In Vitro Studies with Sch 21420 and Sch 22591: Activity in Comparison with Six Other Aminoglycosides and Synergy with Penicillin Against Enterococci

Sanders, Christine C.; Sanders, William E.; Goering, Richard V.

doi:10.1128/aac.14.2.178

Cited by 25 publications

(7 citation statements)

References 7 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Thus, it was deemed probable that the biological activities of the two compounds would be similar. These data, as well as those of others (7,9,11,13,15,17) and amikacin are markedly more active than the other four aminoglycosides.…”

Section: Resultssupporting

confidence: 64%

See 1 more Smart Citation

Comparison of in vitro activity of Sch 21420, a gentamicin B derivative, with those of amikacin, gentamicin, netilmicin, sisomicin, and tobramycin

Thornsberry¹,

Barry²,

Jones³

et al. 1980

Antimicrob Agents Chemother

View full text Add to dashboard Cite

Sch 21420 is a new aminoglycoside synthesized from gentamicin B. Susceptibility tests with Sch 21420, amikacin, gentamicin, netilmicin, sisomicin, and tobramycin were performed on a variety of bacterial species including 44 with known mechanisms of resistance to aminoglycosides. Sch 21420 and amikacin had similar effects on all except Haemophilus influenzae and Neisseria species, which were more susceptible to amikacin. Except with some strains of Serratia marcescens, the drugs used were bactericidal. Sch 21420 and amikacin were more stable than the other four aminoglycosides in the presence of the inactivating enzymes produced by some strains. Strains which were very resistant to Sch 21420 and amikacin either were permeability mutants or produced AAC (6')-I inactivating enzyme. The effect of cations on the susceptibilities of these strains to Sch 21420 and amikacin was seen mostly with Pseudomonas aeruginosa and to Sch 21420 with Acinetobacter. Cations did not affect the susceptibilities of other Pseudomonas species, Enterobacteriaceae, Staphylococcus aureus, or Streptococcus faecalis to Sch 21420 or amikacin.Sch 21420 is an aminoglycoside which was synthesized by a method similar to that used in the synthesis of amikacin, except that gentamicin B was used in place of kanamycin (12). The activity ofthis compound was found to be similar to that of amikacin against the Enterobacteriaceae and Pseudomonas aeruginosa (7,9,11,13,15,17).In this study, we compared the inhibitory and bactericidal activities of Sch 21420 to those of amikacin, gentamicin, netilmicin, sisomicin, and tobramycin against a wide variety of gram-positive and gram-negative organisms. The effect of differences in inoculum size and cation concentration on the activity of these six aminoglycosides was assessed. The activities of these drugs on organisms with various mechanisms of resistance (inactivating enzymes and permeability mutants) were also compared.

show abstract

Section: Resultssupporting

confidence: 64%

“…The activity ofthis compound was found to be similar to that of amikacin against the Enterobacteriaceae and Pseudomonas aeruginosa (7,9,11,13,15,17).…”

mentioning

confidence: 87%

Comparison of in vitro activity of Sch 21420, a gentamicin B derivative, with those of amikacin, gentamicin, netilmicin, sisomicin, and tobramycin

Thornsberry¹,

Barry²,

Jones³

et al. 1980

Antimicrob Agents Chemother

View full text Add to dashboard Cite

show abstract

“…SCH 21420 does, however, cause functional and structural renal injury typical for this class of antimicrobial agents. Since SCH 21420 compares favorably to amikacin with respect to in vitro activity against many aerobic gram-negative bacilli and Staphylococcus aureus (4,9,12) and also exhibits documented synergism with penicillin against enterococci (9), it appears that SCH 21420 may be a valuable addition to the aminoglycoside armamentarium.…”

Section: Resultsmentioning

confidence: 99%

Comparative nephrotoxicity of SCH 21420 and amikacin in rats

Rankin¹,

Luft²,

Yum³

et al. 1979

Antimicrob Agents Chemother

View full text Add to dashboard Cite

The nephrotoxic potentials of the new aminoglycoside SCH 21420 and amikacin were compared in a rat model. Groups of rats received 100, 200, 300, or 600 mg of either drug per kg per day for 14 days. Enzymuria, urine osmolality, protein excretion, and blood urea nitrogen were monitored at periodic intervals, whereas creatinine clearance and pathological changes were determined at sacrifice. Amikacin caused more enzymuria at the two lower doses as well as greater proteinuria and blood urea nitrogen elevations at the highest dose than did SCH 21420 (P < 0.05). Pathological changes were more severe with amikacin than with SCH 21420 at the three lower doses (P < 0.05); however, at the 600 mg/kg per day dose, the pathological scores and creatinine clearances of animals receiving either drug were not significantly different (P > 0.05).

show abstract

“…Isepamicin (Sch 21420) is a semi-synthetic aminoglycoside which is the 1-N-S-a-hydroxy-(3-aminopropionyl derivative of gentamicin B [1,6], Although a member of the gentamicin family, it is structurally related to kanamycin A because it possesses garosamine which is linked to the deoxystreptamine ring [1,7] [8]. Another kanamycin-like activity noted was the excellent activity of isepamicin against Providencia rettgeri and Providencia stuartii which are usually more susceptible to amikacin and kanamycin than to gentamicin because of the presence of chromosomal AAC (6') enzymes in these organisms [17].…”

Section: Materials and M Eth Ods Resultsmentioning

confidence: 99%

In vitro Activity of Isepamicin (Sch 21420), a New Aminoglycoside

Qadri¹,

Ueno²,

Tullo³

et al. 1995

Chemotherapy

View full text Add to dashboard Cite

The narrow therapeutic/toxic ratio of existing aminoglycosides has led to a search for safer drugs of this class. Isepamicin is a semi-synthetic aminoglycoside with a significantly low nephro as well as ototoxicity in animals and which is expected to have a clinical efficacy comparable to that of amikacin. We therefore compared its antibacterial activity with amikacin against 817 recent clinical isolates of gram-positive and gram-negative bacteria. The in vitro activity of isepamicin was comparable or slightly greater than amikacin against Staphylococcus aureus and most Enterobacteriaceae. However, it was significantly more inhibitory towards Serratia marcescens, Enterobacter and Klebsiella pneumoniae.

show abstract

In Vitro Studies with Sch 21420 and Sch 22591: Activity in Comparison with Six Other Aminoglycosides and Synergy with Penicillin Against Enterococci

Abstract: In vitro tests were performed with Sch 21420 and Sch 22591 to determine (i)

Cited by 25 publications

References 7 publications

Comparison of in vitro activity of Sch 21420, a gentamicin B derivative, with those of amikacin, gentamicin, netilmicin, sisomicin, and tobramycin

Comparison of in vitro activity of Sch 21420, a gentamicin B derivative, with those of amikacin, gentamicin, netilmicin, sisomicin, and tobramycin

Comparative nephrotoxicity of SCH 21420 and amikacin in rats

In vitro Activity of Isepamicin (Sch 21420), a New Aminoglycoside

Contact Info

Product

Resources

About