Articles

Vinpocetine

Plant Part Used

Isolated constituent

Active Constituents

Not applicable.

[span class=alert]This section is a list of chemical entities identified in this dietary supplement to possess pharmacological activity. This list does not imply that other, yet unidentified, constituents do not influence the pharmacological activity of this dietary supplement nor does it imply that any one constituent possesses greater influence on the overall pharmacological effect of this dietary supplement.[/span]

Introduction

The lesser periwinkle (Vinca minor) is a native of many parts of Europe, growing in woods and thickets. Isolated chemical constituents have been used in cancer therapy, as the chemotherapeutic drugs vincristine and vinblastine. Vinpocetine is chemically related to, and derived from vincamine, an alkaloid found in the periwinkle plant. Vinpocetine was made available under the trade name Cavinton in 1978 and has since been used widely in Japan, Hungary, Germany, Poland, and Russia for the treatment of cerebrovascular-related pathologies.(1),(2),(3),(4)

Interactions and Depletions

Interactions

Dosage Info

Dosage Range

5-20mg, 3 times a day.

Note – Intravenous (IV) vinpocetine is also available in some Countries

Most Common Dosage

10mg, 3 times a day.

Standardization

[span class=doc]Standardization represents the complete body of information and controls that serve to enhance the batch to batch consistency of a botanical product, including but not limited to the presence of a marker compound at a defined level or within a defined range.[/span]

Standardization is not applicable for this dietary supplement.

Uses

Frequently Reported Uses

  • Cognitive Enhancement
  • Memory
  • Stroke
  • Neuroprotection

Other Reported Uses

  • Antioxidant
  • Tinnitus
  • Hearing loss
  • Anticonvulsant

Toxicities & Precautions

General

Vinpocetine is reported safe in recommended dosages.

Health Conditions

Based on pharmacology, use with caution in individuals with bleeding disorders.

Side Effects

Transient side effects may include skin eruptions, flushing, and sometimes gastrointestinal upset.

Pharmacology

Neuro- and Cerebral protection

Experiments with vinpocetine have indicated the main pharmacological and biochemical actions include:(5) selective enhancement of the brain circulation and oxygen utilization without significant alteration in parameters of systemic circulation; increased tolerance of the brain toward hypoxia and ischemia; anticonvulsant activity; inhibitory effect on phosphodiesterase (PDE) enzyme; endothelial vasodilation; and improvement of rheological properties of the blood and inhibition of aggregation of thrombocytes.(31),(32)

Evidence has been obtained that the neuroprotective action of vinpocetine is related to the inhibition of operation of voltage dependent neuronal Na+-channels, indirect inhibition of some molecular cascades initiated by the rise of intracellular Ca2+-levels, and to a lesser extent, inhibition of adenosine reuptake.(6) Vinpocetine has been reported to be a selective inhibitor of Ca2+-calmodulin dependent cGMP-PDE.(7) It is assumed that this inhibition enhances intracellular GMP levels in the vascular smooth muscle leading to reduced resistance of cerebral vessels and increase of cerebral flow. This effect might also beneficially contribute to the neuroprotective action.(8),(9),(10) The antioxidant effect of vinpocetine may contribute to the protective role in reducing neuronal damage in pathological situations.(11),(33)

Several double-blind trials conducted with patients suffering from mild-to-moderate vascular dementia reported vinpocetine benefited memory, learning, and global clinical measures of cognitive performance.(12),(13),(14),(34) Speech and language, but not mood or coordination, also were reportedly improved by vinpocetine.(15) A study review in 2003 and a Cochrane Database System Review in 2008 both found that the evidence of vinpocetine use in dementia was inconclusive and larger studies need to be performed.(25),(35) In the only double-blind trial conducted to date assessing vinpocetine's effect against Alzheimer's Disease, no significant benefits were reported.(16)

Vinpocetine may have clinical utility in the management of stroke, and has been reported to improve the quality of life in chronic cerebrovascular patients.(1),(36) Vinpocetine is a highly potent vasodilator, acting by direct relaxation of the vascular smooth muscle, and has been reported to enhance cerebral blood flow in patients with cerebrovascular disorders.(17) Patients from this population who also manifest increased blood viscosity are at greater risk for thrombotic complications. In one such group of patients, vinpocetine had a viscosity-lowering effect on the blood and plasma.(18) Vinpocetine is reported to decrease platelet and red cell aggregation, and to increase red cell membrane flexibility in stroke patients, as well as in healthy subjects.(19),(20),(21) Any or all of these mechanisms could be involved in vinpocetine's capacity to lower the viscosity of the blood in vivo.

