vinpocetine

Vinpocetine has been used in many Asian and European countries for treatment of cerebrovascular disorders such as stroke and dementia for over three decades.{{cite journal | vauthors = Zhang YS, Li JD, Yan C | title = An update on vinpocetine: New discoveries and clinical implications | journal = European Journal of Pharmacology | volume = 819 | issue = | pages = 30–34 | date = January 2018 | pmid = 29183836 | doi = 10.1016/j.ejphar.2017.11.041 | doi-access = free | pmc = 5766389 }}

The FDA has tentatively ruled that vinpocetine, due to its synthetic nature and proposed therapeutic uses, is ineligible to be marketed as dietary supplement under the Federal Food, Drug, and Cosmetic Act.{{cite magazine| vauthors = Schmitt R |title=Marketers exploit the aged with unproven brain-health claims|url=http://www.newsweek.com/marketers-exploit-aged-unproven-brain-health-claims-541709?rx=us|access-date=January 18, 2016|magazine=Newsweek|date=January 12, 2017}}{{cite web| vauthors = Hank S |title=FDA rules vinpocetine not a legal dietary ingredient despite successful NDI filings |url=http://www.nutraingredients-usa.com/Regulation/FDA-rules-vinpocetine-not-a-legal-dietary-ingredient-despite-successful-NDI-filings|website=NutraIngredients|date=7 September 2016 |publisher=William Reed Business Media, England|access-date=September 8, 2016}}{{cite web|title=FDA Concludes Vinpocetine Ineligible as a Dietary Ingredient|url=http://www.nutraceuticalsworld.com/contents/view_online-exclusives/2016-09-20/fda-concludes-vinpocetine-ineligible-as-a-dietary-ingredient|website=Nutraceuticals World|publisher=Rodman Media|access-date=January 18, 2017|date=September 20, 2016}}{{cite magazine| vauthors = Schmitt R |title=Dubious doses|url=https://www.pressreader.com/usa/newsweek/20170203/282071981620035|access-date=September 24, 2017|magazine=Newsweek|date=February 3, 2017}} Despite this, vinpocetine remains widely available in dietary supplements often marketed as nootropics.{{cite journal | vauthors = Avula B, Chittiboyina AG, Sagi S, Wang YH, Wang M, Khan IA, Cohen PA | title = Identification and quantification of vinpocetine and picamilon in dietary supplements sold in the United States | journal = Drug Testing and Analysis | volume = 8 | issue = 3–4 | pages = 334–343 | date = March 2016 | pmid = 26426301 | doi = 10.1002/dta.1853 | doi-access = free }}{{cite journal | vauthors = Cohen PA | title = Vinpocetine: An Unapproved Drug Sold as a Dietary Supplement | journal = Mayo Clinic Proceedings | volume = 90 | issue = 10 | pages = 1455 | date = October 2015 | pmid = 26434971 | doi = 10.1016/j.mayocp.2015.07.008 | doi-access = free }}

Vinpocetine does not fully support a benefit in either dementia or stroke.{{cite journal | vauthors = Szatmari SZ, Whitehouse PJ | title = Vinpocetine for cognitive impairment and dementia | journal = The Cochrane Database of Systematic Reviews | volume = 2003 | issue = 1 | pages = CD003119 | year = 2003 | pmid = 12535455 | pmc = 8406981 | doi = 10.1002/14651858.CD003119 }} As of 2003, three controlled clinical trials had tested "older adults with memory problems".{{cite journal | vauthors = McDaniel MA, Maier SF, Einstein GO | title = "Brain-specific" nutrients: a memory cure? | journal = Nutrition | volume = 19 | issue = 11–12 | pages = 957–975 | year = 2003 | pmid = 14624946 | doi = 10.1016/S0899-9007(03)00024-8 }}

Vinpocetine has also been studied for the prevention and recovery of acquired hearing loss in a phase II, longitudinal and prospective open clinical study on humans.{{cite journal | vauthors = Gutiérrez-Farfán I, Reyes-Legorreta C, Solís-Olguín M, Alatorre-Miguel E, Verduzco-Mendoza A, Durand-Rivera A | title = Evaluation of vinpocetine as a therapy in patients with sensorineural hearing loss: A phase II, open-label, single-center study | journal = Journal of Pharmacological Sciences | volume = 145 | issue = 4 | pages = 313–318 | date = April 2021 | pmid = 33712282 | doi = 10.1016/j.jphs.2021.01.010 | doi-access = free }}

Use during pregnancy may harm the baby or result in miscarriage.{{cite web | author = Office of the Commissioner |date=3 June 2019|title=Statement on warning for women of childbearing age about possible safety risks of dietary supplements containing vinpocetine|url=https://www.fda.gov/news-events/press-announcements/statement-warning-women-childbearing-age-about-possible-safety-risks-dietary-supplements-containing|access-date=5 June 2019|website=FDA|language=en}}{{dead link|date=May 2025|bot=medic}}{{cbignore|bot=medic}}

