Vinpocetine is a well-known substance in the health-hacking community with a variety of claimed health benefits. Vinpocetine is used to increase brain circulation, alertness, cognitive function, concentration, and memory, as well as to lower inflammation and oxidative stress. This article will explore vinpocetine’s history, how it works, its potential benefits, and any possible safety issues you should consider before taking it.
What Is Vinpocetine?
Vinpocetine is an alkaloid derived from the compound vincamine. Vincamine is the main ingredient of the lesser periwinkle plant, Vinca minor – a common garden plant.
In several countries, including Japan, Mexico, Russia, and many in Europe, vinpocetine is prescribed for the treatment of cognitive and circulatory brain disorders such as stroke and dementia.
However, vinpocetine is not approved for any conditions in the United States and Canada. Due to its synthetic nature and therapeutic use, the FDA ruled that it cannot be marketed as a dietary supplement. Despite this, vinpocetine is available as an over-the-counter cognitive-enhancing supplement in these countries.
A Brief History of Vinpocetine
Vinpocetine was first isolated from the lesser periwinkle plant in 1975 by the Hungarian chemist Csaba Szántay. Gedeon Richter, a Hungarian drug company, began manufacturing it in 1978 under the brand name Cavinton [1].
Vinpocetine has historically been used in European countries as a way to enhance blood flow to the brain in the treatment of cognitive decline, stroke recovery, and epilepsy.
More recently, it has been picked up by the nootropic community for its potential to enhance memory and cognition.
Vinpocetine Snapshot
Proponents
- Boosts circulation
- May slow cognitive decline
- Possible benefits for memory, reaction times, hearing loss, and headaches
- Generally safe when taken at normal oral doses
Skeptics
- Insufficient evidence for most uses
- Not FDA-approved
- Severe adverse effects from injecting high doses
How Vinpocetine Works
Vinpocetine influences the flow of important electrolytes by inhibiting several types of ion channels:
These ion channel interactions can result in decreased neurotransmitter release (dopamine and/or glutamate). Excess dopamine and glutamate in the brain can kill its cells due to overactivation (excitotoxicity) and increased oxidative damage. Therefore, vinpocetine is thought to have neuroprotective properties by decreasing the amount of dopamine and/or glutamate released in the brain [6].
Vinpocetine also inhibits PDE1. Blockers of this enzyme have potential cardioprotective and cognitive-boosting properties. By increasing cGMP concentrations, they widen the blood vessels and increase blood flow [7, 8, 2].
Additionally, vinpocetine may lower inflammation by inhibiting IKKβ activation as well as the transportation of NF-kB across cell membranes [9].
Vinpocetine has also been shown to interact with alpha-adrenergic and TPSO (translocator protein) receptors. The effects of vinpocetine actions on these receptors are not fully understood.
How Vinpocetine Is Processed by the Body
Bioavailability
In humans, vinpocetine has a bioavailability of 6.2–6.7% when consumed in a water–based solution [10].
Interestingly, it has a much higher bioavailability in rodents – close to 52%. Some people believe that its bioavailability can be increased to those levels in humans under certain circumstances [10, 11].
For example, ingesting vinpocetine with a meal (regardless of its composition) rather than in a fasted state can increase its bioavailability by 60–100% [12].
Certain delivery systems, such as liposomal delivery, can also increase its absorption [13, 14].
One study found that a topical vinpocetine patch was twice as bioavailable as orally ingested vinpocetine [15].
Metabolism
Upon consumption, vinpocetine is quickly metabolized into its active metabolite cis-apovincaminic acid [16, 17].
Vinpocetine is excreted after being metabolized. This is why no residues can be found in urine – only its metabolites [18].
Blood Levels
Vinpocetine is detectable in the blood within 20 minutes of consumption [19].
Oral administration with 5 mg of vinpocetine resulted in peak blood levels of approximately 64 ng/mL. Its half-life is around 1.46 hours [15].
Vinpocetine is undetectable in the blood 2-3 hours after ingestion and it binds to proteins in the blood at rates from 86.6% to complete binding [20, 2].
Blood levels of apovincamic acid, vinpocetine’s main metabolite, peak within one hour after consumption and return to normal within 3-4 hours [20].
