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

sheath: sucrose (sugar) 114.881 mg, povidone (polyvinylpyrrolidone) 1.515 mg, magnesium shdroksikarbonat (magnesium carbonate basic) 28.747 mg, titanium dioxide 2.204 mg, silicon dioxide colloid (aerosil) 2.204 mg, tropeolin 0 0.021 mg, beeswax 0,083 mg, paraffin liquid (oil vaseline) 0.345 mg.

Description:

The tablets covered with a cover, yellow color, biconcave form. On the break the tablets are white. Surface roughness is allowed.

Pharmacotherapeutic group:Nootropic agent.

ATX: & nbsp

N.06.B.X.03 Pyracetam

Pharmacodynamics:

Pyracetam - nootropic agent, has an effect on the central nervous system in various ways: it modifies neurotransmission in the brain; improves the conditions conducive to neuronal plasticity; improves microcirculation, affecting the rheological characteristics of the blood and not causing vasodilation. The use of piracetam in patients with cerebral dysfunction increases attention concentration and improves cognitive function, which is accompanied by changes in the electroencephalogram (increase in α and β activity, decrease in δ activity). Promotes restoration of cognitive functions due to various disorders, such as hypoxia, intoxication or electroconvulsive therapy. Reduces the duration of induced vestibular neuronitis. Pyracetam inhibits increased aggregation of activated platelets and, in the case of abnormal rigidity of erythrocytes, improves their deformability and ability to filter.

Pharmacokinetics:

Absorption

After oral administration piracetam quickly and almost completely absorbed from the gastrointestinal tract. Bioavailability is about 100%.After a single dose of piracetam at a dose of 2 g, the maximum concentration (C_max) is reached in 30 minutes and is 40-60 μg / ml, after 2-8 hours it is found in the cerebrospinal fluid.

Distribution

The volume of the distribution (Vd) is about 0.6 l / kg. Does not bind to plasma proteins. Pyracetam penetrates through blood-brain and placental barriers, as well as hemodialysis membranes. In an animal study, it was found that piracetam selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal nuclei.

Metabolism.

It is not metabolized.

Excretion.

Half-life of blood (T1) is 4-5 h and 8.5 h - from the cerebrospinal fluid. T1, elongated with renal failure. It is excreted unchanged by the kidneys. Excretion by the kidneys is almost complete (> 95%) for 30 hours. The total clearance of piracetam in healthy volunteers is 86 ml / min.

Indications:

Symptomatic treatment of intellectual-mnestic disorders in the absence of an established diagnosis of dementia. Reducing the manifestations of cortical myoclonias in patients susceptible to pyracetam as a monotherapy,and in the complex therapy (in order to determine sensitivity to pyracetam in a particular case, a trial treatment course can be performed).

Contraindications:

Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug.
Goreintton's chorea.
Acute disturbance of cerebral circulation (hemorrhagic stroke).
Terminal stage of renal failure.
Deficiency of glucose-6-phosphate dehydrogenase.

Pregnancy and lactation:

There were no controlled studies in pregnant women. Pyracetam penetrates the placental barrier and into breast milk. The concentration of the drug in newborns reaches 70-90% of its concentration in the blood of the mother. The appointment in pregnancy is possible if the potential benefit to the mother exceeds the potential risk to the fetus.

Pyracetam should not be used during breastfeeding or breastfeeding should be discontinued when treated with piracetam. When deciding whether to abort breastfeeding or refusing piracetam treatment, the benefits of breastfeeding for a child and the benefits of therapy for a woman should be correlated.

Dosing and Administration:

Inside.The tablets, covered with a film membrane, are swallowed, not liquid, squeezed with water. During a meal or on an empty stomach.

In memory disorders, intellectual disorders: 2.4 - 4.8 g / day in several doses during the first few weeks, then pass to maintenance therapy 2.4 g / day in 2-3 doses, taking 1.2 g / day .

Treatment of cortical myoclonia: treatment starts with 7.2 grams per day, gradually increasing every 3-4 days by 4.8 g to 24 g per day. With little or no therapeutic effect, treatment is stopped on the 7th day, in the case of a positive response to treatment, a dose of 24 g is reduced by 1.2 g every two days, until the occurrence 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 myoclonus treatment is not changed. 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. However, 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 (CK) 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 for the elderly, in whom the excretion of creatinine depends on age. The dose should be adjusted depending on the creatinine clearance. The creatinine clearance for men can be calculated based on the serum creatinine concentration (QC_serum), according to the following formula:

CK (ml / min) = [140 - age (years) х body weight (kg)]/[72 х КК_serum (mg / ml)]

The creatinine clearance for women can be calculated by multiplying the obtained value by a factor of 0.85.