Adverse effects of vinpocetine include flushing, nausea, dizziness, dry mouth, transient hypo- and hyper-tension, headaches, heartburn, and decreased blood pressure.{{cite web |author1=National Toxicology Program |author-link=National Toxicology Program |title=Chemical Information Review Document for Vinpocetine (CAS No. 42971-09-5) |url=https://ntp.niehs.nih.gov/ntp/htdocs/chem_background/exsumpdf/vinpocetine091613_508.pdf |publisher=U.S. Department of Health and Human Services |access-date=December 28, 2018 |date=September 2013}} FDA issued a statement in 2019 warning that "vinpocetine may cause a miscarriage or harm fetal development".{{Cite web|url=https://www.fda.gov/news-events/press-announcements/statement-warning-women-childbearing-age-about-possible-safety-risks-dietary-supplements-containing|title=Statement on warning for women of childbearing age about possible safety risks of dietary supplements containing vinpocetine | author = Office of the Commissioner |date=2019-06-03|website=FDA|language=en|access-date=2019-06-04}}{{dead link|date=May 2025|bot=medic}}{{cbignore|bot=medic}}

Vinpocetine’s mechanism of action has been postulated to involve three potential effects: blockage of sodium channels, reduction of cellular calcium influx, and antioxidant activity.{{cite journal | vauthors = Bereczki D, Fekete I | title = Vinpocetine for acute ischaemic stroke | journal = The Cochrane Database of Systematic Reviews | volume = 2008 | issue = 1 | pages = CD000480 | date = January 2008 | pmid = 18253980 | pmc = 7034523 | doi = 10.1002/14651858.CD000480.pub2 }} Studies have also suggested that vinpocetine can inhibit PDE-1 in isolated rabbit aorta;{{cite journal | vauthors = Hagiwara M, Endo T, Hidaka H | title = Effects of vinpocetine on cyclic nucleotide metabolism in vascular smooth muscle | journal = Biochemical Pharmacology | volume = 33 | issue = 3 | pages = 453–457 | date = February 1984 | pmid = 6322804 | doi = 10.1016/0006-2952(84)90240-5 }} inhibit IKK in vitro, preventing IκB degradation and the following translocation of NF-κB to the cell nucleus;{{cite journal | vauthors = Jeon KI, Xu X, Aizawa T, Lim JH, Jono H, Kwon DS, Abe J, Berk BC, Li JD, Yan C | title = Vinpocetine inhibits NF-kappaB-dependent inflammation via an IKK-dependent but PDE-independent mechanism | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 107 | issue = 21 | pages = 9795–9800 | date = May 2010 | pmid = 20448200 | pmc = 2906898 | doi = 10.1073/pnas.0914414107 | doi-access = free }}{{cite journal | vauthors = Medina AE | title = Vinpocetine as a potent antiinflammatory agent | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 107 | issue = 22 | pages = 9921–9922 | date = June 2010 | pmid = 20495091 | pmc = 2890434 | doi = 10.1073/pnas.1005138107 | doi-access = free | bibcode = 2010PNAS..107.9921M }} and increase DOPAC, a metabolic breakdown product of dopamine, in isolated striatal nerve endings of rats.{{cite journal | vauthors = Trejo F, Nekrassov V, Sitges M | title = Characterization of vinpocetine effects on DA and DOPAC release in striatal isolated nerve endings | journal = Brain Research | volume = 909 | issue = 1–2 | pages = 59–67 | date = August 2001 | pmid = 11478921 | doi = 10.1016/S0006-8993(01)02621-X | s2cid = 38990597 }}

File:Vinpocetine Life Extension.jpg, 10mg per tablet]]

The inclusion of vinpocetine in dietary supplements in the U.S. has come under scrutiny due to the lack of defined dosage parameters, unproven short- and long-term benefits, and risks to human health.{{cite journal | vauthors = French JM, King MD, McDougal OM | title = Quantitative Determination of Vinpocetine in Dietary Supplements | journal = Natural Product Communications | volume = 11 | issue = 5 | pages = 607–609 | date = May 2016 | doi = 10.1177/1934578X1601100512 | pmid = 27319129 | pmc = 5345962 }} In the U.S., vinpocetine supplements are marketed as sports supplements, brain enhancers, and weight loss supplements.

A 2015 analysis of 23 brands of vinpocetine dietary supplements sold at GNC and Vitamin Shoppe retail stores reported widespread labeling errors. Only 6 of the 23 supplement labels (26%) provided consumers with accurate dosages of vinpocetine (ranging from 0.3 to 32 mg per recommended daily serving), while 6 of 23 (26%) contained no vinpocetine at all, despite their labels claiming that the ingredient was in them. In total, 9 of the 23 products tested were mislabeled, and 17 of 23 (74%) did not provide any information on the quantity of vinpocetine.

