2017年2月18日星期六
Sisomicin, netilmicin and dibekacin. A review of their antibacterial activity and therapeutic use.
Sisomicin is a naturally occurring aminoglycoside antibiotic which is produced by Micromonospora inyoensis while dibekacin and netilmicin are both semi-synthetic aminoglycosides. Dibekacin is 3 ', 4'-dideoxykanamycin B and netilmicine is 1-N-Ethylsisomicin. In both cases, these modifications make the means sensitive to certain enzymes found in the resistant strains of bacteria which inactivate the parent compounds. Antibacterial activity: All three drugs exhibit bactericidal activity against a variety of gram-negative bacteria, as well as against staphylococci (including E. coli, Enterobacter, Klebsiella and Proteus spp and Ps aeruginosa). Streptococci (except when beta lactams used in combination) are generally resistant and anaerobic organisms are not sensitive. Sisomicin is structurally closely related to gentamicin Cla but in vitro studies have shown that it has superior activity compared to gentamicin against Ps. Aeruginosa which maintain tobramycin activity largely parallel, while they possess Still high gentamicin activity against Serratia and other Gram-negative bacilli. However sisomicin is inactivated by enzymes almost all bacteria that inactivate gentamicin and tobramycin. Nevertheless, it retains useful activity against a number of resistant strains of Ps aeruginosa gentamicin, the mechanisms are (permeability barrier may) resistant by non-enzymatic. In this regard, it is very similar to Bramycin. Dibekacin similar Bramycin structurally and in vitro, it seems to have a very similar antibacterial spectrum, including activity against certain strains of Ps. Aeruginosa resistant to gentamicin. Netilmicin has a generally wider antibacterial spectrum than gentamicin, tobramycin, sisomicin or Debekacin and inactivation by phosphorylation and resistant Adenylylierungsenzyme; However, it is inactivated by all but acetylases acetylase 3-I. Its spectrum is therefore not as broad as that of amikacin against the strains of "resistant gentamicin". Nevertheless, it is actually more active than amikacin, weight-weight, against susceptible strains. May of Ps. Aeruginosa In fact, their activity against sensitive gentamicin species of Enterobacteriaceae and Staphylococci in the same order as this and maybe better for Klebsiella Enterobacter species. The three antibacterial agents show marked synergy with a variety of beta-lactam antibiotics against a variety of bacteria. Pharmacokinetic sisomicine to behave, netilmicine and dibekacin as gentamicin. All 3 drugs are excreted unchanged in urine and have a half-life beta elimination of about 2 to
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