Document Detail


Pharmacodynamic variability beyond that explained by minimum inhibitory concentrations (MICs).
MedLine Citation:
PMID:  23357773     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Monte-carlo simulations (MCS) present a powerful tool to evaluate candidate regimens by determining the probability of target attainment. Although these assessments have traditionally incorporated variability in PK parameters and MICs, consideration of inter-strain PD variability has been neglected. A population PK/PD model was developed for doripenem using murine-thigh infection data based on 20 bacterial strains. PK data were fit to a linear two-compartment model with first-order input and elimination processes and an absorption lag-time from a separate site (r(2)>0.96). PK parameters were utilized to simulate free drug profiles for various regimens in PD studies, from which the %fT>MIC was calculated. Doripenem PD was excellently described with Hill-type models (r(2)>0.98); significant differences were not observed between mean PD estimates determined using a two-stage versus population analyses (p>0.05), however the variance in EC(50) and E(max) amongst strains was much greater using the two-stage approach. Even using the population approach, interstrain variability in EC(50) (CV%=29.2) and H (CV%=46.1) parameters was substantive, while the variability in E(max) (CV%=19.7) was modest. This resulted in extensive variability in the range of %fT>MIC targets associated with stasis to 2-log(10)-reduction in bacterial burden (CV%∼50%). It appears that MCS, based on the assumption that PD variability is due to MIC alone underestimates variability, and may consequently underestimate treatment failures.
Authors:
Rachel L Soon; Neang Ly; Gauri Rao; Lance Wollenberg; Kuo Yang; Brian Tsuji; Alan Forrest
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-1-28
Journal Detail:
Title:  Antimicrobial agents and chemotherapy     Volume:  -     ISSN:  1098-6596     ISO Abbreviation:  Antimicrob. Agents Chemother.     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2013-1-29     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0315061     Medline TA:  Antimicrob Agents Chemother     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
State University of New York at Buffalo School of Pharmacy and Pharmaceutical Science, Buffalo, New York.
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