アルベカシン·硫酸塩

アルベカシン·硫酸塩 化学特性,用途語,生産方法

• 効能

  抗生物質, タンパク質合成阻害薬

• 説明

  Arbekacin is a semi-synthetic derivative of dibekacin useful in the treatment of bacterial infections. This aminoglycoside is active against a broad spectrum of bacteria, including some of the gentamycin-, kanamycin-, and tobramycin-resistant pathogens. Compared to amikacin and dibekacin, ototoxicity is reportedly milder.

• 定義

  ChEBI: A kanamycin that is kanamycin B bearing an N-(2S)-4-amino-2-hydroxybutyryl group on the aminocyclitol ring.

• 抗菌性

  The 1-N-(4-amino-2-hydroxybutyryl) derivative of dibekacin, to which it bears the same relation as amikacin bears to kanamycin A. Supplied as the sulfate.
  Activity and stability to aminoglycoside-modifying enzymes are comparable with those of amikacin. It is active against many strains of methicillin-resistant Staph. aureus, either alone or in combination with β-lactam or other agents. Synergy with ampicillin has been observed for high-level gentamicin- and vancomycin-resistant enterococci.
  A 3 mg/kg intravenous dose achieved a peak concentration of c. 8 mg/L after 1 h. The plasma half-life is about 2 h and protein binding 3–12%.
  About 85% of the dose can be recovered from urine over 48 h. It is retained in renal failure, but moderately well removed by hemodialysis with a plasma half-life of 2–4 h. Peak concentrations of 10.9 mg/L and trough concentrations of 1.7 mg/L have been reported in patients treated for MRSA infection where C_max:MIC ratios of >25 and AUC:MIC ratios of >186 were associated with improved cure rates, and both Cmin and AUC were associated with the incidence of nephrotoxicity.
  Toxicity and side effects are typical of the aminoglycoside class. It is used in severe infection cause by susceptible microorganisms, but is not widely available.

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