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

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Dosage form: & nbspfilm coated tablets

Composition:

Composition per 1 tablet:

Tablets with a dosage of 16 mg beta-histidine + 800 mg piracetam:

Active substances: Betahistine dihydrochloride 16.00 mg, pyracetam 800.00 mg;

Excipients: cellulose microcrystalline 75.00 mg, crospovidone 38.00 mg, giprolose 14.25 mg, magnesium stearate 4.75 mg, citric acid 2.00 mg;

Film Sheath: Opaprai pink 50.00 mg [polyvinyl alcohol 40.00%, titanium dioxide 24.77%, macrogol 20.20%, talc 14.80%, iron dye oxide red 0.16%, iron oxide dye yellow 0.07% ].

Tablets with a dosage of 24 mg beta-histidine + 800 mg pyracetam:

Active substances: Betahistine dihydrochloride 24.00 mg, pyracetam 800.00 mg;

Excipients: microcrystalline cellulose 66.00 mg, crospovidone 38.00 mg, giprolose 14.25 mg, magnesium stearate 4.75 mg, citric acid 3.00 mg;

Film Sheath: Opaprai pink [polyvinyl alcohol 40.00%, titanium dioxide 22.37%, macrogol 20.20%, talc 14.80%, iron dye oxide red 1.64%, iron dye oxide yellow 0.59%, iron dye oxide black 0 , 40%].

Description:

Tablets with a dosage of 16 mg betahistine + 800 mg of piracetam: Oval biconvex tablets, covered with a film shell of light pink color. On The tablet core is white or almost white in cross section.

Tablets with a dosage of 24 mg betahistine + 800 mg of piracetam: Oval biconvex tablets, covered with a film shell of dark pink color. On The tablet core is white or almost white in cross section.

Pharmacotherapeutic group:Histamine drug + nootropic drug

ATX: & nbsp

Other psychostimulants and nootropic drugs

Pharmacodynamics:

The drug Nooserc contains 2 active substances:

Betagistin (a remedy for symptomatic therapy of vestibular vertigo and / or Ménière syndrome) and piracetam (a remedy for the treatment of symptomatic memory disorders, intellectual disorders in the absence of a diagnosis of dementia).

Pharmacodynamics

Betagistin

The mechanism of action of betagistin is known only in part. There are several possible hypotheses, confirmed by preclinical and clinical data:

- Influence on the gistaminergic system.

Partial agonist H₁-gistaminovyh and antagonist H₃-gistaminovyh receptors of the vestibular nuclei of the central nervous system (CNS), has little activity in relation to H₂receptors. Betagistin increases histamine metabolism and its release by blocking presynaptic H₃-receptors and decrease in the number of H₃receptors.

- Increased blood flow of the cochlear region, as well as the entire brain.

According to preclinical studies betagistin improves blood circulation in the vascular stria of the inner ear by relaxing precapillary sphincters of the vessels of the inner ear. It is also shown that betagistin increases the blood flow of the brain in humans.

- Facilitating the process of central vestibular compensation.

Betagistin accelerates the recovery of vestibular function in animals after unilateral vestibular neurectomy, speeding up and facilitating central vestibular compensation due to antagonism with H₃-histamine receptors. The recovery time after vestibular neurectomy in humans in the treatment with betahistine is also reduced.

- Excitation of neurons in the vestibular nuclei.

It dose-dependently reduces the generation of action potentials in the neurons of the lateral and medial vestibular nuclei.

Pharmacodynamic properties found on animals,provide a positive therapeutic effect of betahistine in the vestibular system. The efficacy of betahistine has been demonstrated in patients with vestibular dizziness and Meniere syndrome, which was manifested by a decrease in the severity and frequency of dizziness.

Pyracetam

Pyracetam is a nootropic drug that acts on the central nervous system in various ways: it modifies neurotransmission in the brain; improves metabolic conditions that promote neuronal plasticity; improves microcirculation, affecting the rheological characteristics of the blood and not causing vasodilation.

Both long-term and short-term use of piracetam in patients with cerebral dysfunction increases attention concentration and improves cognitive functions, which is manifested by significant changes in the electroencephalogram (increase in activity, decrease in 5 activity).

The drug helps restore cognitive abilities after various cerebral injuries due to hypoxia, intoxication or electroconvulsive therapy.

