TY - JOUR
T1 - Protein binding of rifapentine and its 25-desacetyl metabolite in patients with pulmonary tuberculosis
AU - Egelund, Eric F.
AU - Weiner, Marc
AU - Singh, Rajendra P.
AU - Prihoda, Thomas J.
AU - Gelfond, Jonathon A.L.
AU - Derendorf, Hartmut
AU - MacKenzie, William R.
AU - Peloquin, Charles A.
PY - 2014/8
Y1 - 2014/8
N2 - 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.
AB - 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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U2 - 10.1128/AAC.01730-13
DO - 10.1128/AAC.01730-13
M3 - Article
C2 - 24841270
AN - SCOPUS:84905397050
VL - 58
SP - 4904
EP - 4910
JO - Antimicrobial Agents and Chemotherapy
JF - Antimicrobial Agents and Chemotherapy
SN - 0066-4804
IS - 8
ER -