Vinpotropile capsules, 60pcs

Composition

1 capsule contains

active ingredients:  

• vinpocetine 5 mg, piracetam 400 mg;

excipients:  

• colloidal silicon dioxide 2.6 mg,

• lactose monohydrate 107.4 mg, talc 5 mg;

composition of solid gelatin capsule No. 0:

body:  titanium dioxide 1.7421 mg, quinoline yellow dye 0.5226 mg, sunset yellow dye 0.0233 mg, gelatin 55.782 mg;

cap:  titanium dioxide 0.4552 mg, dye azorubin 0.1896 mg, gelatin 37.2852 mg

Pharmacological action

Pharmacodynamics

Vinpotropile is a combination drug. It has properties characteristic of a psychostimulant (vinpocetine) and a nootropic (vinpocetine, piracetam).

As a psychostimulant

Improves brain metabolism by increasing the consumption of glucose and oxygen by brain tissue. Increases the resistance of neurons to hypoxia; increases the transport of glucose to the brain, through the blood-brain barrier; transfers the process of glucose breakdown to an energy-efficient, aerobic pathway; selectively blocks Ca2+ – dependent phosphodiesterase; increases the levels of adenosine monophosphate (AMP), cyclic guanosine monophosphate (cGMP) and adenosine triphosphate (ATP) of the brain. Increases the exchange of norepinephrine and serotonin in the brain; stimulates the ascending branch of the noradrenergic system, has an antioxidant effect.

Reduces platelet aggregation and increased blood viscosity; increases the elasticity of red blood cells and blocks the utilization of adenosine by red blood cells; helps to increase the return of oxygen by red blood cells. Increases cerebral blood flow; reduces resistance of cerebral vessels without significant changes in the parameters of systemic circulation.

It does not have the effect of” stealing ” and increases blood supply, primarily in ischemic areas of the brain. Penetrates the placental barrier.

As a nootropic agent

It has a positive effect on the metabolic processes of the brain, slightly increases the concentration of ATP in the brain, enhances the synthesis of ribonucleic acid and phospholipids, stimulates glycolytic processes, enhances glucose utilization; improves the integrative activity of the brain, promotes memory consolidation, facilitates the learning process; changes the speed of excitation propagation in the brain, improves microcirculation, without having a vasodilating effect, inhibits the aggregation of activated platelets; has a protective effect in brain damage caused by hypoxia, intoxication, electric shock; increases alpha and beta activity, reduces delta activity on the electroencephalogram, reduces the severity of vestibular nystagmus; improves connections between the cerebral hemispheres and synaptic conduction in neocortical structures, increases mental activity, increases cerebral blood flow; does not have a sedative, psychostimulating effect.

The effect develops gradually.

It has a pronounced effect on the symptoms of the initial manifestations of cognitive disorders of cerebral and vascular genesis in elderly and senile patients. Recommended in psychogeriatric practice.

Pharmacokinetics

Vinpocetine

Absorption rate

After oral use, it is rapidly absorbed from the gastrointestinal tract. Time to reach the maximum concentration (TMAX) in blood plasma is 1 h. Absorption occurs mainly in the proximal parts of the gastrointestinal tract. When passing through the intestinal wall, it is not metabolized.

Distribution

When radiolabeled vinpocetine was administered orally to rats, the highest concentrations were found in the liver and gastrointestinal tract. The maximum concentration in the tissues was observed 2-4 hours after use. The concentration of radiolabeled vinpocetine in the brain did not exceed the values found in the blood.

In humans, plasma protein binding is 66%, and oral bioavailability is 7%. The volume of distribution is 246.7-88.5 liters, which indicates a high binding to tissues. Total clearance (66.7 l/h) exceeds the rate of hepatic blood flow (50 l / h), which indicates extrahepatic metabolism.

Metabolism

The main metabolite is apovincaminate (ABA), which makes up 25-30% of the initial compound. The area under the concentration —time curve of ABA after oral use is twice

that of intravenous vinpocetine. Thus, vinpocetine is subject to a pronounced effect of “primary passage” through the liver. Other metabolites include: hydroxyvinpocetine, hydroxy-ABA, ABA-dioxyglycinate and their conjugates (sulfates and / or glucuronides).

Deduction

The elimination of unchanged vinpocetine is low (several percent). When repeatedly administered at doses of 5 mg and 10 mg, the kinetics is linear, the equilibrium plasma concentration is 1.2±0.27 and 2.1±0.33 ng / ml, respectively. The human half-life is 4.8±1.29 hours.

It is excreted by the kidneys and through the intestines in a ratio of 60: 40. In rats and dogs, high radioactivity is detected in the bile when radiolabeled vinpocetine is administered, but significant enterohepatic recirculation is noted.

Pharmacokinetics in special groups of patients (age, comorbidities)

It was found that the pharmacokinetics of vinpocetine in elderly patients did not significantly differ from those in young patients, and there was no accumulation of the drug.

Piracetam

Absorption rate

After oral use, piracetam is rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability is about 100%.

