Friday, April 4, 2008

V is for brain Viagra....REALLY?



Since I spent the last post questioning the validity of an herbal supplement, I wanted to balance my blog by sharing another herb with some evidence-based potential.

One of my friends is very into nutrition...and his questions for me challenge me to keep up-to-date and be cutting edge. One day he wrote to ask if I'd ever heard of an herb called "vinpocetine." He'd heard it was like Viagra for the brain, in that it increased brain blood flow and circulation of vital nutrients, while making it easier for the brain to remove toxic waste products.

I rolled my eyes as I read his email, thinking I'd heard it all. But, curious, I went to PubMed. Sure enough, there were 23 pages of titles about vinpocetine and the hopeful actions it seemed to have on the brain and nervous system; the first one was published way back in 1979!

If you happen to be reading this, Michael, I greatly appreciate your voracious curiosity and your generosity in sharing things you learn with me. You get credit for this "find" and I want to thank you for giving me a great opportunity to help a lot of people who may benefit from this information. :)

Vinpocetine, also known as Caviton, is a derivative of a plant in the periwinkle family. In the brain, some of the effects of vinpocetine appear to be:
(1) protecting the brain against ischemic cell damage (the kind of damage that occurs when there is insufficient oxygen). Improved glucose utilization and blood flow in damaged areas has been shown when vinpocetine was administered even a week or two after the ischemic damage occurred;
(2) acting as a vasodilator (as my friend suggested, improves blood flow), which has been shown to be beneficial in treating vascular dementia and stroke;
(3) reducing seizure activity and potentially helping to manage epilepsy;
(4) improving the flexibility of red blood cells, making it easier for them to move through constricted spaces and therefore improving blood flow;
(5) preventing death to neurons that have been overstimulated by excitatory substances such as glutamate;
(6) protecting cells from the damage created by amyloid beta peptides, making it a potential treatment for Alzheimer's disease;
(7) improving the function of norepinephrine, a neurotransmitter important to memory function;
(8) enhancing the neuroprotective activity of other compounds such as adenosine;
(9) improving the uptake of glucose through the blood-brain barrier (glucose is the brain's primary energy source);
(10)acting as an antioxidant, protecting neurons from stress-related damage; and
(11) protecting astrocytes, another type of brain cell that supports the blood-brain barrier, nourishes other brain cells, and repairs brain tissue.

Vinpocetine appears to be particularly effective in the hippocampus, the brain's factual memory center. Learning and memory have actually been shown to improve in individuals who have been given vinpocetine.

Vinpocetine may also promote health outside of the brain and nervous system. It has been shown to lessen menopausal symptoms, prevent the development of gastric lesions created on exposure to substances such as alcohol, and help with urinary incontinence. It reduces gallbladder motility and, potentially, gallstone formation. It has been used to treat tumoral calcinosis, (calcium-based masses). And it shows potential in controlling pain.

One small nutritional note: vinpocetine appears to be better absorbed when taken after a meal than it does when taken on an empty stomach.

Many of the articles about vinpocetine are in Russian, Chinese, and Hungarian. On the chance that anyone reading this may wish to read some of the references, I only cited studies written in English. But if you go to Pub Med (http://www.ncbi.nlm.nih.gov/sites/entrez)and key in "vinpocetine", you can see for yourself just how much this herb has been studied.

I will note, there are also studies refuting the effectiveness of vinpocetine, but the results seem to vary depending on study design. My guess is that, just like with medications, different people will respond to different treatments in a variety of ways. The one thing I DID like about what I found, was that there were no studies suggesting any dangers to using vinpocetine. If it can't hurt...and it might help...why not try it?

Abdel Salam OM. Vinpocetine and piracetam exert antinociceptive effect in visceral pain model in mice. Pharmacol Rep. 2006 Sep-Oct;58(5):680-91.

Araki T, Kogure K, Nishioka K. Comparative neuroprotective effects of pentobarbital, vinpocetine, flunarizine and ifenprodil on ischemic neuronal damage in the gerbil hippocampus. Res Exp Med (Berl). 1990;190(1):19-23.

