Lopinavir/Ritonavir Induces the Hepatic Activity of Cytochrome P450 Enzymes CYP2C9, CYP2C19, and CYP1A2 But Inhibits the Hepatic and Intestinal Activity of CYP3A as Measured by a Phenotyping Drug Cocktail in Healthy Volunteers

@article{Yeh2006LopinavirRitonavirIT,
  title={Lopinavir/Ritonavir Induces the Hepatic Activity of Cytochrome P450 Enzymes CYP2C9, CYP2C19, and CYP1A2 But Inhibits the Hepatic and Intestinal Activity of CYP3A as Measured by a Phenotyping Drug Cocktail in Healthy Volunteers},
  author={Rosa F. Yeh and Vincent Gaver and Kristine B. Patterson and Naser L. Rezk and Faustina Baxter-Meheux and Michael J. Blake and Joseph J. Eron and Cheri E. Klein and John C Rublein and Angela D. M. Kashuba},
  journal={JAIDS Journal of Acquired Immune Deficiency Syndromes},
  year={2006},
  volume={42},
  pages={52-60}
}
  • R. Yeh, V. Gaver, A. Kashuba
  • Published 1 April 2006
  • Medicine, Biology
  • JAIDS Journal of Acquired Immune Deficiency Syndromes
Objective: The effect of lopinavir/ritonavir (LPV/r) administration on cytochrome P450 (CYP) enzyme activity was quantified using a phenotyping biomarker cocktail. Changes in CYP2C9, CYP2C19, CYP3A, CYP1A2, N-acetyltransferase-2 (NAT-2), and xanthine oxidase (XO) activities were evaluated using warfarin (WARF) + vitamin K, omeprazole (OMP), intravenous (IV) and oral (PO) midazolam (MDZ), and caffeine (CAF). Design: Open-label, multiple-dose, pharmacokinetic study in healthy volunteers. Methods… 
A Phenotype–Genotype Approach to Predicting CYP450 and P‐Glycoprotein Drug Interactions With the Mixed Inhibitor/Inducer Tipranavir/Ritonavir
TLDR
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TLDR
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TLDR
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The Role of Cytochrome P450 3A Inducers and Inhibitors in the Metabolism and the Effects of Oxycodone
TLDR
Clinicians should avoid concomitant administration of CYP3A inducers or inhibitors and oral oxycodone if this is not possible, and be prepared to interactions leading to impaired analgesia or increased adverse effects after CYP2D6 inducers and oral Oxycodone.
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The results demonstrate that exposures of probes of CYP3A4, CYP2D6, or CYP 2C19 activity are potentially altered by administration of sorafenib at 400 mg twice daily, however, these differences are sufficiently small that a clinically significant inhibition or induction of these important drug metabolizing P450 isoenzymes is unlikely.
Pharmacodynamics of Carbamazepine‐mediated Induction of CYP3A4, CYP1A2, and Pgp as Assessed by Probe Substrates Midazolam, Caffeine, and Digoxin
TLDR
The possibility of modeling the pharmacodynamics of enzyme induction using a turnover model was illustrated, and the time course of the process was estimated with good precision.
CYP3A induction and inhibition by different antiretroviral regimens reflected by changes in plasma 4β-hydroxycholesterol levels
TLDR
Changes in plasma 4β-hydroxycholesterol following the initiation of efavirenz- or atazanavir/ritonavir-based antiretroviral therapy reflected the respective net increase and decrease of CYP3A activity of these regimens.
Effect of Ginkgo biloba extract on lopinavir, midazolam and fexofenadine pharmacokinetics in healthy subjects
TLDR
The results suggest that GBE induces CYP3A metabolism, as assessed by a decrease in midazolam concentrations, which appears unlikely to reduce the exposure of ritonavir-boosted protease inhibitors, while concentrations of unboosted proteins may be affected.
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