Nolodatak
Nolodatak: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Nolodatac
ATX code: N02BG07
Active ingredient: flupirtine (flupirtine)
Manufacturer: Akrikhin, JSC (Russia)
Description and photo updated: 22.11.2018
Nolodatak is an analgesic non-narcotic drug.
Release form and composition
Nolodatak is produced in the form of capsules: brown, gelatinous solid, size No. 1; the contents of the capsules are powder from white to white with a gray or yellow shade of color (10 pcs. in a blister strip, in a cardboard box of 1, 3 or 5 packages).
1 capsule contains:
- active substance: flupirtine maleate - 100 mg (in terms of 100% substance);
- additional substances: sodium carboxymethyl starch, magnesium stearate, calcium hydrogen phosphate dihydrate, copovidone, colloidal silicon dioxide;
- capsule shell: titanium dioxide, gelatin, dyes - iron oxides red, yellow and black.
Pharmacological properties
Pharmacodynamics
Flupirtine is a centrally acting non-opioid analgesic and belongs to the class of Selective Neuronal Potassium Channel Opener (SNEPCO). The active substance Nolodatak does not lead to addiction and withdrawal syndrome, and also exhibits a muscle relaxant effect.
Due to the ability of flupirtine to activate neuronal potassium channels of internal rectification associated with G-protein, potassium ions are released, leading to stabilization of the resting potential and a decrease in the excitability of neuronal membranes. This process provides inhibition of the activity of NMDA (N-methyl-D-aspartate) receptors due to the fact that the blockade of NMDA receptors by magnesium ions proceeds before the onset of depolarization of the cell membrane (indirect antagonism against NMDA receptors).
Flupirtine at therapeutic concentrations does not show a connection with alpha1-, alpha2-adrenergic receptors, serotonin 5HT1-, 5HT2-receptors, benzodiazepine, dopamine, opioid, central muscarinic and nicotine-sensitive cholinergic receptors (m- and n-cholinergic receptors).
The central action of the active substance Nolodataka is realized due to three main effects:
- analgesic effect: flupirtine, as a result of the activation of voltage-independent potassium channels, stabilizes the membrane potential of the nerve cell; this is accompanied by suppression of the activity of NMDA receptors and causes the blockade of neuronal calcium ion channels and a decrease in the current of calcium ions inside the cell; due to the arising inhibition of neuron excitation in response to nociceptive stimuli (inhibition of nociceptive activation), an analgesic effect occurs and a slowdown in the response of neurons to repeated exposure to pain stimuli is observed, which prevents the intensification of pain and its transition into a chronic form, and in the presence of chronic pain syndrome, it provides its weakening intensity;also revealed the ability of flupirtine to affect the perception of pain through the descending noradrenergic system;
- muscle relaxant effect: the antispastic effect of the substance on muscles is due to inhibition of the transmission of impulses to motoneurons and intercalary neurons, as a result of which muscle tension is relieved; this property of flupirtine demonstrates against the background of many chronic diseases occurring with painful muscle spasms (fibromyalgia, tension headaches, arthropathies, musculoskeletal pain in the neck and back);
- the effect of the processes of chronization: the processes of chronization are considered as processes of impulse conduction by neurons associated with the ability of the latter to regenerate and create new neural connections (elasticity of neuronal functions); by activating intracellular processes, the plasticity of neuronal functions provides conditions for triggering mechanisms such as inflation, during which an increase in the response to each subsequent pain impulse is noted, NMDA receptors play an important role in the implementation of such changes (gene expression); due to the influence of flupirtine, an indirect blockade of these receptors and suppression of their action occurs; thus, the drug prevents the transition of pain into a chronic form, and in case of already existing chronic pain, it helps to erase pain memory by stabilizing the membrane potential,leading to a decrease in pain sensitivity.
Pharmacokinetics
After oral administration of Nolodatak, flupirtine is rapidly and almost completely (90%) absorbed from the gastrointestinal tract, the level of the active substance in the blood plasma is proportional to the dose.
In the liver, up to 75% of the taken dose of the agent undergoes metabolic transformation with the formation of an active metabolite M1 and an inactive metabolite M2. The metabolite M1 [2-amino-3-acetamino-6- (4-fluoro) -benzylaminopyridine], formed by hydrolysis of the urethane structure (phase I of the reaction) and further acetylation (phase II of the reaction), provides about 25% of the analgesic effect of flupirtine. The second metabolite M2 is formed as a result of the oxidation reaction (phase I) of p-fluorobenzyl, followed by conjugation (phase II) of p-fluorobenzoic acid with glycine.
