Vinpocetine concentrate solution for infusion 5mg/ml 2ml ampoules, 10pcs

Composition

One ampoule contains:

Active ingredient:

vinpocetine – 5 mg;

excipients:

ascorbic acid-0.5 mg,

benzyl alcohol-10 mg,

sodium disulfite (sodium metabisulfite) – 1 mg,

sorbitol (sorbitol) – 75 mg,

tartaric acid-3 mg,

water for injection-up to 1 ml

Pharmacological action

Psychostimulant and nootropic mediatx: N. 06. B. X. 18 Vinpocetin Pharmacodynamics :

The mechanism of action of vinpocetine consists of several elements: it improves cerebral blood flow and metabolism, and has a beneficial effect on the rheological properties of blood.

Neuroprotective effect is realized by reducing the adverse cytotoxic effect of excitatory amino acids. Blocks Na and Ca2+channels and NMDA and AMPA receptors. Selectively inhibits Ca2+ – calmodulin-dependent-cGMP-phosphodiesterase. Increases the metabolism of serotonin and norepinephrine in the brain, stimulates the noradrenergic neurotransmitter system and has an antioxidant effect.

Improves microcirculation in the brain by inhibiting platelet aggregation, reducing pathologically increased blood viscosity, increasing red blood cell deformability and inhibiting adenosine reuptake; promotes oxygen transfer to cells by reducing the affinity of red blood cells for it.

Selectively increases cerebral blood flow by reducing cerebral vascular resistance without significantly affecting systemic circulatory parameters (blood pressure (BP), cardiac output, heart rate, total peripheral vascular resistance); does not cause the effect of “stealing”.

Pharmacokinetics:

Distribution

Distribution of radioactively labeled vinpocetine, when administered to rats, the highest radioactivity was detected in the liver and gastrointestinal tract. The maximum concentration in the tissues was observed 2-4 hours after use. The concentration in the brain did not exceed the values found in the blood.

In humans, the binding to plasma proteins is 66%. Bioavailability is about 7%. The volume of distribution is 246.7±88.5 l, 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 apovincamic acid (AVA), which makes up 25-30% of the initial compound. The area under the concentration-time curve of AVC after oral use is twice that of intravenous vinpocetine. Thus, vinpocetine is subject to a pronounced “first pass” effect through the liver.

Other metabolites include: hydroxyvinpocetine, hydroxy-AVA, AVA-dioxyglycinate and their conjugates (sulfates and / or glucuronides). The excretion of unchanged vinpocetine is low (several percent).

If liver or kidney function is impaired, no dose adjustment is required, since vinpocetine does not accumulate.

Deduction

When administered repeatedly at doses of 5 and 10 mg, vinpocetine exhibits linear pharmacokinetics, with steady-state plasma concentrations of 1.2±0.27 and 2.1±0.33 ng / ml, respectively. The human half-life is 4.83±1.29 hours. In studies with radioactively labeled vinpocetine, it was found that excretion by the kidneys and intestines occurs in a ratio of 60: 40%.

In rats and dogs, a high concentration is found in the bile, but significant enterohepatic recirculation is noted.

Pharmacokinetics in special patient groups

Since vinpocetine is primarily intended for the treatment of the elderly, it is necessary to take into account the slowing of distribution and metabolism, as well as elimination in this age group, especially with prolonged use. Based on the results of clinical studies, it was found that the kinetics of vinpocetine in the elderly does not significantly differ from the young, accumulation does not occur.

In cases of impaired liver and kidney function, accumulation is not noted, which allows for long-term therapy.

Indications

Neurology: transient ischemic attack, symptomatic treatment of the consequences of ischemic stroke, vascular vertebrobasilar insufficiency, vascular dementia, cerebral vascular atherosclerosis, post-traumatic, hypertensive encephalopathy.

Ophthalmology: chronic vascular diseases of the retina and choroid of the eye.

Otology: perceptual hearing loss, Meniere’s disease, tinnitus sensation, vascular or toxic (including drug-induced) hearing loss.

Use during pregnancy and lactation

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, its concentration in breast milk of animals exceeded that in the mother’s blood by 10 times. For 1 hour,0.25% of the dose taken penetrates into the milk.

Since vinpocetine penetrates into breast milk and there is no experience of its use in children, use during breastfeeding is contraindicated.

