Universal reference book for medicines
Product name: NEURODOLON (NEIRODOLON)

Active substance: flupirtine

Type: Non-opioid analgesic of central action

Composition, form of production and packaging
Capsules hard gelatinous, the size №0, with the case and a lid of orange color; the contents of the capsules are almost white powder with inclusions in the form of small pieces of compressed mass or compacted mass of almost white color, crumbling when pressed lightly.
1 caps.

flupirtine maleate 100 mg

Excipients: calcium hydrophosphate dihydrate - 132 mg, pregelatinized starch - 62 mg, magnesium stearate - 3 mg, talc - 3 mg.

The composition of the capsule shell No. 0: 96 mg, incl.
body - dye sunset yellow sun - 0.059 mg, titanium dioxide - 1.18 mg, gelatin - 57.761 mg; lid - dye sunset yellow - 0.037 mg, titanium dioxide - 0.74 mg, gelatin - 36.223 mg.
10 pieces.
- Packings contour mesh (1) - packs cardboard.
10 pieces.
- Packings contour mesh (3) - packs cardboard.
10 pieces.
- Packings contour mesh (5) - packs cardboard.
15 pcs.
- Packings contour mesh (1) - packs cardboard.
15 pcs.
- packings contour mesh (2) - packs cardboard.
15 pcs.
- Packings contour mesh (3) - packs cardboard.
15 pcs.
- packings contour mesh (4) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2016.

PHARMACHOLOGIC EFFECT

Flupirtine is the representative of the "Selective Neuronal Potassium Channel Opener (SNEPCO)" and refers to the non-opioid analgesics of the central action.

Flupirtine activates G-protein-associated neuronal K + internal rectification channels.
The yield of K + ions causes stabilization of the resting potential and a decrease in the excitability of neuronal membranes. As a result, indirect inhibition of NMDA receptors (N-methyl-D-aspartate) occurs, since NMDA receptor blockade with Mg 2+ ions is maintained until cell membrane depolarization occurs (indirect NMDA receptor antagonistic action).
At therapeutically significant concentrations, flupirtine does not bind to alpha 1 , alpha 2 , 5HT 1 (5-hydroxy-tryptophan), 5HT 2 -serotonin, opioid, central m-and n-cholinergic receptors.

Such a central action of flupirtine leads to the realization of three main effects.

Analgesic effect

Due to the selective opening of potential-dependent K + channels of neurons with the concomitant release of K + ions, the resting potential of the neuron is stabilized.The neuron becomes less irritable.

The indirect antagonism of flupirtine against NMDA receptors protects neurons from the entry of Ca 2+ ions .
Thus, the sensitizing effect of increasing the intracellular concentration of Ca 2+ ions is mitigated.
Consequently, when the neuron is excited, inhibition of the transfer of ascending nociceptive impulses occurs.

Miorelaxing effect

The pharmacological effects described for the analgesic effect are functionally supported by the increased absorption of Ca2 + ions by mitochondria, which occurs at therapeutically significant concentrations.
The miorelaksiruyuschee effect arises as a result of concomitant inhibition of the transfer of impulses to motor neurons and the corresponding effects of interstitial neurons. Thus, this effect is manifested mainly in relation to local muscle spasms, and not in relation to the whole musculature as a whole.
The effect of the chronification processes

Chronicification processes should be considered as processes of neuronal conduction, due to the plasticity of the functions of neurons.

Through the induction of intracellular processes, the elasticity of the functions of the neurons creates the conditions for the implementation of mechanisms such as "inflation", under which the response for each subsequent impulse increases.
NMDA receptors (gene expression) are responsible for the launch of such changes.Indirect blockade of these receptors under the influence of flupirtine leads to suppression of these effects. Thus, unfavorable conditions are created for the clinical significance of chronic pain, and in the case of previous chronic pain, for "erasing" the pain memory by stabilizing the membrane potential, which leads to a decrease in pain sensitivity.
PHARMACOKINETICS

After ingestion flupirtine quickly and almost completely (90%) is absorbed into the digestive tract.
Up to 75% of the dose is metabolized in the liver with the formation of metabolites M 1 and M 2 . The active metabolite M 1 (2-amino-3-acetamino-6- (4-fluoro) -benzylaminopyridine) is formed as a result of hydrolysis of the urethane structure (1st reaction phase) and subsequent acetylation (reaction 2-stage) and provides, on average 25% of analgesic activity of flupirtine. Another metabolite M 2 - is not biologically active, is formed as a result of the oxidation reaction (1st phase) of p-fluorobenzyl, followed by conjugation (2nd phase) of p-fluorobenzoic acid with glycine. Studies on which isoenzyme is predominantly involved in the oxidative pathway of degradation have not been carried out. It should be expected that flupirtine will have only a small capacity for interaction.
T 1/2 flupirtine from the blood plasma is about 7 hours (10 hours for the main substance and metabolite M 1 ), which is sufficient to provide an analgesic effect.