Which of the isoenzymes is predominantly involved in the oxidative destruction pathway has not been established. It is assumed that flupirtine has only a slight ability to interact with other drugs.
The half-life (T1 / 2) from blood plasma is approximately 7 hours (10 hours for the M1 metabolite and flupirtine), which is a sufficient condition for providing an analgesic effect when the drug is taken in accordance with the recommended dosing regimen.
About 69% of the administered dose is excreted by the kidneys: in the form of the M1 metabolite (acetyl metabolite) - 28%, in the form of the M2 metabolite (p-fluorohydrapuric acid) - 12%, unchanged - 27%, the remaining part (1/3) is excreted in the form of metabolites, the structure of which has not yet been clarified. A small part of the dose is excreted in the intestines with bile.
Indications for use
According to the instructions, Nolodatak is recommended for the treatment of acute pain of mild to moderate intensity in adults.
Contraindications
Absolute:
- the presence of a risk of developing hepatic encephalopathy and cholestasis (encephalopathy may occur or the course of an already existing encephalopathy or ataxia may be complicated);
- myasthenia gravis (due to the muscle relaxant effect of flupirtine);
- concomitant liver disease;
- alcoholism;
- age up to 18 years;
- existing or recently healed tinnitus (due to a high risk of increased activity of liver enzymes);
- combined use with other drugs that can have a hepatotoxic effect;
- hypersensitivity to any of the constituents of the drug.
Relative (requires using Nolodatak with caution):
- advanced age (over 65);
- hypoalbuminemia;
- renal failure.
Instructions for using Nolodatak: method and dosage
Nolodatak is taken orally. The capsule, without chewing, is swallowed whole with 100 ml of liquid. It is advisable to take the remedy while sitting or standing.
If necessary, in some cases, you can open the capsule and use only the powder contained in it, dissolving it in water. To neutralize the very bitter taste of the resulting solution, it is recommended to eat.
The dose is selected taking into account the degree of pain intensity and the patient's individual sensitivity to flupirtine. It is recommended to take Nolodatak 1 capsule (100 mg) 3-4 times a day with equal intervals between doses. With severe pain syndrome, 2 capsules (200 mg) are prescribed 3 times a day. The maximum allowable daily dose should not exceed 6 capsules (600 mg). The duration of treatment is determined by the attending physician after assessing the dynamics of the pain syndrome and depending on the tolerance of the drug. Against the background of long-term use, it is required to monitor the activity of hepatic transaminases to detect possible early signs of hepatotoxicity. The course of therapy should not exceed 14 days.
For patients with hypoalbuminemia, Nolodatak is prescribed in a daily dose not exceeding 3 capsules (300 mg). If it is necessary to take higher doses, it is necessary to monitor the patient's condition.
Side effects
- nervous system: often - dizziness, sleep disturbance, headache, tremors, anxiety / nervousness, depression; infrequently - confused consciousness;
- liver and biliary tract: very often - increased activity of hepatic transaminases; with an unknown frequency - liver failure, hepatitis;
- metabolism: often - lack of appetite;
- Gastrointestinal tract: often - nausea, pain in the epigastric region, dyspepsia, vomiting, abdominal pain, constipation, flatulence, dryness of the oral mucosa, diarrhea;
- immune system: infrequently - allergic reactions (sometimes manifested by skin rash, itching, hives, fever), hypersensitivity to the drug;
- skin and subcutaneous tissue: often - sweating;
- organ of vision: infrequently - visual impairment;
- others: very often - fatigue / weakness (in 15% of patients), in most cases at the beginning of the course.
Side effects, as a rule, depend on the dose of flupirtine (with the exception of allergic reactions) and in many cases go away on their own with further therapy or after its completion.
Overdose
There are isolated cases of Nolodatak overdose with the aim of committing suicide. At the same time, while taking flupirtine at a dose of 5 g, the following reactions were observed: dry mouth, nausea, tearfulness, a state of prostration, stunnedness, confusion, tachycardia. After forced diuresis or vomiting, the introduction of electrolytes and the intake of activated charcoal, the improvement in well-being was noted after 6-12 hours. There were no reports of the development of life-threatening symptoms.
It should be borne in mind that against the background of an overdose or when signs of intoxication appear, undesirable effects from the central nervous system and the manifestation of toxic effects on the liver by the type of aggravation of metabolic disorders in the liver may occur. In this case, symptomatic treatment is prescribed. There is no specific antidote.
special instructions
Nolodatak is recommended to be taken only when therapy with other pain relievers, including non-steroidal anti-inflammatory drugs (NSAIDs) or opioids, is contraindicated.
