Universal reference book for medicines

Active substance: flupirtine

Type: Non-opioid analgesic of central action

Manufacturer: Teva Pharmaceutical Industries (Israel) manufactured by TEVA Operations Poland (Poland)
Composition, form of production and packaging

Capsules hard gelatinous, size 2, opaque, reddish brown;
the contents of the capsules - powder from white to light yellow or grayish-yellow, or light green color.
1 caps.

flupirtine maleate 100 mg

Excipients: calcium hydrophosphate dihydrate - 212 mg, kopovidone - 4 mg, magnesium stearate - 3.5 mg, silicon dioxide colloid - 0.5 mg.

Capsule shell: gelatin - 52.9704 mg, purified water - 8.82 mg, iron dye red oxide (E172) - 0.945 mg, titanium dioxide - 0.2079 mg, sodium lauryl sulfate - 0.0567 mg.

10 pieces.
- blisters (1) - packs of cardboard.
10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (5) - packs of cardboard.

Description of the drug approved by the manufacturer for the printed edition of 2017.


A non-opioid analgesic of central action.
Flupirtine is a representative of selective activators of neuronal potassium channels.
activates G-protein-associated neuronal potassium channels of internal rectification. The yield of potassium ions causes the stabilization of the potential rest and decreased excitability membranes of neurons. As a result, indirect inhibition of NMDA receptors (N-methyl-D-aspartate) occurs, since the blockade NMDA receptors are retained by magnesium ions up to As long as there is no depolarization of the cellular membrane (indirect antagonistic action on NMDA-receptors).
At therapeutically significant concentrations, flupirtine does not bind to?
1 -,? 2- adrenoreceptors, 5HT 1 (5-hydroxytryptophan) -, 5HT 2 -serotonin, dopamine, benzodiazepine, opioid, central m-and n-cholinergic receptors.
Such a central action of flupirtine leads to the realization of 3 main effects.

Analgesic effect

As a result of the selective discovery of potential-dependent neuronal potassium channels with the concomitant release of potassium 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 intake of calcium ions.
Thus, the sensitizing effect of increasing the intracellular concentration of calcium ions is mitigated.
Consequently, when the neuron is excited, inhibition of the transfer of ascending nociceptive impulses occurs.

Miorelaksiruyuschee action

The pharmacological effects described for analgesic action are functionally
are supported by increased absorption of calcium 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 function of neurons.

Through the induction of intracellular processes, the elasticity of the functions of neurons creates the conditions for the realization of mechanisms such as "inflation", under which the response to 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 clinically significant chronic pain, and in the case of previous chronic pain, to "erase" the pain memory by stabilization of the membrane potential, which leads to a decrease in pain sensitivity.


After oral administration almost completely (up to 90%) and quickly absorbed from the digestive tract.

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


Metabolised in the liver (up to 75% of the dose) to form the active metabolite M1 (2-amino-3-acetaminino-6- [4-fluoro] -benzylaminopyridine) and M2.
The active metabolite M1 is formed as a result of hydrolysis of the urethane structure (1 phase of the reaction) and subsequent acetylation (phase 2 reaction). This metabolite provides an average of 25% of the analgesic activity of flupirtine. Another metabolite (M2 - biologically inactive) is formed as a result of the oxidation reaction (1 phase) of para-fluorobenzyl followed by conjugation (2 phase) of para-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 is about 7 hours (10 hours for the main substance and metabolite M1), which is sufficient to provide an analgesic effect.

It is excreted mainly by the kidneys (69%): 27% is unchanged, 28% - in the form of the metabolite M1 (acetyl metabolite), 12% - in the form of the metabolite M2 (para-fluoroghippuric acid) and 1/3 of the administered dose is excreted in the form of metabolites with an unclear structure.
A small part of the dose is excreted from the body with bile and feces.
Pharmacokinetics in special clinical cases

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


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


The drug is taken orally.
The capsule should be swallowed whole, without chewing and washing down with a sufficient amount of liquid (preferably water). If possible, the drug should be taken while in a vertical position.
In exceptional cases, the capsule of the preparation Catadolon В® 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.
The recommended dose of the drug is 100 mg (1 caps.) 3-4 times / day, if possible, with equal intervals between doses.
At the expressed pains - on 200 mg (2 caps.) 3 times / sut. The maximum daily dose is 600 mg (6 caps.).
The dose is selected depending on the intensity of pain and individual sensitivity to the drug.
Use the minimum effective dose for the shortest possible time. Duration of treatment should not exceed 2 weeks.
Older patients (over 65 years) at the beginning of treatment are prescribed 100 mg (1 caps.) 2 times / day, morning and evening.

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 (3 caps.). In patients with mild to moderate renal failure, dose adjustment is not required. In patients with severe renal insufficiency or hypoalbuminemia, themaximum daily dose should not exceed 300 mg (3 caps.).
If it is necessary to prescribe the drug at higher doses, careful monitoring is established for the patients.