Vinpocetine does not accumulate in the body when moderate oral doses (5-30 mg daily) are ingested [20].
Does Vinpocetine Reach the Brain?
Yes. Studies in primates and humans have shown that vinpocetine can pass through the blood-brain barrier [21, 22].
Indeed, vinpocetine is rapidly absorbed into the human brain, with 3.18-4.27% entering the brain within 2 minutes of an IV dose [21].
After consumption, vinpocetine appears to increase in the human brain more than in the rest of the body [2].
Vinpocetine has a special affinity to specific areas of the brain such as the thalamus (24% higher than average), basal ganglia, putamen, and visual cortex. These brain regions receive the most additional blood flow in response to vinpocetine [23, 24].
Benefits of Vinpocetine
Likely Effective for:
Increasing Brain Blood Flow & Oxygenation
In six healthy men, an infusion of 20 mg vinpocetine resulted in a 7% increase in blood flow to the brain [25].
Vinpocetine also improved brain oxygenation in 700 individuals with brain circulation issues. It improved blood flow without altering their average blood pressure [26, 27, 28].
This enhanced blood flow is linked with cognitive protection, based on 2 studies on 46 people recovering from brain strokes [29, 30].
Vinpocetine may also increase microcirculation in the brain, as seen in a pilot study on 30 people. It probably does so by enhancing red blood cell flexibility and, therefore, reducing blood viscosity [31, 32, 33].
All in all, the evidence suggests that vinpocetine increases blood flow in the brain, which may be beneficial to people recovering from a brain stroke. Remember to use vinpocetine as prescribed by your doctor (in countries where it is approved) or discuss its potential use with them (in the US and Canada).
Possibly Effective for:
Slowing Cognitive Decline
In a clinical trial on over 200 people with dementia, treatment with vinpocetine (10-20 mg, 3x/day) for 16 weeks improved their overall cognitive performance and reduced the subjective rating of their “severity of illness” [34].
One week of intravenous infusions of vinpocetine, followed by 90 days of 30 mg oral dosage, significantly improved the symptoms of cognitive decline in a trial on over 4,000 individuals with poor blood circulation in the brain. For example, their physical balance was markedly improved [35].
Another study gave vinpocetine (vinpotropile) to 20 patients aged 50-78 with low blood flow to the brain. The rate of cognitive decline slowed significantly (based on the results of speech performance tests), and subjective measures of well-being improved [36].
The TPSO system (a sensor of brain injury and microglial activation) is upregulated in people with cognitive impairment or brain trauma. By attaching to receptors in the TSPO system, vinpocetine might be able to reduce the activity of this system and, thus, reduce cognitive decline [37, 38, 21, 23].
Taken together, the evidence suggests that vinpocetine may help slow cognitive decline in people with low blood flow in the brain. You may discuss with your doctor if vinpocetine may help you or your relatives. Never use vinpocetine in place of what your doctor recommends or prescribes.
Insufficient Evidence for:
The following purported benefits are only supported by limited, low-quality clinical studies. Most of them are small or haven’t been translated into English. Therefore, there is insufficient evidence to support the use of vinpocetine for any of the below-listed purposes. Remember to speak with a doctor before taking vinpocetine supplements. It should never be used as a replacement for approved medical therapies.
1) Enhancing Memory
In a small pilot study on 12 healthy women, 40 mg of vinpocetine, taken 3 times per day, improved memory and memory scanning speed [39].
In another small trial on 8 healthy volunteers, vinpocetine counteracted the short-term memory impairment caused by a sedative (flunitrazepam) [40].
The inhibition of sodium and calcium channels leads to memory improvement. Vinpocetine’s inhibition of these ion channels may explain it’s memory-enhancing properties [41, 42].
Vinpocetine may also increase memory by long-term potentiation – the strengthening of synapses based on recent patterns of activity – based on a study in Guinea pigs [43].
Another way vinpocetine may enhance memory is by affecting alpha-adrenergic receptors in the brain [44].
2) Improving Reaction Times
In a small trial on 12 healthy female volunteers between the ages of 25-40, 40 mg of vinpocetine per day significantly reduced reaction times, from approximately 610 ms to 430 ms [39].
