Expiration date: 09/2026
Active substance: Piracetam
Pharmachologic effect: nootropic
Pharmacodynamics
Active ingredient - Piracetam, a cyclic derivative of GABA.
Piracetam - nootropic drug that directly improves brain function performed. The drug has an effect on the central nervous system in different ways: modifies neurotransmission in the brain, improves the metabolic conditions that promote neuronal plasticity, improves microcirculation by acting on the rheological properties of blood and causing vasodilation.
Long or short the use of piracetam in patients with cerebral dysfunction increases concentration and improves cognitive function, as manifested by significant changes in the EEG (increased ? and ? activity, decreased activity of ?).
The drug helps restore cognitive abilities after various cerebral damage due to hypoxia, intoxication, or electroconvulsive therapy. Piracetam is indicated for the treatment of cortical myoclonus, both as monotherapy and as part of combination therapy.
It reduces the duration of vestibular neyronita provoked.
Piracetam increased inhibits aggregation of activated platelets and, in the case of pathological erythrocytes rigidity, deformability and improves their ability to filtration.
Pharmacokinetics
Suction. After oral administration Piracetam is rapidly and almost completely absorbed from the gastrointestinal tract. The bioavailability of piracetam is close to 100%. After a single dose of the drug at a dose of 3.2 g of Cmax was 84 mcg / mL after multiple dose 3.2 mg three times a day - 115 .mu.g / ml achieved after 1 h in the blood plasma after 5 hours and - in the cerebrospinal fluid. Ingestion decreases Cmax by 17% and increase the Tmax to 1.5 hours. In women, when receiving a dose of piracetam 2.4 g of Cmax and AUC is 30% higher than in men.
Distribution. It binds to plasma proteins. Vd is about 0.6 liter / kg. Piracetam penetrate the BBB and placental barrier. In animal studies found that piracetam selectively accumulates in the tissues of the brain cortex, predominantly in the frontal, parietal, and occipital lobes in the basal ganglia and cerebellum.
Metabolism. Do not metabolized in the body.
Withdrawal. T1 / 2 4-5 h of blood plasma and 8.5 hours - from cerebrospinal fluid. T1 / 2 is not dependent on the route of administration. 80-100% piracetam excreted by the kidneys in unchanged form by glomerular filtration. Piracetam total clearance in healthy volunteers is 80-90 ml / min. T1 / 2 is prolonged in renal failure (ESRD when - up to 59 hours). Pharmacokinetics piracetam not altered in patients with hepatic failure.
Testimony
Symptomatic treatment of memory disorders, intellectual disorders in the absence of a diagnosis of dementia.
Nootropil has the ability to reduce the symptoms of cortical myoclonus in susceptible patients. For determining sensitivity to a specific case piracetam trial treatment may be conducted.
Contraindications
Hypersensitivity to piracetam or pyrrolidone derivatives, and other ingredients;
- Huntington's chorea;
- acute ischemic stroke (hemorrhagic stroke);
- end-stage chronic renal failure.
Pregnancy and breast-feeding
Preclinical studies have not shown a direct or indirect impact on pregnancy, embryo / fetal, parturition or postnatal development.
Controlled studies of the drug have not been conducted during pregnancy. Piracetam crosses the placental barrier and into breast milk. The concentration of the drug in infants up to 70-90% of its concentration in the blood of the mother. Piracetam should not be administered during pregnancy.
It should refrain from breast-feeding in the appointment of a woman piracetam.
Side effects
From the blood and lymphatic system: hemorrhagic disorders.
Immune system: anaphylactoid reactions, hypersensitivity.
Metabolic and Nutritional Disorders: weight gain (1.29%).
On the part of the psyche: agitation, nervousness (1.13%), anxiety, depression (0.83%), hallucinations, confusion, drowsiness (0.96%).
From the nervous system: hyperkinesis (1.72%), ataxia, balance disorders, exacerbation of epilepsy, headache, insomnia, asthenia (0.23%), tremor.
From the digestive system: nausea, vomiting, diarrhea, abdominal pain (including gastralgia).
From the hearing: vertigo.
For the skin: dermatitis, pruritus, urticaria, angioedema.
Reproductive system: increased sexual desire.
Interaction
The ability to change under the influence of piracetam pharmacokinetics of other drugs is low, since 90% of the drug is excreted unchanged in the urine.
While the use of thyroid hormones noted reports of confusion, irritability and sleep disorders.
