Pharmacokinetics of single- and multiple-dose teicoplanin in healthy volunteers

Teicoplanin, an investigational glycopeptide antibiotic related chemically and microbiologically to vancomycin, has in vitro and in vivo activity against gram-positive aerobic and anaerobic bacteria. We compared the single- and multiple-dose pharmacokinetics of intravenous teicoplanin in healthy volunteers. Serum and urine samples were collected for 35 days after single-dose (3 mg/kg) and 72 days after multiple-dose (3 mg/kg per day for 21 days) administration. A three-exponent equation with zero-order input was fitted to concentrations in serum. The mean half-lives (t1/2s) were significantly different (P = 0.0075) after single- and multiple-dose administration (130 +/- 14.9 and 176 +/- 29.8 h, respectively). The clinically relevant t1/2 obtained from multiple-dose data was approximately 61 h. Total and renal clearances determined at steady state were not statistically different, indicating that teicoplanin is eliminated almost entirely by renal mechanisms.