[Pharmacokinetics and clinical observations of sisomicin, a newly developed aminoglycoside derivative (author's transl)]

Abstract

In a randomized study of 12 healthy subjects the pharmacokinetics of gentamicin, sisomicin and tobramycin were determined after a one-hour infusion of each drug (1.0 mg/kg body-weight) four weeks apart. There were no pharmacokinetic differences of therapeutic significance between the three drugs. The mean serum concentrations at the end of infusion were 3.85 mug/ml for gentamicin and 4.66 mug/ml for sisomicin, falling to 0.12 and 0.26 mug/ml, respectively, after eight hours. The biological half-life varied between 96 and 122 min and the apparent volumes of distribution corresponded closely tothe size of the extracellular space. The antibacterial effectiveness, tolerance and modes of application were studied in 24 patients, most of them with urinary infection, at a dosage of 1.0 mg per kg body-weight two to three times daily. Good clinical results were achieved in 15, satisfactory ones in three, and in 16 the causative bacteria were eradicated. Sisomicin was well tolerated, except for minor and reversible renal (2 patients), hepatic (3 patients), and hearing (1 patient) disturbances.