Pyracetam reduces the duration of provoked 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:

Betagistin

Suction

When taken orally betagistin quickly and almost completely absorbed in the gastrointestinal tract. After absorption, the drug is quickly and almost completely metabolized to form an inactive metabolite of 2-pyridylacetic acid. The concentration of betagistin in the blood plasma is very low. Thus, pharmacokinetic analyzes are based on measuring the concentration of the metabolite of 2-pyridylacetic acid in plasma and urine.

When taking the drug with food, the maximum concentration (C_m_Oh) of the drug is lower than when taken on an empty stomach. However, the total absorption of betahistin is the same in both cases, indicating that eating only slows the absorption of betahistine.

Distribution

Binding of betahistine to plasma proteins is less than 5%.

Biotransformation

After suction betagistin quickly and almost completely metabolized to form a metabolite of 2-pyridylacetic acid (which does not have pharmacological activity).FROM_m_Oh 2-pyridylacetic acid in blood plasma (or urine) is achieved 1 h after administration. The half-life (T1 / 2) is approximately 3.5 hours.

Excretion

2-pyridylacetic acid is rapidly excreted in the urine. When taking the drug at a dose of 8 to 48 mg, about 85% of the initial dose is found in the urine. The excretion of betagistin by the kidneys or through the intestine is negligible.

Linearity

The rate of excretion remains constant with an oral intake of 8 to 48 mg of the drug, indicating the linearity of the pharmacokinetics of betahistine, and suggests that the involved metabolic pathway remains unsaturated.

Pyracetam

Suction

After oral administration piracetam quickly and almost completely absorbed from the gastrointestinal tract. The bioavailability of piracetam is about 100%.

After a single dose in a dose of 2 g C_ma_x is reached after 30 minutes and is 40 - 60 μg / ml, after 2 - 8 hours piracetam is found in the cerebrospinal fluid.

Distribution

Volume of distribution (Vd) is about 0.6 l / kg. Does not bind to blood plasma proteins. Pyracetam penetrates through blood-brain and placental barriers, as well as hemodialysis membranes. In animal studies, 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

T1 / 2 pyracetam from plasma is 4 to 5 hours and 8.5 hours from the cerebrospinal fluid. T1/2 lengthened with renal failure.

It is excreted unchanged by the kidneys. Excretion by the kidneys is almost complete (more than 95%) for 30 hours.

The total clearance of piracetam in healthy volunteers is 86 ml / min.

Indications:

The drug Noerserk is prescribed for patients who are already receiving combination therapy with betahistine and piracetam at previously selected doses to replace this combination therapy with Nooserc if the following indications are available:

- Betagistin: for symptomatic treatment of vestibular dizziness (vertigo) and / or Meniere's syndrome, characterized by the following main symptoms:

- dizziness (accompanied by nausea / vomiting);

- Hearing loss (hearing loss);

- noise in ears.

- Pyracetam: for symptomatic treatment of memory disorders, intellectual-mnestic disorders in the absence of an established diagnosis of dementia.

Contraindications:

- Hypersensitivity to any of the components of the drug, or a derivative of pyrrolidone;

- Pregnancy;

- Lactation period (breastfeeding);

- Pheochromocytoma;

- Horea Huntington;

- Acute disorders of cerebral circulation (hemorrhagic stroke);

- Medium, severe and terminal stages of chronic renal failure;

- It is not recommended for use in children under the age of 18 due to the lack of safety and efficacy data.

Carefully:

Patients with bronchial asthma or peptic ulcer of the stomach and / or duodenum require careful observation during the treatment period. Due to the antiaggregant effect of piracetam, which is part of the combination, the Nooserc drug should be administered with caution to patients with severe hemorrhagic disorders, a risk of bleeding (eg, with an ulcer stomach), hemostasis disorders, haemorrhagic cerebrovascular disorders in the anamnesis; patients with surgical interventions, including dental interventions; patients taking anticoagulants and antiaggregants, including low doses of acetylsalicylic acid.

Because the piracetam is excreted through the kidneys, caution should be exercised when prescribing Nooserc drug to patients with renal insufficiency. Long-term treatment of elderly patients requires regular monitoring of creatinine clearance, since dose adjustment may be required.

Piracetam penetrates the filtration membranes of hemodialysis apparatus.

Pregnancy and lactation:

Controlled studies of the use of Nooserc drug during pregnancy have not been conducted. Therefore, Nooserc preparation is contraindicated for use throughout the period of pregnancy.

