Netilmicin drug data and news

Netilmicin drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Netilmicin
Brand Names/Synonyms Netilmicin; Netilmicin Base; Netromycin
Indication For the treatment of bacteremia, septicaemia, respiratory tract infections, skin and soft-tissue infectsion, burns, wounds and peri-operative infections caused by susceptible strains of Escherichia coli, Klebsiella-Enterobacter-Serratia sp., Citrobacter sp., Proteus sp., Pseudomonas aeruginosa and Staphylococcus sp
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Description Not Available
Pharmacology Netilmicin is a semisynthetic, aminocyclitol, aminoglycoside antibiotic prepared from a dehydrogenated analog of gentamicin. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. Netilmicin 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. In the past the aminoglycosides have been used in conjunction with penicillin-related antibiotics in streptococcal infections for their synergistic effects, particularly in endocarditis. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses.
Mechanism Of Action 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.
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Dosage Forms SOLUTION
Drug_Category Anti-bacterial Agents; Aminoglycosides; ATC:J01GB07; ATC:S01AA23
Absorption Rapidly and completely absorbed after IM administration, peak serum levels were achieved within 30-60 minutes. Aminoglycosides are poorly absorbed from the gastrointestinal tract.
Interactions Interactions for :
Netilmicin should not be administered concomitantly with potent loop diuretics such as furosemide and ethacrynic acid as the potential for ototoxicity is enhanced by the combination.
Toxicity Netilmicin has the potential to cause disturbances in balance and a hearing loss.
Organisms Affected Enteric bacteria and other eubacteria
Chemical IUPAC Name 2-[4-amino-3-[[3-amino-6-(aminomethyl)-3,4-dihydro-2H-pyran-2-yl]oxy]-6-ethylamino-2-hydroxy-cyclohexoxy]-5-methyl-4-methylamino-tetrahydropyran-3,5-diol
Chemical Formula C21H41N5O7
Molecular Weight 475.58 g/mol
Smiles String CCNC1CC(C(C(C1OC2C(C(C(CO2)(C)O)NC)O)O)OC3C(CC=C(O3)CN)N)N
Melting Point Not Available
Water Solubility 100 mg/mL
State Solid
LogP/Hphobicity -3.981
Isoelectric Point Not Available
Biotransformation No evidence of metabolic transformation, typically 80% is recoverable in the urine within 24 hours
Half Life 2.5 hours
Protein Binding [%] Not Available
RxList Link Not Available>RXlist
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Drug Reference http://www.drugs.com/cons/Netilmicin.html
http://www.medsafe.govt.nz/profs/Datasheet/n/Netromycininj.htm
Drug Type Approved Drug
Accession No APRD00232
CAS Registry Number 56391-56-1
KEGG Compound ID C07657
PubChem ID SID:9859
PharmGKB ID PA450614
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 503371

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