EC Pharmacology And Toxicology

Vinpocetine is a semi-synthetic derivative of vincamine, an alkaloid component of the lesser periwinkle plant (Vinca minor L). In the United States, vinpocetine is sold directly to consumers as a dietary supplement. More than 300 brands of dietary supplements containing vinpocetine are commercially available. Vinpocetine supplements are most commonly marketed as weight loss supplements, sports supplements, and brain function enhancers. Given the widespread potential use of vinpocetine as a dietary supplement by pregnant women and women of childbearing age, recent studies were conducted in rats and rabbits by the National Toxicology Program (NIEHS) to characterize the potential effects of vinpocetine exposure on reproduction and embryo-fetal development. Pregnant rats dosed with vinpocetine demonstrated dose-dependent increases in post-implantation loss, higher frequency of early and total resorptions, lower fetal body weights, and fewer live fetuses following administration of 60 mg/kg, in the absence of maternal toxicity. Rat fetuses displayed dose-dependent increases in the incidences of ventricular septum defects (VSDs) and full supernumerary thoracolumbar ribs (SNRs). Similarly, pregnant rabbits administered vinpocetine displayed an increase in post-implantation loss and fewer live fetuses (300 mg/kg), as well as significantly lower fetal body weights (≥ 75 mg/kg). In addition, comparisons of human and animal systemic exposure data revealed that the blood levels of vinpocetine measured in pregnant animals were similar to those reported in humans after taking a single dose of vinpocetine. These results support a causal role of vinpocetine exposure in producing developmental and reproductive toxicities in both the rat and rabbit and strongly suggest potential safety risks associated with exposure to vinpocetine during pregnancy in humans, including the potential for miscarriages and alterations in embryo-fetal development. Pregnant women and women of childbearing age should not take dietary supplement products containing vinpocetine. Safety warnings against use by pregnant women and women who could become pregnant must be added to the labels of all commercially available vinpocetine supplements.

 Keywords: Vinpocetine; Ethyl Apovincaminate; Common Periwinkle Vinpocetine; Lesser Periwinkle Extract; Vinca Minor Extract; Dietary Supplements; Dietary Supplement Ingredient; Developmental Toxicity; Reproductive Toxicity

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