Antibacterial activity and ototoxicity in guinea pigs, and nephrotoxicity in rats of arbekacin.
Arbekacin (HBK), 1-N[(S)-4-amino-2-hydroxybutyl]-3',4'-dideoxykanamycin B, showed broad antibacterial spectra against gram-positive and gram-negative bacteria including Pseudomonas aeruginosa. It was also effective against gentamycin- or tobramycin-resistant bacteria. HBK was resistant to various aminoglycoside-inactivating enzymes except for AAC (2') and AAC (6')-IV, both of which slowly inactivated it. Even at higher dosages (150 mg/kg i.m. or greater, which resulted in some deaths), HBK never decreased the pinna reflex in guinea pigs, while 150 mg/kg or more of dibekacin (DKB) or amikacin (AMK) caused loss of this reflex. HBK has less ototoxicity than do DKB and AMK. This was confirmed by histopathological examination of the inner ear. The degree of nephrotoxicity of HBK was suggested to be similar to that of DKB as judged from serum biochemical tests, urinalysis, and histopathological findings.
D000583:Amikacin / Q000494:pharmacology; D000617:Aminoglycosides; D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology* / Q000633:toxicity; D001424:Bacterial Infections / Q000188:drug therapy*; D003982:Dibekacin / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000633:toxicity; D004352:Drug Resistance, Microbial; D007758:Ear, Inner / Q000187:drug effects* / Q000473:pathology; D006168:Guinea Pigs; D007273:Injections, Intramuscular; D007612:Kanamycin / Q000031:analogs & derivatives*; D007668:Kidney / Q000187:drug effects* / Q000473:pathology; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D012018:Reflex / Q000187:drug effects; D013329:Structure-Activity Relationship
D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; D003982:Dibekacin; D007612:Kanamycin; D000583:Amikacin; C031986:arbekacin