Piracetam

General characteristics. Structure:

Structure on 1 tablet of 200 mg: Active agent — piracetam of 200 mg,

Excipients — starch prezhelatinizirovanny — 3,0 mg, croscarmellose sodium — 3,0 mg, povidone (polyvinylpirrolidone) — 5,0 mg, magnesium stearate — 2,0 mg.

Excipients (cover): a gipromelloza — 3,8 mg, a macrogoal of 4000 — 1,0 mg, titanium dioxide — 2,2 mg.

Structure on 1 tablet of 400 mg: Active agent — piracetam of 400 mg,

Excipients — starch prezhelatinizirovanny — 6,0 mg, croscarmellose sodium — 6,0 mg, povidone (polyvinylpirrolidone) — 10,0 mg, magnesium stearate — 4,0 mg.

Excipients (cover): a gipromelloza — 7,6 mg, a macrogoal of 4000 — 2,0 mg, titanium dioxide — 4,4 mg.

Pharmacological properties:

Pharmacodynamics. Nootropic means. Exerts positive impact on exchange processes of a brain: increases concentration of ATP in brain fabric, strengthens synthesis of RNA and fosfolpid, stimulates glycoclastic processes, strengthens glucose utilization. Improves integrative activity of a brain, promotes memory consolidation, facilitates training process.
Changes the speed of spread of activation in a brain, improves microcirculation, without having at the same time vasodilating effect, suppresses aggregation of the activated thrombocytes. Has protective action at the injuries of a brain caused by a hypoxia, intoxications, an electroshock; strengthens alpha and beta activity, reduces delta activity on the electroencephalogram, reduces expressiveness of a vestibular nystagmus.
Improves bonds between cerebral hemispheres and synaptic conduction in neocortical structures, recovers and stabilizes cerebral functions, especially consciousness, memory and the speech, increases intellectual working capacity, improves a brain blood stream. The effect develops gradually. Practically has no sedative and psychogogic influence.

Pharmacokinetics. After intake it is well soaked up and gets into various bodies and fabrics. Bioavailability makes 95%. Time of achievement of the maximum concentration of 0,5-1 h. The drug elimination half-life from a blood plasma makes 4-5 hours and 8,5 hours of cerebrospinal fluid which is extended at a renal failure. Gets through hematoencephalic and placental barriers, collects in brain fabric in 1-4 h after intake. Does not contact proteins of a blood plasma, it is practically not metabolized. An elimination half-life of 4,5 h (7,7 h — from a brain). It is removed by kidneys — 2/3 in not changed look during 30 h.

 

Indications to use:

Symptomatic treatment of a psychoorganic syndrome, in particular at the elderly patients suffering from decrease in the memory, dizziness lowered by concentration of attention and the general activity, lability of mood, disorder of behavior, gait disturbance and also at patients with Alzheimer's disease and senile dementia like Alzheimer.
posledstviye of an ischemic stroke, such as disturbances of the speech, disturbances of the emotional sphere, for increase in motor and mental performance.
khronichesky alcoholism - for treatment of psychoorganic and abstinent syndromes.
♦Период recovery after craniocereberal injuries and intoxications of a brain.
golovokruzheny and related disorders of balance, except for dizziness of a vasculomotor and psychogenic origin.

Route of administration and doses:

Inside, during meal or on an empty stomach, washing down with liquid. Attention: to accept the last single dose no later than 17:00 for prevention of a sleep disorder. A daily dose — 30-160 mg/kg of body weight, frequency rate of reception — 2 times a day, if necessary — 3 — 4 times a day. A baking course from 2-3 weeks to 2-6 months. If necessary the course of treatment is repeated.
At therapy of a psychoorganic syndrome at elderly drug is appointed on 1,2-2,4 g/days; a load dose within the first weeks of therapy — to 4,8 g/days. Treatment by piracetam if necessary can be combined using psychotropic, cardiovascular and other medicines.
At treatment of effects of a stroke appoint 4,8 g/days. This dosage form is recommended for children of 3 years — on 1 tablet 3 times a day. The maximum daily dose — 1,8 g. A course of treatment from 2 weeks to 2-6 months.
At alcoholism — a maintenance dose — 2,4 g.
At dizziness and the related frustration
balances of 2,4-4,8 g/days.
Dosing by the patient with a renal failure.
As piracetam is removed from an organism by kidneys, it is necessary to be careful at treatment of patients with a renal failure in compliance with this scheme of dosing.

Renal nedo-                Clearance                       Dosing
                     creatinine statochnost
                                       (ml/min.)      

Norm                                 > 80                         Usual dose 
Easy                                          50-79 2/3 usual doses in a 2-3priyem 
Average                                      30-49 1/3 usual doses in 2 receptions 
Heavy                              <          30 1/6 usual doses, once
Final stage                                               contraindicated

The dose korrigirutsya by the elderly patient in the presence of a renal failure and at long therapy control of a functional condition of kidneys is necessary. Dosing by the patient with an abnormal liver function. Patients with an abnormal liver function do not need dose adjustment. The patient with disturbance of functions and kidneys and a liver, dosing is carried out according to the scheme (see the section "Dosing by the Patient with a Renal Failure").

