Loracarbef is an investigational oral
antibiotic but its pharmacokinetics have not been studied after multiple oral doses in pediatric patients. The pharmacokinetics of
loracarbef were determined in 18 pediatric patients after multiple oral doses. 8 patients with streptococcal
pharyngitis received 7.5 mg/kg every 12 h, and 10 patients with
otitis media were given 15 mg per kg every 12h. Multiple blood and urine samples were collected to measure
loracarbef concentrations. In patients with streptococcal
pharyngitis, the mean maximum serum concentration (Cmax), the time to achieve maximum concentration (Tmax), area under the serum concentration-time curve (AUC) and elimination half-life (t1/2) were 10.6 +/- 3.6 mcg/ml, 0.78 +/- 0.21 h, 21.4 +/- 7.2 mcg.h/ml, and 1.2 + 0.4 h, respectively. The mean Cmax, Tmax, AUC and t1/2 were 18.0 +/- 5.4 mcg/ml, 0.83 +/- 0.44 h, 35.6 +/- 9.4 mcg.h/ml, and 1.1 +/- 0.5 h, respectively, in patients with
otitis media. The Cmax exceeded the minimum inhibitory concentration of common susceptible pathogens causing
pharyngitis and
otitis media by severalfold. Nearly 60% of the dose was excreted unchanged in the urine during the dosage interval. The pharmacokinetics were independent of dose.
Loracarbef was well tolerated in all patients. These data suggest that
loracarbef may be used safely at doses of 7.5 mg/kg every 12 h in pediatric patients with streptococcal
pharyngitis and 15 mg/kg every 12 h in those with
otitis media.