3) Hearing Loss
In 2 studies on 140 people with hearing loss caused by nerve damage, vinpocetine (both alone and combined with ganglioside) improved the condition in 73-80% of the patients. Unfortunately, neither of the studies has been translated into English and we couldn’t access their specifics for a critical analysis [45, 46].
In Guinea pigs, vinpocetine, given at 2 mg/kg injections, offers protection against hearing loss caused by taking antibiotics [47].
4) Headaches
In a clinical trial on 126 people with tension headaches, vinpocetine combined with acupressure and other drugs (the muscle relaxer Zanaflex and the antidepressant Prozac) provided some relief. The treatment was more effective when it also included the antioxidant Emoxypine, which is only approved in Russia [48].
Animal and Cell Research (Lack of Evidence)
No clinical evidence supports the use of vinpocetine for any of the conditions listed in this section. Below is a summary of the existing animal and cell-based research, which should guide further investigational efforts. However, the studies should not be interpreted as supportive of any health benefit.
Heart Health
In mice with a deficiency in ApoE (Apolipoprotein E), 5 mg/kg vinpocetine given every other day almost halved the amount of plaque in the arteries [49].
This improvement was likely due to a reduction in the receptor for oxidized LDL (LOX-1) and, thus, less LDL oxidation [50].
The process of atherosclerosis is associated with vascular smooth muscle cell (VSMC) proliferation, which worsens atherosclerosis [51]. At 5 mg/kg, vinpocetine reduces VSMC proliferation by 50% [52].
Liver Function
Vinpocetine, given orally at 2.1-8.4 mg/kg, reduced elevations of liver enzymes (ALT, AST, ALP) caused by a liver toxin in rats. At the highest dose (8.4 mg/kg) there was an 82.6% reduction in liver cell death [53].
Anti-Inflammatory
Vinpocetine (5 mg/kg per day) had potent anti-inflammatory effects in mice [54].
Vinpocetine may exert its anti-inflammatory effects by inhibiting IKKβ and reducing the transportation of NF-kB across cell membranes [55, 54].
Mitochondrial Function
Vinpocetine reduced the loss in mitochondrial membrane potential (needed to create ATP) caused by overactivation of neurotransmitter receptors (excitotoxicity) in brain cells [56].
Similarly, high blood levels reversed the decrease in mitochondrial function seen with beta-amyloid pigmentation in a cell-based study [57].
Pain
Vinpocetine blocked certain sodium channels associated with pain (e.g. NaV1.8) in 2 studies in brain cells [58, 59].
Cancer
Below, we will discuss some preliminary research on the potential anticancer effect of vinpocetine. Keep in mind that many substances have anti-cancer effects in animals and cells, including downright toxic chemicals like bleach. This doesn’t mean that they have any medical value. On the contrary, most substances (natural or synthetic) that are researched in cancer cells fail to pass further clinical trials due to a lack of safety or efficacy.
In mice, 10-20 mg/kg of injected vinpocetine reduced breast tumor growth and caused no adverse effects. It possibly did so by interfering with the cell cycle and inhibiting the activation of certain signaling pathways (PI3K) and proteins (STAT3) [60].
Side Effects & Dosage
Side Effects
This list does not cover all possible side effects. Contact your doctor or pharmacist if you notice any other side effects.
Call your doctor for medical advice about side effects. In the US, you may report side effects to the FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch. In Canada, you may report side effects to Health Canada at 1-866-234-2345.
The intravenous administration of high doses has been reported to cause serious adverse effects, including death from sudden falls in blood pressure and heart rate [61, 62].
However, this is not an issue with the oral form at standard dosages. Only one case of a sudden drop in white blood cell count from an oral dose of 15 mg/day has been reported [63].
There have also been reports of skin allergy to vincamine [64].
Dosage
If your doctor prescribes you vinpocetine, carefully follow your treatment plan and never change the dose without consulting it with your doctor.
If you purchased vinpocetine as an over-the-counter supplement, discuss with your doctor how it may help you and follow his or her recommendations.
The standard low dose is 5 mg at each of these three meals, with 20 mg per meal seen as a high dose. This dose range is suitable for the purposes of neuroprotection, enhancing cerebral blood flow, and reducing the rate of cognitive decline.
Remember that taking vinpocetine with meals will enhance absorption.