A reduction in red blood cell deformability was reported with the use of vinpocetine.(21) Red blood cell deformity is a contributory factor in stroke disease, and it has been postulated that improvement of red blood cell rigidification may improve stroke rate and survival, even being more effective than pentoxifylline in this regard.(24)

Vinpocetine reportedly has anticonvulsant action, possibly linked to its neuronal protective capacity and/or its modulation of several chemical transmitter systems.(26),(27) In these respects, vinpocetine resembles adenosine, thought to be a major endogenous anticonvulsant and cerebral protectant. Vinpocetine happens to be an effective adenosine re-uptake inhibitor. It reportedly increases cerebral metabolism and raises ATP levels in nerve cells, perhaps also raising neuronal excitability more directly by modulating cellular enzymatic control systems.(4),(28)

Other Uses

Vinpocetine appears to be an effective scavenger of tumoral calcinosis in hemodialysis patients with renal failure without any side effects during treatment.(29) Another study of interest found that vinpocetine, a Na+ channel antagonist, prevented ototoxicity induced the aminoglycoside amikacin in laboratory animals.(30) Several human studies report improvement in loss of hearing when using vinpocetine.(37)

Vinpocetine may be beneficial in treating symptoms associated with tinnitus, due to its positive effects on microvasculature.(22) The effects of vinpocetine on the cerebral glucose metabolism of chronic stroke patients have been studied with positron emission tomography (PET).(23) Results indicated that a single-dose vinpocetine treatment, although not significantly affecting the regional or global metabolic rates of glucose, improved the transport of glucose (both uptake and release) through the blood-brain barrier in the whole brain, the entire contralateral hemisphere, and in the brain tissue around the infarct area of the symptomatic hemisphere.

