Piracetam pills 800mg Renewal, 30pcs

Composition

Per tablet: Active ingredient: piracetam — 800.0 mg.

Excipients (core):

croscarmellose sodium – 12.0 mg,

pregelatinized starch-12.0 mg,

povidone (polyvinylpyrrolidone) – 20.0 mg,

magnesium stearate-8.0 mg.

Excipients (shell):

hypromellose – 15.2 mg,

macrogol-4000-4.0 mg,

titanium dioxide-8.8 mg

Pharmacological action

Pharmacotherapy group: Nootropic agent. ATX code: N06BX03.

Pharmacological properties

Pharmacodynamics

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

The available data suggest that the main mechanism of action of piracetam is not cell-specific or organ-specific.

Piracetam binds to the polar phospholipid heads 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 the restoration of the three-dimensional structure of membrane and transmembrane proteins and the restoration of their function.

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

The hemorheological effects of piracetam are related to 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.

Animal studies have shown that piracetam inhibits vasospasm and counteracts various vasospastic substances.

In studies on healthy volunteers, piracetam reduced the adhesion of red blood cells to the vascular endothelium and stimulated the production of prostacyclines by healthy endothelium.

Pharmacokinetics

Suction.

After oral use, piracetam is rapidly and almost completely absorbed from the gastrointestinal tract. The bioavailability of piracetam is close to 100%. After a single dose of 3.2 g, the maximum concentration (Cmax) is 84 mcg/ml, after repeated use of 3.2 mg 3 times a day – 115 mcg/ml and is reached after 1 hour in blood plasma and after 5 hours in the cerebrospinal fluid. Food intake reduces Cmax by 17% and increases the time to reach it (Tmax) to 1.5 hours. In women, when taking piracetam at a dose of 2.4 g, the cmax and area under the concentration – time curve (AUC) are 30% higher than in men.

Distribution.

The volume of distribution (Vd) is about 0.6 l / kg. Piracetam penetrates the blood-brain and placental barriers. 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.

Metabolism.

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

Output.

The elimination half-life (T 1/2) is 4-5 hours from blood 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. T 1/2 is prolonged in case of renal failure (in case of end-stage chronic renal failure – up to 59 hours). The pharmacokinetics of Piracetam do not change in patients with hepatic insufficiency.

Indications

For adults:

– Symptomatic treatment of psycho-organic syndrome, particularly in elderly patients, accompanied by memory loss, dizziness, decreased concentration and decreased activity, change of mood, behavior disorder, with gait disturbance (these symptoms may be early signs of age-related diseases, such as Alzheimer’s disease and senile dementia of Alzheimer’s type);

– Treatment of vertigo and associated disorders of balance, with the exception of vascular and psychogenic dizziness;

– Complex therapy and monotherapy cortical myoclonia;

– Complex therapy of sickle cell anaemia (to prevent sickle cell crisis vasoocclusive).

For children:

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

– Complex therapy of sickle-cell anemia (for the prevention of sickle-cell vasoocclusive crisis).

Use during pregnancy and lactation

Controlled studies of the use of the drug during pregnancy have not been conducted. Piracetam penetrates through the placental barrier and into breast milk. The concentration of the drug in newborns reaches 70-90% of its concentration in the blood of the mother. Piracetam should not be given during pregnancy. During lactation, you should decide whether to stop breastfeeding.

Contraindications

-Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug;- Psychomotor agitation at the time of drug use;- Huntington’s chorea; – Acute cerebrovascular accident (hemorrhagic stroke);- End-stage renal failure (with creatinine clearance less than 20 ml / min);- Children under 3 years of age.

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

Side effects

Nervous system disorders:  motor disinhibition, irritability, drowsiness, depression, asthenia, headache, insomnia, agitation, imbalance, ataxia, exacerbation of epilepsy, anxiety, hallucinations, confusion.

From the digestive system:  nausea, vomiting, diarrhea, abdominal pain (including gastralgia).

From the side of metabolism:  weight gain.

From the side of the hearing organs:  vertigo.

From the side of the skin:  dermatitis, pruritus, urticaria.

Allergic reactions:  angioedema, hypersensitivity, anaphylactic reactions.

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 in patients with recurrent venous thrombosis, piracetam at a dose of 9.6 g/day increases the effectiveness of indirect anticoagulants (there was a more pronounced decrease in platelet aggregation, fibrinogen levels, Von Willebrand factors, blood and plasma viscosity compared to the use of indirect anticoagulants alone).

In vitro, piracetam does not inhibit cytochrome P 450 isoenzymes such as CYP1A2,2B6,2C8,2C9,2C19,2B6,2e1and 4A9/11 at concentrations of 142,426 and 1422 mcg / ml. At a concentration of 1422 mcg/ml, there was a slight inhibition of CYP2A6 (21%) and OVER 4/5 (11%), but the Ki level of these two isoenzymes is sufficient when exceeding 1422 mcg/ml, and therefore metabolic interaction with other drugs is unlikely.

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

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, course of use and dosage

Inside.

During a meal or on an empty stomach, washed down with liquid.

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

Treatment of dizziness and related balance disorders: 2.4-4.8 g / day in 2-3 doses.

Treatment of cortical myoclonia: start with a dose of 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 in 2-3 doses. Treatment is continued throughout the entire period of the disease. Every 6 months, attempts should be made to reduce the dose or discontinue the drug, gradually reducing the dose by 1.2 g / day every 2 days.

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

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

Dosage in patients with impaired renal function: 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 for women can be calculated by multiplying the obtained value by the coefficient

In elderly patients, the dose is adjusted in the presence of renal insufficiency, with long-term therapy, monitoring of the functional state of the kidneys is necessary.

Dosage in patients with impaired liver function:patients with impaired liver function do not need to adjust the dose. Patients with impaired renal and hepatic function, dosage is carried out according to the scheme.

Overdose

Symptoms: diarrhea mixed with blood, abdominal pain.

Treatment: in case of a significant overdose, you should flush the stomach or induce vomiting. Symptomatic therapy, which may include hemodialysis, is recommended. There is no specific antidote. The effectiveness of hemodialysis for piracetam is 50-60%.

Special instructions

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

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

Penetrates through the filter membranes of hemodialysis machines.

Influence on the ability to drive vehicles and work with 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 dark place at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date.

Active ingredient

Piracetam

Conditions of release from pharmacies

By prescription

Dosage form

Tablets