Vinpocetine Products



Vinpocetine
 

Vinpocetine Introduction

Vinpocetine (vinpocetine-ethyl apovincaminate) is a derivative of a compound found in the leaves of the plant, Lesser Periwinkle (Vinca minor). [1] It is a synthetic ethyl ester of apovincamine, which is a vinca alkaloid of the plant. Vinpocetine was discovered in the late 1960s and was introduced into clinical practice as cavinton (containing vinpocetine as the active ingredient) in Hungary for the treatment of cerebrovascular disorders and related symptoms.

A review of the mechanisms of action of vinpocetine summarized the five main pharmacological and biochemical actions: [1-5]

  • 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 and improvement of rheological properties of the blood
  • inhibition of aggregation of thrombocytes

In addition, neuroprotective effects via inhibition of operation of voltage dependent neuronal Na(+)-channels, indirect inhibition of some molecular cascades initiated by the rise of intracellular Ca(2+)-levels, and inhibition of adenosine reuptake have also been demonstrated. There also appears to be involvement of a prostaglandin-mediated mechanism which may be important in gastric mucosal damage. [3] Furthermore, vinpocetine exerts anti-oxidant effects through hydroxyl radical scavenging. [4]

Vinpocetine Food Sources

Vinpocetine is a synthetic compound; therefore, no food sources exist.

Vinpocetine Uses

Vinpocetine has been studied for a range of health conditions. However, the main focus of vinpocetine therapy has been in addressing cerebral vascular disorders. Vinpocetine was examined for treatment of acute ischemic stroke. A pilot study of thirty consecutive patients with a computed tomography verified diagnosis of acute ischemic stroke, who could receive drug treatment within 72 hours of stroke onset, was conducted. [5] Patients were randomly assigned to either low-molecular weight dextran alone or in combination with vinpocetine. The results showed that The National Institute of Health (NIH–NINDS) Stroke Scale score was significantly improved in the vinpocetine group at 3 months of follow-up; no significant adverse effects were observed.

Another study examined the effect of vinpocetine on cerebral blood flow in 43 patients with ischemic stroke. [6] Subjects were enrolled in a randomized double-blind, placebo-controlled study and given either a single-dose intravenous infusion of 20 milligrams (mg) of vinpocetine or placebo. The results of the study showed that vinpocetine increased cerebral perfusion and parenchymal oxygen extraction. As well, research has shown that vinpocetine exerts a cytoprotective effects induced by hypoxia and prevents apoptosis in astrocytes. [7]

Vinpocetine is also useful in chronic cerebrovascular disease. A study of patients with chronic ischemic cerebrovascular disease given either low dose (30mg per day) or high dose (70mg per day) of vinpocetine for 7 days was conducted. [8] The high dose of vinpocetine significantly decreased various rheological parameters including hematocrit, whole blood and plasma viscosity, and red blood cell aggregation, indicating this treatment may be quite beneficial. Another study showed that a two week course of intravenous vinpocetine can contribute effectively to the redistribution of cerebral blood flow in chronic ischemic stroke patients. [9] A review published in 2003 concluded that vinpocetine may be of benefit for the treatment in early stage of cerebrovascular disease, termed asymptomatic ischemic cerebrovascular disorders, and may provide a new therapeutic approach to prophylactic neuroprotection in patients at high risk of ischemic stroke. [10]

Patients with dementia may also benefit from vinpocetine therapy. In a placebo-controlled, randomized double-blind, multicentre trial, subjects with mild to moderate organic psychosyndromes including primary dementia received either 10mg of vinpocetine three times daily, 20mg of vinpocetine three times daily, or placebo for 16 days. [11] The results showed that clinical global improvement, cognitive performance, and severity of illness were all improved with both doses of vinpocetine in comparison to placebo.

A Cochrane Review published in 2003 examined vinpocetine for cognitive impairment and dementia. [12] Only trials that were double-blind, randomized, and in which treatment with vinpocetine was administered for more than a day and compared to control in patients with vascular dementia, Alzheimer’s dementia, or mixed Alzheimer’s and vascular dementia and other dementias were included in the review. The reviewers concluded that the results show benefit associated with treatment with vinpocetine 30mg per day and 60mg per day when compared with placebo.

