Piracetam капс. 400 mg No. 60

General characteristics. Structure:

One capsule contains 400 mg of piracetam as active agent; excipients: magnesium carbonate the main, calcium stearate. Structure of the capsule: gelatin, water, titanium dioxide.
Description: Capsules of white color No. 0. Contents of capsules – powder of white or almost white color.

Pharmacological properties:

Pharmacodynamics. Drug exerts positive impact on exchange processes of neurons, improves activity of the central nervous system. By biochemical researches it is established that piracetam normalizes the intracellular content of adenosinetriphosphate and adenosinediphosphate, improving function of neurons in anoxic conditions, poisoning or aging of an organism. It promotes activation of synthesis of nuclear RNA, phospholipids and the corresponding kinases. Piracetam improves information transfer between parencephalons and strengthens a kortiko-subcortical impulsation. Promotes improvement of integrative function of a brain, memory, concentration of attention and mental abilities at patients with functional and organic disturbances of the central nervous system.
Improvement of power processes under the influence of piracetam leads to strengthening of utilization of glucose and high-energy connections in brain tissue. Increasing concentration of phosphoric connections in a brain, drug normalizes its function after a hypoxia and toxic influences of barbiturates.
Drug reduces aggregation of thrombocytes, and at the broken elasticity of erythrocytes, improves their ability to change of a form and passing on brain vessels, reduces duration of a vestibular nystagmus.
Has no the antihistaminic, calming analgetic properties and does not cause undesirable changes in cardiovascular and respiratory systems.
It does not kumulirutsya in an organism and does not result in medicinal dependence.
Does not turn into piperidic acid and does not increase its contents in a brain.

Pharmacokinetics. We will easily dissolve piracetam in water, it is bad in organic compounds. Is not exposed to ionization and does not contact blood proteins. It is not metabolized in an organism. Biocomprehensibility of drug makes about 100%. At intake it is almost completely soaked up in a digestive tract. After reception of a single dose in 2 g, the maximum concentration of drug in blood (40-60 mkg/ml) is reached in 30 minutes, and in cerebrospinal fluid – in 2-8 hours. The maximum concentration of drug is fixed in frontal, temporal and occipital shares of brain bark, and also in a cerebellum and the basis of a brain. Piracetam gets into all fabrics, passes through hematoencephalic and placental barriers and gets into breast milk. Plasma elimination half-life makes 4-5 hours, and of cerebrospinal fluid – 6-8 hours. It is removed, generally with urine in an invariable look (about 98%) and only 1-2% with a stake.

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.
- effects of an ischemic stroke, such as disturbances of the speech, disturbances of the emotional sphere, for increase in motor and mental performance.
- an alcoholism – for treatment of psychoorganic and abstinent syndromes.
- the recovery period after craniocereberal injuries and intoxications of a brain.
- dizzinesses and the related disorders of balance, except for dizzinesses of a vasculomotor and mental origin.
- as a part of complex therapy of low learnability at children with a psychoorganic syndrome.
- complex therapy of drepanocytic anemia.

Route of administration and doses:

Inside. A daily dose – 30-160¼ú/kg, frequency rate of reception – 2-4 times a day. It is inside appointed during meal or on an empty stomach, capsules should be washed down with liquid (water, juice).
Attention! To accept the last single dose of drug no later than 17:00 for overcoming sleep disorders.
At a symptomatic treatment of a chronic psychoorganic syndrome, depending on expressiveness of symptoms appoint 1,2-2,4g and within the first week lead up to 4,8g in day.
At treatment of effects of a stroke appoint 4,8 g/days.
At patients with a craniocereberal injury the initial dose makes 9-12g/days, supporting – 2,4g/days. Treatment continues not less than 3 weeks.
At an alcoholic abstinence syndrome – a maintenance dose of 2,4 g/days.
At dizziness and the related disorders of balance of 2,4-4,8 g/days.
To children for correction of the lowered learnability – the average dose of drug makes 3,3 g/days. Treatment continues during all academic year.
At drepanocytic anemia the daily preventive dose makes 160 mg/kg of body weight, divided into four equal doses. This dosage can be appointed to children since 1.
Dosing by the patient with a renal failure: As Nootropil is removed from an organism by kidneys, it is necessary to be careful at treatment of patients with a renal failure according to this scheme of dosing.

