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.
Carver
P L
PL
College of Pharmacy, University of Michigan, Ann Arbor 48109-1065.
Nightingale
C H
CH
Quintiliani
R
R
Sweeney
K
K
Stevens
R C
RC
Maderazo
E
E
D000328:Adult; D005260:Female; D006020:Glycopeptides / Q000008:administration & dosage / Q000032:analysis / Q000493:pharmacokinetics; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D017334:Teicoplanin
D006020:Glycopeptides; D017334:Teicoplanin