Notrocetam solution 200mg/ml ampoules 5ml, 10pcs

Composition

Per 1 ml:

Active ingredient: piracetam – 200 mg.

Excipients: sodium acetate trihydrate (sodium acetic acid 3-water), acetic acid diluted 30%, water for injection.

Pharmacological action

Pharmacotherapeutic group: nootropic agent

ATX code: [N06BX03]

Pharmacological properties

Pharmacodynamics

Piracetam is a nootropic agent that affects the central nervous system in various ways: it modifies neurotransmission in the brain; improves conditions that promote neuronal plasticity; improves microcirculation, affecting the rheological characteristics of the blood and not causing vasodilation. The use of piracetam in patients with cerebral dysfunction increases concentration and improves cognitive functions, which is accompanied by changes in the electroencephalogram (increased α and β activity, decreased δ activity).

Promotes recovery 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 ability to filter.

Pharmacokinetics

The pharmacokinetic profile of piracetam is linear and independent of time. It is characterized by low variability in a large dose range.

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

Animal studies have shown 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.

It does not bind to plasma proteins, is not metabolized in the body and is excreted unchanged by the kidneys. The elimination half-life (T 1/2) is 4-5 hours from plasma and 8.5 hours from cerebrospinal fluid. The elimination half-life is independent of the route of use.

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 h. >

T 1/2 is prolonged in case of renal failure (in case of end-stage chronic renal failure – up to 59 h). The pharmacokinetics of piracetam do not change in patients with hepatic insufficiency.

Indications

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

– reduction of cortical myoclonia manifestations in patients sensitive to piracetam, both as monotherapy and as part of complex therapy (in order to determine sensitivity to piracetam, a trial course of treatment may be performed in a particular case).

Use during pregnancy and lactation

Pregnancy

There are no sufficient data on the use of the drug 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 breast-feeding should be discontinued when treated 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

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

– psychomotor agitation at the time of use of the drug;

– 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, gastric ulcers), hemostatic disorders, a history of hemorrhagic cerebrovascular disorders, in patients with surgical procedures, including dental procedures, in patients taking anticoagulants and antiplatelet agents, including low doses of acetylsalicylic acid. Caution should be exercised when prescribing the drug to patients with renal insufficiency.

Side effects

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

very common (≥ 10%), common (≥ 1% and < 10%), infrequent (≥ 0.1% and < 1%), rare (≥ 0.01% and < 0.1%), very rare (

With post-marketing use, due to insufficient data, it is impossible to estimate the frequency.

Blood and lymphatic system disorders:

frequency unknown-bleeding.

From the immune system:

frequency unknown – anaphylactoid reactions, hypersensitivity.

From the side of the psyche:

often – nervousness; infrequently-depression;

frequency unknown-agitation, anxiety, confusion, hallucinations.

Nervous system disorders:

often – hyperactivity; infrequently-drowsiness;

frequency unknown – ataxia, balance disorders, exacerbation of epilepsy, headache, insomnia, tremor.

Hearing disorders and labyrinth disorders:

frequency unknown-vertigo.

From the side of blood vessels:

rarely-thrombophlebitis, hypotension.

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 side of 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 listed 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, since 90% of piracetam is excreted unchanged by the kidneys.

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

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 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 blood and serum.

At concentrations of 142,426, and 1422 mg/ml, piracetam does not inhibit cytochrome P 450 isoenzymes.

At a concentration of 1422 mg/ml, minimal inhibition of SUR was observed for 2A6 (21%) and 3A 4/5 (11%). However, normal values of the inhibition constant (Ki) can probably be achieved at a higher concentration. Thus, 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 who received 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 valproates).

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

How to take it, course of use and dosage

Either intravenously or intramuscularly.

Parenteral use of piracetam is prescribed when it is impossible to use oral forms of the drug (unconsciousness, difficulty swallowing).

Intravenous use is preferred.

Intravenous infusion of a daily dose is performed through a catheter at a constant rate for 24 hours a day (for example, in the initial stage of treatment of severe myoclonia).

Previously, the drug is diluted in one of the compatible infusion solutions: dextrose 5%,10% or 20%;

fructose 5%,10%,20%; sodium chloride 0.9%;

dextran 40 10% (in a solution of sodium chloride 0.9%);

Ringer’s solution; mannitol solution 20%.

The total volume of the solution intended for use is determined taking into account the clinical indications and the patient’s condition.

Intramuscularly, the drug is administered if the introduction through a vein is difficult or the patient is overexcited. The volume of the solution administered intramuscularly should not exceed 5 ml. The frequency of use of the drug is similar to that of its intravenous or oral use.

If possible, switch to oral use of the drug (see the instructions for medical use of the corresponding dosage forms).

The duration of treatment is determined by the doctor depending on the disease and taking into account the dynamics of symptoms.

For memory disorders, intellectual disabilities:

2.4-4.8 g / day in several doses during the first few weeks, then switch to maintenance therapy 2.4 g / day in 2-3 doses, it is possible to take 1.2 g/day. Treatment of cortical myoclonia:

treatment begins with 7.2 g / day, every 3-4 days the dose is increased by 4.8 g / day until a maximum dose of 24 g/day is reached, divided into 2-3 injections. The dose of other drugs for the treatment of myoclonia is not changed. In the future, based on the results of treatment, it is necessary, if possible, to reduce the dose of medications for the treatment of myoclonia.

After starting treatment with piracetam, treatment is continued as long as the symptoms of the disease persist. In patients with an acute episode, the course of the disease may change over time, so attempts should be made to reduce the dose or discontinue the drug every 6 months. To avoid a sudden relapse, the dose is reduced by 1.2 g every 2 days (in order to prevent the possibility of a sudden relapse of seizures in Lance-Adams syndrome – every 3-4 days).

Elderly patients:

Elderly patients with renal insufficiency should undergo dose adjustment (see “Renal insufficiency”). During long-term treatment, creatinine clearance should be evaluated regularly to determine whether dose adjustment is necessary. Kidney failure:

Piracetam is excreted almost exclusively by the kidneys, and caution should be exercised when treating patients with renal insufficiency or requiring monitoring of renal function.

The elimination half-life increases in direct proportion to the deterioration of renal function and creatinine clearance, and this is also true in elderly patients, whose creatinine excretion depends on age.

The dose should be adjusted depending on the value of creatinine clearance (CC): Creatinine clearance for men can be calculated based on the concentration of serum creatinine, using the following formula:

Creatinine clearance (ml / min) =

72 x Creatinine clearance (mg / dl)

Creatinine clearance for women can be calculated by multiplying the obtained value by a factor of 0.85.

Liver failure:

Patients with isolated hepatic impairment do not need to adjust the dose. In patients with impaired renal and hepatic functions, the dosage is carried out according to the scheme (see the section “Renal failure”).

Overdose

Increased potential side effects.

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

Description

Transparent colorless or slightly yellowish liquid

Special instructions

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

In the treatment of cortical myoclonia, abrupt interruption of treatment should be avoided, as this may cause a resumption of seizures.

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

In long-term treatment of elderly patients, regular monitoring of creatinine clearance is necessary, as dose adjustment may be required.

Piracetam penetrates through the filter membranes of hemodialysis machines.

Influence on the ability to drive vehicles and mechanisms

During treatment, caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

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

Shelf

life is 5 years.

Do not use after the expiration date.

Active ingredient

Piracetam

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion