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Weight-adjusted versus fixed dose of linezolid for Chinese healthy volunteers of higher and lower body weight: a Phase I pharmacokinetic and pharmacodynamic study.
- Source :
-
Expert opinion on investigational drugs [Expert Opin Investig Drugs] 2013 Mar; Vol. 22 (3), pp. 309-15. Date of Electronic Publication: 2013 Jan 30. - Publication Year :
- 2013
-
Abstract
- Objectives: The objective was to evaluate the pharmacokinetic and pharmacodynamic properties of a single intravenous fixed dose compared with a weight-adjusted dose of linezolid.<br />Methods: A Phase I, comparative clinical trial was conducted involving 20 healthy male Chinese volunteers, assigned into low weight (LW) (50 kg < weight ≤ 55 kg) and high weight (HW) (≥ 80 kg) groups. All subjects were administrated single dose of linezolid (600 mg/30 min) and, after 72 h washout period, another single-dose (10 mg/kg/30 min). Plasma linezolid concentrations were measured by liquid chromatography-tandem mass spectrometry. A Monte Carlo simulation was used to evaluate the probability of pharmacodynamic target attainment (PTA).<br />Results: With 600 mg dose, plasma concentrations in LW group were much higher than that in HW group. A persistent serum inhibitory activity was observed in LW group; the inhibitory activity was lower in HW group. The PTA in HW group was lower than in LW group. For 10 mg/kg dose, both HW and LW groups had similar plasma concentrations. The HW and LW groups had similar serum inhibitory effects. The PTA in HW and LW groups also showed no difference.<br />Conclusions: Our findings suggest that a weight-adjusted, 10 mg/kg regimen of linezolid may be more appropriate than fixed dosing for patients of different body weight.
- Subjects :
- Acetamides adverse effects
Acetamides blood
Administration, Intravenous
Adult
Anti-Infective Agents administration & dosage
Anti-Infective Agents adverse effects
Anti-Infective Agents blood
Anti-Infective Agents pharmacokinetics
Asian People
Body Weight
Dose-Response Relationship, Drug
Humans
Linezolid
Male
Monte Carlo Method
Oxazolidinones adverse effects
Oxazolidinones blood
Acetamides administration & dosage
Acetamides pharmacokinetics
Oxazolidinones administration & dosage
Oxazolidinones pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 1744-7658
- Volume :
- 22
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Expert opinion on investigational drugs
- Publication Type :
- Academic Journal
- Accession number :
- 23360474
- Full Text :
- https://doi.org/10.1517/13543784.2013.766716