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Arbekacin

产品号 DB06696 公司名称 DrugBank
CAS号 51025-85-5 公司网站 http://www.ualberta.ca/
分子式 C22H44N6O10 电 话 (780) 492-3111
分子量 552.61896 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 4434

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产品别名

标题
Arbekacin
IUPAC标准名
4-amino-N-(5-amino-2-{[4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-4-{[3-amino-6-(aminomethyl)oxan-2-yl]oxy}-3-hydroxycyclohexyl)-2-hydroxybutanamide
IUPAC传统名
4-amino-N-(5-amino-2-{[4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-4-{[3-amino-6-(aminomethyl)oxan-2-yl]oxy}-3-hydroxycyclohexyl)-2-hydroxybutanamide
别名
Arbekacine
Arbekacina
Haberacin
Habekacin
Arbekacinum

产品登记号

CAS号 51025-85-5

产品性质

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description An semisynthetic aminoglycoside antibiotic. Often used for treatment of multi-resistant bacterial infection such as methicillin-resistant Staphylococcus aureus (MRSA).
Amikacin is also nephrotoxic and ototoxic.
Indication Arbekacin is used for the short term treatment of multi-resistant bacterial infections, such as methicillin-resistant Staphylococcus aureus (MRSA).
Pharmacology Aminoglycosides, such as Arbekacin, work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA which consequently, leaves the bacterium unable to synthesize proteins vital to its growth. Energy is needed for aminoglycoside uptake into the bacterial cell. Anaerobes have less energy available for this uptake, so aminoglycosides are less active against anaerobes. Aminoglycosides are useful primarily in infections involving aerobic, gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter.
Toxicity Ototoxicity and nephrotoxicity are the most serious adverse effects of aminoglycoside therapy and are more likely to occur in patients with a history of renal impairment or who are receiving other ototoxic and/or nephrotoxic drugs.
Normal duration of IM or IV aminoglycoside therapy is 7-10 days. Although a longer duration may be necessary in some cases, toxicity is more likely to occur when aminoglycoside treatment is continued for longer than 10 days.
Affected Organisms
Enteric bacteria and other eubacteria
Absorption Aminoglycosides are not well absorbed from the gastrointestinal tract. Their absorption is markedly improved by parenteral administration.
Half Life 3 hours
Protein Binding 3-12%
References
Inoue M, Nonoyama M, Okamoto R, Ida T: Antimicrobial activity of arbekacin, a new aminoglycoside antibiotic, against methicillin-resistant Staphylococcus aureus. Drugs Exp Clin Res. 1994;20(6):233-9. [Pubmed]
Morikawa K, Nonaka M, Yoshikawa Y, Torii I: Synergistic effect of fosfomycin and arbekacin on a methicillin-resistant Staphylococcus aureus-induced biofilm in a rat model. Int J Antimicrob Agents. 2005 Jan;25(1):44-50. [Pubmed]
Doi Y, Yokoyama K, Yamane K, Wachino J, Shibata N, Yagi T, Shibayama K, Kato H, Arakawa Y.Plasmid-mediated 16S rRNA methylase in Serratia marcescens conferring high-level resistance to aminoglycosides.Antimicrob Agents Chemother. 2004 Feb;48(2):491-6. [Pubmed]
Akins RL, and Rybak MJ.In Vitro Activities of Daptomycin, Arbekacin, Vancomycin, and Gentamicin Alone and/or in Combination against Glycopeptide Intermediate-Resistant Staphylococcus aureus in an Infection Model. Antimicrobial Agents and Chemotherapy.July 2000, p. 1925-1929, Vol. 44, No. 7 "Antimicrobial agents and Chemotherapy":http://aac.asm.org/cgi/content/full/44/7/1925
External Links
Wikipedia

参考文献

  • Inoue M, Nonoyama M, Okamoto R, Ida T: Antimicrobial activity of arbekacin, a new aminoglycoside antibiotic, against methicillin-resistant Staphylococcus aureus. Drugs Exp Clin Res. 1994;20(6):233-9. Pubmed
  • Morikawa K, Nonaka M, Yoshikawa Y, Torii I: Synergistic effect of fosfomycin and arbekacin on a methicillin-resistant Staphylococcus aureus-induced biofilm in a rat model. Int J Antimicrob Agents. 2005 Jan;25(1):44-50. Pubmed
  • Doi Y, Yokoyama K, Yamane K, Wachino J, Shibata N, Yagi T, Shibayama K, Kato H, Arakawa Y.Plasmid-mediated 16S rRNA methylase in Serratia marcescens conferring high-level resistance to aminoglycosides.Antimicrob Agents Chemother. 2004 Feb;48(2):491-6.Pubmed
  • Akins RL, and Rybak MJ.In Vitro Activities of Daptomycin, Arbekacin, Vancomycin, and Gentamicin Alone and/or in Combination against Glycopeptide Intermediate-Resistant Staphylococcus aureus in an Infection Model. Antimicrobial Agents and Chemotherapy.July 2000, p. 1925-1929, Vol. 44, No. 7 "Antimicrobial agents and Chemotherapy":http://aac.asm.org/cgi/content/full/44/7/1925