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.

• Authors: Eric F Egelund, Marc Weiner, Rajendra P Singh, Thomas J Prihoda, Jonathon A L Gelfond, Hartmut Derendorf, William R Mac Kenzie, Charles A Peloquin
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 58 Issue 8 Pg. 4904-10 (Aug 2014) ISSN: 1098-6596 [Electronic] United States
• PMID: 24841270 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S., Research Support, U.S. Gov't, P.H.S.)
• Copyright: Copyright © 2014, American Society for Microbiology. All Rights Reserved.

Chemical References

• Antibiotics, Antitubercular
• Blood Proteins
• 25-desacetylrifapentine
• Rifampin
• rifapentine

Topics

• Adult
• Antibiotics, Antitubercular (blood, pharmacokinetics, pharmacology)
• Biotransformation
• Black People
• Blood Proteins (metabolism)
• Female
• Humans
• Male
• Middle Aged
• Mycobacterium tuberculosis (drug effects, physiology)
• Protein Binding
• Rifampin (analogs & derivatives, blood, pharmacokinetics, pharmacology)
• Tuberculosis, Pulmonary (blood, drug therapy, ethnology, microbiology)
• White People