References

  1. View Abstract: Burtsev EM, et al. 10-year experience with using Cavinton in cerebrovascular disorders. Zh Nevropatol Psikhiatr Im S S Korsakova. 1992;92(1):56-60.
  2. View Abstract: Domzal T, et al. Cavinton in the treatment of ischemic cerebral stroke. Clinical and computerized-tomographic evaluation. Neurol Neurochir Pol. May1986;20(3):234-40.
  3. Kovacs L. Cavinton in the treatment of acute stroke. Ther Hung. 1985;33(1):50-7.
  4. View Abstract: Kakihana M, et al. Protective effect of vinpocetine on experimental brain ischemia. Nippon Yakurigaku Zasshi. Sep1982;80(3):225-9.
  5. View Abstract: Kiss B, et al. Mechanism of action of vinpocetine. Acta Pharm Hung. Sep1996;66(5):213-24.
  6. View Abstract: Sitges M, et al. Vinpocetine selectively inhibits neurotransmitter release triggered by sodium channel activation. Neurochem Res. Dec1999;24(12):1585-91.
  7. View Abstract: Ishchenko MM, et al. Effect of cavinton and sulfocamphocain on systemic and cerebral hemodynamics in patients with early forms of cerebrovascular diseases. Zh Nevropatol Psikhiatr Im S S Korsakova. 1987;87(8):1160-4.
  8. View Abstract: Tretter L, et al. The neuroprotective drug vinpocetine prevents veratridine-induced [Na+]i and [Ca2+]i rise in synaptosomes. Neuroreport. Jun1998;9(8):1849-53.
  9. View Abstract: Rischke R, et al. Protective effect of vinpocetine against brain damage caused by ischemia. Jpn J Pharmacol. Jul1991;56(3):349-56.
  10. View Abstract: Bonoczk P, Gulyas B, Adam-Vizi V, et al. Role of Sodium Channel Inhibition in Neuroprotection: Effect of Vinpocetine. Brain Res Bull. Oct2000;53(3):245-54.
  11. View Abstract: Santos MS, et al. Synaptosomal response to oxidative stress: effect of vinpocetine. Free Radic Res. Jan2000;32(1):57-66.
  12. View Abstract: Balestreri R, Fontana L, Astengo F. A double-blind placebo controlled evaluation of the safety and efficacy of Vinpocetine in the treatment of patients with chronic vascular senile cerebral dysfunction. J Am Geriatr Soc. 1987;35:425-430.
  13. View Abstract: Hindmarch I, et al. Efficacy and tolerance of vinpocetine in ambulant patients suffering from mild to moderate organic psychosyndromes. Int Clin Psychopharmacol. 1991;6(1):31-43.
  14. View Abstract: Nicholson CD. Pharmacology of nootropics and metabolically active compounds in relation to their use in dementia. Psychopharmacology. (Berl). 1990;101:147-159.
  15. View Abstract: Kidd PM. A review of nutrients and botanicals in the integrative management of cognitive dysfunction. Altern Med Rev. Jun1999;4(3):144-61.
  16. View Abstract: Thal LJ, et al. The safety and lack of efficacy of vinpocetine in Alzheimer's disease. J Am Geriatr Soc. Jun1989;37(6):515-20.
  17. Tamaki N, et al. The effect of Vinpocetine on cerebral blood flow in patients with cerebrovascular disorders. Ther Hung. 1985;33:13-21.
  18. Osawa M, Maruyama S. Effects of TCV-3B (Vinpocetine) on blood viscosity in ischemic cerebrovascular diseases. Ther Hung. 1985;33:7-12.
  19. View Abstract: Bayer R, Plewa S, Borcescu E, et al. Filterability of human erythrocytes - drug induced prevention of aging in vitro. Arzneimittelforschung. 1988;38:1765-1767.
  20. Kuzuya F. Effects of Vinpocetine on platelet aggregability and erythrocyte deformability. Ther Hung. 1985;33:22-34.
  21. View Abstract: Hayakawa M. Effect of Vinpocetine on red blood cell deformability in stroke patients. Arzneimittelforschung. 1992;42:425-427.
  22. View Abstract: Ribari O, Zelen B, Kollar B. Ethyl apovincaminate in the treatment of sensorineural impairment of hearing. Arzneimittelforschung. 1976;26:1977-1980.
  23. View Abstract: Szakall S, et al. Cerebral effects of a single dose of intravenous vinpocetine in chronic stroke patients: a PET study. J Neuroimaging. Oct1998;8(4):197-204.
  24. View Abstract: Hayakawa M. Comparative efficacy of vinpocetine, pentoxifylline and nicergoline on red blood cell deformability. Arzneimittelforschung. Feb1992;42(2):108-10.
  25. View Abstract: Bereczki D, Fekete I. Vinpocetine for Acute Ischaemic Stroke. Cochrane Database Syst Rev. 2000;(2):CD000480.
  26. View Abstract: Schmidt J. Comparative studies on the anticonvulsant effectiveness of nootropic drugs in kindled rats. Biomed Biochim Acta. 1990;49(5):413-9.
  27. View Abstract: Molnar P, et al. Vinpocetine is as potent as phenytoin to block voltage-gated Na+ channels in rat cortical neurons. Eur J Pharmacol. Feb1995;273(3):303-6.
  28. View Abstract: Tohgi H, et al. Effect of vinpocetine on oxygen release of hemoglobin and erythrocyte organic polyphosphate concentrations in patients with vascular dementia of the Binswanger type. Arzneimittelforschung. Jun1990;40(6):640-3.
  29. View Abstract: Kakihana M, et al. Protective effect of vinpocetine on experimental brain ischemia. Nippon Yakurigaku Zasshi. Sep1982;80(3):225-9.
  30. View Abstract: Ueyoshi A, et al. Clinical appraisal of vinpocetine for the removal of intractable tumoral calcinosis in haemodialysis patients with renal failure. J Int Med Res. Sep1992;20(5):435-43.
  31. View Abstract: Nekrassov V, Sitges M. Vinpocetine Protects from Aminoglycoside Antibiotic-induced Hearing Loss in Guinea Pig In Vivo. Brain Res. Jun2000;868(2):222-9
  32. Feher G, Koltai K, Kesmarky G, Horvath B, Toth K, Komoly S, Szapary L. Effect of parenteral or oral vinpocetine on the hemorheological parameters of patients with chronic cerebrovascular diseases. Phytomedicine. Mar 2009;16(2-3):111-117. Epub 2009 Jan 8.
  33. Vaizova OE, Vengerovskiĭ AI, Alifirova VM. [An effect of vinpocetine (cavinton) on endothelium function in patients with chronic cerebral ischemia]. Zh Nevrol Psikhiatr Im S S Korsakova. 2006;Suppl 16:46-50. Russian.
  34. Deshmukh R, Sharma V, Mehan S, Sharma N, Bedi KL. Amelioration of intracerebroventricular streptozotocin induced cognitive dysfunction and oxidative stress by vinpocetine -- a PDE1 inhibitor. Eur J Pharmacol. 12 Oct 2009;620(1-3):49-56. Epub 2009 Aug 21.
  35. Valikovics A. [Investigation of the effect of vinpocetine on cerebral blood flow and cognitive functions]. Ideggyogy Sz. 30 Jul 2007;60(7-8):301-310. Hungarian.
  36. Bereczki D, Fekete I. Vinpocetine for acute ischaemic stroke. Cochrane Database Syst Rev. 23 Jan 2008;(1):CD000480. Review.
  37. Bagoly E, Fehér G, Szapáry L. [The role of vinpocetine in the treatment of cerebrovascular diseases based in human studies]. Orv Hetil. 22 Jul 2007;148(29):1353-1358. Hungarian.
  38. Afon'kin VIu, Dobretsov KG, Sipkin AV. [The new scheme of cavinton application to the treatment of chronic neurosensory loss of hearing]. Vestn Otorinolaringol. 2009;(6):69-70. Russian.