Vinpocetine has also been studied successfully for urge incontinence and low compliance bladder. An initial study revealed that 11 out of 19 patients (57.9%) showed improved clinical symptoms and/or urodynamic parameters. [13] This activity appears to be mediated by inhibition of intracellular phosphodiesterase (PDE)-1 isoenzyme which regulates human detrusor smooth muscle contractility.

An interesting application for vinpocetine is for the removal of intractable tumoral calcinosis in haemodialysis patients with renal failure. In a small study of hemodialysis patients with X-ray evidence of tumoral calcinosis, subjects were given 15mg per day of vinpocetine for 3 - 12 months. [14] The results showed that calcinosis was completely eliminated in all eight cases.

Vinpocetine may enhance memory through exerting a localized effect on the serial comparison stage of the reaction process. [15] Other conditions for which vinpocetine may be beneficial include gastric ulcers, epilepsy, tinnitus, and Meniere’s disease. [3, 16-18]

Vinpocetine Dosages

Most studies employ an oral dose of 10 milligrams of vinpocetine two to three times daily. Vinpocetine is also administered intravenously using a similar dosage. Transdermal delivery systems are under investigation as microemulsions, due to the low water soubility of vinpocetine. [19]

Vinpocetine Deficiencies and Toxicities

Vinpocetine Deficiencies

Vinpocetine is a derivative of a naturally occurring substance which has many benefits throughout the body, most notably in the central nervous system. Because it is not an essential nutrient, deficiency syndromes have not been documented.

Vinpocetine Toxicities

Vinpocetine is generally considered a safe therapeutic substance when taken in recommended doses. The majority of studies reveal the absence of adverse effects or only mild side effects in patients taking vinpocetine. A Cochrane review published in 2003 reported that available data did not demonstrate many problems of adverse effects. [12] Side effects that may occur include rashes, flushing and minor gastrointestinal complaints. [20]

Patients taking anti-coagulant medications should not use vinpocetine because it also has anti-platelet activity.[1]

References

1. Anonymous. Vinpocetine. Alt Med Rev 2002;7(3):240-243.

2. Kiss B, Karpati E. [Mechanism of action of vinpocetine] Acta Pharm Hung. 1996;66(5):213-24.

3. Nosalova V, Machova J, Babulova A. Protective action of vinpocetine against experimentally induced gastric damage in rats. Arzneimittelforschung. 1993;43(9):981-5.

4. Stolc S. Indole derivatives as neuroprotectants. Life Sci 1999;65:1943-1950.

5. Feigin VL et al. Vinpocetine treatment in acute ischaemic stroke: a pilot single-blind randomized clinical trial. Eur J Neurol. 2001;8(1):81-5.

6. Bonoczk 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;15(1-2):85-91.

7. Gabryel B et al. Piracetam and vinpocetine exert cytoprotective activity and prevent apoptosis of astrocytes in vitro in hypoxia and reoxygenation. Neurotoxicology. 2002;23(1):19-31

8. Szapary L et al. [Effect of vinpocetin on the hemorheologic parameters in patients with chronic cerebrovascular disease] Orv Hetil. 2003;144(20):973-8.

9. Szilagyi G et al. 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;229-230(1):275-84.

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

11. 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.

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

13. Truss MC et al. 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;18(6):439-43.

14. Ueyoshi A, Ota K. Ueyoshi A, Ota K. Clinical appraisal of vinpocetine for the removal of intractable tumoral calcinosis in haemodialysis patients with renal failure. J Int Med Res. 1992;20(5):435-43.

15. Subhan Z, Hindmarch I. Psychopharmacological effects of vinpocetine in normal healthy volunteers. Eur J Clin Pharmacol. 1985;28(5):567-71.

16. Nekrassov V, Sitges M. Vinpocetine inhibits the epileptic cortical activity and auditory alterations induced by pentylenetetrazole in the guinea pig in vivo. Epilepsy Res. 2004;60(1):63-71.

17. Konopka W et al. Treatment of acoustic trauma. Otolaryngol Pol 1997; 51:281S-284S.

18. Ribari O et al. Ethyl apovincaminateint eh treatment of sensorineural impairment of hearing.

19. Hua L et al. Preparation, evaluation, and NMR characterization of vinpocetine microemulsion for transdermal delivery. Drug Dev Ind Pharm. 2004;30(6):657-66.

20. Nagy Z et al. Metaanalysis of cavinton. Praxis 1998;7:63-68.