Notrocetam, 200 mg/ml 5 ml 10 pcs

Pharmacotherapeutic group: nootropic agent

ATX code: [N06BX03]

Pharmacological properties

Pharmacodynamics

Piracetam is a nootropic drug that affects the central nervous system in different ways: modifies neurotransmission in the brain; improves conditions that promote neuronal plasticity; improves microcirculation, affecting blood rheological characteristics and without causing vasodilation. Piracetam administration in patients with cerebral dysfunction increases attention concentration and improves cognitive functions, which is accompanied by changes on the electroencephalogram (increased α and β activity, reduced δ activity).

It promotes cognitive recovery due to various disorders such as hypoxia, intoxication or electroconvulsive therapy.

Piracetam is indicated for the treatment of cortical myoclonias both as monotherapy and as part of complex therapy. It reduces the duration of induced vestibular neuronitis.

Piracetam inhibits increased aggregation of activated platelets and, in case of pathological erythrocyte stiffness, improves their deformability and filtration capacity.

Pharmacokinetics

The pharmacokinetic profile of piracetam is linear and independent of time. Low variability over a large dose range is characteristic.

The steady-state plasma concentration is reached 3 days after the start of administration. The volume of distribution (Vd) is about 0.6 l/kg. Piracetam penetrates through the blood-brain and placental barriers, as well as hemodialysis membranes.

In animal studies it was found that piracetam selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal nuclei.

It is not bound to plasma proteins, is not metabolized in the body and is excreted unchanged by the kidneys. Period of half-life (T1/2) is 4-5 hours from plasma and 8.5 hours from cerebrospinal fluid. The elimination half-life does not depend on the route of administration.

80-100 % of piracetam is excreted unchanged by the kidneys through glomerular filtration. Total clearance of piracetam in healthy volunteers is 80-90 ml/min. Renal excretion is almost complete (> 95%) within 30 h.

The T1/2 is prolonged in renal insufficiency (in terminal chronic renal failure up to 59 h). Pharmacokinetics of piracetam does not change in patients with hepatic insufficiency.

Indications

– symptomatic treatment of intellectual-mnestic disorders in the absence of an established diagnosis of dementia;

– reducing the manifestations of cortical myoclonus in patients sensitive to piracetam, both as monotherapy and as part of complex therapy (in order to determine sensitivity to piracetam in a particular case, a trial course of treatment can be carried out).

Pharmacological effect

Pharmacotherapeutic group: nootropic agent

ATX code: [N06BX03]

Pharmacological properties

Pharmacodynamics

Piracetam is a nootropic drug that affects the central nervous system in various ways: it modifies neurotransmission in the brain; improves conditions conducive to neuronal plasticity; improves microcirculation, affecting the rheological characteristics of the blood and without causing vasodilation. The use of piracetam in patients with cerebral dysfunction increases concentration and improves cognitive function, which is accompanied by changes in the electroencephalogram (increased α and β activity, decreased δ activity).

Promotes the restoration of cognitive functions due to various disorders, such as hypoxia, intoxication or electroconvulsive therapy.

Piracetam is indicated for the treatment of cortical myoclonus both as monotherapy and as part of complex therapy. Reduces the duration of induced vestibular neuronitis.

Piracetam inhibits increased aggregation of activated platelets and, in the case of pathological rigidity of red blood cells, improves their deformability and filtration ability.

Pharmacokinetics

The pharmacokinetic profile of piracetam is linear and independent of time. Characterized by low variability over a wide dose range.

Constant plasma concentrations are achieved 3 days after the start of administration. The volume of distribution (Vd) is approximately 0.6 l/kg. Piracetam penetrates the blood-brain and placental barriers, as well as hemodialysis membranes.

In animal studies, it was found that piracetam selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal ganglia.

Does not bind to blood plasma proteins, is not metabolized in the body and is excreted unchanged by the kidneys. The half-life (T1/2) is 4-5 hours from plasma and 8.5 hours from cerebrospinal fluid. The half-life does not depend on the route of administration.

80-100% of piracetam is excreted unchanged by the kidneys through glomerular filtration. The total clearance of piracetam in healthy volunteers is 80-90 ml/min. Renal excretion is almost complete (>95%) within 30 hours.

T1/2 is prolonged in case of renal failure (in case of end-stage chronic renal failure – up to 59 hours). The pharmacokinetics of piracetam does not change in patients with liver failure.

Special instructions

Due to the antiplatelet effect, piracetam should be administered with caution to patients with severe hemorrhagic disorders, risk of bleeding (for example, gastric ulcers), hemostasis disorders, a history of hemorrhagic cerebrovascular disorders, in patients with surgical interventions, including dental procedures, in patients taking anticoagulants and antiplatelet agents, including low doses of aspirin.

