Scand J Infect Dis Suppl 1990;74:249-57

Efficacy and safety of aminoglycosides once-a-day: experimental and clinical
data.

Tulkens PM

Laboratory of Physiological Chemistry, Catholic University of Louvain, Belgium.

In vitro and animal data show that the efficacy of an aminoglycoside is
primarily related to its serum peak levels and AUC, whereas its toxicity is
critically dependent upon the schedule of the administration of the daily dose
as well as the duration of the treatment and the total amount of drug
administered. The reduction of toxicity by intermittent dosing, e.g. once-a-day
dosing (q.d.) versus splitting the daily dose in multiple administrations is
connected with the saturable character of the aminoglycoside transport within
inner ear and renal tissues. Clinical trials have been conducted in various
types of infections in order to investigate the efficacy and tolerance of
aminoglycosides q.d. Using conventional criteria of evaluation, this mode of
administration was found to be equally efficacious and marginally less toxic
than aminoglycosides in conventional dosing regimens. We have studied the
pharmacokinetics and the early signs of renal (phospolipiduria) and auditory
(high frequency audiometry) alterations of aminoglycosides given q.d. and by
conventional dosage schedules to patients with pelvic inflammatory disease. It
was shown that netilmicin and amikacin were better tolerated q.d. than after
t.i.d. or b.i.d. administration. In addition, amikacin induced less alterations
than netilmicin.

Publication Types:
Review
Review, tutorial

PMID: 2097713, UI: 91271870