Carbamazepine side effects. Video about self-correction of a psychosomatic condition. How does a drug overdose manifest?

Among wide range With modern medicines, you can increasingly find medications in pharmacies for the treatment of rare diseases. Today, one of these drugs is “Carbamazepine” (instructions for use, price, reviews, analogues and other data will be described in this article).

General information

This drug is an anticonvulsant drug produced by the manufacturer only in tablet form.

This medication can be purchased at any hospital pharmacy at a price of about 60 rubles, depending on the owner’s markup. Any analogue of "Carbamazepine" (reviews of which are both positive and negative) costs many times more. Their price category starts from 200 rubles for a similar dosage of the active ingredient.

Analogs of "Carbamazepine" (the price and reviews about them are very different):

• "Tegretol";
• "Finlepsin".

Composition and form of production

In addition to the main active ingredient in a dosage of 0.2 g for each tablet, the drug also contains additional ingredients:

• potato starch;
• talc;
• magnesium stearate;
• polysarbate;
• povidone;
• silica.

The drug is produced exclusively in the form of tablets, packaged in blisters of 10 pieces. Plates with medication, in turn, can be packaged in cardboard boxes of 5 or 10 blisters. An annotation for the drug must be included in the packaging.

Pharmacology

Reviews of "Carbamazepine" characterize it as a medicine wide range impact, which is very popular today. Due to its composition, it has an antiepileptic effect, but among individual patients can additionally act as an analgesic, antidiuretic, and so on. This is associated with patient diseases such as diabetes insipidus or neurological disorders.

Thanks to its composition, the drug strengthens the membranes of neurons, strengthens seizure threshold, reducing the risk of an attack. Besides, medical product"Carbamazepine" (instructions for use and reviews confirm this) has a positive effect on general formation the patient's personality. Patients become more sociable and recover faster in society.

The medical drug may be prescribed as a component complex treatment or as a standalone remedy. The drug demonstrates maximum effectiveness in therapy in patients younger age. Children and adolescents become less anxious and irritable.

The effect of the substance in most cases becomes noticeable within a few hours after administration. Sometimes the effect may linger for several days due to slow metabolism.

"Carbamazepine" also receives positive reviews from patients diagnosed with neuralgia trigeminal nerve, tabernacle spinal cord or post-traumatic paresthesia. In these cases, the drug further reduces pain syndromes. The medication also normalizes water balance in patients with diabetes insipidus and states of psychosis with neurological disorders.

Pharmacokinetics

The absorption of the active substance into the body takes quite a long time, but at the same time it is almost 100%. Its maximum concentration in the body appears 10-12 hours after the first dose and normalizes only after two weeks of therapy. The substance binds to plasma proteins in adults by almost 80%, and in children only by a maximum of 60%.

The main component is able to penetrate the placental barrier, so taking it during pregnancy is prohibited. In mother's milk, the substance is concentrated in an amount approximately equal to half that in the plasma of a nursing woman.

The breakdown of the ingredient occurs in the liver. Its half-life when used independently is about 36 hours, and when complex therapy no more than 10 hours. According to reviews from doctors, "Carbamazepine" is excreted in feces and urine. All described data in adult patients of any age are identical.

Indications for use

Tablets "Carbamazepine" (instructions for use, reviews and recommendations from experts are given below) are a medication for the elimination of epilepsy with various symptoms and of any form.

In addition, the drug is used to treat:

• trigeminal nerve diseases;
• affective states;
• schizophrenic disorders;
• psychosis;
• pain due to diabetic polyneuropathy and other diseases.

Prohibitions on use

It is first of all prohibited to take such complex drugs on your own. Only a doctor can prescribe them, having correctly calculated the dosage for each specific case. In addition, during therapy the individual sensitivity of the patient to the active substance, any similar antidepressant or excipient.

Reviews of "Carbamazepine" confirm that the drug cannot be used together with MAO inhibitors. You can start therapy with this drug only two weeks after. Also contraindications for everyone are problems with hematopoiesis, and for women, additionally, during pregnancy and breastfeeding.

Particular care should be taken when treating with the drug:

• elderly patients;
• together with alcoholic drinks;
• in case of disturbances in the functioning of the heart muscle;
• kidney and liver diseases;
• increased intraocular pressure.

Doses

Instructions for use of "Carbamazepine" (price, reviews, analogues are presented in the article) recommend the use of the drug for the treatment of adults and children with three years old. The drug is always taken regardless of food and with a small amount liquids. The dosage always depends on the diagnosis and characteristics of the patient’s body, but average indicators can be distinguished among them.

Thus, in the treatment of epilepsy, the drug is most often used as an independent remedy. The course for adults begins with a minimum daily dose of 100-200 mg, which gradually increases to the maximum therapeutic effect (up to 2 grams per day and up to 400 mg per dose). The drug is also added gradually to complex therapy.

For children, the initial dosage of the substance is no more than 60 mg per day. It is also gradually increased by 20-60 mg every other day to the maximum allowable. If an initial dosage of 0.1 g is prescribed, it is increased by another 100 mg over the course of a week. For children under 5 years old daily norm is a maximum of 0.4 g, up to 10 years - a maximum of 0.6 g, and up to 15 years - a maximum of 1 gram.

