Vinpotropil, 10 mg+800 mg 60 pcs

Pharmacodynamics

Vinpotropil is a combined drug. It has properties typical for a brain blood flow enhancer (Vinpocetine) and for a nootropic (Piracetam).

As a medication that improves cerebral blood flow

It improves brain metabolism by increasing glucose and oxygen uptake by brain tissue. Increases resistance of neurons to hypoxia, enhances the transport of glucose to the brain through the blood-brain barrier, and shifts the process of glucose breakdown to a more energy-saving aerobic route; selectively blocks Ca2+-dependent phosphodiesterase; increases levels of adenosine monophosphate (AMP), cyclic guanosine monophosphate (cGMP) and adenosine triphosphate (ATP) of the brain. Increases the metabolism of brain noradrenaline and serotonin; has an antioxidant effect.

Decreases platelet aggregation and increased blood viscosity; increases red blood cell elasticity and blocks red blood cell utilization of adenosine; promotes red blood cell oxygenation. Increases cerebral blood flow; reduces cerebral vascular resistance without significant changes in systemic blood flow. Does not have the effect of “stealing” and increases blood supply, especially in ischemic areas of the brain. It penetrates through the placental barrier.

As a nootropic agent

It improves integrative activity of the brain, promotes memory consolidation, facilitates the learning process; it changes the speed of excitation distribution in the brain, improves microcirculation without having a vasodilatory effect, suppresses aggregation of activated platelets; has a protective effect in brain damage caused by hypoxia, intoxication, electric shock; it enhances α- and β-activity, reduces δ-activity in electroencephalogram, reduces the severity of vestibular nystagmus; improves communication between cerebral hemispheres and synaptic conduction in neocortical structures, increases mental activity, increases cerebral blood flow; it has no sedative, psychostimulant effect. The effect develops gradually.

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

Pharmacokinetics

Vinpocetine is rapidly absorbed. Therapeutic plasma concentration is 10-20 ng/ml. Time to reach maximum plasma concentration is 1 hour. Absorption occurs mainly in the proximal parts of the gastrointestinal tract. During passage through the intestinal wall it is not metabolized.

The maximum concentration in tissues is observed 2-4 hours after oral administration. Protein binding is 66 %, bioavailability when administered orally is 7 %. Clearance 66.7 l/h exceeds liver plasma volume (50 l/h), which indicates extrahepatic metabolism. The main metabolite is apovincamic acid, which has some pharmacological activity. Other inactive metabolites are hydroxyvinpocetine, hydroxy-apovincamic acid, and hydroxyvinpocetine-glycinate. The kinetics is linear in repeated administration. The half-life (T1/2) in humans is 4.83±1.29 h. It is excreted by the kidneys and through the intestine at a ratio of 3:2.

Piracetam after oral administration is well absorbed and penetrates into various organs and tissues. Bioavailability is about 100%. After a single oral dose of 3.2 g the maximum concentration is 84 mcg/ml, after repeated (3.2 g 3 times a day) – 115 mcg/ml. Time of reaching maximum concentration in plasma – 1 hour, cerebrospinal fluid – 5 hours.

The volume of distribution is about 0.6 l/kg. It penetrates through the blood-brain barrier and placental barrier, is selectively accumulated in the cerebral cortex tissues. It is practically not biotransformed and is excreted unchanged by the kidneys through glomerular filtration. Total clearance is 80-90 ml/min. T1/2 from blood plasma is 4-5 hours, from cerebrospinal fluid – 8.5 hours.

Indications

Active ingredient

Composition

1 film-coated tablet contains:

acting substances:

vinpocetine 10 mg,

piracetam 800 mg;

excipients:

calcium hydrophosphate dihydrate 120 mg,

croscarmellose sodium (primellose) 33 mg,

magnesium stearate 7 mg,

povidone 21 mg,

talc 7 mg,

Microcrystalline cellulose 102 mg;

composition of the film coating:

Opadray II brown 35 mg, including: Hypromellose (hydroxypropyl methylcellulose) 9.8 mg, macrogol (polyethylene glycol) 3.5 mg, lactose monohydrate (milk sugar) 12.6 mg, iron oxide red dye 3.08 mg, iron oxide black dye 5.985 mg, titanium dioxide 0.035 mg.

How to take, the dosage

The course of treatment and dosage is determined by the attending physician.

For patients 18 years and older: orally, regardless of meals, 1 tablet 2 to 3 times a day with enough water. The last dose four hours before sleep. The duration of the treatment course is from 2-3 weeks to 2-6 months.

Before we stop the drug it is recommended to decrease the dose gradually (it is possible to use Winpotropil® in other dosage form: capsules containing 5 mg of Vinpocetine and 400 mg of Piracetam).

Interaction

Increases: the risk of hemorrhagic complications against heparin therapy, the effects of thyroid hormones, antipsychotic drugs (neuroleptics), psychostimulants, indirect anticoagulants, including acenocoumarol (more pronounced reduction of platelet aggregation, fibrinogen, Willebrand factor, plasma and blood viscosity).

Some increase of the hypotensive effect is possible with concomitant use with methyldopa (blood pressure control is necessary).

Weakens: the effect of anticonvulsants (reduces the seizure threshold).

While there is no data to support the possibility of interaction, caution is recommended when concomitant administration with drugs of central, antiarrhythmic action.

Special Instructions

The presence of prolonged QT interval syndrome and the use of drugs that cause prolongation of the QT interval require periodic ECG monitoring.

Due to the effect of Piracetam on platelet aggregation, caution is recommended when prescribing the drug in patients with impaired hemostasis, during major surgery or in patients with symptoms of severe bleeding.

Effect on driving and operating machinery

Caution should be exercised when driving and operating machinery during treatment.

Contraindications

With caution:
Hemostasis disorder, major surgical interventions, severe bleeding, CKD (CK 20-80 ml/min).

Side effects

Cardiovascular system: ECG changes (ST-segment depression, Q-T interval prolongation), tachycardia, extrasystole, blood pressure (BP) lability (often decrease).

The central nervous system (CNS): motor agitation, irritability, depression, asthenia, dizziness, headache, sleep disorders (insomnia, hypersomnia), mental agitation, loss of balance, worsening of epilepsy, anxiety, hallucinations, confusion, extrapyramidal disorders, reduced ability to concentrate.

Digestive system disorders: nausea, vomiting, heartburn, diarrhea, abdominal pain, decreased appetite, gastralgia, constipation.

Metabolism disorders: weight gain, increased sweating.

Sensory organs: vertigo.

Skin disorders: dermatitis, itching, urticaria, skin hyperemia.

Allergic reactions: hypersensitivity, anaphylactic reactions, angioedema.

Local reactions: pain at the injection site, thrombophlebitis.

Other: fever, general weakness (may be a manifestation of the underlying disease), increased sexual activity.

Overdose

Symptoms: abdominal pain, diarrhea with blood.

Treatment: symptomatic therapy, hemodialysis (effectiveness 50-60%).

Pregnancy use

The drug is contraindicated in pregnancy and lactation.