Neurodolone (Neurodolon)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceFlupirtineFlupirtine
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    • Dosage form: & nbspcapsules
    Composition:

    1 capsule contains:

    active substance: flupirtine maleate 100 mg;

    Excipients: calcium hydrogen phosphate dihydrate 132 mg, corn pregelatinized corn starch 62 mg, magnesium stearate 3 mg, talc 3 mg;

    hard gelatin capsule № 0 - 96 mg, including: body - dye sunset sunset yellow 0.059 mg, titanium dioxide 1.18 mg, gelatin 57.761 mg, cap - dye sunset sunset yellow 0.037 mg, titanium dioxide 0.74 mg. gelatin 36.223 mg.

    Description:
    Hard gelatin capsules No. 0. Cap and orange colored body. The contents of the capsules are almost white powder with inclusions in the form of several pieces of compressed mass or compacted mass of almost white color, crumbling when pressed lightly.
    Pharmacotherapeutic group:Analgesic non-narcotic remedy
    ATX: & nbsp

    N.02.B.G.07   Flupirtine

    Pharmacodynamics:

    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+ channels of morning rectification. The yield of ions K+ causes stabilization of the resting potential and a decrease in the excitability of neuronal membranes. As a result, there is direct inhibition of NMDA receptors (N-methyl-D-aspartate), since NMDA receptor blockade by Mg ions2+ is maintained until the cell membrane depolarization occurs (an indirect antagonistic effect on NMDA receptors).

    At therapeutically significant concentrations flupirtii does not bind to alpha1, alpha2-, 5HT1 (5-hydroxytryptophan) -, 5HT2serotonin, opioid, central m- and n-cholinergic receptors.

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

    Analgesic effect

    Because of the selective discovery of potential-dependent K+ channels of neurons with a concomitant release of ions K+ The resting potential of the neuron is stabilized. The neuron becomes less irritable.

    The indirect apatagonism of flupirtine against MNDA receptors protects neurons from the entry of Ca ions2+. Thus, the sensitizing effect of increasing the intracellular concentration of Ca2+.

    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 reinforced by the enhancement of the absorption of Ca2+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 processes of chronicle

    Chronicification processes should be considered as neuronal conductivity processes caused by the plasticity of neuronal functions, the means of induction of intracellular processes, the elasticity of the functions of 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, to "erase" the pain memory by stabilizing the membrane potential, which leads to a decrease in left sensitivity.

    Pharmacokinetics:

    After oral administration 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 M1 them2. Active metabolite M1 (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 an average of 25% analgesic activity flupirtine. Another metabolite of M2 - is not biologically active, is formed as a result of the oxidation reaction (1st phase) of p-fluorobeisyl with the following conjugation (2nd phase) of n-fluorobenzoic acid with glycine. Studies on which isoenzyme predominantly participates in the healing pathway of destruction have not been carried out. It should be expected that flupirtine will have only a small capacity for interaction.

    T1/2 flupirtine from the blood plasma is about 7 hours (10 hours for the main substance and metabolite M1), which is sufficient to provide an analgesic effect.

    The concentration of flupirtine in the blood plasma is proportional to the dose, of the elderly (over 65 years), compared with young patients, an increase in the half-life (T1/2) (up to 14 hours with a single dose and up to 18.6 hours with admission for 12 days) and the maximum concentration of the drug in the blood plasma (Cmax), respectively, 2-2.5 times higher.

    Mostly excreted by the kidneys (69%): 27% - unchanged, 28% in the form of metabolite M1 (acetyl-metabolite), 12% - in the form of metabolite M2 (n-fluorohippuric 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 in adults
    Contraindications:

    Hypersensitivity to the active ingredient or any other component of the drug.

    Patients with a risk of developing hepatic encephalopathy and patients with cholestasis, since.can develop encephalopathy or aggravate the course of already existing encephalopathy or ataxia.

    Patients with myasthenia gravis in connection with the muscle relaxant effect of flupirtine.

    Patients with concomitant liver disease or alcoholism.

    The simultaneous use of flupirtine with other drugs that may have hepatotoxic effects.

    Patients with newly healed or existing ringing in the ears, because 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 flupirtine showed a productive 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 studies, flupirtine in a small amount penetrates into breast milk.In this regard, Neurodolone can not be used during breastfeeding, except when there is an extreme need for taking the drug. If you need to use the drug Neurodolone during lactation should stop breastfeeding.