Bereczki D, Fekete I. Vinpocetine for acute ischaemic stroke. Cochrane Database Syst Rev. 2008 Jan 23;(1):CD000480.

Bönöczk P, Gulyás B, Adam-Vizi V, Nemes A, Kárpáti E, Kiss B, Kapás M, Szántay C, Koncz I, Zelles T, Vas A. Role of sodium channel inhibition in neuroprotection: effect of vinpocetine. Brain Res Bull. 2000 Oct;53(3):245-54.

Bönöczk P, Panczel G, Nagy Z. Vinpocetine increases cerebral blood flow and oxygenation in stroke patients: a near infrared spectroscopy and transcranial Doppler study. Eur J Ultrasound. 2002 Jun;15(1-2):85-91.

Erdö SL, Cai NS, Wolff JR, Kiss B. Vinpocetin protects against excitotoxic cell death in primary cultures of rat cerebral cortex. Eur J Pharmacol. 1990 Oct 23;187(3):551-3.

Feigin VL, Doronin BM, Popova TF, Gribatcheva EV, Tchervov DV. Vinpocetine treatment in acute ischaemic stroke: a pilot single-blind randomized clinical trial. Eur J Neurol. 2001 Jan;8(1):81-5.

Gaál L, Molnár P. Effect of vinpocetine on noradrenergic neurons in rat locus coeruleus. Eur J Pharmacol. 1990 Oct 23;187(3):537-9.

Gabryel B, Adamek M, Pudełko A, Małecki A, Trzeciak HI. Piracetam and vinpocetine exert cytoprotective activity and prevent apoptosis of astrocytes in vitro in hypoxia and reoxygenation. Neurotoxicology. 2002 May;23(1):19-31.

Hadjiev D. Asymptomatic ischemic cerebrovascular disorders and neuroprotection with vinpocetine.Ideggyogy Sz. 2003 May 20;56(5-6):166-72.

Hayakawa M. Comparative efficacy of vinpocetine, pentoxifylline and nicergoline on red blood cell deformability. Arzneimittelforschung. 1992 Feb;42(2):108-10.

Hayakawa M. Effect of vinpocetine on red blood cell deformability in vivo measured by a new centrifugation method. Arzneimittelforschung. 1992 Mar;42(3):281-3.

Hayakawa M. Effect of vinpocetine on red blood cell deformability in stroke patients. Arzneimittelforschung. 1992 Apr;42(4):425-7.

Hindmarch I, Fuchs HH, Erzigkeit H. Efficacy and tolerance of vinpocetine in ambulant patients suffering from mild to moderate organic psychosyndromes. Int Clin Psychopharmacol. 1991 Spring;6(1):31-43.

Horvath B, Marton Z, Halmosi R, Alexy T, Szapary L, Vekasi J, Biro Z, Habon T, Kesmarky G, Toth K. In vitro antioxidant properties of pentoxifylline, piracetam, and vinpocetine. Clin Neuropharmacol. 2002 Jan-Feb;25(1):37-42.

Ishihara K, Katsuki H, Sugimura M, Satoh M. Idebenone and vinpocetine augment long-term potentiation in hippocampal slices in the guinea pig. Neuropharmacology. 1989 Jun;28(6):569-73.

Kaneda T, Watanabe A, Shimizu K, Urakawa N, Nakajyo S. Effects of various selective phosphodiesterase inhibitors on carbachol-induced contraction and cyclic nucleotide contents in the guinea pig gall bladder. J Vet Med Sci. 2005 Jul;67(7):659-65.

Kemény V, Molnár S, Andrejkovics M, Makai A, Csiba L. Acute and chronic effects of vinpocetine on cerebral hemodynamics and neuropsychological performance in multi-infarct patients. J Clin Pharmacol. 2005 Sep;45(9):1048-54.

Kidd PM. A review of nutrients and botanicals in the integrative management of cognitive dysfunction. Altern Med Rev. 1999 Jun;4(3):144-61.

Kiss E. Adjuvant effect of cavinton in the treatment of climacteric symptoms. Ther Hung. 1990;38(4):170-3.

