Pharmacological properties
Pharmacodynamic parameters. Vinpocetine is a semi-synthetic derivative of vincamine, an alkaloid isolated from the leaves of periwinkle (Vinca minor).
The main effects of vinpocetine:
selective enhancement of cerebral blood flow and oxygen utilization without significant changes in systemic blood circulation parameters; increased tolerance of brain tissues to hypoxia and ischemia; inhibition of phosphodiesterase activity; improvement of blood rheological properties and inhibition of platelet aggregation.
Vinpocetine selectively inhibits Ca2+-calmodulin-dependent cGMP phosphodiesterase, thereby increasing the intracellular content of cGMP in the smooth muscles of the vascular wall. This leads to a decrease in cerebral vascular resistance and an increase in cerebral blood flow (including in ischemic areas in patients with cerebrovascular diseases).
Vinpocetine enhances cerebral metabolism by increasing oxygen and glucose uptake and stimulating ATP production in brain neurons (including those exposed to hypoxia/ischemia).
Vinpocetine has a protective effect on ischemic tissue damage, including the brain, liver, and vascular endothelium. Thus, vinpocetine reduces the metabolic needs of the retina under conditions of hypoxia/ischemia; reduces cell death, and improves retinal function after ischemia-reperfusion.
The neuroprotective effect of vinpocetine is associated with a decrease in the activity of voltage-gated neuronal Na + channels, indirect inhibition of some molecular cascades caused by increased intracellular Ca 2+ levels, and, to a lesser extent, inhibition of adenosine reuptake.
The following properties of vinpocetine contribute to the implementation of neuroprotection: increased cerebral blood circulation and cerebral metabolism, reduced blood viscosity, as well as the reduction of oxidative stress, removal of hydroxyl radicals, and modulation of immune reactions.
By inhibiting the activity of IκB kinase, vinpocetine acts as a potent anti-inflammatory agent. In addition, vinpocetine inhibits lipid accumulation in macrophages, prevents vascular smooth muscle cell proliferation, and vascular remodeling.
Vinpocetine improves cognitive functions: both short-term and long-term memory; increases alertness and attentiveness; reduces the severity of senile cerebral dysfunction.
Vinpocetine enhances spatial memory through antioxidant mechanisms, modulation of cholinergic functions, and prevention of neuronal damage; it increases levels of neurotransmitters involved in memory functions (norepinephrine, dopamine, acetylcholine, and serotonin).
Pharmacokinetic parameters. After ingestion, vinpocetine is rapidly absorbed from the small intestine, C max of the drug in the blood is reached after 1 hour. Due to its high lipophilicity, vinpocetine easily penetrates the blood-brain barrier.
Vinpocetine undergoes extensive metabolism, during which about 75% of vinpocetine is hydrolyzed to its main active metabolite - apovincamic acid. T ½ of vinpocetine after oral administration is 1-2 hours. 60% of the dose is excreted by the kidneys, 40% is excreted in the feces.
Indication
Conditions after a stroke, impaired blood flow in the arteries of the vertebrobasilar system, dementia (vascular genesis), cerebral atherosclerosis, encephalopathy (post-traumatic, hypertensive); chronic pathology of the uveal tract and retina. presbycusis (perceptive type), Meniere's disease, tinnitus.
Application
Solution: IV drip (rate ≤80 drops/min). Starting dose: 20 mg in 500 ml of infusion solution containing glucose (dilution with 0.9% NaCl solution is possible). The diluted solution is stored for ≤3 hours. Maximum daily dose is 1 mg/kg of body weight (increased from the starting dose within 2-3 days). Course is 10-14 days.
Tablets: adults per os (after meals) 5-10 mg 3 times a day.
Contraindication
Hypersensitivity to the active ingredient of the drug or its other components;
The use of vinpocetine solution is also contraindicated in patients with the following pathologies:
hemorrhagic stroke (acute phase); coronary artery disease (severe form); severe heart rhythm disturbances.
Parenteral and oral administration of vinpocetine is well tolerated and has a favorable safety profile. No significant treatment-related adverse events have been reported. The following adverse events have been reported:
decreased platelet count (150 ∙ '10 9 / l), erythrocyte agglutination, anemia, rarely - agranulocytosis; increased blood cholesterol levels, diabetes mellitus, lack of appetite (with an objective need for food); depression, euphoria, irritability, agitation, anxiety; headache, dizziness, drowsiness, fainting, pre-fainting state, hemiparesis, tremor, inhibition, sleep disturbance; hemorrhage into the anterior chamber of the eye, decreased visual acuity, hyperopia, myopia, diplopia, conjunctival hyperemia, swelling of the optic nerve head; hearing impairment, hyper-, hypoacusis, vertigo, tinnitus; ischemia / necrosis of the heart muscle, angina pectoris, cardiac arrhythmias, decrease (40 beats / min) or increase (90 beats / min) heart rate, extrasystole, palpitations, heart failure, atrial fibrillation; venous insufficiency, thrombophlebitis, flushing; hypersalivation, dry mouth, heartburn, nausea, vomiting, abdominal discomfort, dyspepsia; hypersensitivity reactions (including flushing, rash, itching, urticaria), dermatitis, excessive sweating; feeling of heat, discomfort in the chest, weakness; inflammatory process, thrombosis at the injection site. decrease (or increase, fluctuations in level) of blood pressure; ECG disorders: prolongation of the PR interval, QT, depression of the ST segment; in blood plasma: increase in urea level, LDH activity.
Special instructions
Caution should be exercised when used in patients with angina pectoris and severe heart rhythm disturbances.
During vinpocetine therapy, alcohol should not be consumed.
Not prescribed during pregnancy and breastfeeding.
There is no information on the effect of the drug on the reaction speed when driving vehicles or other mechanisms.
Interactions
The pronounced inhibition of p-gp by Vinpocetine indicates the possibility of drug interactions by altering the pharmacokinetics of drugs that are p-gp substrates.
Vinpocetine may not affect CYP-mediated drug metabolism.
Since vinpocetine reduces platelet aggregation, its simultaneous use with anticoagulants should be avoided.
Concomitant use with α-methyldopa enhances the antihypertensive effect.
There is no effect of vinpocetine on the pharmacokinetic parameters of imipramine and oxazepam.
The simultaneous use of vinpocetine and glibenclamide is safe.
Overdose
Data is missing.
Storage conditions
At a temperature ≤25 °C in the original packaging. Do not freeze the solution.
Translation of the instructions can be
