Katadolon: instructions for using the medicine, structure, Contraindications
Active material: Flupirtine
When ATH: N02BG07
CCF: Centrally acting non-opioid analgesic
ICD-10 codes (testimony): N94.4, N94.5, R51, R52.0, R52.2
When CSF: 03.02
Manufacturer: AWD.pharma GmbH & Co.KG (Germany)
Katadolon: dosage form, composition and packaging
Capsules hard gelatin, size №2, opaque, red-brown; contents of capsules – powder, white to pale yellow or grayish yellow, or light green color.
| 1 caps. | |
| flupirtine maleate | 100 mg |
Excipients: calcium hydrogen phosphate dihydrate, kopovydon, magnesium stearate, colloidal silicon dioxide.
The capsule shell: gelatin, Purified water, iron oxide red dye (E172), Titanium dioxide, sodium lauryl.
10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
Katadolon: pharmachologic effect
Selective neuronal potassium channel activator. By its pharmacological effects of the drug is a non-opioid analgesic central action, It does not cause dependence and addiction, Besides, It has muscle relaxant and neuroprotective effect.
At the heart of the action of flupirtine is the activation of potassium channels potentsialnezavisimyh, which leads to stabilization of the membrane potential of the neuron. Effect on potassium ion current is mediated by the action of the drug regulatory system on the G-protein.
At therapeutic concentrations, flupirtine does not bind to α1-, a2-adrenoreceptor, serotonin 5HT1-, 5NT2-receptors, dopamine, benzodiazepine, opioid, central m- and n-holinoretseptorami.
The central action of flupirtine based on 3 main effects:
Analgesic effect
Analgesic effect is based on indirect antagonism of NMDA-receptors, and by modulating pain mechanisms, associated with the effect on GABA-ergic system.
Therapeutic doses of flupirtine activates (opens) potentsialnezavisimye potassium channels, which leads to stabilization of the membrane potential of nerve cells. Thus there is inhibition of the NMDA-receptor and, Consequently, blockade of neuronal calcium ion channels. Due to suppression of developing neuronal excitation in response to nociceptive stimuli, inhibition of activation of nociceptive, realized analgesic effect. This results in inhibition of the growth of neuronal response to repeated painful stimuli. This action prevents the amplification of pain and its transition to a chronic form, and with already existing chronic pain leads to a reduction of its intensity. It was also established modulating effect of flupirtine on the perception of pain through descending noradrenergic system.
Miorelaksiruyuschee action
Antispasmodic effect on the muscle to block the transfer of excitation in the motor neurons and intermediate neurons, leading to the removal of muscle tension. This action is manifested flupirtine for many chronic diseases, accompanied by painful muscle spasms (musculoskeletal pain in the neck and back, artropatii, tenzionnye headaches, fibromyalgia).
The neuroprotective effect
The neuroprotective properties of the drug cause nerve structures protection from toxic effects of high concentrations of ions in intracellular calcium, due to its ability to cause blockage of neuronal ion channels and calcium to reduce intracellular calcium ion current.
Katadolon: pharmacokinetics
Absorption
After oral administration almost completely (to 90%) and rapidly absorbed from the gastrointestinal tract.
Metabolism
It is metabolized in the liver (to 75% of the dose) to form the active metabolite M1 (2-amino-3-acetamino-6-[4-fluorine]-ʙenzilaminopiridin). The active metabolite M1 formed by the hydrolysis of the urethane structures (1 phase reaction) and subsequent acetylation (2 phase reaction). This provides an average metabolite 25% analgesic activity of flupirtine. Color Other metabolite (M2 – biologically inactive) formed by the oxidation reaction (I phase) p-fluorobenzyl followed by conjugation (2 phase) p-fluorobenzoic acid with glycine.
Deduction
T1/2 is about 7 no (10 h for the main substance and metabolite M1), that is sufficient to provide an analgesic effect. The concentration of active substance in plasma is proportional to dose.
Write mainly kidneys (69%): 27% excreted unchanged, 28% – It saw in the metabolite M1 (acetyl metabolite), 12% – It saw in the metabolite M2 (para-acid ftorgippurovaya) and 1/3 of the administered dose is excreted as metabolites of metabolites of unknown structure. A small part of the dose excreted in the bile and feces.
Pharmacokinetics in special clinical situations
Patients over the age of 65 years, compared with younger patients, an increase T1/2 (to 14 h in single dose and up 18.6 h when administered within 12 days) and Cmax respectively in plasma above 2-2.5 times.
Katadolon: testimony
Acute and chronic pain:
- due to muscle spasm (musculoskeletal pain in the neck and back, artropatii, fibromyalgia);
- headache;
- malignancy;
- algomenorrhea;
- posttraumatic pain;
- in traumatological / orthopedic operations and interventions.