    Dosing and Administration:

    Inside, without chewing the capsule and washing down with a sufficient amount of liquid is preferable to water). If possible, the drug is taken while in an upright position.

    In exceptional cases, the capsule of the drug Neurodolone can be opened and taken inside / inserted 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 capsule) 3-4 times a day with equal intervals between doses. At the expressed pains - but 200 mg (2 capsules) 3 times a day ,.

    The maximum daily dose is 600 mg / day (6 capsules).

    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 starting at 65 years of age: at the beginning of treatment, 100 mg (1 capsule) 2 times a 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 should monitor the concentration of creatinine in the blood plasma. The maximum daily dose should not exceed 300 mg / day (3 capsules).

    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 capsules). If it is necessary to use the drug in a higher dose, patients should be under the supervision of a doctor.

    Side effects:

    Classification of WHO frequency of development of side effects:

    very often ≥1 / 10 appointments (> 10%)

    often from ≥1 / 100 to <1/10 of prescriptions (> 1% and <10%)

    infrequently from ≥1 / 1000 to <1/100 of prescriptions (> 0.1% and <1%)

    rarely from ≥1 / 10000 to <1/1000 assignments (> 0.01% and <0.1%)

    very rarely <1/10000 prescriptions (<0.01%)

    frequency is unknown (can not be estimated based on available data)

    Disorders from the hepatobiliary system:

    Very often - an increase in the activity of "Hepatic" transamiaasis;

    frequency unknown - hepatitis, hepatic insufficiency.

    From the immune system:

    often - hypersensitivity to the drug, allergic reactions (in some cases accompanied by fever, skin, urticaria, skin itching).

    From the side of metabolism:

    often - lack of appetite.

    From the nervous system:

    often - sleep disturbance, depression, anxiety / nervousness, dizziness, tremor, headache;

    not often confused.

    From the side of the organ of vision:

    often - visual impairment.

    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 to themselves as they take place or after the end of treatment.

    Overdose:

    There are reports of single cases of overdose with suicidal intentions. In doing so, taking a dose of 5 g of flupirtine caused the following symptoms: nausea,tachycardia, prostration, tearfulness, stupor, confusion, stunned consciousness, dryness of the oral mucosa.

    After vomiting or using forced diuresis, reception of activated carbon and the introduction of electrolytes, the state of health was restored within 6-12 hours. No life-threatening conditions have been reported.

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

    Interaction:

    Strengthens the effect of alcohol, sedatives and muscle relaxants. Due to flupirtine has a high degree of connection with proteins, it can change the degree of binding to proteins of other simultaneously used drugs. As a result of the in vitro study of the interaction of flupirtine with warfarin, tilsalicylic acid, diazepam, benzylpenicillip, digoxin, glypenclamide, propranolol, cloidin, it was found that only veropamil and diazepam are displaced by flupirtine from the bond with 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 anticoagulant or antiplatelet agents (acetylsalicylic acid and etc.). With the simultaneous use of flupirtine with drugs that are metabolized in the liver, regular monitoring of the activity of "liver" enzymes is required. Combined use of flupirtine and medications containing paracetamol and carbamazepine.

    Special instructions:

    The drug Neurodolone should be used if treatment with other analgesics (for example, non-steroidal anti-inflammatory drugs (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 insufficiency or hypoalbuminemine, dose adjustment is necessary. During treatment with the drug Neurodolone, once a week should monitor the status of liver function, as with flupirtin therapy may 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 the drug, the neurodolone should pay attention 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 agnostic strips on bilirubin, urobilinogen and protein in the urine are possible, a similar reaction is possible in the 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.

    Effect on the ability to drive transp. cf. and fur: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 dangerous species of wholeness. It is especially important to remember this when using alcohol at the same time.
    Form release / dosage:Capsules 100 mg.
    Packaging:

    For 10 and 15 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    For 1, 3, 5 contour cell packs of 10 capsules or 1,2,3.4 outline packagings of 15 capsules together with the instructions for use are placed in a pack of cardboard.

    Storage conditions:
    In a dry, protected from light 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 the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-003082
    Date of registration:10.07.2015
    Expiration Date:10.07.2020
    The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia
    Information update date: & nbsp27.06.2018
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