Isepamicine

Description

Isepamicin is a aminoglycoside antibiotic indicated for use in the treatment of urinary and respiratory tract infections. Although it is less potent than most other aminoglycosides, it is also less nephrotoxic. The broad-spectrum activity of isepamicin generally parallels that of amikacin in vitro.

Chemical Properties

Isepamicin Sulfate: C22H43N5O12xH2SO4 (x≤2). [67814-76-0]. [α]{D}^²⁶+110.9° (C=1, hydrated in water). Acute toxicity LD50 for male and female mice, male and female rats (mg/kg): 3312, 3320, 3451, 3392 for subcutaneous injection; 234, 236, 489, 476 for intravenous injection; all >5000 for oral administration.

Originator

Schering Plough (USA)

Uses

Antibacterial (aminoglyco side).

brand name

Isepacin; Exacin

Antimicrobial activity

Hydroxyamino propionyl gentamicin B. A semisynthetic derivative of gentamicin B, modified to render it more resistant to microbial inactivation.
In-vitro activity is comparable to or slightly greater than amikacin against Staph. aureus and most enterobacteria; it is much more active against Ser. marcescens, Enterobacter spp. and Klebsiebella pneumoniae. It is also active in vitro against the Mycobacterium avium complex and Nocardia asteroides. It is less susceptible than amikacin or gentamicin to inactivation by β-lactam antibiotics. It retains activity against some strains resistant to most other aminoglycosides.
Pharmacokinetics in neonatal, pediatric, adult, elderly and renally impaired patients are similar to those of other aminoglycosides. In adult volunteers the plasma half-life was 2.1 h. Clearance is reduced in neonates and the elderly. A 7.5 mg/kg once-daily dosage is recommended for children less than 16 days old. No dosage adjustment is required for the elderly unless renal function is impaired. Clearance is proportional to creatinine clearance in patients with chronic renal impairment, and it is eliminated by hemodialysis.
It has been used in respiratory tract infections, urinary tract infections and intra-abdominal infections, in adults and children. It appears to be as effective and well tolerated as amikacin. It is available in Japan.