After a single dose of piracetam in a dose of 2 g, the maximum concentration (Cmax) is reached in 30 minutes and is 40-60 mcg / ml, after 2-8 hours it is detected in the cerebrospinal fluid.

Distribution

The volume of distribution (Vd) is about 0.6 l / kg. It does not bind to plasma proteins. Piracetam penetrates the blood-brain and placental barriers, as well as hemodialysis membranes.

An animal study found that piracetam selectively accumulates in the cortical tissues of the brain, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal nuclei.

Metabolism

It is not metabolized.

Deduction

The half-life from the blood (T 1/2) is 4-5 hours and 8.5 hours-from the cerebrospinal fluid. T 1/2 is prolonged in case of renal failure.

It is excreted unchanged by the kidneys. Renal excretion is almost complete (>95%) within 30 h. The total clearance of piracetam in healthy volunteers is 86 ml / min. >

Indications

Symptomatic treatment: intellectual and mnestic disorders, consequences of ischemic stroke, vascular vertebrobasilar insufficiency, vascular dementia, cerebral vascular atherosclerosis, post-traumatic, hypertensive encephalopathy.

Chronic vascular diseases of the retina and choroid of the eye. Perceptual hearing loss, Meniere’s disease, tinnitus.

Use during pregnancy and lactation

Vinpocetine

Use during pregnancy and lactation is contraindicated.

Pregnancy

Vinpocetine passes through the placenta, but the plasma concentration in the placenta and in the fetus is lower than in the mother. Teratogenic and embryotoxic effects were not detected. In animal studies, placental bleeding and abortions (presumably due to increased placental blood flow) occurred when high doses were administered.

Breast-feeding

Vinpocetine passes into breast milk. According to preclinical studies with radioactively labeled vinpocetine, the concentration in the breast milk of newborn animals exceeded that in the mother’s blood by 10 times. For 1 hour,0.25% of the dose taken penetrates into the milk.

Do not use during breast-feeding or stop breastfeeding during treatment with vinpocetine.

Piracetam

Pregnancy

There are no sufficient data on the use of piracetam during pregnancy. Animal studies have shown no direct or indirect effects on pregnancy, embryo/fetus development, delivery, or postnatal development.

Piracetam penetrates the placental barrier. The plasma concentration of piracetam in newborns reaches 70-90% of that in the mother. Piracetam should be used during pregnancy only in exceptional cases, if the benefit to the mother exceeds the potential risk to the fetus, and the clinical condition of the pregnant woman requires treatment with piracetam.

Breast-feeding

Piracetam passes into breast milk. Piracetam should not be used during breast-feeding, or breastfeeding should be discontinued during treatment with piracetam. When

deciding whether to discontinue breast-feeding or not to use piracetam, the benefits of breast-feeding for the child and the benefits of therapy for the woman should be considered.

Contraindications

Hypersensitivity, pregnancy, lactation, severe cardiac arrhythmias, severe coronary heart disease, acute stage of hemorrhagic stroke, renal and / or hepatic insufficiency, children under 18 years of age (due to insufficient data). Patients with rare hereditary problems such as galactose intolerance, lactase deficiency, or glucose-galactose malabsorption should not take Vinpotropile.

Side effects

Side effects are quite rare.The frequency gradation is defined as follows: very common (≥1/10), common (≥1/100 to <1/10), infrequent (≥1/1000 to <1/100), rare (≥1/10000 to <1/1000), very rare (

Vinpocetine

Disorders of the blood and lymphatic system

Rare: leukopenia, thrombocytopenia.

Very rare: anemia, agglutination of red blood cells.

Immune system disorders

Very rare: hypersensitivity.

Metabolic and nutritional disorders

Infrequently: hypercholesterolemia

Rare: decreased appetite, anorexia, diabetes mellitus.

Mental disorder

Rare: insomnia, sleep disturbance, agitation, restlessness.

Very rare: euphoria, depression.

Nervous system disorders

Infrequently: headache. Rare: dizziness, taste disorders, stupor, hemiparesis, drowsiness, amnesia.

Very rare: tremor, spasms.

Visual impairment

Rare: Edema of the optic disc

Very rare: conjunctival hyperemia.

Hearing and labyrinth disorders

Infrequently: vertigo. Rare: hyperacusis, hypoacusia, tinnitus.

Violation of the heart

Rare: myocardial ischemia / infarction, angina, bradycardia, tachycardia, extrasystole, palpitation sensation.

Very rare: arrhythmia, atrial fibrillation.

Vascular disorders

Infrequently: arterial hypotension.

Rare: hypertension, hot flashes, thrombophlebitis.

Very rare: fluctuations in blood pressure.

Gastrointestinal disorders

Infrequently: abdominal discomfort, dry mouth, nausea.

Rare: abdominal pain, constipation, diarrhea, dyspepsia, vomiting.

Very rare: dysphagia, stomatitis.

