Pharmacokinetics of Ertapenem in Healthy Young Volunteers
| Autor: | Deutsch Paul J, R. Haesen, Liwen Xi, G. Mistry, Michael Hesney, Jacqueline B. McCrea, Chester J. Kitchen, S. Holland, Scott A. Waldman, R. L. Lins, Howard E. Greenberg, J.D. Rogers, Kimberly L. Birk, A. K. Majumdar, S. X. Li, Robert A. Blum, Donald G. Musson |
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| Rok vydání: | 2002 |
| Předmět: |
Adult
Ertapenem Male Lactams Urine Pharmacology beta-Lactams chemistry.chemical_compound Double-Blind Method Pharmacokinetics Blood plasma polycyclic compounds Humans Pharmacology (medical) Antibacterial agent Sex Characteristics Dose-Response Relationship Drug Area under the curve Half-life Blood Proteins Blood proteins Anti-Bacterial Agents body regions Infectious Diseases chemistry Area Under Curve Injections Intravenous Female Spectrophotometry Ultraviolet Half-Life Protein Binding |
| Zdroj: | Antimicrobial Agents and Chemotherapy. 46:3506-3511 |
| ISSN: | 1098-6596 0066-4804 |
| DOI: | 10.1128/aac.46.11.3506-3511.2002 |
| Popis: | Ertapenem (INVANZ) is a new once-a-day parenteral β-lactam antimicrobial shown to be effective as a single agent for treatment of various community-acquired and mixed infections. The single- and multiple-dose pharmacokinetics of ertapenem at doses up to 3 g were examined in healthy young men and women volunteers. Plasma and urine samples collected were analyzed using reversed-phase high-performance liquid chromatography with UV detection. Ertapenem is highly bound to plasma protein. The protein binding changes from ∼95% bound at concentrations of 0-∞ ) of total ertapenem. The single-dose AUC 0-∞ of unbound ertapenem was nearly dose proportional over the dose range of 0.5 to 2 g. The mean concentration of ertapenem in plasma ranged from ∼145 to 175 μg/ml at the end of a 30-min infusion, from ∼30 to 34 μg/ml at 6 h, and from ∼9 to 11 μg/ml at 12 h. The mean plasma t 1/2 ranged from 3.8 to 4.4 h. About 45% of the plasma clearance (CL P ) was via renal clearance. The remainder of the CL P was primarily via the formation of the β-lactam ring-opened metabolite that was excreted in urine. There were no clinically significant differences between the pharmacokinetics of ertapenem in men and women. Ertapenem does not accumulate after multiple once-daily dosing. |
| Databáze: | OpenAIRE |
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