Kidney function	CK (ml / min)	Dosing regimen
Norm	>80	The standard dose of 2-3 doses
Mild renal insufficiency	50-79	2/3 of the standard dose in 2-3 doses
Mild renal insufficiency		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	-	Contraindicated

Liver failure

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

Side effects:

The undesirable drug reactions listed below were detected in clinical trials and post-detection observations and grouped according to system-organ classes.

The frequency gradient is defined as follows: very often (> 1/10), often (> 1/100 to <1/10), infrequently (> 1/1000 to <1/100), rarely (> 1/10 000 to < 1/1000), very rarely (<1/10 000) and the frequency is unknown (it is impossible to estimate based on available data).

From the side of the blood and lymphatic system: frequency is unknown - bleeding.

From the immune system: frequency unknown - anaphylactoid reactions, hypersensitivity.

From the side of the psyche: often - nervousness; infrequently - depression; frequency unknown - agitation, anxiety, confusion, hallucinations.

From the nervous system: often - hyperactivity; infrequently - drowsiness; frequency unknown - ataxia, imbalance, exacerbation of epilepsy, headache, insomnia, tremor.

From the side of the hearing and labyrinth organs: frequency unknown - vertigo.

From the side of the digestive system, frequency unknown - abdominal pain (including in the upper divisions), diarrhea, nausea, vomiting

From the skin and subcutaneous tissues: frequency unknown - Quincke's edema, dermatitis, itchy skin, urticaria

On the part of the reproductive system, frequency unknown - increased sexual desire.

Common violations: infrequently - asthenia.

Laboratory and instrumental data: often - an increase in body weight.

Overdose:

Symptoms, a single case of development of diarrhea in the form of diarrhea with blood and pain in the abdomen when taking the drug inside at a daily dose of 75 g (according to USB Farma SpA, Italy) is recorded.

Treatment: In case of an overdose, symptomatic therapy is recommended, which may include hemodialysis. There is no specific antidote. The efficacy of hemodialysis for piracetam is 50-60%.

Interaction:

Thyroid hormones

With the simultaneous use of piracetam and thyroid extract (triiodothyronine, L thyroxine), confusion, irritability and sleep disturbance were noted

Acenocoumarol

According to a published blind clinical trial in patients with recurrent venous thrombosis piracetam in a dose of 9.6 g / sug. does not affect the dose of acenecumarol necessary to achieve an international normalized ratio of 2.5-3.5, but compared with the effects of acenocoumarol alone, the addition of pyracetam at a dose of 9.6 g / day significantly reduces platelet aggregation, the release of (3- thromboglobin, the concentration of fibrinogen and von Willebrand factors (VIII: C; VIII: vW: Ag; VIII: vW: RCo), as well as the viscosity of whole blood and plasma Pharmacokinetic interactions At concentrations of 142, 426 and 1422 mg / ml piracetam does not inhibit isoenzymes of cytochrome P450 (RAS 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9 / 11) in vitro.At a concentration of 1422 mg / ml, a minimal inhibition of the isoenzyme CYP2A6 (21%) and SA4 / 5 (11%) was observed. However, the values of the inhibition constant (Ki) are likely to go well beyond the concentration of 1422 mg / ml. Thus, the metabolic interactions of piracetam with other drugs are unlikely.

Special instructions:

Due to the antiaggregant effect (see the section "Pharmacodynamics"), piracetam should be administered with caution to patients with severe hemorrhagic disorders, risk of bleeding (eg, gastric ulcer), hemostasis disorders, in patients with surgical interventions, including dental interventions, in patients taking anticoagulants and antiaggregants, incl. low doses of acetylsalicylic acid.

Renal failure. Because the piracetam is excreted by the kidneys, care should be taken when prescribing the drug to patients with renal insufficiency (see section "Dosing and Administration").

In the treatment of patients with cortical myoclonia, sudden interruption in treatment should be avoided, which can lead to the resumption of seizures.

It penetrates the hemodialysis apparatus through the filter membranes.

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

During the period of treatment it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Piracetam MS coated tablets, 200 mg.

Packaging:

For 60, 120 or 150 tablets in cans of polymeric.

10 tablets per contour cell pack.

Each jar or 1, 2, 3, 4, 5, 6 contour squares, together with instructions for use, are placed in a pack of cardboard.

Storage conditions:

In a dry, dark place, in a well-ukuporennoy container. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N001618 / 01

Date of registration:02.11.2009

The owner of the registration certificate:MEDISORB, CJSC MEDISORB, CJSC Russia

Manufacturer: & nbsp

MEDISORB, CJSC Russia

Information update date: & nbsp23.09.2015

Illustrated instructions

Instructions

Piracetam MS (Pyracetam MS)