The concentration of flupirtine in the blood plasma is proportional to the dose.

In elderly people (over 65 years), compared with young patients, an increase in T 1/2 (up to 14 hours with a single admission and up to 18.6 hours with admission for 12 days) and C max of the drug in the blood plasma, respectively in 2-2.5 times higher.

Mostly excreted by the kidneys (69%): 27% - unchanged, 28% - in the form of metabolite M 1 (acetyl-metabolite), 12% - in the form of metabolite M 2 (p-fluorohypuric acid);
1/3 of the administered dose is excreted as metabolites of an unexplained structure. A small part of the dose is excreted from the body with bile and feces.
INDICATIONS

- Treatment of acute pain of mild to moderate severity in adults.

DOSING MODE

Inside, without chewing the capsule and washing down with a sufficient amount of liquid (preferably water).
If possible, the drug is taken while standing upright.
In exceptional cases, the capsule of the drug Neurodolone can be opened and taken inside / through the probe only the contents of the capsule.
When ingestion of the contents of the capsule, it is recommended to neutralize its bitter taste by eating food, for example, a banana.
Apply 100 mg (1 caps.) 3-4 times / day with equal intervals between doses.
At the expressed pains - on 200 mg (2 caps.) 3 times / sut. The maximum daily dose is 600 mg / day (6 caps.).
Doses are selected depending on the intensity of pain and individual tolerance of the drug.
Use the lowest effective dose for the shortest possible time. Duration of treatment should not exceed 2 weeks.
Patients older than 65 years: at the beginning of treatment, 100 mg (1 caps.) 2 times / day in the morning and evening.
The dose may be increased to 300 mg, depending on the intensity of pain and the tolerability of the drug.
In patients with renal insufficiency , the concentration of creatinine in the blood plasma should be monitored.
The maximum daily dose should not exceed 300 mg / day (3 caps.).
In patients with mild to moderate renal failure: dose adjustment is not required.

In patients with severe renal failure or with hypoalbuminemia: the maximum daily dose should not exceed 300 mg / day (3 caps.).
If it is necessary to use the drug in a higher dose, patients should be under the supervision of a doctor.
SIDE EFFECT

Classification of WHO frequency of development of side effects: very often -? 1/10 appointments (> 10%), often - from? 1/100 to <1/10 appointments (> 1% and <10%), infrequently from? 1 / 1000 to <1/100 of prescriptions (> 0.1% and <1%), rarely from? 1/10 000 to <1/1000 appointments (> 0.01% and <0.1%), very rarely - <1/10 000 prescriptions (<0.01%), the frequency is unknown (it is impossible to estimate based on available data).

From the hepatobiliary system: very often - increased activity of "liver" transaminases;
frequency unknown - hepatitis, hepatic insufficiency.
On the part of the immune system: often - increased sensitivity to the drug, allergic reactions (in some cases accompanied by fever, skin rashes, hives, skin itching).


From the side of metabolism: often - lack of appetite.

From the nervous system: often - sleep disturbance, depression, anxiety / nervousness, dizziness, tremor, headache;
infrequently - confused consciousness.
From the side of the organ of vision: often - impaired vision.

From the gastrointestinal tract: often - dyspepsia, nausea, vomiting, pain in the stomach, constipation, abdominal pain, dryness of the oral mucosa, flatulence, diarrhea.

From the skin and subcutaneous tissues: often - sweating.

Other: very often fatigue / weakness (in 15% of patients), especially at the beginning of treatment.

Side effects mainly depend on the dose of the drug (with the exception of allergic reactions).
In many cases, they disappear by themselves as they take place or after the end of treatment.
CONTRAINDICATIONS

- hypersensitivity to the active substance or any other component of the drug;

- Patients with a risk of developing hepatic encephalopathy and patients with cholestasis,
can develop encephalopathy or aggravate the course of already existing encephalopathy or ataxia;
- patients with myasthenia gravis in connection with the miorelaksiruyuschim action flupirtina;

- patients with concomitant liver disease or alcoholism;

- simultaneous use of flupirtine with other drugs that can have hepatotoxic effects;

patients with newly healed or existing ringing in the ears;
these patients have a high risk of activity of "hepatic" enzymes;
- Children under 18 years.

Carefully

Renal failure, hypoalbuminemia, elderly age over 65 years.

