Nolodatak - instructions for use, reviews, analogs and form of release (capsules or tablets 100 mg) of an anesthetic for the treatment of headaches, during menstruation and after surgery in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Nolodatak. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Nolodataka in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Nolodatak in the presence of existing structural analogs. Use for the treatment of headaches, during menstruation and after surgery in adults, children, as well as during pregnancy and lactation. Composition of an anesthetic drug.

Nolodatak - a non-opioid analgesic of central action. Flupirtine (the active substance of the preparation Nolodatak) is a representative of the class of selective activators of neuronal potassium channels. Does not cause addiction and addiction, it has a miorelaksiruyuschee effect.

Flupirtine activates G-protein-associated neuronal potassium channels of internal rectification. The yield of potassium 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 the NMDA receptor blockade with magnesium ions persists until the cell membrane depolarization occurs (indirect NMDA receptor antagonism).

In therapeutic concentrations, flupirtine does not bind to alpha1, alpha2-adrenoreceptors, serotonin 5HT1, 5HT2 receptors, dopamine, benzodiazepine, opioid, central m-and n-cholinergic receptors.

Analgesic effect

Nolodate activates potential-independent potassium channels, which leads to stabilization of the membrane potential of the nerve cell.This inhibits the activity of NMDA receptors and, as a consequence, blockade of neuronal ionic calcium channels, a decrease in the intracellular current of calcium ions. Due to the developing inhibition of neuron excitation in response to nociceptive stimuli (inhibition of nociceptive activation), an analgesic effect is realized. This inhibits the growth of the neuronal response to repeated pain stimuli, which prevents the increase of pain and its transition to a chronic form, and with the existing chronic pain syndrome leads to a decrease in its intensity. The modulating effect of flupirtine on the perception of pain through the descending noradrenergic system was also established.

Miorelaksiruyuschee action

Antispastic action on muscles is associated with blocking the transmission of excitation to motoneurons and intercalary neurons, leading to the removal of muscle tension. This action of Nolodatak is manifested in many chronic diseases accompanied by painful muscular spasms (musculoskeletal pain in the neck and back, arthropathy, tension headaches, fibromyalgia).

Composition

Flupirtine maleate + excipients.

Pharmacokinetics

After ingestion of Nolodatak quickly and almost completely (90%) is absorbed from the digestive tract. The concentration of the active substance in the blood plasma is proportional to the dose. Up to 75% of the dose is metabolized in the liver with the formation of metabolites M1 and M2. Active metabolite M1 (2-amino-3-acetamino-6- [4-fluoro] -benzilaminopiridin) formed by the hydrolysis of the urethane structures (phase 1 reactions) followed by acetylation (2 phase reaction), provides an average of 25% of analgesic activity of flupirtine . Another metabolite M2 - biologically inactive, is formed by the oxidation reaction (phase 1 reactions), para-fluorobenzyl followed by conjugation (two phase reaction) of p-fluorobenzoic acid with glycine. It should be expected that flupirtine will have only a small capacity for interaction. Write mainly kidneys (69%): 27% - unchanged, 28% - as a metabolite M1 (acetyl metabolite), 12% - in the form M2 metabolite (para-ftorgippurovaya 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 in the intestine.

Indications

• treatment of acute pain of mild to moderate intensity in adults (muscle spasm, malignant neoplasms, algodismenorea, headache, posttraumatic pain,traumatological / orthopedic operations and interventions).

Forms of release

Capsules 100 mg.

Other dosage forms, be it tablets or injections in ampoules for injection at the time of publication of the drug in the Directory did not exist.

Instructions for use and dosage

The drug is taken orally. The capsule should be swallowed whole, not liquid and squeezed with a small amount of liquid (100 ml). If possible, take the drug in a sitting or standing position. In exceptional cases, the capsule can be opened and dissolved in water; neutralize the bitter taste of the contents of the capsule is recommended by eating food.

The dose is selected depending on the intensity of pain and individual sensitivity of the patient to the drug.

The recommended dose is 1 capsule 3-4 times a day at equal intervals between doses. At the expressed pains - on 2 capsules 3 times a day. The maximum daily dose is 600 mg (6 capsules).

The duration of therapy is determined by the attending physician and depends on the dynamics of the pain syndrome and tolerability. With prolonged use, the activity of hepatic transaminases should be monitored in order to identify early symptoms of hepatotoxicity.Duration of treatment should not exceed 2 weeks.

Patients over the age of 65 years at the beginning of treatment are prescribed 1 capsule 2 times a day (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 reduced liver function, the daily dose should not exceed 200 mg (2 capsules).

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 per day (3 capsules). In patients with mild to moderate renal failure, dose adjustment is not required. In patients with severe renal insufficiency or hypoalbuminemia, the maximum daily dose should not exceed 300 mg per day (3 capsules).

If it is necessary to prescribe the drug at higher doses, careful monitoring is established for the patients.

