Instructions for Piracetam-Darnitsa tablets 400 mg No. 30
Composition
active ingredient: piracetam;
1 tablet contains piracetam 400 mg;
excipients: crystalline sugar, microcrystalline cellulose, potato starch, talc, colloidal anhydrous silicon dioxide, magnesium stearate.
Dosage form
Pills.
Main physicochemical properties: tablets of white or white with a creamy tint, marbling is allowed, with a flat surface, with a chamfer and a score.
Pharmacotherapeutic group
Psychostimulants and nootropics.
ATX code N06B X03.
Pharmacological properties
Pharmacodynamics.
Piracetam is a nootropic that acts on the brain, improving cognitive processes such as learning ability, memory, attention, and mental performance. Piracetam affects the central nervous system in various ways: by changing the speed of propagation of excitation in the brain, improving metabolic processes in nerve cells, improving microcirculation, and positively affecting the rheological characteristics of the blood. At the same time, it does not have a vasodilating effect.
Improves connections between the cerebral hemispheres and synaptic conduction in non-cortical structures. Piracetam inhibits platelet aggregation and restores the elasticity of the erythrocyte membrane, reduces erythrocyte adhesion. At a dose of 9.6 g, it reduces the level of fibrinogen and von Willebrand factors by 30–40% and prolongs bleeding time. Piracetam has a protective and restorative effect in impaired brain function due to hypoxia and intoxication. Piracetam reduces the severity and duration of vestibular nystagmus.
Pharmacokinetics.
After oral administration, piracetam is rapidly and almost completely absorbed, with peak concentrations achieved 1 hour after administration. The bioavailability of the drug is approximately 100% after a single dose of 2 g. The volume of distribution of piracetam is approximately 0.6 l/kg. The half-life of the drug from blood plasma is 4–5 hours and 8.5 hours from cerebrospinal fluid, which is prolonged in renal failure. It does not bind to plasma proteins and is not metabolized in the body. 80–100% of piracetam is excreted unchanged by the kidneys by renal filtration. The renal clearance of piracetam in healthy volunteers is 86 ml/min. The pharmacokinetics of piracetam does not change in patients with hepatic failure. Piracetam penetrates the blood-brain and placental barriers and membranes used in hemodialysis.
Indication
Adults:
symptomatic treatment of pathological conditions accompanied by memory impairment and cognitive disorders, with the exception of diagnosed dementia;
Treatment of cortical myoclonus, as monotherapy or as part of complex therapy.
Contraindication
Hypersensitivity to piracetam or pyrrolidone derivatives, as well as to other components of the drug.
Acute cerebrovascular accident (hemorrhagic stroke).
End-stage renal failure.
Huntington's cholera.
Interaction with other medicinal products and other types of interactions
Thyroid hormones.
When used together with thyroid hormones, increased irritability, disorientation, and sleep disturbances are possible.
Acenocoumarol.
Clinical studies have shown that in patients with severe recurrent thrombosis, the use of piracetam in high doses (9.6 g/day) did not affect the dosage of acenocoumarol to achieve a prothrombin time (INR) of 2.5–3.5, but with its simultaneous use, a significant decrease in the level of platelet aggregation, fibrinogen levels, von Willebrand factors (coagulation activity (VIII: C); ristocetin cofactor (VIII: vW: Rco) and plasma protein (VIII: vW: Ag;)), blood viscosity and blood plasma was observed.
Pharmacokinetic interactions.
The likelihood of changes in the pharmacodynamics of piracetam under the influence of other drugs is low, since 90% of the drug is excreted unchanged in the urine.
In vitro, piracetam does not inhibit cytochrome P450 isoforms CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9/11 at concentrations of 142, 426, 1422 μg/ml.
At a concentration of 1422 μg/ml, a slight inhibition of CYP2A6 (21%) and ZA4/5 (11%) was observed. However, the Ki level of these two CYP isomers is sufficient above 1422 μg/ml. Therefore, metabolic interactions with drugs that are biotransformed by these enzymes are unlikely.