Data on the use of Nooserc preparation in women during lactation are absent, therefore, the use of the drug during breastfeeding is contraindicated.

Dosing and Administration:

Inside, during meals, squeezed with liquid.

Tablets with a dosage of 16 mg betahistine + 800 mg of piracetam: 1 tablet three times a day.

Tablets with a dosage of 24 mg betahistine + 800 mg of piracetam: 1 tablet twice a day.

Dosing to patients with impaired renal function:

The dose should be selected depending on the amount of creatinine clearance (CC):

The creatinine clearance for men can be calculated by the formula:

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

Renal insufficiency	CK (ml / min)	Dosing regimen Nooserka
Norm	>80	16 mg beta-histidine + 800 mg piracetam 3 times a day
Lightweight	50-79	24 mg beta-histidine + 800 mg piracetam 2 times a day
Average	30-49	Contraindicated
Heavy	<30	Contraindicated
Terminal stage	-	Contraindicated

Dosing to patients with impaired liver function:

Patients with a dysfunction of the liver do not need a dose adjustment.

Dosing to patients with impaired liver and kidney function:

Patients with a violation of the liver and kidneys are dosed according to the scheme given above (see section "Dosing to patients with impaired renal function ").

Elderly patients

Long-term treatment of elderly patients requires regular monitoring of creatinine clearance, since dose adjustment may be required.

Piracetam penetrates the filtration membranes of hemodialysis apparatus.

Side effects:

To assess the incidence of adverse events, the following criteria were used: very often (≥ 1/10) (more than 10%); often (from ≥ 1/100 to <1/10) (more than 1% but less than 10%), infrequently (from ≥ 1/1000 to <1/100) (more than 0.1% but less than 1%),rarely (from ≥ 1/10000 to <1/1000) (more than 0.01% but less than 0.1%), very rarely (<1/10000) (less than 0.01%), including individual reports.

Disorders from the gastrointestinal tract:

Often: nausea and indigestion.

Impaired nervous system:

Often: headache.

In addition to these effects, revealed during clinical trials, post-marketing application and in the scientific literature, the following side effects were reported. The available data are insufficient to estimate their frequency.

Betagistin

Immune system disorders: hypersensitivity reaction, including anaphylactic reaction.

Disorders from the gastrointestinal tract: complaints of mild severity from the gastrointestinal tract, such as vomiting, gastrointestinal pain, bloating. These effects can be reduced by taking Nooserc drug during meals or when the dose is lowered.

Disturbances from the skin and subcutaneous tissues: hypersensitivity reactions from the skin and subcutaneous tissue, especially angioedema, itching and rash.

Pyracetam

Violations from the blood and lymphatic system:

The frequency is unknown: bleeding.

Immune system disorders:

The frequency is unknown: anaphylactoid reactions, hypersensitivity.

Disorders from the metabolism and nutrition:

Often: weight gain.

Disorders of the psyche:

Often: nervousness;

Infrequently: depression;

The frequency is unknown: agitation, anxiety, hallucinations, confusion.

Impaired nervous system:

Often: hyperactivity;

Infrequently: drowsiness;

The frequency is unknown: ataxia, imbalance, exacerbation of epilepsy, headache, insomnia, tremor.

Disorders from the gastrointestinal tract:

The frequency is unknown: nausea, vomiting, diarrhea, abdominal pain (including gastralgia).

Hearing disorders and labyrinthine disturbances:

Frequency unknown: vertigo.

Disturbances from the skin and subcutaneous tissues:

The frequency is unknown: dermatitis, itching, hives, angioedema.

On the part of the reproductive system:

Frequency unknown: increased sexual desire.

General disorders and disorders at the site of administration:

Infrequently: asthenia.

Overdose:

There is no information on overdose for Nooserc drug.

Betagistin

There are several cases of overdose of betagistin. Some patients experienced mild to moderate symptoms (nausea, drowsiness, abdominal pain) after taking the drug at doses up to 640 mg. More serious complications (seizures, cardiopulmonary complications) were observed with the deliberate use of increased doses of betagistin, especially in combination with overdose of other medications.

Treatment: symptomatic treatment is recommended.

Pyracetam

An isolated case of development of diarrhea in the form of diarrhea with blood and pain in the abdominal region after oral administration of piracetam orally in a daily dose of 75 g. Apparently, this was due to the use of a large total dose of sorbitol, which was previously part of the solution for oral administration.

