Piracetam, 200 mg capsules 60 pcs

Pharmacotherapeutic group:

Notropic agent.

ATX code

[N06BX03].

Pharmacological properties

Pharmacodynamics

Piracetam is a cyclic derivative of gamma-aminobutyric acid (GABA), is a nootropic agent that directly affects the brain, improves cognitive processes (learning ability, memory, attention, mental performance). It affects the central nervous system in different ways: it changes the speed of excitation distribution in the brain, improves metabolic processes in nerve cells, improves microcirculation, affecting blood rheological characteristics and does not cause vasodilation.

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 Willibrand factors, prolongs the bleeding time.

It improves interhemispheric connections in the brain and synaptic conduction in the neocortical structures.

Piracetam has a protective and restorative effect in cases of brain dysfunction due to hypoxia and intoxication.

Limits the severity and duration of vestibular nystagmus.

Pharmacokinetics

In oral administration the drug is quickly and almost completely absorbed, the peak concentration is reached 1 hour after administration. The bioavailability of the drug is approximately 100%. After a single dose of 2 g the maximum concentration is 40-60 mcg/ml, which is reached in blood after 30 minutes and after 5 hours in cerebrospinal fluid after intravenous injection. Estimated volume of distribution of piracetam is about 0.6 l/kg. Period of half-life of the drug from plasma is 4-5 hours and 8.5 hours from cerebrospinal fluid, which is prolonged in case of renal insufficiency. Pharmacokinetics of piracetam does not change in patients with hepatic insufficiency.

It penetrates through the blood-brain and placental barrier and membranes used in hemodialysis. In animal studies piracetam selectively accumulates in tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, cerebellum and basal ganglia. It does not bind with blood plasma proteins and is not metabolized in the body. 80-100% of piracetam is excreted unchanged by the kidneys through renal filtration. Renal clearance of piracetam in healthy volunteers is 86 ml/min.

Indications

Symptomatic treatment of psychoorganic syndrome, in particular in elderly patients with memory loss, dizziness, decreased concentration and general activity, mood changes, behavior disorders, gait disturbances, as well as in patients with Alzheimer’s disease and senile dementia of the Alzheimer type.

The consequences of ischemic stroke are speech disorders, emotional disturbances, decreased motor and mental activity.

Chronic alcoholism – for the treatment of psychoorganic and withdrawal syndromes.

The period of recovery from trauma and intoxication of the brain.

Dizziness and related balance disorders, with the exception of vertigo of vasomotor and mental origin.

In the complex therapy of learning disability in children with psychorganic syndrome.

For the treatment of cortical myoclonias as mono- or complex therapy.

In the complex therapy of sickle cell anemia.

Active ingredient

Piracetam

Composition

Active ingredient:

piracetam – 200 mg;

Excipients:

croscarmellose sodium – 6.0 mg,

magnesium stearate – 2.0 mg,

povidon-K17 – 5.0 mg;

Composition of the capsule body: titanium dioxide – 2.0%, gelatin to 100%;

Composition of the capsule cap: iron oxide black dye – 0.53%, iron oxide red dye – 0.93%, iron oxide yellow dye – 0.2%, titanium dioxide – 0.3333%, gelatin to 100%.

.

How to take, the dosage

Ingestion.

With a meal or on an empty stomach with fluids.

In case of memory disorders, intellectual disorders:

2.4 – 4.8 g/day in 2-3 doses.

The treatment of cortical myoclonias:

The treatment 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 -3 doses. Treatment is continued throughout the entire period of the disease. Every two months, attempts should be made to reduce the dose or cancel the drug, gradually reducing the dose by 1.2 g/day every two days.

Dosing in patients with impaired renal function:

The dose should be adjusted according to creatinine clearance (CK):

The creatinine clearance for men can be calculated based on serum creatinine concentration using the following formula:

CK (ml/min) = [140 – age (years) x body weight (kg)]/[72 x CK serum creatinine (mg/mL)]

Creatinine clearance for women can be calculated by multiplying the resulting value by a factor of 0.85.

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

Dosing in patients with impaired liver function:

Patients with impaired liver function do not require dose adjustment. Patients with both renal and hepatic dysfunction are dosed according to the scheme.

Interaction

The possibility of changes in pharmacokinetics of piracetam under the influence of other drugs is low, because 90% of piracetam is excreted unchanged by the kidneys.

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

In a published study in patients with recurrent venous thrombosis the dosage of piracetam 9.6 g/day increased anticoagulant efficacy (more significant decreases of platelet aggregation, fibrinogen, Willebrand factors, blood viscosity and plasma level were noted compared to the use 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.

It penetrates the filter membranes of hemodialysis machines.

Impact on driving and operating machinery

At the time of treatment, caution should be exercised when driving motor vehicles and engaging in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug.

Acute impairment of cerebral circulation (hemorrhagic stroke).

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

Children under 1 year of age.

Pregnancy and lactation.

Piracetam passes through the placental barrier and into the breast milk. The concentration of the drug in the infant reaches 70-90% of its concentration in the blood of the mother. Except in special circumstances, piracetam should not be prescribed during pregnancy. Breastfeeding should be refrained from while prescribing piracetam to a woman.

Side effects

CNS disorders: motor disinhibition, irritability, somnolence, depression, asthenia, headache, insomnia, mental agitation, impaired balance, ataxia, worsening of epilepsy, anxiety, hallucinations, confusion.

Digestive system disorders: nausea, vomiting, diarrhea, abdominal pain.

Metabolic disorders: weight gain.

Sensory system disorders: vertigo.

Skin disorders: dermatitis, itching, urticaria.

Allergic reactions: hypersensitivity, anaphylactic reactions, angioedema.

Local reactions: pain at the injection site, thrombophlebitis

Other (when parenteral administration): fever, decreased BP.

Overdose

Symptoms: diarrhea with a mixture of blood, pain in the abdominal area.

Treatment: in case of significant overdose the stomach should be flushed 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

No controlled studies have been conducted on the use of the drug during pregnancy. Animal studies have shown no direct or indirect effect on pregnancy, embryo/fetal development, childbirth or postnatal development.

Piracetam penetrates through the placental barrier and into the breast milk. Plasma concentrations of piracetam in newborns reach 70-90% of that in the mother. Piracetam should not be prescribed during pregnancy.

During lactation the decision should be made to stop breastfeeding.

Similarities

Nootropil, Piracetam, Piracetam bufus, Notrocetam