NDLI: Disposition, Metabolism, and Excretion of [14C]Doripenem after a Single 500-Milligram Intravenous Infusion in Healthy Men▿

Content Provider	PubMed Central
Author	Cirillo, Iolanda Mannens, Geert Janssen, Cor Marc, Vermeir Filip, Cuyckens Desai-krieger, Daksha Vaccaro, Nicole Kao, L. Mark Devineni, Damayanthi Redman, Rebecca Turner, Kenneth
Abstract	In this open-label, single-center study, eight healthy men each received a single 500-mg dose of [14C]doripenem, containing 50 μCi of [14C]doripenem, administered as a 1-h intravenous infusion. The concentrations of unchanged doripenem and its primary metabolite (doripenem-M-1) resulting from β-lactam ring opening were measured in plasma and urine by a validated liquid chromatography method coupled to a tandem mass spectrometry assay. Total radioactivity was measured in blood, plasma, urine, and feces by liquid scintillation counting. Further metabolite profiling was conducted on urine samples using liquid chromatography coupled to radiochemical detection and high-resolution mass spectrometry. Unchanged doripenem and doripenem-M-1 accounted for means of 80.7% and 12.7% of the area under the plasma total-radioactivity-versus-time curve (area under the concentration-time curve extrapolated to infinity) and exhibited elimination half-lives of 1.1 and 2.5 h, respectively. Total clearance of doripenem was 16 liters/h, and renal clearance was 12.5 liters/h. At 7 days after the single dose, 95.3% of total doripenem-related radioactivity was recovered in urine and 0.72% in feces. A total mean of 97.2% of the administered dose was excreted in the urine as unchanged doripenem (78.7% ± 5.7%) and doripenem-M-1 (18.5% ± 2.6%). Most of the urinary recovery occurred within 4 h of dosing. Three additional minor metabolites were identified in urine: the glycine and taurine conjugates of doripenem-M-1 and oxidized doripenem-M-1. These results show that doripenem is predominantly eliminated in urine as unchanged drug, with only a fraction metabolized to doripenem-M-1 and other minor metabolites.
Related Links	http://dx.doi.org/10.1128/aac.00424-08
Ending Page	3483
Page Count	6
Starting Page	3478
File Format	PDF
ISSN	00664804
e-ISSN	10986596
Journal	Antimicrobial Agents and Chemotherapy
Issue Number	10
Volume Number	52
Language	English
Publisher	American Society for Microbiology (ASM)
Publisher Date	2008-10-01
Access Restriction	Open
Rights Holder	American Society for Microbiology (ASM)
Subject Keyword	Pharmacology (medical) Pharmacology Infectious Diseases Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Infectious Diseases Pharmacology Pharmacology (medical)

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