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Brief Report: Significant Decreases in Both Total and Unbound Lopinavir and Amprenavir Exposures During Coadministration: ACTG Protocol A5143/A5147s Results.
- Source :
-
Journal of acquired immune deficiency syndromes (1999) [J Acquir Immune Defic Syndr] 2015 Dec 15; Vol. 70 (5), pp. 510-4. - Publication Year :
- 2015
-
Abstract
- This secondary analysis explored changes in protein-unbound concentrations of lopinavir and amprenavir when coadministered in HIV-infected subjects. Total and unbound pharmacokinetic parameters were calculated and compared between subjects receiving each agent alone and coadministration. When coadministered, unbound and total concentrations decrease. Coadministration significantly increased lopinavir unbound clearance, while significant changes in fraction unbound (fu) were not detected. For amprenavir, significant increases in fu and unbound clearance occurred with coadministration. This demonstrates the complex nature of drug-drug interactions between highly protein-bound, CYP-metabolized drugs, and the need to measure unbound concentrations in disease states such as hepatitis C, where such agents are coadministered.
- Subjects :
- Adult
Anti-HIV Agents administration & dosage
Anti-HIV Agents blood
Area Under Curve
Carbamates administration & dosage
Carbamates blood
Carbamates pharmacokinetics
Drug Interactions
Drug Therapy, Combination
Female
Furans
Humans
Lopinavir administration & dosage
Lopinavir blood
Lopinavir pharmacokinetics
Male
Middle Aged
Sulfonamides administration & dosage
Sulfonamides blood
Sulfonamides pharmacokinetics
Viral Load
Anti-HIV Agents therapeutic use
Carbamates therapeutic use
HIV Infections drug therapy
Lopinavir therapeutic use
Sulfonamides therapeutic use
Subjects
Details
- Language :
- English
- ISSN :
- 1944-7884
- Volume :
- 70
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Journal of acquired immune deficiency syndromes (1999)
- Publication Type :
- Academic Journal
- Accession number :
- 26230332
- Full Text :
- https://doi.org/10.1097/QAI.0000000000000777