Pyracetam - instructions for use, dose, side effects, contraindications

Hard gelatin capsules number 0. The capsule body is white, the cap of the capsule is white. The contents of capsules are white or almost white powder.

Pharmacotherapeutic group:Nootropic agent.

ATX: & nbsp

N.06.B.X.03 Pyracetam

Pharmacodynamics:

Cyclic derivative of gamma-aminobutyric acid (GABA), nootropic agent; acts directly on the brain, improving cognitive (cognitive) processes, such as learning ability, memory, attention, and mental performance.It affects the central nervous system (CNS) in various ways: changes the velocity of propagation of the excitation in the brain, improves metabolic processes in nerve cells, improves acts on the rheological characteristics of the blood, without causing vasodilating action.

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

Inhibits the aggregation of platelets and restores the configuration properties of the outer membrane of rigid red blood cells, as well as the ability of the latter to pass through the vessels of the microcirculatory bed. At a dose of 9.6 g reduces the concentration of fibrinogen and von Willebrand factor by 30-40% and prolongs bleeding time.

It has a protective and restoring effect when the brain function is impaired due to hypoxia and intoxication.

Reduces the severity and duration of the vestibular nystagmus.

Pharmacokinetics:

Absorption at ingestion is fast and complete. Bioavailability is about 100%. After a single oral dose of 3.2 g, the maximum concentration (C_max) - 84 μg / ml, after repeated (3.2 g 3 times a day) -115 μg / ml, the time to reach the maximum concentration (TC_max) in plasma -1 h, cerebrospinal fluid (CSF) -5 h. Food intake lowers Smach by 17% and increases TS_max up to 1.5 hours. In women C_max and AUC after taking 2.4 grams is 30% higher than in men.

Vd - about 0.6 l / kg. Penetrates through the blood-brain barrier (BBB) and placental barrier; is removed during 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.

Does not bind to plasma proteins, it is not metabolized.

The half-life (T_1/2) - 4-5 hours from the blood plasma and 8.5 hours - from the CSF. 80-100% of pyracetam is excreted by the kidneys unchanged by glomerular filtration. The total clearance is 80-90 ml / min. T_1/2prolonged in chronic renal failure (CRF) (with terminal CRF - up to 59 hours). Hepatic insufficiency does not affect the pharmacokinetics of piracetam.

Indications:

Symptomatic treatment of intellectual-mnestic disorders in the absence of an established diagnosis of dementia.

Reduction of the manifestations of cortical myoclonia in piracetam sensitive patients both as monotherapy and as part of complex therapy.(In order to determine sensitivity to pyracetam in a particular case, a trial treatment course can be performed).

Contraindications:

Hypersensitivity, severe renal failure (creatinine clearance less than 20 mL / min), hemorrhagic stroke, agitation, Huntington's chorea, pregnancy, lactation.

Carefully:

Violation of hemostasis, extensive surgical interventions, severe bleeding, CRF (KK 20-80 ml / min).

Dosing and Administration:

Inside. Capsules are swallowed, not liquid, squeezed with water. During a meal or on an empty stomach.

In memory disorders, intellectual disorders

On 2,4-4,8 g / day in several receptions during the first several weeks, then pass to supporting therapy of 2,4 g / day in 2-3 receptions, reception of 1,2 g / day is possible.

Treatment of cortical myoclonia

Treatment begins with a dose of 7.2 g-24 g per day, with little therapeutic effect or its absence, treatment is stopped on the 7th day, in case of a positive response to treatment, a dose of 24 g is reduced by 1.2 g every 2 days, until the emergence of myoclonus. This allows you to know the average effective dose. The daily dose of piracetam should be divided into 2-3 doses.The dose of other drugs for the treatment of myoclonus does not change. Then, later on the results of treatment, it is allowed to review the dose of other drugs for the treatment of myoclonus.

After initiation of piracetam treatment, treatment is continued as long as the symptoms of the disease persist.

Nevertheless, every 6 months, attempts should be made to reduce the dose or cancel the drug. To avoid sudden relapse, the dose is reduced by 1.2 g every 2 days. If oral administration is not possible, the drug is administered intravenously at the same dose.

Elderly patients

Elderly patients with renal insufficiency should be corrected for the dose (see below "Renal failure").

With long-term treatment to assess the need for dose adjustment, creatinine clearance should be assessed regularly.

Renal insufficiency

Piracetam is excreted almost exclusively by the kidneys, care should be taken when treating patients with renal insufficiency or requiring renal function control. The elimination half-life increases in direct proportion to the impairment of kidney function and creatinine clearance; this is also true of the elderly,in which the excretion of creatinine depends on age.

In this regard, the dose is adjusted in accordance with the table below:

Kidney function	CK (ml / min)	Dosing regimen
Norm	>80	The standard dose of 2-4 admission
Mild renal insufficiency	50-79	2/3 of the standard dose in 2-3 doses
Mean renal insufficiency	30-49	1/3 of the standard dose in 2 divided doses
Severe renal insufficiency	<30	1/6 of the standard dose once
Terminal Renal Failure		Opposite kazano

Liver failure

Patients with isolated dysfunction of the liver do not need correction of the dose. Patients with impaired function and kidney and liver dosing is carried out according to the scheme (see above "Renal failure")

Side effects:

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

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

From the side of metabolism: weight gain.

From the senses: vertigo.

From the skin: dermatitis, itching, urticaria.

Allergic reactions: hypersensitivity, anaphylactic reactions, angioedema.

Overdose:

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

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

Interaction:

When used simultaneously with iodine-containing hormones of the thyroid gland, confusion, irritability and sleep disturbance may occur.

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

Special instructions:

Be wary appoint patients with hemostasis, before the forthcoming extensive surgical interventions vb or in patients with symptoms of severe bleeding.

In the treatment of cortical myoclonia, sudden cessation of treatment should be avoided, this can cause a resumption of seizures.

When treating a veno-occlusive crisis with sickle-cell anemia, a dose of less than 160 mg / kg or an irregular intake of the drug may cause a recurrence of the crisis.

With prolonged therapy in elderly patients, regular monitoring of renal function is recommended, if necessary, dose adjustment is performed depending on the QC. It penetrates the hemodialysis apparatus through the filter membranes.

Effect on the ability to drive transp. cf. and fur:

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

Form release / dosage:

Capsule 400 mg.

Packaging:

10 capsules in the outline package. 2 or 6 contour mesh packages together with the instruction for use are placed in a bundle.

Storage conditions:

In dry, dark place at a temperature of no higher than 25 ° C.

In a place inaccessible to children.

Shelf life:

3 years. Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N003123 / 02

Date of registration:03.12.2008

The owner of the registration certificate:Promomed Rus, Open CompanyPromomed Rus, Open Company Russia

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Information update date: & nbsp22.09.2015

Illustrated instructions

Instructions

Pyracetam (Piracetam)