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News About Vinpocetine

20-September-2008 09:55:58 - Vinpocetine Vinpocetine Systematic IUPAC name 3α,16α-Eburnamenine-14-carboxylic acid ethyl ester Identifiers CAS number 42971-09-5 ATC code N06BX18 PubChem 5673 Chemical data Formula C22H26N2O2 Mol. mass 350.454 g/mol Pharmacokinetic data Bioavailability 56.6 +/- 8.9% Metabolism hepatic Half life 2.54 +/- 0.48 hours Excretion renal Therapeutic considerations Pregnancy cat. not recommended Legal status OTC Routes oral, intravenous Vinpocetine brand names: Cavinton, Intelectol; chemical name: ethyl apovincaminate is a semisynthetic derivative alkaloid of vincamine,1 an extract from the periwinkle plant Vinca minor. Vinpocetine is reported to have cerebral blood-flow enhancing2 and neuroprotective effects,3 and is used as a drug in Eastern Europe for the treatment of cerebrovascular disorders and age-related memory impairment.4 Vinpocetine is widely marketed as a supplement for vasodilation and as a nootropic for the improvement of memory. There exists anecdotal report of uncomfortable adverse reactions to vinpocetine in a small subset of users. A low initial dosage is often recommended. Contents 1 Possible Nootropic Properties 2 Use as a Vasodilator 3 Mechanism of Action 4 Side-effects 5 Dosage 6 External links 7 References Possible Nootropic Properties A number of studies on healthy volunteers have demonstrated vinpocetine may elicit improvement on some aspects of memory. 5 6 The degree which the nootropic effects of vinpocetine are mediated by mechanisms beyond vasodilation is currently unknown. Use as a Vasodilator Vinpocetine widely used in the body building community as a vasodilator. However, no studies have been conducted on the effectiveness of vinpocetine on performance enhancement during exercise. There exists anecdotal evidence that a small subset of users may experience adverse reactions. Due to the possibility of adverse reactions a low initial dose is typically recommended. The small size of existing studies precludes conclusion on the prevalence or severity of possible adverse reactions in vinopocetine usage. Mechanism of Action Vinpocetine has been shown to selectively inhibit voltage-sensitive Na+ channels, resulting in a dose-dependent decrease in evoked extracellular Ca+ ions in striatal nerve endings.7 The Na+ channel inhibiting properties of vinpocetine are thought to contribute to a general neuroprotective effect through blockade of excitotoxicity and attenuation of neuronal damage induced by cerebral ischemia/reperfusion.8 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.1011 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 No adverse reactions to vinpocetine have been reported in human trials. Due to the small sample size of existing trials the prevalence of adverse reactions is still unknown although thought to be rare. The safety of vinpocetine in pregnant women has not been evaluated. 