| Cerebral Vasodilator |
Винпоцетин является препаратом, расширяющим сосуды головного мозга, и имеет относительно более сильное действие, чем винкамин.. Он может избирательно увеличивать мозговой кровоток., улучшить и улучшить снабжение мозга кислородом, способствовать метаболизму, повысить способность деформации эритроцитов, уменьшить вязкость крови, ингибировать агрегацию тромбоцитов, улучшить тканевый метаболизм. Винпоцетин в основном применяется при лечении последствий инфаркта головного мозга., последствия кровоизлияния в мозг, церебральный атеросклероз, и т.д. Его также можно использовать при лечении склероза сосудов сетчатки и спазма кровеносных сосудов., глухота у пожилых людей, и головокружение.
Винпоцетин – полусинтетическое производное винкамина., и имеет аналогичный эффект с винкамином. Он имеет более сильную функцию расширения избирательно для сосудов головного мозга.. 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, уменьшить вязкость крови, ингибировать агрегацию тромбоцитов, 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.
Фигура 1 is the structural formula of vinpocetine. |
| Фармакокинетика |
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, уменьшить вязкость крови, ингибировать агрегацию тромбоцитов, 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 час, then metabolize into Vinpocetine in the body. The half-life of plasma elimination is about 1 час. Для 4 weeks in a row, no accumulation in the body. Clinical used in cerebral infarction sequela, последствия кровоизлияния в мозг, церебральный атеросклероз, cerebral vasospasm, brain endarteritis caused vertigo, tinnitus, головная боль, головокружение, limb numbness, incontinence and other clinical manifestations, депрессия, беспокойство, 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. |
| Показания |
1.Neurology: all kinds of cerebrovascular disease and its sequelae.
2.Cardiology: coronary heart disease, hardening of the arteries and blood clotting abnormalities, и т.д.
3.Eye: all kinds of views of visual impairment caused by poor circulation, и т.д.
4.Otolaryngology: hearing loss, tinnitus, vestibular dysfunction, и т.д.
5.Neurosurgery: all kinds of craniocerebral surgery back function rehabilitation. |
| Побочные эффекты |
Nervous system: head heavy, головокружение, occasional tiredness and side limb numbness, и т.д.
Digestive system: тошнота, рвота, потеря аппетита, боль в животе, диарея, и т.д.
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, и т.д. |
| Химические свойства |
Белый кристаллический порошок, odourless and tasteless. Soluble in chloroform or 96% спирт этиловый, нерастворим в воде. The melting point is 147-147 оС (разложение). [а]D20+114°(C=1,pyridine). UV maximum absorption (96% спирт этиловый): 229,275,315 нм (ε28200120, 00710). Acute toxicity LD50 in mice and rats (мг/кг): 534503 оральный; 240133.8 intraperitoneal injection; 58.7, 42.6 intravenous injection. |
| использование |
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, головная боль, memory disorders, movement disorder, афазия, hypertensive encephalopathy, и т. д.. Can also be used in brain blood circulation obstacle caused by mental or neurological symptoms.
This information is edited by ChemicalBook Xiao Nan. |
| Метод производства |
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 г, 0.003 mo1) а также 1.0 g of potassium hydroxide in 80 ml of drying ethanol, add bromine ethane (0.4 г, 0.0036 моль), reflux 3 час. After the completion of reaction, cooling, evaporation to dry. Dissolve the leftovers in 500 Нандролон деканоат порошок 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 оС, 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. |
| Появление |
Белое кристаллическое твердое вещество |
| Использует |
A calcium/calmodulin-dependent phosphodiesterase 1 (PDE1) ингибитор |
| Использует |
A derivative of Vincamine with vasodilating activity. Сосудорасширяющее средство (cerebral). |
| Использует |
calcium regulator |
| Использует |
Gleevec metabolite, tyrosine kinase inhibitor |
| Биологическая активность |
Phosphodiesterase inhibitor, selective for PDE1 (IC 50 знак равно 21 μ M). Also blocks voltage-gated Na + каналы. |
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