Antiepileptic drugs.
The use of piracetam at a dose of 20 g daily for 4 weeks or more did not change the concentration-level curve and maximum concentration (Cmax) of antiepileptic drugs in serum (carbamazepine, phenytoin, phenobarbital, sodium valproate) in patients with epilepsy.
Alcohol.
Co-administration with alcohol did not affect the serum concentration of piracetam, and serum alcohol concentration did not change with a single dose of 1.6 g of piracetam.
In elderly people, piracetam enhances the effect of antianginal drugs and increases the effectiveness of antidepressants.
Application features
Due to the fact that piracetam reduces platelet aggregation (see section "Pharmacological properties"), the drug should be prescribed with caution to patients with impaired hemostasis, conditions that may be accompanied by bleeding (gastrointestinal ulcer), during major surgical operations (including dental interventions), patients with symptoms of severe bleeding or patients with a history of hemorrhagic stroke; patients taking anticoagulants, platelet antiaggregants, including low doses of acetylsalicylic acid. The drug is excreted by the kidneys, so special attention should be paid to patients with renal failure.
Elderly patients.
During long-term therapy in elderly patients, regular monitoring of renal function is recommended, and if necessary, the dose should be adjusted depending on the results of the creatinine clearance study (see section "Method of administration and dosage"). Penetrates through the filtering membranes of hemodialysis machines.
When treating patients with cortical myoclonus, abrupt discontinuation of treatment should be avoided due to the risk of generalization of myoclonus or the occurrence of seizures.
The medicine contains crystalline sugar as an excipient, which should be taken into account by patients with diabetes.
Use during pregnancy or breastfeeding
Pregnancy: There are no data on the use of piracetam in pregnant women. The results of non-clinical studies do not indicate the existence of direct or indirect harmful effects on the course of pregnancy, on the development of the embryo, fetus and postnatal development of the child.
Piracetam crosses the placental barrier. The concentration of the drug in newborns ranges from 70% to 90% of its concentration in the mother. Piracetam should not be used during pregnancy unless clearly necessary, except when the clinical condition of the pregnant mother requires treatment with piracetam and the expected benefit to the mother outweighs the risk to the fetus.
Breastfeeding. Piracetam is excreted in breast milk. It should not be used during breast-feeding, and if necessary, use of the drug should be discontinued. A decision must be made whether to discontinue breast-feeding or to discontinue piracetam therapy taking into account the benefit of breast-feeding for the child and the benefit of therapy for the woman.
Fertility: There are no clinical data on the effects of piracetam on fertility. The results of preclinical studies show that piracetam does not affect fertility in male and female rats.
Ability to influence reaction speed when driving vehicles or other mechanisms
Caution should be exercised when driving or operating other machinery due to the possibility of developing adverse reactions from the central nervous system.
Method of administration and doses
Administer the medicine orally with a small amount of water.
The medicine is for use by adults.
Treatment of conditions accompanied by memory impairment and cognitive disorders.
The initial daily dose is 4.8 g during the first week of treatment. The dose is usually divided into 2–3 doses. The maintenance dose is 2.4 g per day. In the future, a gradual dose reduction of 1.2 g per day is possible.
Treatment of cortical myoclonus.
The initial daily dose is 24 g for 3 days. If during this time the desired therapeutic effect is not achieved, continue using the drug in the same dosage (24 g per day) for up to 7 days. If the desired therapeutic effect is not obtained on the 7th day of treatment, treatment should be discontinued. If the therapeutic effect has been achieved, then starting from the day when a stable improvement is achieved, begin to reduce the dose of the drug by 1.2 g of piracetam every 2 days until the manifestations of cortical myoclonus reappear. This will make it possible to establish an average effective dose. The daily dose should be divided into 2–3 doses.
