Katadolon
Katadolon: 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: Katadolon
ATX code: N02BG07
Active ingredient: flupirtine (flupirtine)
Manufacturer: TEVA Operations Poland Sp. z o.o. (TEVA Operations Poland, Sp.z oo) (Poland)
Description and photo update: 2019-20-08
Katadolon is a non-opioid analgesic, centrally acting muscle relaxant.
Release form and composition
Katadolon is produced in the form of capsules: size No. 2, gelatinous solid, opaque, the cap and body are red-brown; the contents of the capsules are white powder with a light yellow, grayish-yellow or light green tint (10 pcs. in blisters of polyvinyl chloride / aluminum foil, 1, 3 or 5 blisters in a cardboard box).
Composition of 1 capsule:
- Active ingredient: flupirtine maleate - 100 mg;
- Auxiliary components: magnesium stearate, copovidone, colloidal silicon dioxide, calcium hydrogen phosphate dihydrate;
- Capsule body: gelatin, titanium dioxide, iron dye red oxide (E172), sodium lauryl sulfate, purified water.
Pharmacological properties
Katadolon is a drug that has a muscle relaxant and central analgesic effect.
Pharmacodynamics
The active substance of Katadolon is flupirtine, a representative of Selective Neuronal Potassium Channel Opener (SNEPCO), which belongs to non-opioid centrally acting analgesics.
Flupirtine activates neuronal K + -channels of internal rectification associated with the G-protein, which leads to the release of K + ions, as a result of which the resting potential is stabilized and the excitability of neuronal membranes is reduced. As a result, N-methyl-D-aspartate (NMDA) receptors are indirectly inhibited, since their blockade with Mg 2+ ions persists until depolarization of the cell membrane occurs (indirect antagonistic effect on NMDA receptors).
When used in therapeutically significant concentrations, flupirtine does not bind to 5-HT 2 -serotonin, 5-HT 1 - (5-hydroxytryptophan), alpha 1 - and alpha 2 -, opioid, benzodiazepine, dopamine, central n- and m-cholinergic receptors.
Thanks to this central action of Katadolon, three of its main effects are realized:
- Analgesic effect: due to the selective opening of voltage- dependent K + -channels of neurons and the concomitant release of K + ions, the resting potential of the neuron is stabilized. The neuron becomes less excitable. The indirect antagonism of flupirtine towards NMDA receptors prevents the entry of Ca 2+ ions into neurons, thereby mitigating the sensitizing effect of an increase in the intracellular concentration of Ca 2+ ions. Thus, in the case of neuron excitation, the transmission of ascending nociceptive impulses is inhibited.
- Muscle relaxant effect: the pharmacological effects described for the analgesic effect of flupirtine are functionally supported by an increase in the absorption of Ca 2+ ions by mitochondria, which is observed when Katadolon is used in therapeutically significant doses. The muscle relaxant effect occurs due to the concomitant suppression of impulse transmission to motor neurons and the corresponding effects of interneurons. Therefore, this effect of flupirtine is manifested mainly in relation to local muscle spasms, and not to the entire musculature as a whole.
- Effect of Chronification Processes: Chronization processes are considered as neuronal conduction processes due to the plasticity of neuronal functions. The elasticity of the functions of neurons by the induction of intracellular processes creates favorable conditions for the implementation of mechanisms of the "winding" type, in which the response to each subsequent impulse is enhanced. NMDA receptors are largely responsible for triggering these changes. Their indirect blockade under the influence of flupirtine leads to the suppression of these effects. Thus, unfavorable conditions are created for clinically significant chronicity of pain. And in the presence of chronic pain, conditions are created for erasing pain memory (due to stabilization of the membrane potential), as a result of which pain sensitivity decreases.
Pharmacokinetics
After oral administration of Katadolon, flupirtine is absorbed in the gastrointestinal tract. The drug is absorbed quickly and almost completely (by about 90%).
About 75% of the dose taken is metabolized in the liver, resulting in the formation of metabolites M1 and M2.
M1 (2-amino-3-acetamino-6- (4-fluoro) -benzylaminopyridine) is an active metabolite formed as a result of hydrolysis of the urethane structure (1st phase of the reaction) and further acetylation (2nd phase of the reaction). It provides about 25% of the analgesic effect of flupirtine.
M2 is a biologically inactive metabolite resulting from the oxidation reaction of p-fluorobenzyl (1st phase) and further conjugation of p-fluorobenzoic acid with glycine (2nd phase).
Which isoenzyme is predominantly involved in the oxidative destruction pathway has not been studied. Flupirtine is believed to have only minor interactions.
