Document Detail


Pharmacokinetics of lidocaine and bupivacaine and stable isotope labelled analogues: a study in healthy volunteers.
MedLine Citation:
PMID:  3342287     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The pharmacokinetics of lidocaine and bupivacaine and tri-deuteromethyl-labelled lidocaine and bupivacaine were investigated in healthy volunteers. The deuterium-labelled and the unlabelled form of the drug to be investigated were simultaneously infused in 10 min. Plasma concentrations were determined using a combination of capillary gas chromatography and mass fragmentography. Bi-exponential functions were fitted to the plasma concentration-time data. The mean distribution and elimination half-lives were 8.4 +/- 5.9 min and 96 +/- 26 min for lidocaine, 9.2 +/- 7.0 min and 98 +/- 27 min for deuterium-labelled lidocaine, 15.3 +/- 9.9 min and 111 +/- 32 min for bupivacaine, and 15.2 +/- 10.9 min and 109 +/- 31 min for deuterium-labelled bupivacaine, respectively. The mean volumes of the central compartment and mean steady state volumes of distribution were: lidocaine 37 +/- 151 and 97 +/- 201, deuterium-labelled lidocaine 39 +/- 161 and 98 +/- 181, bupivacaine 27 +/- 111 and 66 +/- 231 and deuterium-labelled bupivacaine 28 +/- 121, and 65 +/- 221, respectively. The respective mean plasma clearances were 0.88 +/- 0.181 min-1, 0.87 +/- 0.181 min-1, 0.61 +/- 0.151 min-1, and 0.62 +/- 0.171 min-1. The results of the study indicate that substitution of a deuterated methyl group does not alter the pharmacokinetics of lidocaine and bupivacaine in healthy subjects.
Authors:
A G Burm; A G de Boer; J W van Kleef; N P Vermeulen; L G de Leede; J Spierdijk; D D Breimer
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Publication Detail:
Type:  Clinical Trial; Controlled Clinical Trial; Journal Article    
Journal Detail:
Title:  Biopharmaceutics & drug disposition     Volume:  9     ISSN:  0142-2782     ISO Abbreviation:  Biopharm Drug Dispos     Publication Date:    1988 Jan-Feb
Date Detail:
Created Date:  1988-04-06     Completed Date:  1988-04-06     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  7911226     Medline TA:  Biopharm Drug Dispos     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  85-95     Citation Subset:  IM    
Affiliation:
Department of Anaesthesiology, University Hospital, Leiden, The Netherlands.
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MeSH Terms
Descriptor/Qualifier:
Adult
Bupivacaine / blood,  pharmacokinetics*
Deuterium
Half-Life
Humans
Lidocaine / blood,  pharmacokinetics*
Male
Metabolic Clearance Rate
Chemical
Reg. No./Substance:
137-58-6/Lidocaine; 2180-92-9/Bupivacaine; 7782-39-0/Deuterium

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


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