Skin and subcutaneous tissue disorders

Rare: erythema, excessive sweating, pruritus, urticaria, rash.

Very rare: dermatitis.

General disorders and disorders at the injection site

Rare: asthenia, malaise.

Very rare: chest discomfort, hypothermia.

Influence on the results of laboratory and instrumental studies

Infrequently: reducing blood pressure. Rarely: increased blood pressure, increased serum triglyceride concentrations, ST-segment depression on an electrocardiogram, decreased / increased eosinophils, impaired liver function tests.

Very rare: increase/decrease in the number of white blood cells, decrease in the number of red blood cells, decrease in thrombin time, increase in body weight.

Piracetam

From the blood and lymphatic system

, the frequency is unknown: bleeding.

From the immune system

, the frequency is unknown: anaphylactoid reactions, hypersensitivity.

From the side of the psyche

Often: nervousness. Infrequently: depression. Frequency unknown: agitation, anxiety, confusion, hallucinations.

From the nervous system

Often: hyperactivity. Infrequently: drowsiness.

Frequency unknown: ataxia, balance disorders, exacerbation of epilepsy, headache, insomnia, tremor.

From the side of the organ of hearing and labyrinth

, the frequency is unknown: vertigo.

From the digestive system

, the frequency is unknown: abdominal pain (including in the upper parts), diarrhea, nausea, vomiting.

Skin and subcutaneous tissue

disorders Frequency unknown: angioedema, dermatitis, pruritus, urticaria.

From the reproductive system

Frequency unknown: increased sexual desire

General disorders and disorders at the injection site

Infrequently: asthenia

Laboratory and instrumental data

Often: weight gain

Interaction

Vinpocetine

According to the results of clinical studies, drug interactions with beta-blockers (pindolol), clomipramide, glibenclamide, digoxin, hydrochlorothiazide and acenocoumarol were not detected.

Methyldopa may increase the antihypertensive effect of vinpocetine, so when they are used simultaneously, systematic blood pressure monitoring is required.

Despite the lack of clinical data, concomitant use with agents that affect the central nervous system, anticoagulants and antiarrhythmics should be carried out with caution.

Piracetam

Thyroid Hormones

Concomitant use of piracetam and thyroid extract (triiodothyronine + thyroxine) resulted in confusion, irritability, and sleep disturbances.

Acenokoumarol

According to a published blind clinical study in patients with recurrent venous thrombosis, piracetam at a dose of 9.6 g/day does not affect the dose of acenocoumarol required to achieve an international normalized ratio of 2.5-3.5, but compared to the effects of acenocoumarol alone, the addition of piracetam at a dose of 9.6 g/day significantly reduces platelet aggregation, beta-thromboglobin release, fibrinogen concentration and von Willebrand factor (VIII: C; VIII: vW: Ag; VIII: vW: RCo), as well as the viscosity of whole blood and plasma.

Pharmacokinetic interactions

The possibility of changing the pharmacokinetics of piracetam under the influence of other drugs is low, since 90% of piracetam is excreted unchanged in the urine.

At concentrations of 142,426, and 1422 mg/ml, piracetam does not inhibit cytochrome P 450 isoenzymes (CYP 1 A 2,2 B 6,2 C 8,2 C 9,2 C 19,2D6,2 E 1, and 4 A 9/11) in vitro.

At a concentration of 1422 mg/ml, minimal inhibition of the CYP2A6 isoenzyme was observed (21%) and for 4/5 (11%). However, the values of the inhibition constant (Ki) probably go far beyond the concentration of 1422 mg / ml. Thus, metabolic interactions of piracetam with other drugs are unlikely.

Anticonvulsants

Taking piracetam at a dose of 20 g / day for 4 weeks in patients with epilepsy who took constant doses of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and valproic acid) did not change their maximum and minimum concentrations.

Alcohol

Concomitant use with alcohol did not affect the concentration of piracetam in plasma; when taking 1.6 g of piracetam, the concentration of ethanol in plasma did not change.

How to take, course of use and dosage

For patients 18 years and older: inside, before meals,1-2 capsules,2-3 times a day. The last appointment is 4 hours before bedtime.

The duration of treatment is 2-3 months.

Before discontinuation, the dose of the drug should be gradually reduced.

Overdose

Symptoms: increased severity of side effects.

Treatment: gastric lavage, taking activated charcoal, symptomatic therapy.

Special instructions

The presence of prolonged QT syndrome and the use of drugs that cause prolongation of the QT interval requires periodic monitoring of the ECG. In case of lactose intolerance, it should be noted that one tablet contains about 225 mg of lactose. Influence on the ability to drive motor vehicles and manage mechanisms: taking into account possible side effects, care should be taken when driving a car and working with mechanisms.

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25 ° C. Keep out of reach of children.

Shelf life

4 years

Active ingredient

Vinpocetine, Piracetam

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

For adults as directed by your doctor

Indications

Asthenia, Migraines, Cerebrovascular accident, Meniere’s disease, Concussion and other traumatic brain injuries, Consequences of stroke