The concentration of flupirtine in blood plasma is proportional to the dose taken.
The half-life (T 1/2) of the drug from the blood is ~ 7 hours (for the main substance and metabolite M1 - 10 hours). This time is sufficient to provide the required analgesic effect.
In elderly patients over the age of 65, T 1/2 increases to 14 hours with a single dose of the drug and up to 18.6 hours when using Katadolon for 12 days. Also, in old age, the maximum concentration of the drug in the blood increases by about 2.5 times.
Flupirtine is excreted mainly (69%) by the kidneys: unchanged - 27%, in the form of M1 metabolite (acetyl metabolite) - 28%, in the form of M2 metabolite (p-fluorohydropuric acid) - 12%. The third part of the received dose is excreted from the body in the form of metabolites of unknown structure. A small part of the dose is excreted in feces and bile.
Indications for use
According to the instructions, Katadolon is prescribed for adults for the treatment and relief of attacks of chronic and acute pain of mild to moderate severity, namely:
- Headaches of various origins;
- Muscle spasms (fibromyalgia, arthropathy, musculoskeletal pain in the back and neck);
- Pain in malignant neoplasms;
- Post-traumatic pain;
- Pain syndrome during orthopedic / traumatological operations and interventions;
- Dysmenorrhea.
Contraindications
- Cholestasis and the risk of developing hepatic encephalopathy (since there is a high probability of the development or progression and aggravation of an existing encephalopathy or ataxia);
- Liver dysfunction;
- Chronic alcoholism;
- Myasthenia gravis (myasthenia gravis) (due to the muscle relaxant effect of flupirtine);
- Tinnitus (ringing in the ears), including recently healed;
- Simultaneous use with other drugs of hepatotoxic action;
- Age under 18;
- Hypersensitivity to drug components.
Katadolon is used with caution in hypoalbuminemia, renal failure, as well as in old age (from 65 years).
Instructions for the use of Katadolon: method and dosage
Capsules Katadolon is taken orally with a little water and without chewing (it is desirable to be in an upright position).
As an exception, if the patient cannot swallow the capsule, it can be opened and inserted through a tube, or only the contents can be ingested. The bitter taste of flupirtine can be neutralized with food, for example, by eating a banana.
The recommended standard dosage regimen of Katadolon: 1 capsule (100 mg) 3-4 times a day, maintaining, if possible, equal intervals between doses. In case of severe pain - 2 capsules (200 mg) 3 times a day. The maximum daily dose is 6 capsules (600 mg).
The dose is selected depending on the individual tolerance of Katadolon and the intensity of pain. For therapeutic purposes, it is necessary to apply the minimum effective dose for the shortest period of time. The maximum course of treatment should not exceed 2 weeks.
In elderly patients aged 65 and over, treatment begins with 2 capsules (200 mg) per day, taken in the morning and evening.
In severe renal failure or hypoalbuminemia, plasma creatinine concentration should be monitored. The maximum daily dose for such patients should not exceed 3 capsules (300 mg). If a higher dose is required, patients should be monitored continuously.
In the case of mild to moderate renal failure, dose adjustment of Katadolon is not necessary, but monitoring of the concentration of creatinine in the blood plasma is required.
Side effects
Side effects from systems and organs, depending on the frequency of manifestation (≥1 / 10 - very often; ≥1 / 100- <1/10 - often; ≥1 / 1000- <1/100 - infrequently; ≥1 / 10,000 - <1/1000 - rarely; <1/10 000 - extremely rare; unknown frequency - it is not possible to make an assessment based on the data obtained):
- Hepatobiliary system: very often - increased activity of hepatic transaminases; unknown frequency - hepatitis, liver failure;
- Gastrointestinal tract: often - nausea, vomiting, dyspepsia, stomach pains, constipation, dryness of the oral mucosa, abdominal pain, flatulence, diarrhea;
- Immune system: infrequently - hypersensitivity to the drug, allergic responses (sometimes accompanied by a skin rash, hives, fever, itching);
- Skin and subcutaneous tissues: often - hyperhidrosis (sweating);
- Nervous system: often - depression, sleep disturbance, anxiety / nervousness, tremors, headache, dizziness; infrequently - confusion of consciousness;
- Metabolism: often - decreased or lack of appetite;
- Organ of vision: infrequently - visual impairment;
- Others: very often (in 15% of cases, especially at the beginning of therapy) - weakness / fatigue.
Side effects, with the exception of allergic reactions, are in most cases dose-dependent, and often go away on their own during or after the end of therapy.
Overdose
There are isolated reports of cases of intentional overdose of Katadolon for the purpose of suicide.
