| Cerebral Vasodilator |
La vinpocetina es un fármaco de expansión cerebrovascular y tiene una función relativamente más fuerte que la vincamina.. Puede aumentar selectivamente el flujo sanguíneo cerebral., mejorar y mejorar el suministro de oxígeno al cerebro, promover el metabolismo, mejorar la capacidad de deformación de los glóbulos rojos, reducir la viscosidad de la sangre, inhibir la agregación plaquetaria, mejorar el metabolismo de los tejidos. La vinpocetina se utiliza principalmente en el tratamiento de las secuelas del infarto cerebral., secuelas de hemorragia cerebral, arteriosclerosis cerebral, etc.. También se puede utilizar en el tratamiento de la esclerosis vascular de la retina y el espasmo de los vasos sanguíneos., la sordera de los ancianos, y mareos.
La vinpocetina es un derivado semisintético de la vincamina., y tiene un efecto similar con la vincamina.. Tiene una función de expansión más fuerte para cerebrovascular selectivamente.. Pharmacological effects are as follows:
①Inhibit the activity of calcium dependency phosphodiesterase, increase the content of cAMP which can relax vascular smooth muscle, then relax vascular smooth muscle, and further increase cerebral blood flow.
②Enhance the capacity of deformation of red blood cells, reducir la viscosidad de la sangre, inhibir la agregación plaquetaria, and thus improve blood flow and microcirculation.
③Promote the brain tissue to absorb glucose, and promote the transformation of brain monoamine metabolism.
④Inhibit the increase of brain lactic acid during cerebral ischemia, increase the ATP content, inhibit the generation of lipid peroxide in the brain, delay the occurring of spasm caused by cerebral ischemia, have the function of improving cerebral metabolism and protecting brain.
Figure 1 is the structural formula of vinpocetine. |
| Farmacocinética |
Vinpocetine is of high fat-solubility, easy to be absorbed by the organization, and widely distributed. It can through the blood brain barrier, mainly metabolism to Vinpocetine in the liver, and be excreted by the kidney. |
| Medicinal properties and Application |
Vinpocetine is also called Ethyl apovincaminate, Conway, Karan and Vinpocetine. It is a kind of natural medicine extracted from small vinca flower, and belongs to the indole alkaloids. Can be synthetic now. The mechanism of its pharmacological action is to inhibit the activity of calcium dependency phosphodiesterase, increase the content of CGMP which can relax vascular smooth muscle, then relax vascular smooth muscle, and further increase cerebral blood flow; Enhance the capacity of deformation of red blood cells, reducir la viscosidad de la sangre, inhibir la agregación plaquetaria, and thus improve blood flow and microcirculation; Promote the brain tissue to absorb glucose, and promote the transformation of brain monoamine metabolism; Inhibit the increase of brain lactic acid during cerebral ischemia, increase the ATP content, increase thedegree of oxygen dissociation in hemoglobin; Increase the resistance capacity for cerebral anoxia and occurring of spasm caused by cerebral ischemia, inhibit the generation of lipid peroxide in the brain. Oral absorption effectively, reach peak at 1 H, then metabolize into Vinpocetine in the body. The half-life of plasma elimination is about 1 hour. Para 4 weeks in a row, no accumulation in the body. Clinical used in cerebral infarction sequela, secuelas de hemorragia cerebral, arteriosclerosis cerebral, cerebral vasospasm, brain endarteritis caused vertigo, tinnitus, dolor de cabeza, mareo, limb numbness, incontinence and other clinical manifestations, depresión, ansiedad, sleep disorder and other mental symptoms. Clinical experience has shown that it is effective regardless of the length of the course of the disease, and the symptom is fixed or not. |
| Indicación |
1.Neurology: all kinds of cerebrovascular disease and its sequelae.
2.Cardiology: coronary heart disease, hardening of the arteries and blood clotting abnormalities, etc..
3.Eye: all kinds of views of visual impairment caused by poor circulation, etc..
4.Otolaryngology: hearing loss, tinnitus, vestibular dysfunction, etc..
5.Neurosurgery: all kinds of craniocerebral surgery back function rehabilitation. |
| Efectos secundarios |
Nervous system: head heavy, mareo, occasional tiredness and side limb numbness, etc..
Digestive system: náuseas, vómitos, pérdida de apetito, dolor abdominal, diarrea, etc..
Circulatory system: facial blushing, dizziness and other symptoms.
Blood system: white blood cells reduction.
Liver reaction: AST, ALT elevations, rare elevation of alkaline phosphatase.
Kidney reaction: blood urea nitrogen increasing.
Sometimes allergic reactions like skin rash, urticarial and pruritus may appear, then drug should be discontinued. Occasional mild lowering blood pressure, tachycardia, etc.. |
| Propiedades químicas |
Polvo de cristal blanco, odourless and tasteless. Soluble in chloroform or 96% etanol, insoluble en agua. The melting point is 147-147 jefe (decomposition). [a]D20+114°(C=1,pyridine). UV maximum absorption (96% etanol): 229,275,315 Nuevo Méjico (ε28200120, 00710). Acute toxicity LD50 in mice and rats (mg/kg): 534503 oral; 240133.8 intraperitoneal injection; 58.7, 42.6 intravenous injection. |
| Uso |
Cerebrovascular drug. A alkaloid extracted from apocynaceae plant, Vincamine derivatives. Selectively inhibit vascular smooth muscle calcium dependency phosphodiesterase, and increase the content of cGMP, expanse cerebral vascular, which in turn increase cerebral blood flow, improve cerebral circulation, but has little effects on the cardiovascular and blood pressure. Effectively, good tolerance, less adverse reaction. Used for dizziness, dolor de cabeza, memory disorders, movement disorder, aphasia, hypertensive encephalopathy, etc.. Can also be used in brain blood circulation obstacle caused by mental or neurological symptoms.
This information is edited by ChemicalBook Xiao Nan. |
| Production Method |
Vincamine extracted from small periwinkle (Vinca mino) of apocynaceae plant as raw material, dehydration to Apovincamine, then hydrolysis to Apovincaminic acid. Dissolved the acid (1.0 gramo, 0.003 mo1) Estanozolol semielaborado de la serie líquida de esteroides 1.0 g of potassium hydroxide in 80 ml of drying ethanol, add bromine ethane (0.4 gramo, 0.0036 mol), reflux 3 H. After the completion of reaction, cooling, evaporation to dry. Dissolve the leftovers in 500 Polvo de decanoato de nandrolona 2% sulfuric acid, and adjust the Ph to 8. Extracted with methylene chloride, drying with potassium carbonate, after the majority of methylene chloride has been evaporated, add in ethanol. Be placed overnight At 0 jefe, filter the collected precipitation crystallization, washing with cold ethanol, drying, 0.66 g of Vinpocetine could be obtained. Tabersonine extracted from apocynaceae plant willow small licorice leaf or periwinkle seed can also be as raw material, through multi-step synthesis. |
| Apariencia |
Sólido cristalino blanco |
| Usos |
A calcium/calmodulin-dependent phosphodiesterase 1 (PDE1) inhibidor |
| Usos |
A derivative of Vincamine with vasodilating activity. Vasodilator (cerebral). |
| Usos |
calcium regulator |
| Usos |
Gleevec metabolite, tyrosine kinase inhibitor |
| Actividad biológica |
Phosphodiesterase inhibitor, selective for PDE1 (IC 50 = 21 μ M). Also blocks voltage-gated Na + canales. |
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