Piracetam

Piracetam 400 mg.

GABA cyclic derivative, nootropic agent; acts directly on the brain, improving cognitive (cognitive) processes, such as learning ability, memory, attention, as well as mental performance. 
It affects the central nervous system in various ways: it changes the rate of excitation in the brain, improves metabolic processes in nerve cells, improves microcirculation, affects the rheological characteristics of the blood without having a vasodilating effect.

Improves the connection between the cerebral hemispheres and synaptic conduction in neocortical structures, improves cerebral blood flow.

It inhibits platelet aggregation and restores the configuration properties of the outer membrane of rigid erythrocytes, as well as the ability of the latter to pass through the vessels of the microvasculature. At a dose of 9.6 g, it reduces the concentration of fibrinogen and von Willebrand factor by 30-40% and lengthens the bleeding time.

It has a protective and restorative effect in case of impaired brain function due to hypoxia and intoxication.
Reduces the severity and duration of vestibular nystagmus.

Pharmacokinetics:

 Absorption upon ingestion is fast and complete. Bioavailability is about 100%. After a single oral administration at a dose of 3.2 g Cmax - 84 μg / ml, after repeated (3.2 g 3 times a day) - 115 μg / ml, TCmax in plasma - 1 h, CSF - 5 h. Eating reduces Cmax by 17% and increases TCmax up to 1.5 hours. In women, Cmax and AUC after taking 2.4 g are 30% higher than in men.

Vd - about 0.6 l / kg. Penetrates through the BBB and the placental barrier; removed by hemodialysis. In animal experiments, it selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal nuclei.

It does not bind to plasma proteins, is not metabolized.

T1 / 2 - 4-5 hours from blood plasma and 8.5 hours from CSF. 80-100% of piracetam is excreted by the kidneys unchanged by glomerular filtration. The total clearance is 80-90 ml / min. T1 / 2 lengthens with chronic renal failure (with terminal chronic renal failure - up to 59 hours).

Hepatic insufficiency does not affect the pharmacokinetics of piracetam.

In adults: symptomatic treatment of the psycho-organic syndrome, accompanied by a decrease in memory, a decrease in concentration and activity, mood changes, behavior disorders, impaired gait;

treatment of dizziness (vertigo) and related disorders of balance (with the exception of dizziness of vasomotor and psychogenic origin);

cortical myoclonia (monotherapy or as part of complex therapy);

prevention (oral) and relief (parenteral) of sickle cell vaso-occlusive crisis.

In children: dyslexia in children from 8 years old in combination with other methods, including speech therapy treatment;

prevention (oral) and relief (parenteral) of sickle cell vaso-occlusive crisis.

Hypersensitivity, severe CRF (CC less than 20 ml / min), hemorrhagic stroke, psychomotor agitation, Huntington's chorea, pregnancy, lactation.

Carefully. Violation of hemostasis, extensive surgery, severe bleeding, chronic renal failure (CC 20-80 ml / min).

From the side of the central nervous system: motor disinhibition, irritability, drowsiness, depression, asthenia, headache, insomnia, mental agitation, imbalance, ataxia, exacerbation of the course of epilepsy, anxiety, hallucinations, confusion.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain.

From the side of metabolism: weight gain.

From the sensory organs: vertigo.

From the skin: dermatitis, itching, urticaria.

Allergic reactions: hypersensitivity, anaphylactic reactions, angioedema.

Local reactions: pain at the injection site, thrombophlebitis

Other (with parenteral administration): fever, decreased blood pressure.

With simultaneous use with iodine-containing thyroid hormones, confusion, irritability and sleep disturbance may occur.

At high doses (9.6 g / day) in patients with venous thrombosis, it increases the anticoagulant effect of indirect anticoagulants (a more pronounced decrease in platelet aggregation, fibrinogen, von Willebrand factor, blood viscosity and plasma).

Pharmaceutically compatible with solutions of dextrose (5%, 10%, 20%), fructose (5%, 10%, 20%), 0.9% NaCl solution, Ringer's solution, 20% mannitol solution, hydroxyethyl starch (6%, 10%).

Inside (during meal or on an empty stomach, washing down with liquid); in / in a stream or drip, in / m (in case of difficulty swallowing or in an unconscious state).

The last dose is taken no later than 17 hours (to prevent sleep disturbance).

The daily dose is divided into 2-4 doses.

Symptomatic treatment of the psycho-organic syndrome: 4.8 g / day for the first week, then switch to a maintenance dose of 1.2-2.4 g / day.

Treatment of dizziness and related imbalances: 2.4-4.8 g / day.

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 the maximum dose of 24 g / day is reached. Treatment continues throughout the period of the disease. Every 6 months you should try to reduce the dose or cancel the drug, gradually reducing the dose by 1.2 g / day every 2 days. With a slight therapeutic effect or its absence, treatment is stopped.

In sickle-cell vaso-occlusive crisis (in adults and children): prevention - by mouth, 160 mg / kg / day, divided into 4 equal doses. A dose of less than 160 mg / kg / day or irregular intake of the drug can cause an exacerbation of the disease; iv treatment at 300 mg / kg / day, divided into 4 equal doses.

Treatment of dyslexia in children over 8 years old (in combination with other treatment methods) - 3.2 g divided into 2 equal doses.

With mild chronic renal failure (CC 50-79 ml / min) - 2/3 of the dose, divided into 2-3 doses; medium (CC 30-49 ml / min) - 1/3 of the dose, divided into 2 doses; severe (CC 20-30 ml / min) - 1/6 dose once.

Symptoms: abdominal pain, diarrhea with an admixture of blood.

Treatment: induction of vomiting, gastric lavage, symptomatic therapy, hemodialysis (50-60% effective). There is no specific antidote.

It is prescribed with caution in patients with impaired hemostasis, before upcoming extensive surgical interventions vb or in patients with symptoms of severe bleeding.

In the treatment of cortical myoclonia, abrupt cessation of treatment should be avoided, as this can cause renewed seizures.
In the treatment of veno-occlusive crisis with sickle cell anemia, a dose of less than 160 mg / kg or an irregular intake of the drug can cause a crisis recurrence.

With prolonged therapy in elderly patients, regular monitoring of renal function is recommended, if necessary, dose adjustment is carried out depending on QC.

Penetrates through the filtering membranes of hemodialysis machines.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.