In response to the study, then-senator Claire McCaskill, while at the time serving as the top Democrat on the Senate Special Committee on Aging, urged the FDA to suspend sales of vinpocetine supplements and asked 10 retailers to voluntarily stop selling vinpocetine products. McCaskill stated: "The way we regulate these supplements isn’t working—and it’s putting the lives and well-being of consumers at risk. We’ve seen products with false labels, tainted ingredients, wildly illegal claims, and, now, products containing synthesized ingredients that are classified as prescription drugs in other countries."{{cite journal | vauthors = Erickson BE |title=Vinpocetine: drug or dietary supplement? |journal=Chemical & Engineering News |date=October 31, 2016 |volume=94 |issue=43 |pages=16–17 |url=https://cen.acs.org/content/cen/articles/94/i43/Vinpocetine-drug-dietary-supplement.html |access-date=December 28, 2018 |issn=0009-2347}}

Procera AVH is a dietary supplement containing undisclosed amounts of vinpocetine in combination with huperzine A and acetyl-l-carnitine.{{cite news | vauthors = McGrory K |title=Tampa diet supplement firm pays $1.4 million settlement over 'brain power' pill claims |url=https://www.tampabay.com/news/health/tampa-distributor-related-companies-face-14-million-penalty-for-brain/2236830 |access-date=January 1, 2019 |newspaper=Tampa Bay Times |date=July 9, 2015}}{{cite web | vauthors = Hall H |title=Procera AVH: A Pill to Restore Memory |url=https://sciencebasedmedicine.org/procera-avh-a-pill-to-restore-memory/ |website=Science Based Medicine |access-date=January 1, 2019 |date=September 18, 2012}} In 2012, manufacturer Brain Research Labs (BRL) agreed to pay $500,000 to settle a class action lawsuit which alleged that the company had falsely marketed Procera AVH as capable of improving brain function, in violation of the Consumer Fraud Act.{{cite news | vauthors = Almada B |title=False claims for brain supplement draw $152 million penalty from FTC |url=https://www.ocregister.com/2015/07/06/false-claims-for-brain-supplement-draw-152-million-penalty-from-ftc/ |access-date=January 1, 2019 |newspaper=Orange County Register |date=July 6, 2015}}

In July 2015, the U.S. Federal Trade Commission (FTC) ruled that marketing claims for Procera AVH, which promoted the product as a “solution” to memory loss and cognitive decline, were false, misleading, unsubstantiated, and in violation of the FTC Act.{{cite web |title=Supplement Marketers Will Relinquish $1.4 Million to Settle FTC Deceptive Advertising Charges |newspaper=Federal Trade Commission |url=https://www.ftc.gov/news-events/press-releases/2015/07/supplement-marketers-will-relinquish-14-million-settle-ftc |publisher=U.S. Federal Trade Commission |access-date=January 1, 2019 |date=July 8, 2015}}{{cite magazine |title=Procera AVH Marketers Can Forget About Claiming to Reverse Memory Loss |date=July 30, 2015 |url=https://www.natlawreview.com/article/procera-avh-marketers-can-forget-about-claiming-to-reverse-memory-loss |access-date=1 January 2019 |magazine=National Law Review}}{{cite web | vauthors = Myers S |title=Memory Supplement Marketers Settle FTC Case for $150M |url=https://www.naturalproductsinsider.com/claims/memory-supplement-marketers-settle-ftc-case-150m |website= Natural Products Insider |access-date=1 January 2019 |date=July 8, 2015}} BRL and its affiliated companies Brain Power Partners, Brain Power Founders, and MedHealth Direct (all based in Laguna Beach, California) were fined $91 million. KeyView Labs, the Tampa, Florida-based company that purchased BRL in 2012, was fined $61 million. Also named in the FTC complaint were George Reynolds (aka Josh Reynolds), founder and chief science officer of BRL, and John Arnold, the sole officer and employee of MedHealth. The FTC complaint charged Reynolds with making deceptive expert endorsements for Procera AVH. The defendants in the case ultimately agreed to pay $1.4 million to settle the allegations of deceptive advertising brought by the FTC and California law enforcement officials. In addition, a permanent injunction barred the defendants from making similar deceptive claims about Procera AVH in the future and from misrepresenting the existence, results, or conclusions of any scientific study.

{{Reflist}}

{{Phosphodiesterase inhibitors}}

Category:Nootropics

Category:PDE1 inhibitors

Category:Vasodilators

Category:Ethyl esters

Category:Vinca alkaloids