Piracetam, 400 mg 60 pcs

Pharmacotherapeutic group: Nootropic agent.

ATX code: N06BX03.
Pharmacological properties

Pharmacodynamics

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

The evidence suggests that the underlying mechanism of action of piracetam is not cell-specific or organ-specific.

Piracetam binds to the polar heads of phospholipids and forms mobile drug-phospholipid complexes. As a result, the two-layer structure of the cell membrane and its stability are restored, which in turn leads to restoration of the three-dimensional structure of membrane and transmembrane proteins and restoration of their function.

At the neuronal level, piracetam facilitates various types of synaptic transmission with a preferential effect on the density and activity of postsynaptic receptors (data obtained in animal studies). Piracetam improves such functions as learning, memory, attention and consciousness without any sedative or psychostimulant effects.

Hemorheological effects of Piracetam are associated with its effect on red blood cells, platelets and the vascular wall.

In patients with sickle cell anemia, piracetam increases the ability of red blood cells to deform, reduces blood viscosity and prevents the formation of “coin columns”. In addition, it reduces platelet aggregation without significantly affecting their number.

Piracetam has been shown in animal studies to inhibit vasospasm and counteract various vasospastic agents.

In studies on healthy volunteers, piracetam reduced erythrocyte adhesion to the vascular endothelium and stimulated prostacyclin production by healthy endothelium.

Pharmacokinetics

Intake.

After oral administration, piracetam is rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability of piracetam is close to 100%. After a single dose of 3.2 g, maximum concentration (Cmax) is 84 mcg/ml, after 3.2 mg 3 times daily – 115 mcg/ml, and is reached after 1 hour in plasma and after 5 hours in cerebrospinal fluid. Food intake reduces Cmax by 17% and increases the time of its achievement (Tmax) up to 1.5 hours. In women when receiving piracetam at a dose of 2.4 g the Cmax and area under the curve “concentration – time” (AUC) is 30% higher than in men.

Distribution.

The volume of distribution (Vd) is about 0.6 l/kg. Piracetam penetrates through the blood-brain barrier and the placental barrier. In animal studies it was found that piracetam selectively accumulates in the cortical tissues, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal nuclei.

Metabolism.

It does not bind to plasma proteins and is not metabolized in the body.

Elimination.

The elimination half-life (T1/2) is 4-5 hours from blood 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. T1/2 is prolonged in renal failure (up to 59 hours in terminal chronic renal failure). Pharmacokinetics
piracetam does not change in patients with hepatic impairment.

Indications

– Symptomatic treatment of psychorganic syndrome, particularly in elderly patients, accompanied by decreased memory, dizziness, decreased concentration and activity, mood changes, conduct disorder, and gait disturbances (these symptoms may be early signs of age-related diseases such as Alzheimer’s disease and senile Alzheimer-type dementia);

– Treatment of vertigo and related balance disorders, except for vascular and psychogenic vertigo;

– Comprehensive therapy and monotherapy of cortical myoclonias;

– Comprehensive therapy of sickle cell anemia (for prevention of sickle cell vaso-occlusive crisis).

In children:

– Treatment of dyslexia (in combination with other methods);

– Complex therapy of sickle cell anemia (for prevention of sickle cell vaso-occlusive crisis).

Active ingredient

Composition

One capsule contains:

the active ingredient – piracetam – 400 mg,

excipients: stearic acid, sodium lauryl sulfate, magnesium carbonate basic,

coating composition: gelatin, glycerin, sodium lauryl sulfate, titanium dioxide (E171), purified water.

How to take, the dosage

With meals or on an empty stomach with fluids.

Symptomatic treatment of psychoorganic syndrome: 2.4 – 4.8 g/day in 2-3 doses.

The treatment of dizziness and related balance disorder: 2.4 to 4.8 g/day in 2-3 doses.

The treatment of cortical myoclonias: it starts with a dose of 7.2 g/day, every 3-4 days the dose is increased by 4.8 g/day until the maximum dose of 24 g/day in 2 to 3 doses. Treatment is continued throughout the entire period of the disease. Every 6 months, attempts should be made to reduce the dose or to cancel the drug, gradually reducing the dose by 1.2 g/day every 2 days.

The treatment of sickle cell anemia: The daily prophylactic dose is 160 mg/kg body weight divided into 4 equal doses.

The treatment of dyslexia in children (in combination with other treatments): the recommended daily dose for children from 8 years and adolescents is 3.2 g divided into 2 doses.

Dosing in patients with impaired renal function: the dose should be adjusted according to creatinine clearance (CK) values:
Creatinine clearance for men can be calculated based on serum creatinine concentration using the following formula:

The creatinine clearance for women can be calculated by multiplying the resulting value by a factor

Elderly patients have the dose adjusted in the presence of renal insufficiency, with prolonged therapy, monitoring of renal function is necessary.

Dosage to patients with impaired liver function:
Patients with impaired liver function do not require dose adjustment. Patients with impaired both renal and liver function, dosing is according to the scheme.

Interaction

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

According to the published study in patients with recurrent venous thrombosis the dose of piracetam 9.6 g/day improves the effectiveness of indirect anticoagulants (more significant decreases of platelet aggregation, fibrinogen, Willebrand factors, blood viscosity and plasma level were noted in comparison with application of indirect anticoagulants only).

In vitro, piracetam does not inhibit cytochrome P450 isoenzymes such as CYP1A2, 2B6, 2C8, 2C9, 2C19, 2B6, 2E1 and 4A9/11 at 142, 426 and 1422 µg/mL. A slight inhibition of CYP2A6 (21%) and ZA4/5 (11%) was observed at the concentration of 1422 µg/ml, but Ki levels of these two isoenzymes are sufficient above 1422 µg/ml, in connection with which a metabolic interaction with other drugs is unlikely.

The administration of piracetam at a dose of 20 g/day for 4 weeks did not alter the maximum serum concentration and area under the concentration-time curve of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital, valproic acid).

Co-administration with alcohol had no effect on serum concentrations of piracetam; serum ethanol concentrations were not altered when 1.6 g of piracetam was taken.

Special Instructions

In the treatment of cortical myoclonias, abrupt interruption of treatment should be avoided as it may cause a recurrence of seizures.

In the treatment of sickle cell anemia, a dose of less than 160 mg/kg or irregular administration of the drug may cause exacerbation of the disease.

Permeasures through the filter membranes of hemodialysis machines.

Contraindications

With caution: impaired hemostasis; extensive surgical interventions; severe bleeding; chronic renal failure (with creatinine clearance 20-80 ml/min).

Side effects

Digestive system disorders: nausea, vomiting, diarrhea, abdominal pain (including gastralgia).

Metabolic disorders: weight gain.

Hearing disorders: vertigo.

Skin disorders: dermatitis, itching, urticaria.

Allergic reactions: angioedema, hypersensitivity, anaphylactic reactions.

Overdose

Treatment: in case of significant overdose, gastric lavage or vomiting should be induced. Symptomatic therapy is recommended, which may include hemodialysis. There is no specific antidote. The effectiveness of hemodialysis for piracetam is 50-60%.

Pregnancy use

Similarities