Isepamycin

General information

Isepamicin is similar to amikacin but has better activity against strains that produce type I 6′-acetyltransferase. It can cause nephrotoxicity, vestibular toxicity, and ototoxicity. However, it is one of the less toxic of the aminoglycosides [ ]. The antibacterial spectrum of isepamicin includes Enterobacteriaceae and staphylococci; anaerobes, Neisseriae , and streptococci are resistant [ ]. Isepamicin was as effective and safe as amikacin in the treatment of acute pyelonephritis in children and might prove an advantageous alternative in areas with a high incidence of resistance to other aminoglycosides [ ].

Isepamicin is given intravenously or intramuscularly in a dosage of 15 mg/kg/day or 7.5 mg/kg bd. It is not bound to plasma proteins, it distributes in extracellular fluids, and it enters some cells (outer hair cells, kidney cortex) by an active transport mechanism [ ]; the transference of isepamicin to the bone marrow is excellent [ ]. Isepamicin is not metabolized and is renally excreted with a half-life of 2–3 hours in adults with normal renal function. Its clearance is reduced in neonates, and a dose of 7.5 mg/kg/day is recommended in children younger than 16 days. Its clearance is also reduced in elderly people, but no dosage adjustment is required. In patients with chronic renal impairment, isepamicin clearance is proportional to creatinine clearance.

The bone tissue penetration of isepamicin has been studied in an open, non-comparative study, and the results compared with microbiologic data to estimate the clinical efficacy of isepamicin in bone infections [ ]. In 12 subjects of similar age, body weight, height, and creatinine clearance, who were undergoing elective total hip replacement, a single parenteral dose of isepamicin 15 mg/kg achieved concentrations in both cancellous and cortical bone tissue greater than the minimum concentrations required to inhibit the growth of 90% of strains of most of the susceptible pathogens commonly involved in bone infections.

Organs and systems