Nootropil 200 mg/ml 5 ml, 12 pcs.

Pharmacotherapeutic group:

Notropic agent.

ATC code: N06BX03.

Pharmacological properties

Pharmacodynamics.

The active ingredient is piracetam, a cyclic derivative of gamma-aminobutyric acid (GABA).

Piracetam is a nootropic which directly affects the brain, improving cognitive (learning) processes such as learning ability, memory, attention, and mental performance. Piracetam affects the central nervous system in different ways: by changing the rate of propagation of excitation in the brain, improving metabolic processes in nerve cells, improving microcirculation, affecting rheological characteristics of the blood and causing no vasodilator effect.

It improves connections between the cerebral hemispheres and synaptic conduction in the neocortical structures, increases mental performance, improves cerebral blood flow.

Piracetam inhibits platelet aggregation and restores the elasticity of the red blood cell membrane, reduces red blood cell adhesion. At a dose of 9.6 g, it reduces the level of fibrinogen and Willebrand factors, by 30-40% and prolongs the bleeding time.

Piracetam has a protective and restorative effect in disorders of brain function due to hypoxia and intoxication.

Piracetam reduces the severity and duration of vestibular nystagmus.

Pharmacokinetics.

The elimination half-life of the drug from plasma is 4-5 hours and 8.5 hours from cerebrospinal fluid, which is prolonged in renal insufficiency.

The pharmacokinetics of piracetam is not changed in patients with hepatic insufficiency.

It penetrates through the blood-brain and placental barriers and membranes used in hemodialysis. In animal studies piracetam selectively accumulates in cortical tissues, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal ganglia. It does not bind with blood plasma proteins, is not metabolized in the body and is excreted unchanged by the kidneys by renal filtration. Renal clearance of piracetam in healthy volunteers is 86 ml/min.

Indications

Active ingredient

Composition

One ampoule contains:

the active substance: piracetam – 1 g/5 ml;

excipients: sodium acetate trihydrate, glacial acetic acid, water for injection.

How to take, the dosage

Interaction

Piracetam increases the effectiveness of thyroid hormones and antipsychotic drugs (neuroleptics). When administered simultaneously with neuroleptics, piracetam reduces the risk of extrapyramidal disorders. When concomitant use with drugs which have stimulating effect on CNS, strengthening of the stimulating effect on CNS is possible.

No interaction with clonazepam, phenytoin, phenobarbital, valproic acid was noted.

High doses (9.6 g/day) of piracetam increase the efficacy of indirect anticoagulants in patients with venous thrombosis (there was a greater decrease of platelet aggregation, fibrinogen, von Willebrand factors, blood viscosity and plasma level compared to indirect anticoagulants alone).

The possibility of changes in pharmacodynamics of piracetam under the influence of other drugs is low because 90% of the drug is excreted unchanged in the urine.
In vitro piracetam does not inhibit cytochrome Р450 isoenzymes, such as CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9/11 at concentrations of 142, 426 and 1422 mkg/ml. A slight inhibition of CYP2A6 (21%) and 3A4/5 (11%) was observed at the concentration of 1422 µg/ml, but Ki levels of these two isoenzymes are sufficient above 1422 µg/ml, due to which metabolic interaction with other drugs is unlikely.

The administration of piracetam at a dose of 20 mg/day did not alter the peak and serum concentration curve of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital, valproic acid) in epilepsy patients receiving a constant dose.

Co-administration with alcohol had no effect on serum concentrations of piracetam, and serum alcohol concentrations were not altered by 1.6 g of piracetam.

Special Instructions

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. When treating patients with cortical myoclonias, abrupt interruption of treatment should be avoided, which may cause recurrence of seizures.

In long-term therapy of elderly patients, regular monitoring of renal function parameters is recommended; if necessary, the dose should be adjusted depending on the results of creatinine clearance study.

Bearing in mind the possible side effects, caution should be exercised when operating machinery and driving a vehicle. It penetrates through the filter membranes of hemodialysis machines.

Contraindications

Psychomotor agitation at the time of prescribing the drug.

Gentington’s chorea.

Acute impairment of cerebral circulation (hemorrhagic stroke).

End-stage renal failure (with creatinine clearance less than 20 ml/min).

Children under 3 years of age.

With caution:

Side effects

CNS and peripheral nervous system disorders: motor disinhibition (1.72%), irritability (1.13%), somnolence (0.96%), depression (0.83%), asthenia (0.23%).

These side effects occur more frequently in elderly patients who received the drug in doses greater than 2.4 g/day. In most cases it is possible to achieve regression of such symptoms by reducing the dose of the drug. In single cases – dizziness, headache, ataxia, worsening of epilepsy course, extrapyramidal disorders, tremor, lack of balance, decreased ability to concentrate, insomnia, agitation, anxiety, hallucinations, increased libido.

Cardiovascular system disorders: rarely – decreased or increased blood pressure.

Digestive system disorders: in single cases – nausea, vomiting, diarrhea, abdominal pain (including gastralgia).

Metabolism: weight gain (1.29%) – more often in elderly patients who received the drug in dose more than 2.4 g/day.

Skin disorders: dermatitis, itching, rash.

Allergic reactions: angioedema.

Overdose

Pregnancy use

Similarities