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Review on Vinpocetine Review Article ISSN: 0976-7126 CODEN (USA): IJPLCP Dubey et al., 11(5):6590-6597, 2020 [[ Review on Vinpocetine Anubhav Dubey*, Neeraj Kumar, Ashish Mishra, Yatendra Singh and Mamta Tiwari 1, Department of Pharmacology, Advance Institute of Biotech and Paramedical Sciences Kanpur (U.P.) - India Abstract Article info Vinpocetine is a synthetic ethyl ester of apovincamine. It is extracted from the periwinkle plant. Vincamine is extracted from either Received: 12/03/2020 the seeds of Voacanga-Africana or the leaves. Vinpocetine is an herbal supplement used to treat various neurological disorders such as Revised: 29/04/2020 Alzheimer’s and Parkinson’s disease. Vinpocetine has also anti- inflammatory, analgesics, antioxidant property and treat various thinking Accepted: 26/05/2020 and memory problem. The drug has neuroprotective property thus it is used for memory impairment. Vinpocetine drug dilates blood vessels and © IJPLS promotes cerebral blood flow. Pharmacodynamics, Pharmacokinetic and adverse effects were discussed. www.ijplsjournal.com Keywords: Vincamine, neuroprotective, memory enhancement and cerebral blood flow Voacanga-Africana Introduction Vinpocetine was prepared under the trade name possible mechanism by which cerebral ATP levels cavinton in 1978[1], vinpocetine widely used in seemed to be increased after administration of the Germany, Russia, Japan, Hungar for the treatment compound. [3] of the cerebrovascular related disorder. Modern lifestyle has raised life hope but also Vinpocetine is a semi-synthetic derivative increase chronic harm full disease, therefore, obtained from vincamine alkaloid. Vincamine increasing chronic Pharmaceutical usage, it is also present in the aerial part of the vinca minor and called some time nootropic agent meaning plant belongs to the Apocynaceae family. cognition enhancer. Vinpocetine is approved by the European and British pharmacopoeias. Vinpocetine as well as vincamine are used in Europe, Japan and Mexico as a pharmaceutical agent for the treatment of cerebrovascular and cognitive disorders. [2] Catecholamine levels were similarly increased 4-6 hours following the administration of vinpocetine. The authors also reported an inhibition of phosphodiesterase enzyme (PDE) suggesting a *Corresponding Author E.mail: [email protected] International Journal of Pharmacy & Life Sciences Volume 11 Issue 5: May. 2020 6590 Review Article ISSN: 0976-7126 CODEN (USA): IJPLCP Dubey et al., 11(5):6590-6597, 2020 An analgesic role for vinpocetine show that it Vinpocetine uses during pregnancy condition may inhibits neuronal tetrodotoxin-resistant NAV1.18 harm the baby or result in miscarriage with intraperitoneal (I.P) sodium channel current- [12],the neuroprotective effects induced calcium influx with (I.P) administration of vinpocetine related to blocking effects on of vinpocetine reducing acetic acid visceral the excitotoxicity effectsof glutamate nociception, which is potentates by muscarinic, and aspartate, and partly related adrenergic, opioid receptor and blocked dependent to phosphodiesterase enzyme inhibition increases on adenosine receptor. Vinpocetine drugs also cerebral blood flow and decrease platelet inhibit formalin-induced paw flinching and aggregation.[13,14] inhibition of c- fos expression in Chemistry of vinpocetine the ipsilateral dorsal horn, Ethyl-Apovincamine 22-oate (Ethyl- when intraperineurally administered. Itblocks Apovincaminate) is also known neuropathic pain through retrograde as vinpocetine, [15] Ethyl- axoplasmic transport of nerve growth factor.[4] Apovincaminatewas first synthesized by Lo¨rincz Although vinpocetine is not a microtubule et al. from alkaloid vincamineobtained from the inhibitor and its chemical structure shows no leaves of Vinca.[16]The IUPACName of resemblance to that of vincristine, we found that vinpocetineEburnamenin-14-carboxylic acid at adequate concentration, vinpocetine inhibits ethyl esterand has molecular weight of retrograde axoplasmic transport of nerve growth 350.46g/m0l,Formula:C22H26N202 (Fig. 1), it is factor (NGF), as shown by radiochemical studies. marketed in Hungary, Japan and several other [5] countries for the treatment of cerebral diseases Vincamine is widely used as a neuroprotective originating from vascular or cerebral metabolic agent for the prevention and treatment of central disturbances,[17]the drug improves the cerebral use nervous system disorder of cerebrovascular of oxygen and protects the brain cells against origin.[6]In the U.S. vinpocetine supplements are ischemic anoxia. marketed as sports supplements, brain enhancers, and weight loss supplements.[7, 8] Vinpocetine is easily cross the blood-brain barrier (BBB), the therapeutic effect of vinpocetine high- capacity protect the neuronal cell from cytotoxic effects of inflammation oxidative stress and ion influx. Although vinpocetine inhibits phosphodiesterase-1(PDE-1) enzyme and anti- inflammatory effect present to be PDE-1 A B independent. [9] Fig. 1: AVincamine B vinpocetine [18] Vinpocetine regulates the level of circulating Marketed formulation of vinpocetin TLRS in Parkinson’s disease patients. Toll-like There are the various formulation receptors (TLRs) are a class of proteins that play a of vinpocetine was made various pharmaceutical key role in the innate immune system. Recent company is given in the table, the recommended studies have shown that blockingTLR2 can reduce dose of vinpocetine is 15 to 30 mg in a day and nuclear translocation of nuclear factor kappa- sometimes increase the dose of vinpocetine to 40 light-chain-enhancer of activated B cells. Mg for special cases. Therefore, TLRs provide promising candidates for Table 1: Marketed formulation of vinpocetine the development of PD therapies. The findings BrandNa PharmaceuticalCompa DosageF that vinpocetine causes dilation of isolated me nyName orm cerebral arteries and improves the global cerebral Neurovin Micro Labs Limited 5,10 mg blood flow suggest that cerebral circulatory Cogvin Intas Pharmaceutical 5 mg effects may contribute to its Cerebral protective Limited tablet [10, 11] activity. Vinpotin MJ-Bio-Pharm Private 5mg/ limited tablet and International Journal of Pharmacy & Life Sciences Volume 11 Issue 5: May. 2020 6591 Review Article ISSN: 0976-7126 CODEN (USA): IJPLCP Dubey et al., 11(5):6590-6597, 2020 5mg/ml physiologic and pathophysiologic processes. In injection physiologic circumstances, they play a role in Vinpoceti SRS Pharmaceutical 10,20,30 cellular metabolism and cellular-defense systems. ne mg vial On the other hand, a large amount of oxygen-free injection radicals is highly toxic for tissues and cells Mechanism of action because they can oxidatively modify and damage Vinpocetine has many pharmacological and a variety of biologic systems. [26] biochemical activity, including Epilepsy-Vinpocetine is a potent inhibitor of the cerebral vasodilatation, enhancing the tolerance epileptic cortical activity induced by the of cerebral tissue to hypoxia and ischemia convulsing agents, pentylenetetrazole and 4- insults, anticonvulsant property, inhibitory effects aminopyridine in the guinea pig in vivo, also we on (phosphodiesterase), improving hematological have shown that vinpocetine inhibits the release of flow property and several neurotransmitters triggered by the inhibitory thrombolytic aggregation. entrance of Nab,[27]vinpocetine and The neuroprotective effect carbamazepine,valproic acid, whose mechanism of vinpocetine promotes the selective inhibition of of action mainly involves an increase in GABA calcium calmodulin-dependent CGMP-PDE1, this nergic transmission was unable to decrease inhibition may enhance intracellular CGMP level presynaptic ionic channels permeability in a broad in vascular smooth muscle leading to reduced range of concentrations.[28]The involvement of cerebrovascular resistance and increased cerebral brain pre-synaptic Na+channels in the mechanism blood flow This property is also responsible of action of vinpocetine and carbamazepine is for neuroprotection.[19]It could be hypothesized supported by the sensitivity of the increase in the that vinpocetine may be useful for the treatment of internal concentration of Na+ induced by 4-AP and Rheumatoid Arthritis (RA) due to its well veratridine depolarization to those anticonvulsants established anti-inflammatory effects. [20, 21] in cerebral isolated nerve endings.[29]The effects Furthermore, a recent study has revealed that of two classic antiepileptic drugs (carbamazepine vinpocetine also has an ant hyperglycemic effect, and phenytoin) a potential antiepileptic [22] vinpocetine has antioxidant activity, and it (vinpocetine) and a monoamine oxidase inhibitor prevents reactive free radical generation which (clorgyline) on the simultaneous changes contributed to the reduction of high glucose- (detected by HPLC) on Glue, Asp, dopamine, and induced oxidative damage. [23] DOPAC inside and outside striatal isolated nerve Pharmacology endings were investigated.[30] Vinpocetine has many pharmacological and Alzheimer’s and Related Dementias- biochemical action is given below. Alzheimer’s disease (AD) is a progressive Inhibit the voltage-dependent sodium (Na+) neurodegenerative disorder associated with channel-Voltage-sensitive sodium channels cognitive and behavioral dysfunction. It is the (VSSC) play a fundamental role in the normal leading cause of dementia in the elderly, [31]since function of the CNS because they are responsible dementia and particularly senile dementia of the for the initiation and
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