Other diagnoses

For the treatment of the trigeminal nerve, the drug is prescribed to patients at 0.2-0.4 g, gradually increasing the dosage until pain is eliminated. After this, the substance is taken in a minimum maintenance amount until the end of treatment.

It is important to know that if there is hypersensitivity To active ingredient, the initial dose for any diagnosis should be no more than 0.2 g per day.

According to reviews of "Carbamazepine", it can be used as a remedy for diabetic neuropathy or neurogenic origin. The substance eliminates pain of any nature gradually. For diabetes insipidus, the dose is calculated taking into account age and weight. To eliminate neurotic disorders, it should be at least 600 mg per initial stage therapy.

Possible negative manifestations

Can disturbances occur in the body when using Carbamazepine? Reviews from both specialists and patients characterize this remedy, as a drug with minimal risk of occurrence side effects, but still their list is quite extensive. Disturbances may occur in the nervous system, digestion, work endocrine gland, of cardio-vascular system and other internal organs.

The most commonly observed:

• nausea;
• stomach ache;
• migraine;
• drowsiness;
• muscle weakness;
• aggressive behavior;
• hives;
• dry mouth;
• sweating;
• conjunctivitis.

Very rarely listed side effects hepatitis, anemia, liver failure, convulsions, kidney dysfunction, sexual function disorders, ischemic exacerbations, and so on occur.

What to do if there is an overdose of the drug "Carbamazepine"? Instructions and reviews in in this case It is recommended to immediately perform gastric lavage and take sorbents.

The fact is that there is no direct antidote and treatment must be carried out symptomatically. Interestingly, due to the slowdown in metabolism, the effect activated carbon may appear only a day after administration. In cases of overdose in young patients, blood transfusions may very rarely be required.

An overdose is manifested by an increase in any of the side effects, supplemented by respiratory depression and the functioning of the digestive tract.

Interaction with other medications

The drug "Carbamazepine" (instructions for use, price, reviews are presented in the article) is characterized by consumers as an effective anticonvulsant, but its danger may also be hidden in its effect on other medications taken. This substance can inhibit the actions of some chemicals, especially those metabolized in the liver, so you must inform your doctor about taking any medications.

The drug in question may also be affected by Negative influence medications taken in parallel, increasing or decreasing its concentration in the blood.

It is very important to undergo comprehensive examination. To do this, you need to give blood and urine samples at the clinic to determine the level of iron, platelets, electrolytes and reticulocytes in the body.

Throughout the course of treatment, the level of these substances must be monitored by regularly taking appropriate tests. For the first month of therapy, these procedures are required every week, after which they can be reduced to once every 30 days.

If a patient is diagnosed with intraocular pressure, then during treatment it must be periodically measured, and if the situation worsens, the drug must be immediately discontinued.

Working on complex mechanisms

You should know that for the entire period of treatment with Carbamazepine it is recommended to refrain from driving or complex mechanisms. This is due to the fact that the drug causes drowsiness and slows down reactions.

Period of gestation and feeding

"Carbamazepine" (the price and reviews of which make the drug popular) can increase the likelihood of malformations in the development of the fetus, like other antiepileptic drugs. In this regard, it is forbidden to take it while pregnant, especially in the first trimester.

In addition, the medication increases the deficiency folic acid, which is already in short supply during pregnancy, which further increases the occurrence of problems in the development of newborns. It is also undesirable to use the drug while breastfeeding, since it active substance It enters the child’s body along with milk. It is best in such situations to switch to artificial feeding or perform breastfeeding only under strict medical supervision.

Release and storage

The drug is dispensed from pharmacies only with a doctor's prescription and must be stored in places inaccessible to children. Tablets should be placed in dark, dry places with a temperature no higher than 25 degrees. The shelf life from the date of manufacture is 2 years.

Epilepsy is very serious illness. A patient with such a disease must regularly visit a doctor and follow the correct treatment.

N.03.A.F.01 Carbamazepine

5 years.

The doctor prescribing this medicine will tell you how to take Carbamazepine tablets, what they help with and for what diagnoses they are prescribed. The drug belongs to the class of antiepileptics. The main component is obtained from the processing of dibenzazepine. Under the influence of the drug, the conductivity of sodium channels is inhibited, and the ascension of neurotransmitters slows down. The medication is effective against cramps and pain. The drug belongs to the class of antidiuretics, mood stabilizers, and antipsychotics.

Technical information

The 200 mg of carbamazepine contained in the Carbamazepine tablets is the very ingredient that determines the activity of the drug. Also, each tablet contains additional components. To make the drug, the manufacturer used Aerosil, starch compounds, povidone and polysorbate. The preparation contains magnesium stearate. It is especially important for persons suffering from hypersensitivity or sensitivity to compounds used in the pharmaceutical industry to read the instructions in detail describing the ingredients used.