When taking the drug at a dose of 5000 mg, the following symptoms were noted: dryness of the oral mucosa, nausea, stunnedness, tearfulness, a state of prostration, confusion, tachycardia. No life-threatening conditions have been reported.
It is recommended to induce vomiting or to conduct a formed diuresis, then prescribe activated charcoal or enter electrolytes. In these cases, the state of health is usually restored within 6-12 hours. The specific antidote is unknown.
In case of an overdose of Katadolon, one should take into account the possibility of developing disorders of the central nervous system and the appearance of symptoms of hepatotoxicity by the type of increased metabolic disorders of the liver. Treatment in this case is symptomatic.
special instructions
In patients with reduced renal or hepatic function, it is necessary to monitor the urine creatinine and liver enzyme activity.
At the age of 65 and older, with pronounced signs of hepatic and / or renal failure, as well as with hypoalbuminemia, dose adjustment is required.
With flupirtine therapy, false positive tests for bilirubin, urine protein and urobilinogen are possible. A similar reaction can be observed in the quantitative determination of the level of bilirubin in blood plasma.
The use of Katadolon in high doses in some cases can cause urine staining in green, which is not a clinical sign of any disease.
Influence on the ability to drive vehicles and complex mechanisms
Given the ability of Katadolon to weaken attention and slow down the reaction rate, during treatment it is recommended to refrain from driving vehicles and engaging in potentially hazardous activities.
Application during pregnancy and lactation
There are insufficient data on the use of flupirtine during pregnancy to assess the extent of its effect. In experimental studies conducted on animals, the reproductive toxicity of flupirtine was established, teratogenicity was not revealed. However, during pregnancy, Katadolon is prohibited for use, except in cases where the expected benefit to the woman is definitely higher than the possible risks to the fetus.
In breast milk, according to research data, flupirtine penetrates in small quantities. However, breastfeeding is recommended to be discontinued if treatment is required during lactation.
Pediatric use
Katadolon is contraindicated in children and adolescents (under 18 years of age).
With impaired renal function
In case of mild to moderate renal failure, there is no need to adjust the dose of the drug.
In severe renal failure or hypoalbuminemia, treatment should be carried out with caution, using Katadolon in a daily dose of not more than 300 mg, under constant monitoring of the plasma concentration of creatinine. If higher doses are needed, close medical supervision is required.
For violations of liver function
The use of Katadolon is contraindicated in the presence of liver disease, alcoholism, the risk of cholestasis or hepatic encephalopathy (due to the likelihood of aggravation of an existing ataxia or encephalopathy, or the development of encephalopathy).
Use in the elderly
Care should be taken when prescribing Katadolon to persons over 65 years of age. The initial recommended dose for patients of this age category is 100 mg 2 times a day, morning and evening.
Drug interactions
With the simultaneous use of flupirtine with certain drugs, the following effects may occur:
- Alcohol, muscle relaxants, sedatives: their effect is enhanced;
- Acetylsalicylic acid, benzylpenicillin, digoxin, glibenclamide, propranolol, clonidine, warfarin and diazepam: due to the possible displacement of these substances by flupirtine from the protein bond, their activity may increase (especially pronounced for diazepam and warfarin in combination with Catadolone);
- Coumarin derivatives: regular monitoring of the prothrombin index is required in order to adjust the coumarin dose in time;
- Anticoagulants or antiplatelet agents: no data on interactions;
- Drugs metabolized by the liver: requires regular monitoring of the level of liver enzymes;
- Medicines containing carbamazepine and paracetamol: combined use with Katadolon should be avoided.
Analogs
Analogs of Katadolon are: Katadolon Retard, Acupan, Milistan, Nefopam, Nolodatak, Neurodolon, Sinmeton, Flugesik.
Terms and conditions of storage
Keep out of the reach of children at a temperature not exceeding 25 ° C.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Katadolon
According to reviews, Katadolon is an effective, fast-acting analgesic that helps to relieve severe pain. However, the drug often causes side effects, including lethargy, drowsiness, numbness of the lips, feeling of intoxication, and disorientation. Some also refer to the disadvantages of the relatively high cost of capsules.
Despite the fact that Katadolon is a non-opioid analgesic (as indicated in the instructions), there are separate reviews that describe that it is addictive, and patients are not able to refuse to take the drug on their own, they need medical help.
Price for Katadolon in pharmacies
Approximate prices of Katadolon (100 mg capsules):
- pack of 10 - 450-465 rubles;
- pack of 30 - 900-950 rubles;
- pack of 50 - 1220-1540 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