While taking the drug, you need to pay attention to any symptoms that are characteristic of liver damage (for example, feeling tired, nausea, loss of appetite, vomiting, abdominal pain, dark urine, itching, jaundice). If any of these violations occurs, you must stop taking Nolodatak and urgently consult a doctor.
During the period of therapy, false-positive results of establishing the concentration of urobilinogen, bilirubin and protein in urine are possible when a test with diagnostic strips is performed. There is a likelihood of a similar reaction when quantifying plasma bilirubin.
Against the background of the use of flupirtine in high doses, in some cases, urine may turn green; this phenomenon does not apply to clinical signs of any disorder.
Influence on the ability to drive vehicles and complex mechanisms
In connection with the possible appearance of drowsiness and dizziness when using Nolodatak during treatment, patients should refrain from driving vehicles and other potentially dangerous and complex mechanisms. It is imperative to keep this in mind while drinking alcohol.
Application during pregnancy and lactation
There is insufficient information on the use of flupirtine during pregnancy. In experimental studies on animals, the active substance demonstrated reproductive toxicity, but no teratogenic effect was detected. The potential threat to humans is unknown.
The use of Nolodatak during pregnancy is allowed only in extreme cases, when the intended benefits of therapy for the mother significantly outweigh the possible risk to the fetus.
Flupirtine, according to research results, is found in small amounts in breast milk. As a result, it is impossible to take the drug during breastfeeding, except in cases where its appointment is extremely necessary, during the course it is required to stop breastfeeding.
Pediatric use
Nolodatak is contraindicated in patients under 18 years of age.
With impaired renal function
In the presence of renal failure during the period of drug therapy, it is required to control the level of creatinine in the blood plasma. No dose adjustment of Nolodatak is required for patients with mild to moderate renal impairment.
Patients with severe renal failure need to change the dosage of the drug, the maximum daily dose in this category of patients should not be more than 3 capsules (300 mg). If it is necessary to prescribe Nolodatak in a higher dose, patients need careful medical supervision.
For violations of liver function
In view of the risk of increased activity of hepatic transaminases, as well as the occurrence of liver failure and hepatitis, during treatment with Nolodatak, it is recommended to monitor the state of liver function once a week.
If the results of the study of liver activity deviate from the norm or the manifestation of clinical symptoms characteristic of liver diseases, the drug should be discontinued.
If the patient has reduced liver function, the drug must be taken in a daily dose not exceeding 2 capsules (200 mg).
Use in the elderly
In the elderly, when compared with young patients, an increase in T1 / 2 of flupirtine was noted (with a single dose - up to 14 hours, when used for 12 days - up to 18.6 hours), and the maximum plasma concentration in the blood, respectively, in 2 –2.5 times.
Patients over 65 are recommended to take Nolodatak at the beginning of therapy, 1 capsule (100 mg) 2 times a day - in the morning and in the evening. Depending on the severity of the pain and the tolerance of the drug, it is possible to increase the dose to 3 capsules.
Drug interactions
- sedatives, muscle relaxants, ethanol: the effect of these drugs is enhanced;
- benzylpenicillin, glibenclamide, acetylsalicylic acid, digoxin, clonidine, propranolol, diazepam, warfarin: an increase in the activity of these drugs caused by flupirtine when they are displaced from the connection with proteins is possible (this is especially true for warfarin and diazepam);
- coumarin derivatives (including warfarin): it is possible to change the prothrombin index (increase the anticoagulant effect), it is required to regularly monitor this indicator for the timely appropriate adjustment of the coumarin dose; there is no information on the interaction of the drug with other anticoagulants / antiplatelet agents;
- drugs, the metabolism of which occurs in the liver: an increase in the activity of liver enzymes is possible, regular monitoring of their level is required;
- medicines containing carbamazepine and paracetamol: this combination is not recommended.
Analogs
Analogs of Nolodatak are Katadolon, Neurodolon, Katadolon Forte, Flugesik.
Terms and conditions of storage
Store in a place protected from light and moisture, at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Nolodatak
According to numerous reviews, Nolodatak is an effective tool used to relieve pain syndrome of mild to moderate severity of various origins. Patients note that the drug effectively and quickly relieves headache, toothache and muscle pain, pain in the back, lower back and buttocks against the background of an intervertebral hernia, pain after fractures, and does not cause addiction and dependence.
At the same time, during the intake, there is a frequent development of undesirable effects, such as nausea, stomach pain, heartburn, diarrhea, headache, dizziness, nervousness.
Price for Nolodatak in pharmacies
The approximate price for Nolodatak is (capsules 100 mg): 10 pcs. in a package - 300-380 rubles, 30 pcs. - 570-680 rubles, 50 pcs. - 1,080-1140 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
