition, many isolates of Serratia, which are resistant to multiple antibiotics, are inhibited by synergistic combinations of netilmicin with carbenicillin, azlocillin, mezlocillin, cefamandole, cefotaxime or moxalactam. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses.
Protein Binding
Netilmicin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Protein-binding of is low and depends on the test conditions (mainly the concentration of cations in the test medium).
Half-life
Netilmicin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2.5 hours
Absorption
Netilmicin¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly and completely absorbed after IM administration, peak serum levels were achieved within 30-60 minutes. Aminoglycosides are poorly absorbed from the gastrointestinal tract.
Netilmicin¿¡ ´ëÇÑ Biotransformation Á¤º¸ No evidence of metabolic transformation, typically 80% is recoverable in the urine within 24 hours
Toxicity
Netilmicin¿¡ ´ëÇÑ Toxicity Á¤º¸ Netilmicin has the potential to cause disturbances in balance and a hearing loss.
Drug Interactions
Netilmicin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Atracurium The agent increases the effect of muscle relaxantDoxacurium The agent increases the effect of muscle relaxantGallamine Triethiodide The agent increases the effect of muscle relaxantMetocurine The agent increases the effect of muscle relaxantMivacurium The agent increases the effect of muscle relaxantPancuronium The agent increases the effect of muscle relaxantPipecuronium The agent increases the effect of muscle relaxantRocuronium The agent increases the effect of muscle relaxantSuccinylcholine The agent increases the effect of muscle relaxantTubocurarine The agent increases the effect of muscle relaxantVecuronium The agent increases the effect of muscle relaxantThalidomide Thalidomide increases the renal toxicity of the aminoglycosideTorasemide Increased ototoxicityFurosemide Increased ototoxicityEthacrynic acid Increased ototoxicityBumetanide Increased ototoxicityCefamandole Increased risk of nephrotoxicityCefazolin Increased risk of nephrotoxicityCefonicid Increased risk of nephrotoxicityCefoperazone Increased risk of nephrotoxicityCeforanide Increased risk of nephrotoxicityCefotaxime Increased risk of nephrotoxicityCefotetan Increased risk of nephrotoxicityCefoxitin Increased risk of nephrotoxicityCeftazidime Increased risk of nephrotoxicityCeftizoxime Increased risk of nephrotoxicityCeftriaxone Increased risk of nephrotoxicityCefuroxime Increased risk of nephrotoxicityCephalothin Group Increased risk of nephrotoxicityCephapirin Increased risk of nephrotoxicityCisplatin Increased risk of nephrotoxicityCefradine Increased risk of nephrotoxicity
Netilmicin¿¡ ´ëÇÑ Description Á¤º¸ Semisynthetic 1-N-ethyl derivative of sisomycin, an aminoglycoside antibiotic with action similar to gentamicin, but less ear and kidney toxicity. [PubChem]