Treatment: In case of a significant overdose, rinse the stomach or induce vomiting. It is recommended to carry out symptomatic therapy, which may include hemodialysis. There is no specific antidote. The efficacy of hemodialysis for piracetam is 50-60%.

Interaction:

Betagistin

Research of interaction with other medicinal preparations in vivo not conducted. Based on research data in vitro it can be assumed that there is no inhibition of the activity of cytochrome P450 isoenzymes in vivo.

Study Data in vitro showed inhibition of the metabolism of betahistin by monoamine oxidase (MAO) inhibitors, including MAO type B (for example, selegiline). Caution should be exercised while using betagistin and MAO inhibitors (including MAO-B).

Betagistin is an analog of histamine, so binding of betahistine with H blockers₁-gistaminovyh receptors can theoretically affect the effectiveness of one of these drugs.

Pyracetam

Thyroid hormones

At simultaneous application with hormones of a thyroid gland the reports on confusion of consciousness, irritability and disturbance of a dream are marked.

Acenocoumarol

According to the published study, in patients with recurrent venous thrombosis piracetam at a dose of 9.6 g / day does not change the dose of acenocoumarol necessary to achieve an international normalized ratio (INR) of 2.5 to 3.5, but compared with the effects of acenocoumarol alone,the addition of pyracetam at a dose of 9.6 g per day significantly reduces platelet aggregation, the release of (3-thromboglobulin, fibrinogen concentration and von Willebrand factor (VIII; C; VIII; vW; Ag; VIII; vW; RCo), as well as the viscosity of blood and plasma.

Pharmacokinetic interactions

The possibility of changing the pharmacokinetics of piracetam under the influence of other drugs is low, since 90% of the drug is excreted unchanged in urine.

In concentrations of 142, 426, 1422 μg / ml piracetam Does not inhibit cytochrome P450 isoenzymes (CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9 / 11).

For a concentration of 1422 μg / ml, minimal inhibition was observed CYP 2A6 (21%) and 3A4 / 5 (11%). However, the normal values of the inhibition constant (Ki), probably, can be achieved at a higher concentration. Thus, the metabolic interaction of piracetam with other drugs is unlikely.

Anticonvulsants

Admission piracetam at a dose of 20 g / day for 4 weeks in patients with epilepsy who received stable doses of antiepileptic drugs did not change the maximum and minimum concentration of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and valproic acid).

Alcohol

Joint intake with alcohol did not affect the concentration of piracetam in the serum; the concentration of ethanol in the serum did not change with the intake of 1.6 g of piracetam.

Special instructions:

Betagistin

Betagistin, which is a part of the drug Noerserk, can cause minor undesirable reactions from the stomach, so it is preferable to take tablets during meals, which reduces the severity of unwanted reactions.

The dose of Nooserk is prescribed after previously selected doses of individual components of the drug: betagistin and piracetam. If necessary, the dose of Nooserc can be changed, or individual doses of individual components can be preliminarily performed.

Pyracetam

Effect on platelet aggregation

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

Sodium

When treating patients on a hyponatrial diet, it is recommended that piracetam tablets in a dose of 24 g contain 46 mg of sodium.

Renal insufficiency

Because the piracetam is excreted by the kidneys, caution should be exercised when prescribing Nooserc to the patients with renal insufficiency.

Elderly patients

Long-term treatment of elderly patients requires regular monitoring of creatinine clearance, since dose adjustment may be required.

Piracetam penetrates the filtration membranes of hemodialysis apparatus.

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

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

Form release / dosage:

Tablets, film-coated, 16 mg + 800 mg; 24 mg + 800 mg.

Packaging:

For 28 or 56 tablets in a polyethylene bottle capped with a polypropylene lid with a desiccant. The bottle together with the instruction for use is placed in a pack of cardboard.

Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-004436

Date of registration:29.08.2017

Expiration Date:29.08.2022

The owner of the registration certificate:Abbott Productions AJAbbott Productions AJ Switzerland

Manufacturer: & nbsp

Research Institute of Chemical Diversity, JSC Russia

Representation: & nbspEBOBOT PRODUKTS LLCEBOBOT PRODUKTS LLCRussia

Information update date: & nbsp28.09.2017

Illustrated instructions

Instructions

Nooserk (Nooserc)