When treating cortical myoclonus, abrupt interruption of treatment should be avoided, as this may cause resumption of attacks.

Since piracetam is excreted through the kidneys, caution should be exercised when prescribing the drug to patients with renal failure.

During long-term treatment of elderly patients, regular monitoring of creatinine clearance is necessary, because Dose adjustment may be required.

Piracetam penetrates through the filter membranes of hemodialysis machines.

Impact on the ability to drive vehicles and machinery

During the treatment period, care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Piracetam

Composition

For 1 ml:

Pregnancy

Pregnancy

There are no sufficient data on the use of the drug during pregnancy. Animal studies have not shown direct or indirect effects on pregnancy, embryo/fetal development, childbirth 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 prescribed during pregnancy only in exceptional cases, if the benefit to the mother outweighs the potential risk to the fetus, and the clinical condition of the pregnant woman requires treatment with piracetam.

Breastfeeding

Piracetam passes into breast milk. Piracetam should not be used during breastfeeding or breastfeeding should be discontinued while being treated with piracetam. When deciding whether to stop breastfeeding or refuse treatment with piracetam, the benefits of breastfeeding for the child should be weighed against the benefits of therapy for the woman.

Contraindications

– individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug;

– psychomotor agitation at the time of drug prescription;

– Huntington’s chorea;

– acute cerebrovascular accident (hemorrhagic stroke);

– end-stage renal failure (with creatinine clearance less than 20 ml/min);

– children under 18 years of age.

With caution

Use caution in patients with severe hemorrhagic disorders, risk of bleeding (for example, with a stomach ulcer), hemostasis disorders, a history of hemorrhagic cerebrovascular disorders, in patients with surgical interventions, including dental interventions, in patients taking anticoagulants and antiplatelet agents, incl. low doses of acetylsalicylic acid. Caution should be exercised when prescribing the drug to patients with renal failure.

Side Effects

The adverse drug reactions listed below were identified in clinical studies and based on the results of post-registration surveillance and are grouped by system-organ classes. The frequency gradation is determined as follows:

very common (≥ 10%), common (≥ 1% and < 10%), uncommon (≥ 0.1% and < 1%), rare (≥ 0.01% and < 0.1%), very rare (< 0.01%) and frequency unknown (cannot be estimated from available clinical trial data).

In post-registration use, due to insufficient data, it is impossible to estimate the frequency.

From the blood and lymphatic system:

frequency unknown – bleeding.

From the immune system:

frequency unknown – anaphylactoid reactions, hypersensitivity.

From the mental side:

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.

Hearing and labyrinth disorders:

frequency unknown – vertigo.

From the side of blood vessels:

rarely – thrombophlebitis, arterial hypotension.

From the digestive system:

frequency unknown – abdominal pain, incl. in the upper sections, diarrhea, nausea, vomiting.

For the skin and subcutaneous tissues:

frequency unknown – angioedema, dermatitis, itching, urticaria.

From the reproductive system:

frequency unknown – increased sexual desire.

General disorders and disorders at the injection site:

infrequently – asthenia;

rarely – pain at the injection site, fever.

Laboratory and instrumental data:

often – weight gain.

If any of the side effects indicated in the instructions get worse or you notice any other side effects not listed in the instructions, tell your doctor.

Interaction

The possibility of changing the pharmacokinetics of piracetam under the influence of other drugs is low, because 90% of piracetam is excreted unchanged by the kidneys.

When used concomitantly with thyroid hormones, there have been reports of confusion, irritability, and sleep disturbances.

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

At concentrations of 142, 426 and 1422 mg/ml, piracetam does not inhibit cytochrome P450 isoenzymes.

For a concentration of 1422 mg/ml, minimal inhibition of CYP 2A6 (21%) and 3A4/5 (11%) was observed. However, normal values ​​of the inhibition constant (Ki) can probably be achieved at higher concentrations. Therefore, the metabolic effects of piracetam with other drugs are unlikely. Taking piracetam at a dose of 20 g/day for 4 weeks in patients with epilepsy receiving stable doses of antiepileptic drugs did not change the maximum serum concentration and AUC (area under the curve) of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and valproate).

Co-administration with alcohol did not affect serum concentrations of piracetam; The concentration of ethanol in the blood serum did not change when taking 1.6 g of piracetam.

Overdose

Increased possible side effects.

First aid is symptomatic therapy, hemodialysis is possible (effectiveness 50-60%). There is no specific antidote.

Storage conditions

In a place protected from light at a temperature not exceeding 25 ºС. Keep out of the reach of children.

Shelf life

5 years.

Do not use after expiration date.

Manufacturer

Velfarm LLC, Russia