Krieglstein J. Vinpocetine increases the neuroprotective effect of adenosine in vitro. Eur J Pharmacol. 1991 Nov 19;205(1):7-10.

Lakics V, Sebestyén MG, Erdö SL. Vinpocetine is a highly potent neuroprotectant against veratridine-induced cell death in primary cultures of rat cerebral cortex. Neurosci Lett. 1995 Feb 9;185(2):127-30.

Lakics V, Sebestyén MG, Erdö SL. Cerebral effects of a single dose of intravenous vinpocetine in chronic stroke patients: a PET study.Szakáll S, Boros I, Balkay L, Emri M, Fekete I, Kerényi L, Lehel S, Márián T, Molnár T, Varga J, Galuska L, Trón L, Bereczki D, Csiba L, Gulyás B. J Neuroimaging. 1998 Oct;8(4):197-204.

Lindaman BA, Hinkhouse MM, Conklin JL, Cullen JJ. The effect of phosphodiesterase inhibition on gallbladder motility in vitro. J Surg Res. 2002 Jun 15;105(2):102-8.

Lohmann A, Dingler E, Sommer W, Schaffler K, Wober W, Schmidt W. Bioavailability of vinpocetine and interference of the time of application with food intake. Arzneimittelforschung. 1992 Jul;42(7):914-7.

McDaniel MA, Maier SF, Einstein GO. "Brain-specific" nutrients: a memory cure? Nutrition. 2003 Nov-Dec;19(11-12):957-75. Comment in: Nutrition. 2003 Nov-Dec;19(11-12):955-6.

Molnár P, Erdö SL. Vinpocetine is as potent as phenytoin to block voltage-gated Na+ channels in rat cortical neurons. Eur J Pharmacol. 1995 Feb 6;273(3):303-6.

Nosálová V, Machová J, Babulová A. Protective action of vinpocetine against experimentally induced gastric damage in rats. Arzneimittelforschung. 1993 Sep;43(9):981-5.

Pereira C, Agostinho P, Oliveira CR. Vinpocetine attenuates the metabolic dysfunction induced by amyloid beta-peptides in PC12 cells. Free Radic Res. 2000 Nov;33(5):497-506. Erratum in: Free Radic Res 2001 Oct;35(4):following 446.

Rischke R, Krieglstein J. Effects of vinpocetine on local cerebral blood flow and glucose utilization seven days after forebrain ischemia in the rat. Pharmacology. 1990;41(3):153-60.

Rischke R, Krieglstein J. Protective effect of vinpocetine against brain damage caused by ischemia. Jpn J Pharmacol. 1991 Jul;56(3):349-56.

Santos MS, Duarte AI, Moreira PI, Oliveira CR. Synaptosomal response to oxidative stress: effect of vinpocetine. Free Radic Res. 2000 Jan;32(1):57-66.

Sauer D, Rischke R, Beck T, Rossberg C, Mennel HD, Bielenberg GW, Krieglstein J. Vinpocetine prevents ischemic cell damage in rat hippocampus. Life Sci. 1988;43(21):1733-9.

Schmidt J. Comparative studies on the anticonvulsant effectiveness of nootropic drugs in kindled rats. Biomed Biochim Acta. 1990;49(5):413-9.

Seyahi A, Atalar AC, Ergin HK. Tumoral calcinosis: Clinical and biochemical aspects of a patient treated with vinpocetine. Eur J Intern Med. 2006 Oct;17(6):436-8.

Sitges M, Nekrassov V. Vinpocetine prevents 4-aminopyridine-induced changes in the EEG, the auditory brainstem responses and hearing. Clin Neurophysiol. 2004 Dec;115(12):2711-7.

Sitges M, Chiu LM, Guarneros A, Nekrassov V. Effects of carbamazepine, phenytoin, lamotrigine, oxcarbazepine, topiramate and vinpocetine on Na+ channel-mediated release of [3H]glutamate in hippocampal nerve endings. Neuropharmacology. 2007 Feb;52(2):598-605. Epub 2006 Oct 30.

Szatmari SZ, Whitehouse PJ. Vinpocetine for cognitive impairment and dementia. Cochrane Database Syst Rev. 2003;(1):CD003119.