PREGNANCY AND LACTATION

There is insufficient data on the use of flupirtine in pregnancy.
In experimental studies on animals, flupirtin showed reproductive toxicity, but not teratogenicity. A potential risk to a person is not known. Neurodolone should not be used during pregnancy, except when the benefit to the mother exceeds the potential risk to the fetus.
According to the research, flupirtine penetrates into breast milk in a small amount.
In this regard, Neurodolone can not be used during breastfeeding, except when there is an extreme need for taking the drug. If it is necessary to use Neurodolone during lactation, breastfeeding should be stopped.
APPLICATION FOR FUNCTIONS OF THE LIVER

In patients with mild to moderate renal failure: dose adjustment is not required.

With caution, apply the drug to patients with renal insufficiency.

In patients with renal insufficiency , the concentration of creatinine in the blood plasma should be monitored.
The maximum daily dose should not exceed 300 mg / day (3 caps.).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated use of the drug in patients with concomitant liver disease or alcoholism.

APPLICATION FOR CHILDREN

Contraindicated use of the drug for children and adolescents under the age of 18 years.

APPLICATION IN ELDERLY PATIENTS

With caution apply the drug to patients older than 65 years.

Patients older than 65 years: at the beginning of treatment, 100 mg (1 caps.) 2 times / day in the morning and evening.
The dose may be increased to 300 mg, depending on the intensity of pain and the tolerability of the drug.
SPECIAL INSTRUCTIONS

The drug Neurodolone should be used if treatment with other analgesics (eg, NSAIDs or light opioid drugs) is contraindicated.

In patients with impaired renal function, the concentration of creatinine in the blood plasma should be monitored.

In patients older than 65 years or with severe signs of renal failure or hypoalbuminemia, dose adjustment is necessary.

During treatment with the drug Neurodolone, once a week, it is necessary to monitor the liver function status.
when flupirtin is used, it is possible to increase the activity of "liver" transaminases, the development of hepatitis of hepatic insufficiency.
If the results of the liver test deviate from the norm or if there are clinical symptoms that indicate liver damage, then stop using the drug Neurodolone.

Patients should be warned that during treatment with Neurodolone, attention should be paid to any symptoms of liver damage (eg, lack of appetite, nausea, vomiting, stomach pain, fatigue, dark urine, jaundice, pruritus).
If these symptoms occur, stop taking Neurodolone and consult a doctor urgently.
In the treatment of flupirtin, false positive reactions of the test with diagnostic strips for bilirubin, urobilinogen and protein in the urine are possible.
A similar reaction is possible with a quantitative determination of the concentration of bilirubin in the blood plasma.
When applying the drug in high doses, in some cases, the color of urine can be marked green, which is not a clinical sign of any pathology.

Impact on the ability to manage vehicles and mechanisms

Given that the drug Neurodolone can weaken attention and slow the reaction rate, during treatment it is recommended to refrain from managing transportation and practicing potentially hazardous activities.
It is especially important to remember this when using alcohol at the same time.
OVERDOSE

There are reports of single cases of overdose with suicidal measurements.
In doing so, taking a dose of 5 g flupirtine caused the following symptoms: nausea, tachycardia, prostration, tearfulness, stupor, confusion, stunned consciousness, dryness of the oral mucosa.
After vomiting or use of forced diuresis, reception of activated carbon and the introduction of electrolytes, the state of health was restored within 6-12 hours. There were no reports of life-threatening conditions.

In case of overdose or signs of intoxication, one should bear in mind the possibility of occurrence of disorders from the central nervous system, as well as the manifestation of hepatotoxicity but the type of enhancement of metabolic disorders in the liver.
It should be symptomatic treatment. Specific antidote is not known


DRUG INTERACTION

Strengthens the effect of alcohol, sedatives and muscle relaxants.
Due to the fact that flupirtine has a high degree of connection with proteins, it can change the degree of binding to proteins of other concomitantly used drugs. As a result of the in vitro study of the interaction of flupirtine with warfarin, acetylsalicylic acid, diazepam, benzylpenicillip, digoxin, glibenclamide, propranolol, clonidine, it was found that only veropamil and diazepam are displaced by flupirtine from binding to plasma proteins, which can lead to an increase in their activity.
With simultaneous application of flupirtine and indirect anticoagulants - coumarin derivatives, it is recommended to monitor prothrombin time on a regular basis in order to timely correct the dose of direct anticoagulants.
There are no data on the interaction with other anticoagulants or antiplatelet agents (acetylsalicylic acid, etc.).With the simultaneous use of flupirtine with drugs that are metabolized in the liver, regular monitoring of the activity of "hepatic" enzymes is required. Combined use of flupirtine and drugs containing paracetamol and carbamazepine should be avoided.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored in a dry place inaccessible to children, protected from light at a temperature of no higher than 25 ° C.
Shelf life - 2 years.
Do not use after the expiration date.

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