The Effect of Vinpocetine on Human Cytochrome P450 Isoenzymes by Using a Cocktail Method

Abstract

Vinpocetine is a derivative of the alkaloid vincamine, which had been prescribed for chronic cerebral vascular ischemia and acute ischemic stroke or used as a dietary supplement for its several different mechanisms of biological activities. However, information on the cytochrome P450 (CYP) enzyme-mediated drug metabolism has not been previously studied. The present study was performed to investigate the effects of vinpocetine on CYPs activity, and cocktail method was used, respectively. To evaluate the effects of vinpocetine on the activity of human CYP3A4, CYP2C9, CYP2C19, CYP2D6, and CYP2E1, human liver microsomes were utilized to incubate with the mixed CYPs probe substrates and the target components. The results indicate that vinpocetine exhibited weak inhibitory effect on the CYP2C9, where the IC50 value is 68.96 μM, whereas the IC50 values for CYP3A4, CYP2C19, CYP2D6, and CYP2E1 were all over range of 100 μM, which showed that vinpocetine had no apparent inhibitory effects on these CYPs. In conclusion, the results indicated that drugs metabolized by CYP2C9 coadministrated with vinpocetine may require attention or dose adjustment.

Personalized medicine: Vinpocetine to reverse effects of GABRB3 mutation

“…12,13 Vinpocetine is absorbed after oral administration but undergoes extensive first pass metabolism. 16 The benefit of vinpocetine might be independent or synergistic when combined with other seizure medications. 4 Peak levels are attained within an hour, as its half-life is ~90 minutes.…”

“…Due to this inhibition, when they are used in conjunction with other compounds that are metabolized by CYP enzymes (eg felbamate, carbamazepine, phenytoin, and phenobarbital), the levels of those individual antiseizure drugs might be affected. 16 The benefit of vinpocetine might be independent or synergistic when combined with other seizure medications. Definite interactions between vinpocetine and other seizure medications, however, have yet to be examined.…”

Optimized vinpocetine-loaded vitamin E D-α-tocopherol polyethylene glycol 1000 succinate-alpha lipoic acid micelles as a potential transdermal drug delivery system: in vitro and ex vivo studies

“…Vinpocetine (VNP), derived from the natural vinca alkaloid vincamine, is widely utilized as a vasodilator and a nootropic agent. 1,2 VNP is used for improving memory and cerebral metabolism in patients with cerebrovascular and age-related memory disorders. 3,4 In addition, it has shown potential in the treatment of Parkinson's and Alzheimer's diseases.…”