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 to make sure they are not hypersensitive to it. Users may then increase the dosage to 10-30 mg a day which may, although very rarely, cause some side-effects. External links Erowid Vinpocetine Vault Vinpocetine article from PDRhealth Vinpocetine for cognitive impairment and dementia - Cochrane review References ^ Lörincz C, Szász K, Kisfaludy L. The synthesis of ethyl apovincaminate. Arzneimittel-forschung 1976;2610a:1907. PMID: 1037211. ^ 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. Journal of Neurological Sciences 2005 Mar 15;229-230:275-84. Epub 2005 Jan 8. PMID: 15760651. ^ Dézsi L, Kis-Varga I, Nagy J, Komlódi Z, Kárpáti E. Neuroprotective effects of vinpocetine in vivo and in vitro. Apovincaminic acid derivatives as potential therapeutic tools in ischemic stroke. Acta Pharmaceutica Hungarica 2002;722:84-91. 12498034 ^ Vinpocetine. Monograph. Alternative Medicine Review 2002 Jun;73:240-3, pp. 240. PMID: 12126465. ^ Psychopharmacological effects of vinpocetine in normal healthy volunteers 1. ^ Possible memory-enhancing properties of vinpocetine2. ^ Sitges M, Galván E, Nekrassov V. Vinpocetine blockade of sodium channels inhibits the rise in sodium and calcium induced by 4-aminopyridine in synaptosomes. Neurochemistry International 2005 Jun;467:533-40. PMID: 15843047. ^ Adám-Vizi V. Neuroprotective effect of sodium channel blockers in ischemia: the pathomechanism of early ischemic dysfunction. Orvosi Hetilap 2000 Jun 4;14123:1279-86. PMID: 10905082 ^ Hagiwara M, Endo T, Hidaka H. Effects of vinpocetine on cyclic nucleotide metabolism in vascular smooth muscle. Biochemical Pharmacology 1984 Feb 1;333:453-7. PMID: 6322804. ^ Truss MC, Uckert S, Stief CG, Forssmann WG, Jonas U. Cyclic nucleotide phosphodiesterase PDE isoenzymes in the human detrusor smooth muscle. II. Effect of various PDE inhibitors on smooth muscle tone and cyclic nucleotide levels in vitro. Urological Research 1996;243:129-34. PMID: 8839479. ^ Gurkovskaia AV, Gokina NI, BuryÄ­ VA, Shuba MF. Electrophysiological analysis of the action of kavinton on the smooth muscles. Biull Eksp Biol Med. 1987 Jan;1031:68-71. PMID: 3801654. ^ Trejo F, Nekrassov V, Sitges M. Characterization of vinpocetine effects on DA and DOPAC release in striatal isolated nerve endings. Brain Research 2001 Aug 3;9091-2:59-67. PMID: 11478921. ^ Ibid. ^ Shimizu Y, Saitoh K, Nakayama M, et al. Agranulocytosis induced by vinpocetine. Medicine Online serial online. Available at: http://www.priory.com/med/vinpocetine.htm. Accessed March 08, 2008. ^ The Complete German Commission E Monographs, Therapeutic Guide to Herbal Medicines, 1st ed. 1998, Integrative Medicine Communications, pub; BkCD-Rom ion, 1999. v d e Stimulants Alkylamines Cyclopentamine Geranamine Isometheptene Octodrine Propylhexedrine Tuamine Alphapyrrolidinylalkiophenones α-PPP MDPPP MDPV MPBP MPHP MPPP MOPPP Pyrovalerone Cholinergics ABT-089 ABT-418 Anabasine Arecoline Cotinine Cytisine Dianicline Epibatidine Epiboxidine GTS-21 Ispronicline Nicotine Rivanicline Tebanicline Varenicline Convulsants Bicuculline DMCM Gabazine Pentetrazol Picrotoxin Strychnine Thujone Eugeroics Adrafinil Armodafinil Carphedon Modafinil Phenethylamines 4-Bromomethcathinone 4-Fluoroamphetamine 4-Fluoromethamphetamine 4-Fluoromethcathinone 4-Methylmethcathinone 4-MTA Aletamine Amfepentorex Amphechloral Amphetamine Dextroamphetamine, Adderall Amphetaminil Benzphetamine Bupropion Cathinone Chlorphentermine Clenbuterol Clobenzorex Clortermine Diethylpropion Dimethoxyamphetamine Dimethylamphetamine Dimethylcathinone Ephedrine Epinephrine