Features of use:

Due to the influence of piracetam on aggregation of thrombocytes, care at purpose of drug is recommended to patients with disturbance of a hemostasis, during big surgeries or the patient with symptoms of heavy bleeding. At treatment of patients with a cortical myoclonia it is necessary to avoid sharp interruption of treatment that can cause resuming of attacks. At long therapy of elderly patients regular control of indicators of function of kidneys is recommended, if necessary carry out dose adjustment depending on results of a research of clearance of creatinine. In view of possible side effects, it is necessary to be careful when performing work with mechanisms and driving of the car. Gets through the filtering membranes of devices for a hemodialysis.

Side effects:

- From a nervous system: hyperphrenia, motive disinhibition, irritability, drowsiness, depression, adynamy. These side effects arise at the patients of advanced age receiving drug in a dose more than 2,4 g/days more often. In most cases it is possible to achieve regress of similar symptoms, having lowered a drug dose. In isolated cases — dizziness, a headache, an ataxy, an aggravation of a course of epilepsy, extrapyramidal disturbances, a tremor, disbalance, decline in the ability to concentration of attention, sleeplessness, excitement, alarm, hallucinations, increase in a libido.
- From cardiovascular system: seldom — decrease or increase in arterial pressure, deterioration in a course of stenocardia.
- From the alimentary system: in isolated cases — nausea, vomiting, diarrhea, abdominal pains (including a gastralgia).
- From a metabolism: increase in body weight — arises at the patients of advanced age receiving drug in a dose more than 2,4 g/days more often.
- Allergic reactions: dermatitis, itch, rashes, Quincke's disease.

Interaction with other medicines:

Increases efficiency of hormones of a thyroid gland, antipsychotic medicines (neuroleptics).
At simultaneous use with the medicines stimulating the central nervous system its excessive stimulation is possible.
At appointment with neuroleptics reduces danger of emergence of extrapyramidal disturbances. Interaction with clonazepam, Phenytoinum, phenobarbital, sodium Valproatum is noted. High doses (9,6 g/days) of piracetam increase efficiency of indirect anticoagulants at patients with venous thrombosis (bigger decrease in level of aggregation of thrombocytes, level of fibrinogen, Villebrand's factors, viscosity of blood and plasma in comparison with use only of indirect anticoagulants was noted). The possibility of change of a pharmacodynamics of piracetam under the influence of other medicines is low as 90% of drug are removed in not changed view with urine.
In vitro piracetam does not oppress P450 cytochrome isoenzymes, such as CYP1A2, 2V6, 2S8, 2S9, 2S19, 2D6, 2E1 and 4A9/11 in concentration of 142, 426 and 1422 mkg/ml. At concentration of 1422 mkg/ml small oppression of CYP2A6 (21%) and ZA4/5 (11%) is noted, however the Ki level of these two isoenzymes is sufficient at exceeding of 1422 mkg/ml in this connection metabolic interaction with other drugs is improbable.
Reception of piracetam in a dose of 20 mg/days did not change peak and a curve of level of concentration of antiepileptic drugs in blood serum (carbamazepine, Phenytoinum, phenobarbital, Valproatum) at the patients with epilepsy receiving a constant dosage.
Joint reception with alcohol did not influence the level of concentration of piracetam in serum and concentration of alcohol in blood serum did not change at reception of 1,6 g of piracetam.

Contraindications:

Individual intolerance of piracetam or derivatives of a pirrolidon, and also other components of drug. An end-stage of a renal failure (at clearance of creatine less than 20 ml/min.), an acute disorder of cerebral circulation (a hemorrhagic stroke), psychomotor excitement at the time of purpose of drug, a trochee of Gentington. Children's age up to 3 years (for this dosage form).

WITH CARE:
Disturbance of a hemostasis; extensive surgical interventions; heavy bleeding.

USE AT PREGNANCY AND IN THE PERIOD OF THE LACTATION
Researches on pregnant women were not conducted. Piracetam gets through a placental barrier and into breast milk. Concentration of drug at newborns reaches 70-90% of concentration it in blood at mother. During pregnancy purpose of drug is possible only when the estimated advantage for mother exceeds potential risk for a fruit. In the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Overdose:

After oral administration of piracetam in a dose of 75 g the dispeptic phenomena, such as diarrhea with blood and abdominal pains are noted.
Treatment: right after administration of drug inside it is possible to wash out a stomach or to cause artificial vomiting. Performing symptomatic therapy is recommended, the hemodialysis (efficiency of 50-60%) is possible. There is no specific antidote.

Storage conditions:

List B. To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated on 200 mg and 400 mg.
On 10, 20, 30 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.
On 10, 20, 30, 40, 50, 60 or 100 tablets in a container polymeric for medicines. One container or 1, 2, 3, 4, 5, 6, 8 or 10 blister strip packagings together with the application instruction place in a pack from a cardboard.