Undesirable reactions are classified according to frequency as follows: very often (> 1/10);
often (> 1/100, but <1/10); infrequently (> 1/1000, but <1/100); rarely (> 1/10 000, but <1/1000); very rarely (1/10 000); frequency is unknown (can not be estimated from available data).
On the part of the immune system: infrequently - hypersensitivity to the drug, allergic reactions (in some cases accompanied by fever, skin rash, urticaria, skin itching).

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

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

From the liver and bile ducts: very often - an increase in the activity of hepatic transaminases;
frequency unknown - hepatitis, hepatic insufficiency.
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.

- 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);

- liver disease;

- chronic alcoholism;

- ringing in the ears (including recently healed);

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

- children and adolescence under 18;

- Hypersensitivity to the active substance or any other component of the drug.

Caution is prescribed for renal failure, hypoalbuminemia, elderly patients (over 65 years of age).


There is insufficient data on the use of flupirtine in pregnancy.
In experimental animal studies, flupirtin showed reproductive toxicity, but not teratogenicity. The potential risk to humans is unknown. The drug Catadolon В® should not be used during pregnancy, for except in cases where 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, Cathadolon В® should not be used during breastfeeding, except when there is an extreme need for taking the drug. If you need to use the drug Catadolon В® during lactation should stop breastfeeding.

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 (3 caps.). In patients with mild to moderate renal failure, dose adjustment is not required. In patients with severe renal insufficiency or hypoalbuminemia, themaximum daily dose should not exceed 300 mg (3 caps.).

Contraindicated in patients with liver disease, with the risk of developing hepatic encephalopathy and cholestasis (possibly the development of encephalopathy or aggravation of already existing encephalopathy or ataxia).


Contraindication: children and adolescence under 18 years.


Be wary appoint patients over 65 years.


The preparation Catadolon В® should be used, if the treatment with other analgesics (for example, NSAIDs or opioids) is contraindicated.

When used in patients with reduced renal function, the concentration of creatinine in the blood should be monitored.

Patients over the age of 65 years or with severe renal failure or hypoalbuminemia require a dose adjustment.

During the treatment with Catadolon В® , the liver function should be monitored once a week, tk.
when flupirtin is used, an increase in the activity of transaminases, the development of hepatitis and liver failure may occur. If the results of the liver function test deviate from the norm or if there are clinical symptoms that indicate liver damage, the use of the Catadolon В® drug should be discontinued.
Patients should be warned that during treatment with the Catadolon В® drug, attention must be paid
for any symptoms of liver damage (eg, lack of appetite, nausea, vomiting, pain in stomach, fatigue, dark urine, jaundice, itching). If these symptoms occur, stop taking the drug Catadolon В® and immediately consult a doctor.
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 drive vehicles and manage mechanisms

When using the drug Catadolon В® should refrain from driving
motor transport and management mechanisms, due to the fact that patients may develop drowsiness and dizziness, which can affect on the concentration of attention and the speed of psychomotor reactions. It is especially important to remember this when drinking alcohol at the same time.

There are reports of
single cases of overdose with suicidal intentions.
Symptoms: when taking flupirtine in a dose of 5 g, nausea, tachycardia, prostration, tearfulness, confusion
consciousness, deafness, dryness of the oral mucosa.
Treatment: 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. No life-threatening conditions were reported.
In case of overdose or when signs of intoxication appear, one should be aware of the possibility of occurrence of disorders from the side of the central nervous system, as well as manifestations of hepatotoxicity by type of enhancement of metabolic disorders in the liver. It should be symptomatic treatment. Specific antidote is unknown.

Flupirtine enhances the action of sedatives, muscle relaxants, as well as ethanol.

Due to the fact that flupirtine binds to proteins, it should be taken into account that it can interact with other concomitant medications (eg, acetylsalicylic acid, benzylpenicillin, digoxin, glibenclamide, propranolol, clonidine, warfarin and diazepam), which can be displaced by flupirtine from the bond with proteins, which can lead to an increase in their activity.
Especially, this effect can be expressed by simultaneous administration of warfarin or diazepam with flupirtine.
With the simultaneous administration of flupirtine and coumarin derivatives, it is recommended that the prothrombin index be regularly monitored in order to correct the dose of coumarin in a timely manner.
There are no data on the interaction with other anticoagulants or antiplatelet agents (including acetylsalicylic acid).
With the simultaneous use of flupirtine with drugs that are also metabolized in the liver, regular monitoring of hepatic enzyme activity is required.
Combined use of flupirtine and drugs containing paracetamol and carbamazepine should be avoided.

The drug is released by prescription.



The drug should be stored out of the reach of children at a temperature of no higher than 25 В° C.
Shelf life - 5 years.
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