Side effect

• hypersensitivity to the drug;
• allergic reactions (in some cases accompanied by fever, skin rashes, hives, skin itching);
• lack of appetite;
• sleep disturbance;
• depression;
• anxiety / nervousness;
• dizziness;
• tremor;
• headache;
• confused consciousness;
• impaired vision;
• dyspepsia;
• nausea, vomiting;
• pain in the epigastric region;
• constipation, diarrhea;
• abdominal pain;
• dryness of the oral mucosa;
• flatulence;
• increased activity of hepatic transaminases;
• hepatitis;
• liver failure;
• sweating;
• 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

• patients with a risk of developing hepatic encephalopathy and cholestasis (possibly the development of encephalopathy or aggravation of already existing encephalopathy or ataxia);
• myasthenia gravis (due to the muscle relaxant effect of flupirtine);
• concomitant liver disease;
• alcoholism;
• simultaneous application of flupirtine with other drugs that can have hepatotoxic effects;
• tinnitus (including recently healed);
• children and adolescents under 18;
• hypersensitivity to the active substance or any other component of the drug.

Application in pregnancy and lactation

There is insufficient data on the use of Nolodatak in pregnancy. In experimental animal studies, flupirtin showed reproductive toxicity, but not teratogenicity. The potential risk to humans is unknown. The drug Nolodatak should not be used during pregnancy, except when the intended benefit to the mother exceeds the potential risk to the fetus.

According to the studies, flupirtine in small amounts is excreted in breast milk. In this regard, the drug Nolodatak should not be used during breastfeeding, except when there is an extreme need for taking the drug. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Use in children

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

Application in elderly patients

In patients over the age of 65 years, dose adjustment is necessary.

special instructions

The drug Nolodatak should be used if the treatment with other analgesics (for example,non-steroidal anti-inflammatory drugs (NSAIDs) or opioid drugs) is contraindicated.

In patients with tinnitus (including recently healed), the risk of an increase in hepatic transaminase activity with flupirtine is increased, and the use of the drug is contraindicated in such patients.

When using the drug in patients with reduced renal function should monitor the concentration of creatinine in the blood plasma.

In patients over the age of 65 years or with severe renal insufficiency or hypoalbuminemia, dose adjustment is necessary.

During treatment with Nolodatak, the liver function should be monitored once a week. when flupirtin is used, an increase in hepatic transaminase activity, hepatitis and hepatic insufficiency may occur. If the results of a liver test deviate from the norm or if there are clinical symptoms that indicate liver damage, the drug should be discontinued.

Patients should be warned that during treatment with Nolodatak, 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 the medication and consult the doctor as a matter of urgency.

When treating Nolodatakom, 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 drive vehicles and manage mechanisms

When using the drug should refrain from driving vehicles and controlling mechanisms, due to the fact that patients can develop drowsiness and dizziness, which can affect the concentration of attention and the speed of psychomotor reactions. It is especially important to remember this when using alcohol at the same time.

Drug Interactions

Nolodatak enhances the effect of ethanol (alcohol), sedatives and muscle relaxants.

Due to the fact that flupirtine binds to proteins,it should be taken into account that it can interact with other concurrent drugs (for example, acetylsalicylic acid, benzylpenicillin, digoxin, glibenclamide, propranolol, clonidine, Warfarin and diazepam), which can be displaced by flupirtine from binding to proteins, which can lead to increased activity. Especially this effect can be expressed with the simultaneous use of warfarin or Diazepam with flupirtine.

With simultaneous application of flupirtine and coumarin derivatives, it is recommended to monitor prothrombin time on a regular basis in order to timely adjust the dose of coumarin derivatives. There are no data on the interaction with other anticoagulants or antiplatelet agents (including acetylsalicylic acid).

With the simultaneous use of Nolodatac with drugs that are metabolized in the liver, regular monitoring of hepatic transaminase activity is required. Combined use of flupirtine and drugs containing Paracetamol and Carbamazepine should be avoided.

Analogues of the drug Nolodutak

Structural analogs for the active substance:

• Catadolone;
• Catadolon forte;
• Neurodolone;
• Flugesic;
• Flupirtine maleate.

Analogues on the curative effect (remedies for relief of persistent pain):

• Amitriptyline;
• Bupranal;
• Butorphanol;
• Dexalgin;
• Dicluberl;
• Diclofenac;
• Dimexide;
• Dipidolor;
• Durogesic;
• Zaldiar;
• Indomethacin;
• Ketalgin;
• Ketanov;
• Ketonal DUO;
• Ketonof;
• Ketorolac;
• Ketorol;
• Metindole;
• Metindol retard;
• Moradol;
• Morphine;
• Nalbuphine;
• Nopan;
• Omnopon;
• Promedol;
• Protradon;
• Rapten Duo;
• Rekofol;
• Simbalta;
• Schenan;
• Stad;
• Tiapride;
• Tiapridal;
• Thoradol;
• Tramadol;
• Tramal;
• Tramped retard;
• Tremolin;
• Tramundine retard;
• Transtec;
• Fendivia;
• Fentanyl;
• Flamadex;
• Flamax;
• Flamax forte;
• Flugalin.

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