Studies on Pharmacokinetic Drug Interaction Potential of Vinpocetine
Abstract
:Abstract
Background
Methods
Results
Conclusion
1. Introduction
2. Experimental
3. Culture of hMDR1-MDCK-II, MDCK-II and HepG2 Cells
4. Reversible Inhibition (Co-Incubation Assay) and Time Dependent Inhibition (TDI/pre-Incubation Assay) of CYPs
5. Reversible Inhibition and Enzyme Kinetics of CYP3A4 and CYP2D6 in Pooled HLM
6. PXR Modulation
7. P-gp Inhibition
8. Analytical Methods
9. Statistical Methods
10. Results and Discussion
Compound | CYP3A4 (recombinant) | ||
---|---|---|---|
IC50 (µM) | IC50 (µM) | IC50 | |
Co-incubation | Pre-incubation | Shift (Fold) | |
Vinpocetine | 2.8 ± 0.98 | 5.1 ± 0.1 | 0.54 |
Ketoconazole | 0.04 ± 0.001 | 0.05 ± 0.002 | 0.80 |
Troleandomycin | 2.5 ± 0.8 | 0.42 ± 0.05 | 5.95 |
Compound | CYP2D6 (recombinant) | ||
---|---|---|---|
IC50 (µM) | IC50 (µM) | IC50 | |
Co-incubation | Pre-incubation | Shift (Fold) | |
Vinpocetine | 6.5 ± 1.1 | 37 ± 1.6 | 0.17 |
Quinidine | 0.05 ± 0.001 | 0.08 ± 0.002 | 0.62 |
Paroxetine | 3.4 ± 0.9 | 0.62 ± 0.03 | 5.48 |
11. Conclusions
Acknowledgments
Author Contributions
Conflicts of Interest
References
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Manda, V.K.; Avula, B.; Dale, O.R.; Chittiboyina, A.G.; Khan, I.A.; Walker, L.A.; Khan, S.I. Studies on Pharmacokinetic Drug Interaction Potential of Vinpocetine. Medicines 2015, 2, 93-105. https://doi.org/10.3390/medicines2020093
Manda VK, Avula B, Dale OR, Chittiboyina AG, Khan IA, Walker LA, Khan SI. Studies on Pharmacokinetic Drug Interaction Potential of Vinpocetine. Medicines. 2015; 2(2):93-105. https://doi.org/10.3390/medicines2020093
Chicago/Turabian StyleManda, Vamshi K., Bharathi Avula, Olivia R. Dale, Amar G. Chittiboyina, Ikhlas A. Khan, Larry A. Walker, and Shabana I. Khan. 2015. "Studies on Pharmacokinetic Drug Interaction Potential of Vinpocetine" Medicines 2, no. 2: 93-105. https://doi.org/10.3390/medicines2020093