Protein Binding of Rifapentine and Its 25-Desacetyl Metabolite in Patients with Pulmonary Tuberculosis
Author(s) -
Eric F. Egelund,
Marc Weiner,
Rajendra Singh,
Thomas J. Prihoda,
Jonathon Gelfond,
Hartmut Derendorf,
William R. Mac Kenzie,
Charles A. Peloquin
Publication year - 2014
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.01730-13
Subject(s) - rifapentine , pharmacokinetics , tuberculosis , pharmacodynamics , pharmacology , free fraction , medicine , mycobacterium tuberculosis , latent tuberculosis , pathology
Rifapentine is highly protein bound in blood, but the free, unbound drug is the microbiologically active fraction. In this exploratory study, we characterized the free plasma fraction of rifapentine in 41 patients with tuberculosis. We found a lower total rifapentine concentration but significantly higher free rifapentine levels in African patients of black race compared to non-Africans. These data support larger pharmacokinetic/pharmacodynamic studies to confirm these findings and assess free rifapentine in relation to microbiological and clinical outcomes.
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