Document Detail


The pharmacokinetics of taurolidine metabolites in healthy volunteers.
MedLine Citation:
PMID:  17395893     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Taurolidine is an experimental antibacterial and antiendotoxic compound whose clinical utility as an antitumor agent is being investigated in human clinical trials. Taurolidine in aqueous solution exists in equilibrium with taurultam. Taurultam is subsequently transformed to taurinamide. The pharmacokinetic profiles of these metabolites are not well established. In this study, 18 healthy volunteers were administered 5.0 g of taurolidine in 250 mL of 5% polyvinylpyrrolidone in water over 2, 1, or 0.5 hours by intravenous infusion in a parallel-group design. All subjects noted discomfort at the infusion site, although there were no serious adverse events. t(max) generally occurred at the end of infusion for taurinamide, whereas that of taurultam was reached before completion of infusion. The taurolidine metabolite taurultam demonstrated a shorter half-life and lower systemic exposure than taurinamide. Shortening of infusion duration increased the C(max) and AUC of taurultam. Changes in infusion rate did not substantially change the pharmacokinetic parameters of taurinamide.
Authors:
Li Gong; Howard E Greenberg; James L Perhach; Scott A Waldman; Walter K Kraft
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Publication Detail:
Type:  Clinical Trial; Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2007-03-29
Journal Detail:
Title:  Journal of clinical pharmacology     Volume:  47     ISSN:  0091-2700     ISO Abbreviation:  J Clin Pharmacol     Publication Date:  2007 Jun 
Date Detail:
Created Date:  2007-05-23     Completed Date:  2007-07-24     Revised Date:  2007-12-03    
Medline Journal Info:
Nlm Unique ID:  0366372     Medline TA:  J Clin Pharmacol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  697-703     Citation Subset:  IM    
Affiliation:
Department of Pharmacology and Experimental Therapeutics, Jefferson Medical College, Thomas Jefferson University, Philadelphia, PA 19107, USA.
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MeSH Terms
Descriptor/Qualifier:
Adult
Anti-Bacterial Agents / administration & dosage,  blood,  pharmacokinetics*
Area Under Curve
Drug Administration Schedule
Female
Half-Life
Humans
Male
Pharmaceutic Aids
Povidone
Taurine / administration & dosage,  analogs & derivatives*,  blood,  pharmacokinetics
Thiadiazines / administration & dosage,  blood,  pharmacokinetics*
Grant Support
ID/Acronym/Agency:
5 T32 GM008562-11/GM/NIGMS NIH HHS
Chemical
Reg. No./Substance:
0/Anti-Bacterial Agents; 0/Pharmaceutic Aids; 0/Thiadiazines; 107-35-7/Taurine; 19388-87-5/taurolidine; 9003-39-8/Povidone

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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