Contraindications

Acute phase of hemorrhagic stroke, severe form of ischemic heart disease, severe cardiac arrhythmias.

Hypersensitivity to vinpocetine or other components of the drug.

Pregnancy, breast-feeding period.

Children under 18 years of age (due to the lack of data from clinical studies).

Side effects

Adverse reactions are classified according to their frequency: very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10000, <1/1000), very rare (

Disorders of the blood and lymphatic system:  rarely-thrombocytopenia, agglutination of red blood cells; very rarely-anemia.

Immune system disorders: very rare – hypersensitivity.

Metabolic and nutritional disorders:  rarely-hypercholesterolemia, diabetes mellitus, decreased appetite; very rarely-anorexia.

Mental disorders: infrequently-euphoria; rarely-anxiety; very rarely-depression, sleep disorders.

Nervous system disorders:  rarely-headache, dizziness, hemiparesis, drowsiness; very rarely-tremor, loss of consciousness, hypotension, pre-syncope.

Visual disturbances:  rarely-hemorrhage in the anterior chamber of the eye, hypermetropia, decreased visual acuity, myopia; very rarely-conjunctival hyperemia, optic disc edema, diplopia.

Hearing and labyrinth disorders:  rarely-hearing impairment, hyperacusis, hypoacusia, vertigo; very rarely-tinnitus.

Cardiac disorders:  rarely-myocardial ischemia/infarction, angina, bradycardia, tachycardia, extrasystole, palpitation; very rarely-heart failure, atrial fibrillation, arrhythmia.

Vascular disorders: rarely-hypotension, hypertension, hot flashes; very rarely-fluctuations in blood pressure, thrombophlebitis.

Disorders of the gastrointestinal tract:  rarely-abdominal discomfort, epigastric pain, dry mouth, nausea; very rarely-hypersecretion of saliva, vomiting, dysphagia, stomatitis.

Pathology of the skin and subcutaneous tissue:  rarely-erythema, hyperhidrosis, urticaria; very rarely-dermatitis, pruritus.

General disorders and reactions at the injection site: rarely-asthenia, malaise, burning sensation and inflammation at the injection site, thrombosis, chest discomfort.

Laboratory disorders: infrequently-decreased blood pressure; rarely-increased blood pressure; hypertriglyceridemia, ST-segment depression, eosinopenia, impaired liver function tests, QT segment prolongation; very rarely-increased LDH, abnormal EEG, PR prolongation.

Interaction

According to the results of clinical studies, drug interactions with beta-blockers (pindolol), clopamide, 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.

Vinpocetine solution is pharmaceutically incompatible with heparin and solutions containing amino acids.

How to take it, course of use and dosage

The drug is intended only for intravenous drip infusion, administered slowly (the infusion rate should not exceed 80 drops / min).

Intravenous use of undiluted drug is not allowed. The infusion solution should be administered within 3 hours of preparation!

To prepare the infusion, you can use a 0.9% sodium chloride solution or solutions containing dextrose.

The initial daily dose is 20 mg in 500 ml of infusion solution. Depending on the tolerance, the dose can be increased to no more than 1 mg/kg/day for 2-3 days. The average duration of treatment is 10-14 days.

The average daily dose for a body weight of 70 kg is 50 mg.

No dose adjustment is required for liver or kidney diseases.

After the end of the course of parenteral use, they switch to oral use of the drug (10 mg 3 times a day). Before discontinuing the drug, the dose should be gradually reduced.

Description

Clear, colorless or slightly greenish liquid.

Special instructions

The drug should be used with caution in patients with intracranial hypertension, when used simultaneously with antiarrhythmic drugs, as well as in patients with prolonged QT interval syndrome or when used simultaneously with drugs that prolong the QT interval. ECG monitoring should be performed in patients with prolonged QT syndrome or concomitant use of drugs that prolong the QT interval.

Influence on the ability to drive vehicles and mechanisms:

Studies on the effect on the ability to drive vehicles have not been conducted. In case of adverse reactions from the nervous system, care should be taken when driving vehicles and working with moving mechanisms.

Form of production

Concentrate for preparation of infusion solution,5 mg / ml.

Storage conditions

Keep out of the reach of children in a dark place, at a temperature not exceeding 25 °C.

Shelf

life is 2 years.

Do not use after the expiration date.

Active ingredient

Vinpocetine

Conditions of release from pharmacies

By prescription

Dosage form

concentrate for infusion solution preparation