Katadolon: dosing regimen
The drug is taken orally, liquid squeezed small amounts of liquid (100 ml).
The dose is adjusted depending on the intensity of pain and individual sensitivity to the drug.
Adults appoint 100 mg (1 capsule) 3-4 times / day with equal intervals between doses. At expressed pain syndrome appoint 200 mg (2 capsules) 3 times / day. The maximum daily dose – 600 mg (6 capsules).
Patients over 65 years at the beginning of treatment prescribed by 100 mg (1 capsule) in the morning and in the evening. The dose may be increased to 300 mg depending on the severity of pain and tolerability.
In patients with renal insufficiency severe or with hypoalbuminemia The maximum daily dose is 300 mg (3 capsules).
In patients with impaired liver function The maximum daily dose is 200 mg (2 capsules).
The appointment of the drug in higher doses for patients establish close observation.
The duration of therapy is determined individually by the attending physician and depends on the dynamics of pain and tolerability.
Prolonged use should monitor liver enzymes in order to identify these symptoms of hepatotoxicity.
Katadolon: side effects
CNS: >10% – fatigue / weakness (15%), especially at the beginning of treatment; 1-10% – dizziness, depression, sleep disorders, anxiety, nervousness, tremor, headache, ; 0.1-1% – confusion, visual impairment.
From the digestive system: 1-10% – heartburn, nausea, vomiting, constipation, dyspepsia, flatulence, stomach ache, dry mouth, loss of appetite; less 0.01% – increase in liver transaminases (returns to normal with dose reduction or drug discontinuation), drug-induced hepatitis (acute or chronic, flowing with jaundice or without jaundice, elements with or without cholestasis).
Allergic reactions: 0.1-1% – rash, urticaria and pruritus sometimes fever.
Side effects depend mainly on the dose (except allergic reactions). In many cases they disappear on their own as of the treatment, or after treatment.
Other: 1-10% – Sweating.
Katadolon: Contraindications
- liver diseases in history;
- cholestasis;
- myasthenia gravis;
- Saint Martin's evil;
- pregnancy;
- lactation (breast-feeding);
- childhood and adolescence up 18 years;
- hypersensitivity to flupirtine and other components of the drug.
FROM caution prescribed for violations of the liver and / or kidney, hypoalbuminemia, older patients 65 years.
Katadolon: Pregnancy and lactation
Katadolon® is contraindicated in pregnancy and lactation (breast-feeding).
Katadolon: Special instructions
Prolonged use should monitor liver enzymes in order to detect early symptoms of hepatotoxicity.
Patients older 65 years, or severe renal and / or hepatic impairment or hypoalbuminemia requires correction dose.
In the treatment of flupirtine may be false-positive test results with diagnostic strips for bilirubin, urobilinogen and protein in the urine. A similar reaction is possible for the quantitative determination of bilirubin in the blood plasma.
In applying the drug in high doses, in some cases there may be urine staining in green, that there is clinical evidence of any pathology.
Effects on ability to drive vehicles and management mechanisms
Considering, that Katadolon® may weaken attention and slow responses, It recommended during treatment with refrain from driving and transport activities potentially hazardous activities, require high concentration and speed of psychomotor reactions.
Katadolon: overdose
Symptoms: nausea, tachycardia, prostration, tearfulness, confusion, dry mouth.
Treatment: gastric lavage, diurez, introducing activated carbon and electrolyte. Symptomatic therapy. Spetsificheskiy antidote unknown.
Katadolon: drug interaction
Flupirtine increases the effects of sedatives, muscle relaxants, and ethanol.
Because, that flupirtine is associated with malnutrition, should be considered to interact with other medications taken concurrently, (eg, acetylsalicylic acid, benzilpenicillinom, digoksinom, glibenclamide, propranolol, clonidine, warfarin and diazepam), that flupirtine may be displaced from its association with proteins, that may lead to enhanced activity of. Especially this effect can be expressed while taking warfarin or diazepam with flupirtine.
When concomitant administration of flupirtine and coumarin derivatives should regularly monitor the prothrombin index, in a timely manner to adjust the dose of coumarin. Data on interaction with other anticoagulants or antiplatelet no.
With simultaneous use of flupirtine with drugs, which are also metabolized by the liver, It requires regular monitoring of liver enzymes. Avoid combination use and medicaments of flupirtine, soderzhashtih paracetamol and carbamazepine.
Katadolon: terms of dispensing from pharmacies
The drug is released under the prescription.
Katadolon: terms and conditions of storage
The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 5 years.