Ethcathinone Ethylamphetamine Fenethylline Fenfluramine Fenproporex Fludorex Furfenorex Levomethamphetamine Lisdexamfetamine MDMA Mefenorex Methamphetamine Methcathinone Methoxyphedrine Methylone Octopamine Ortetamine Parahydroxyamphetamine PCA PIA PMA PMEA PMMA PPAP Phendimetrazine Phenmetrazine Phentermine Phenylephrine Phenylpropanolamine Propylamphetamine Pseudoephedrine Selegiline Synephrine Tiflorex Xylopropamine Phenylaminooxazoles 4-Methyl-aminorex Aminorex Clominorex Fenozolone Fluminorex Pemoline Thozalinone Piperazines 2C-B-BZP BZP GBR-12783 GBR-12935 GBR-13069 GBR-13098 GBR-13119 MeOPP MBZP Vanoxerine Piperidines 2-Benzylpiperidine Desoxypipradrol Diphemethoxidine Ethylphenidate HDMP-28 --Methyl-1-methyl-4β-2-naphthylpiperidine-3β-carboxylate Methylphenidate Dexmethylphenidate Nocaine Phacetoperane Pipradrol Tropanes 3α-Bis-4-fluorophenylmethoxytropane 3α-4-Chlorophenylphenylmethoxytropane 3-Pseudotropyl-4-fluorobenzoate Altropane IACFT Brasofensine CFT WIN 35,428 β-CIT RTI-55 Cocaethylene Cocaine β-CPPIT Dichloropane RTI-111 Difluoropine FE-β-CPPIT FP-β-CPPIT PIT PTT RTI-31 RTI-32 RTI-51 RTI-112 RTI-113 RTI-121 IPCIT RTI-126 RTI-150 RTI-171 RTI-177 RTI-336 Tesofensine Troparil β-CPT, WIN 35,065-2 WF-23 WF-33 WF-60 Xanthines Aminophylline Caffeine Dimethazan Paraxanthine Theobromine Theophylline Others Amineptine Bemegride Benzydamine BPAP Bromantane BTQ Clofenciclan Cypenamine Cyprodenate Diclofensine Dimethocaine Diphenyl prolinol Ethamivan Fencamfamine Feprosidnine Gilutensin GYKI-52895 Hexacyclonate Indanorex Indatraline LR-5182 Mazindol Mesocarb Naphthylisopropylamine Nikethamide Nomifensine Phthalimidopropiophenone Prolintane Sibutramine Yohimbine Zylofuramine See also Sympathomimetic amines v d e Selective Phosphodiesterase inhibitors C01CE, G04BE PDE1 Vinpocetine PDE2 EHNA PDE3 Amrinone, Bucladesine, Enoximone, Milrinone PDE4 Cilomilast, Etazolate, Glaucine, HT-0712, Ibudilast, Mesembrine, Rolipram PDE5 Acetildenafil, Avanafil, Sildenafil, Tadalafil, Thiomethisosildenafil, Udenafil, Vardenafil v d e Psychoanaleptics: psychostimulants, agents used for ADHD and nootropics N06B Centrally acting sympathomimetics Amphetamine - Amphetaminil - Atomoxetine - Dextroamphetamine - Dextromethamphetamine - Fencamfamin - Fenozolone - Fenetylline - Methylphenidate - Mesocarb - Pemoline - Pipradrol - Prolintane Xanthine derivatives Caffeine - Propentofylline Glutamate receptor Racetams Aniracetam - Nefiracetam - Oxiracetam - Phenylpiracetam - Piracetam - Pramiracetam Ampakines CX-516 - CX-546 - CX-614 - CX-691 - CX-717 - IDRA-21 - LY-503,430 - PEPA Eugeroics / Benzhydryl compounds Adrafinil - Armodafinil - Modafinil Histamine H3 receptor antagonists ABT-239 - Ciproxifan Other psychostimulants and nootropics Acetylcarnitine - Citicoline - Cyprodenate - Idebenone - Ispronicline - Deanol - Dimebon - Fipexide - Linopirdine - Meclofenoxate - Nizofenone - Pirisudanol - Pyritinol - Sulbutiamine - Taltirelin - Tricyanoaminopropene - Vinpocetine Retrieved from http://en..org/wiki/Vinpocetine Categories: Nootropics | Phosphodiesterase inhibitors | Vasodilators Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Español РуÑ?Ñ?кий SlovenÄ?ina УкраїнÑ?ька This page was last modified on 17 July 2008, at 19:57

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