Renal failure                   Clearance of creatinine (ml/min.)                    Dosing
           Norm                                                > 80                                             Usual dose
            Easy                                                                              50-79 2/3 usual doses in 2-3 receptions
            Average                                                                           30-49 1/3 usual doses in 2 receptions
           Heavy                                            <                                  30 1/6 usual doses, once
           Final stage                                   -                                            it is 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:

                                                          Widespread                      Rare
                                                         (from 1% and less than 10%)                (from 0,1% and less than 1%)
Frustration central and

peripheral nervous system       Hyperkinesia of 1,72% 
Disbolism              Increase in body weight

                                                                  1,29% 
Frustration of mentality                            Nervousness of 1,13%             Drowsiness of 0,96%

                                                                                                        Depression of 0,83%
General frustration                                                                             Adynamy of 0,23%

They arise at the elderly patients receiving doses over 2,4 g/days more often. In most cases it is possible to achieve regress of similar symptoms, having lowered a drug dose. There are single messages on side effects from digestive tract, such as nausea, vomiting, diarrhea, abdominal pains and in a stomach; a nervous system – dizziness, a headache, an ataxy, balance disturbance, an aggravation of a course of epilepsy, sleeplessness; from mentality – confusion, excitement, alarm, hallucinations, increase in sexuality; from integuments – dermatitis, an itch, rashes, hypostasis.

Interaction with other medicines:

At combined use with extract of a thyroid gland (T3+T4) the acrimony, disorientations and sleep disorders is possible. Interaction with clonazepam, Phenytoinum, phenobarbital, sodium Valproatum is noted.
High doses (9,6 g/days) of piracetam increased efficiency of an atsenokumarol at patients with venous thrombosis: bigger decrease in level of aggregation of thrombocytes, level of fibrinogen, Villibrandt's factors, viscosity of blood and plasma was noted, than at appointment only an atsenokumarol.
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 of the CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9/11 isoform in concentration of 142, 426 and 1422 mkg/ml. At concentration of 1422 mkg/ml, small oppression of CYP2A6 (21%) and 3A4/5 is noted (11%). However the Ki level of these two CYP isomers sufficient at exceeding of 1422 mkg/ml. Therefore metabolic interaction with other drugs is a little probable. 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 1,6g piracetam.

Contraindications:

Contraindications:
- individual intolerance of piracetam or derivatives of a pirrolidon, and also other components of drug.
- acute stage of a hemorrhagic stroke.
- a final stage of a renal failure (at clearance of creatinine less than 20 ml/min.).
- children's age till 1 year.

Pregnancy and lactation: Researches on animals did not reveal the damaging action on an embryo and its development, including in the post-natal period, and also the course of pregnancy and childbirth did not change. 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. Except for special circumstances Piracetam should not be appointed during pregnancy. It is necessary to refrain from breastfeeding at appointment to the woman of piracetam.

Overdose:

At reception of 75 g of piracetam in a dosage form solution for intake the dispeptic phenomena, such as diarrhea with blood and abdominal pains most of which likely are connected with the high content of sorbitol as a part of this dosage form are noted. Any other special symptoms of overdose of piracetam are noted. Right after the considerable peroral overdose can wash out a stomach or to cause artificial vomiting. A symptomatic treatment which can include a hemodialysis. There is no specific antidote. Efficiency of a hemodialysis makes 50%-60% for piracetam.

Storage conditions:

List B. In dry protected from light and the place, unavailable to children, at a temperature not over 25 ºС. Period of validity: 3 years. Not to use after the date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Capsules on 400 mg of 10 or 15 capsules in a blister strip packaging. On 10, 20 or 60 capsules in bank of orange glass or bank polymeric, or a bottle polyethylene. Each can or a bottle, or 1, 2 or 6 blister strip packagings on 10 capsules or 4 blister strip packagings on 15 capsules with the application instruction in a pack from a cardboard.