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Protein binding of rifapentine and its 25-desacetyl metabolite in patients with pulmonary tuberculosis.


ABSTRACT: 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.

SUBMITTER: Egelund EF 

PROVIDER: S-EPMC4136068 | biostudies-literature | 2014 Aug

REPOSITORIES: biostudies-literature

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Protein binding of rifapentine and its 25-desacetyl metabolite in patients with pulmonary tuberculosis.

Egelund Eric F EF   Weiner Marc M   Singh Rajendra P RP   Prihoda Thomas J TJ   Gelfond Jonathon A L JA   Derendorf Hartmut H   Mac Kenzie William R WR   Peloquin Charles A CA  

Antimicrobial agents and chemotherapy 20140519 8


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 r  ...[more]

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