Szilágyi G, Nagy Z, Balkay L, Boros I, Emri M, Lehel S, Márián T, Molnár T, Szakáll S, Trón L, Bereczki D, Csiba L, Fekete I, Kerényi L, Galuska L, Varga J, Bönöczk P, Vas A, Gulyás B. Effects of vinpocetine on the redistribution of cerebral blood flow and glucose metabolism in chronic ischemic stroke patients: a PET study. J Neurol Sci. 2005 Mar 15;229-230:275-84. Epub 2005 Jan 8.

Tohgi H, Sasaki K, Chiba K, Nozaki Y. Effect of vinpocetine on oxygen release of hemoglobin and erythrocyte organic polyphosphate concentrations in patients with vascular dementia of the Binswanger type. Arzneimittelforschung. 1990 Jun;40(6):640-3.

Trejo F, Nekrassov V, Sitges M. Characterization of vinpocetine effects on DA and DOPAC release in striatal isolated nerve endings. Brain Res. 2001 Aug 3;909(1-2):59-67.

Truss MC, Stief CG, Uckert S, Becker AJ, Schultheiss D, Machtens S, Jonas U. Initial clinical experience with the selective phosphodiesterase-I isoenzyme inhibitor vinpocetine in the treatment of urge incontinence and low compliance bladder. World J Urol. 2000 Dec;18(6):439-43.

Truss MC, Stief CG, Uckert S, Becker AJ, Wefer J, Schultheiss D, Jonas U. Phosphodiesterase 1 inhibition in the treatment of lower urinary tract dysfunction: from bench to bedside. World J Urol. 2001 Nov;19(5):344-50.

Vas A, Gulyás B, Szabó Z, Bönöczk P, Csiba L, Kiss B, Kárpáti E, Pánczél G, Nagy Z. Clinical and non-clinical investigations using positron emission tomography, near infrared spectroscopy and transcranial Doppler methods on the neuroprotective drug vinpocetine: a summary of evidences. J Neurol Sci. 2002 Nov 15;203-204:259-62.

2 comments:

bobby said...

that's a farce, telling people that vinpocetine is good for the brain and that there are no possible dangers behind taking it. it has been listed on a druggie site called erowid. look at any website in fact there are a few which state that the following is true of vinpocetine:

Vinpocetine is also a phosphodiesterase (PDE) type-1 inhibitor,[9] (with an IC50 of approximately 10-5 M.) leading to increases in intracellular levels of cyclic guanosine 3'5'-monophosphate (cGMP), an action that has been attributed to the vasorelaxant effects of vinpocetine on cerebral smooth muscle tissue.[10][11]

Increases in neuronal levels of DOPAC, a metabolic breakdown product of dopamine, have been shown to occur in striatal isolated nerve endings as a result of exposure to vinpocetine.[12] Such an effect is consistent with the biogenic pharmacology of reserpine, a structural relative of vinpocetine, which depletes catecholamine levels and may cause depression as a side-effect of the cardiovascular and anti-psychotic effects.[13]

Side-effects

Vinpocetine has been implicated in one case to induce agranulocytosis,[14] a condition in which granulocytyes - an important type of white blood cell, are markedly decreased. Some people have anecdotally noted that their continued use of vinpocetine reduces immune function. Commission E warned that vinpocetine reduced immune function and could cause apoptosis in the long term. [15]

Dosage

It is recommended that first-time users ingest only 2-5 mg of vinpocetine with meals to make sure they are not hypersensitive to it. Users may then increase the dosage to 10-40 mg a day (which may, although very rarely, cause some light side-effects).

hormonewoman said...

Bobby,

Thank you for your comments. I'm in the middle of Christmas shopping and have made a note to look at your information more thoroughly when I return from my holiday trip. I can tell you, when I originally posted this information I looked at every reference I found in the National Library of Medicine database, and what I found there is what I based my conclusion on. I will definitely post a followup, and it will be a separate post, to be sure it ends up in a place where people are more likely to find it.

Thanks for taking the time to comment!

Monika