Treatment with other antimyoclonic drugs is maintained at previously prescribed doses. Treatment should be continued until the symptoms of the disease disappear. To prevent deterioration of the patient's condition, the drug should not be abruptly discontinued. The dose should be gradually reduced by 1.2 g of piracetam every 2–3 days. Repeated courses of treatment with the drug should be prescribed every 6 months, adjusting the dose depending on the patient's condition, until the symptoms of the disease disappear or decrease.
Elderly patients.
Dose adjustment is recommended in elderly patients with known or suspected renal impairment (see section "Patients with renal impairment"). During treatment, creatinine clearance should be monitored in order to adjust the dose appropriately in such patients if necessary.
Patients with renal impairment.
Since the drug is excreted from the body by the kidneys, caution should be exercised when treating patients with renal insufficiency.
Dose calculation should be based on an estimate of the patient's creatinine clearance. Calculate using the formula:
| Creatinine clearance = | . [140 - age (in years)]× body weight (kg) . | (× 0.85 for women) |
| 72 × plasma creatinine concentration (mg/dL) |
Treatment for such patients should be prescribed depending on the severity of renal failure, adhering to the following recommendations:
| Degree of renal failure | Creatinine clearance (ml/min) | Dosage |
| No renal failure | > 80 | Usual dose divided into 2 or 4 doses |
| Light | 50–79 | 2/3 of the usual dose in 2–3 doses |
| Moderate | 30–49 | 1/3 of the usual dose in 2 doses |
| Severe | < 30 | 1/6 of the usual dose once |
| Terminal stage | − | Contraindicated |
Patients with impaired liver function.
No dose adjustment is required for patients with only hepatic impairment. In cases of known or suspected hepatic and renal impairment, dose adjustment should be made as described in the section "Patients with renal impairment".
Children.
Do not apply.
Overdose
Symptoms: increased side effects of the drug. Symptoms of overdose were observed with oral administration of the drug in a dose of 75 g.
Treatment is symptomatic. There is no specific antidote, hemodialysis can be used (removal of 50–60% of piracetam).
Side effects
The frequency is defined as follows: very common (≥ 1/10), common (≥ 1/100 <1/10), uncommon (≥ 1/1000 <1/100), rare (≥ 1/10000 <1/1000), very rare (<1/10000), isolated cases (frequency cannot be estimated from the available data).
| System or organ according to the WHO classification system of organs and systems | Often (≥1/100 to <1/10) | Infrequently (≥1/1000 to <1/100) |
| Nervous system disorders | Hyperkinesia | |
| Metabolic and nutritional disorders | Weight gain | |
| Mental disorders | Nervousness | Depression |
| General disorders | | Asthenia |
Adverse reactions reported during post-marketing surveillance are listed below by system organ class.
From the side of the organs of hearing and vestibular apparatus.
Isolated cases: dizziness.
From the gastrointestinal tract.
Isolated cases: abdominal pain, upper abdominal pain, diarrhea, nausea, vomiting.
From the nervous system.
Common: hyperkinesia.
Uncommon: drowsiness.
Isolated cases: ataxia, balance disorders, increased frequency of epileptic seizures, headache, insomnia, tremor.
From the psychological side.
Common: nervousness.
Uncommon: depression.
Isolated cases: increased excitability, anxiety, confusion, hallucinations.
From the blood and lymphatic system.
Isolated cases: hemorrhagic disorders.
From the immune system.
Isolated cases: hypersensitivity reactions, anaphylactoid reactions.
On the skin and subcutaneous tissue.
Isolated cases of angioedema, dermatitis, rash, urticaria, itching.
On the part of the reproductive system and mammary gland function.
Isolated cases: increased sexual activity.
Research.
Common: weight gain.
Expiration date
3 years.
Storage conditions
Store in the original packaging out of the reach of children at a temperature not exceeding 25 °C.
Packaging
10 tablets in a contour blister pack; 3 contour blister packs in a pack.
Vacation category
According to the recipe.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Address
Ukraine, 02093, Kyiv, Boryspilska St., 13.