According to a study of patients with recurrent venous thrombosis, piracetam at a dose of 9.6 g / day does not change the dose of acenocoumarol necessary to reach INR 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, release of ?-tromboglobina, the concentration of fibrinogen and von Willebrand factor as well as the viscosity of blood and serum.
At concentrations of 142, 426 and 1422 mg / ml Piracetam not inhibit isozymes of cytochrome P450.
For concentrations of 1422 mg / ml of a minimal inhibition was observed CYP2A6 (21%) and 3A4 / 5 (11%). However, larger values ??of the inhibition constant (Ki), may be achieved at higher concentrations. Thus, piracetam metabolic interactions with other drugs are unlikely. Admission piracetam at a dose of 20 g / day for 4 weeks in patients with epilepsy treated with stable doses of antiepileptic drugs, did not change the maximum serum concentration and AUC of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and valproate).
Joint reception of alcohol had no effect on piracetam serum concentration; ethanol concentration in serum did not change when receiving 1.6 g piracetam.
Dosing and Administration
Inside (during meals or on an empty stomach, with some liquid).
Disorders of memory, intellectual impairment: 2,4-4,8 g / day in 2-3 divided doses.
Cortical myoclonus: treatment begins with a dose of 7.2 g / day every 3-4 days to increase the dose of 4.8 g / day to a maximum dose of 24 g / day in 2-3 divided doses. Treatment continued throughout the period of the disease. Every 6 months should be to attempt to reduce the dose or discontinuation of the drug, gradually reducing the dose of 1.2 g / day every 2 days.
Special patient groups
Impaired renal function. The dose should be adjusted depending on the creatinine clearance (see. Table below).
Creatinine clearance for males can be calculated from the serum creatinine concentration (Ksyvorot.), Using the following formula:
Cl creatinine, mL / min = [(140 - age, years) × weight in kg] / (72 × Ksyvorot mg / dL).
Creatinine clearance for females can be calculated by multiplying the resulting value by a factor of 0.85.
| Renal failure | Cl creatinine, ml / min | Dosage |
| None (standard) | > 80 | The usual dose |
| Light | 50-79 | 2/3 usual dose in 2-3 doses |
| Average | 30-49 | 1/3 usual dose in 2 hours |
| Weight | <30 | 1/6 usual dose once |
| The final stage | — | Contraindicated |
Elderly patients adjust the dose in the presence of renal failure, prolonged therapy is necessary to monitor renal function.
Abnormal liver function. Patients with impaired liver function the dose does not need correction. Patients with impaired function and kidney and liver dosing is carried out according to the scheme (see. Impaired Renal Function).
Overdose
Symptoms: registered a single case of dyspepsia in the form of diarrhea with blood and pain in the stomach area while taking the drug orally at a daily dose of '75
Treatment: Immediately after taking the drug should be washed inside the stomach or cause an artificial vomiting. Recommended holding of symptomatic therapy, which may include hemodialysis. No specific antidote. The effectiveness of hemodialysis for piracetam is 50-60%.
Special instructions
Because of antiplatelet effect (see. "Pharmacodynamics"), piracetam should be administered with caution to patients with severe hemorrhagic disorders, risk of bleeding (such as a stomach ulcer), disorders of hemostasis, hemorrhagic cerebrovascular disorders in history, in patients with surgery, including dental procedures, in patients taking anticoagulants and antiplatelet agents, including low-dose acetylsalicylic acid.
Abrupt discontinuation should be avoided in the treatment of cortical myoclonus, because this can cause resumption of seizures.
In the treatment of patients on giponatrievoy diet, it is recommended to take into account that piracetam tablets at a dose of 24 g contains 46 mg of sodium.
As piracetam eliminated via the kidneys, caution should be exercised when administering the drug to patients with renal insufficiency.
With long-term treatment of elderly patients requires regular monitoring of creatinine clearance, as may require dose adjustment.
Piracetam penetrates through the filtration membranes for hemodialysis machines.
Effects on ability to drive and use machines. The treatment should be careful when driving vehicles and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions.
Release Form
Film-coated tablets, 800 mg. The blister PVC / aluminum foil, 15 pieces. 2 blisters in a carton box.
Film-coated tablets, 1200 mg. The blister PVC / aluminum foil, 10 pieces. 2 blisters in a carton box.
Manufacturer
YUSB Pharma SA Chemin du Faure, in 1420 Brian l 'Allues, Belgium.
Storage conditions
In a dry place at a temperature no higher than 25 ° C.
Keep out of the reach of children.
The shelf life: 4 years.
Do not use beyond the expiration date printed on the package.