Pharmacology

To understand why Carbamazepine tablets are prescribed, you need to study the instructions for use. It also describes the rules for the safe use of the composition and explains what risks are associated with non-compliance with the recommendations. The medication belongs to the antiepileptic category. It has an anti-manic effect. The drug is a mood stabilizer and helps stabilize diuresis against the background of diabetes insipidus. In case of neuralgia, the medicine is used to relieve pain. The active compound inhibits sodium channels, due to which neuronal membranes are stabilized, serial neutron discharges are inhibited, and the ability to conduct synoptic impulses is weakened.

The active compound, as explained in the instructions for use of Carbamazepine tablets, prevents the re-generation of positive sodium potentials in neutron potentials that have already undergone depolarization. The activity of the release of nervous system mediators associated with glutamate decreases, and the threshold of readiness for seizures increases. The use of the drug can reduce the risk of an epileptic attack. The conductivity of positively charged potassium molecules improves, and the operation of channels that allow the passage of calcium with a positive charge is modulated. To some extent, this determines the effectiveness of the drug against seizures.

Features of the effect

According to the instructions for using Carbamazepine tablets, under the influence of the drug, personality changes caused by epilepsy are reduced. Patients become more sociable, and the patient’s rehabilitation in society becomes easier. The combined use of Carbamazepine and other drugs effective against convulsions is allowed. You can prescribe the drug for partial, focal attacks. It is permissible to use tablets if the attacks are simple or occur in a complex form. You can use the remedy in case of secondary generalization of the process, with a tonic-clonic variant of the course of a generalized type. You can use the tablets for any combination of the mentioned pathological conditions. At the same time, it is noted that Carbamazepine shows a relatively low level of effectiveness in the case of minor myoclonic seizures and absence seizures.

Explaining why Carbamazepine tablets are prescribed in a particular case, the doctor also points to the relief of depressive symptoms and anxiety, which very often bother epileptics. This effect is observed when taking the drug by both adult patients and children. The aggressiveness of patients decreases, people become less irritable. Correction of psychomotor skills and the effect on cognitive aspects is determined by the dosage of the drug. Much depends on the specifics of the case and the state of the body.

Efficiency and effectiveness: when taken correctly

Studies designed to determine how and why Carbamazepine tablets are most effective have proven that the anticonvulsant effect inherent in the drug lasts for hours in some patients, and for days in others. Autoinduction of metabolic processes can cause the effectiveness of the medication for a month. If neuralgia is established, the remedy helps prevent an attack of pain. It can be used to relieve neurogenic pain from tabes dorsalis, paresthesia due to previous trauma, and neuralgia associated with herpes. If the cause of pain is in the trigeminal nerve, pain relief is observed 8-72 hours after taking the composition. In case of alcohol poisoning, taking the drug helps to increase the body’s threshold of readiness for convulsions, which is reduced during the abstinence period. At the same time, the clinical picture of the syndrome as a whole is alleviated - tremor goes away, excessive excitability decreases, and gait stabilizes.

By identifying aspects of the action of Carbamazepine tablets, scientists have found that taking the medicine against the background of diabetes insipidus helps stabilize the fluid balance in the body. The desire to drink weakens, diuresis becomes less. As for the psychotropic effects, the anti-manic effect can be observed a week or a week and a half after the start of the course. It is assumed that this effect is explained by the inhibition of metabolic processes affecting the production of dopamine and norepinephrine.

Kinetic nuances

According to the instructions, which explain what Carbamazepine tablets help with, how they are used and how they are processed in the body, the absorption process is quite slow, but it is highly effective. The process does not depend on meals. After using a single dose, the maximum serum concentration is recorded after 12 hours, and the equilibrium serum concentration is established within a week or two. When processed in the body, the substance is transformed into a metabolite, which has pharmacological activity. Its concentration on average is about a third relative to the original substance.

As indicated in the instructions describing the features of the composition of Carbamazepine, the substance is capable of forming strong bonds with plasma proteins. For a child’s body the parameter is up to 55%, for adult patients it reaches 80%. In the fluid of the spinal cord and secretions of the salivary glands, the substance is observed in a concentration corresponding to the amount of the substance that has not reacted with plasma proteins. The ability to penetrate the placenta has been established. In breast milk, the compound is found in an amount of 25-60% of the plasma content.

Kinetics: how does it all happen?

Regardless of the dosage, Carbamazepine is transformed when passing through the liver. The dominant process option is epoxy. One active metabolite and one reaction product are formed that do not affect the human body. Also, a metabolite is formed in small quantities, which has a very weak effect on the body. There is a possibility of indicating autometabolism.

As studies have shown, the half-life of the active compound with a single dose of the drug varies in the range of about 36 hours, the maximum limit is 65 hours. When taken again, the period reaches 12-24 hours. If a person is treated with multiple drugs in combination to raise the seizure threshold, the half-life varies around 9-10 hours.

The drug is predominantly excreted in the form of inactive transformation products. Up to a third of the total dose leaves the body through the intestinal tract, other amounts - with urine. Establishing when, to whom and from what “Carbamazepine” helps, it was not possible to identify specific kinetic features in the elderly. It has not yet been possible to collect enough reliable information about the kinetics of the drug in the event that patients have impaired liver and kidney function.

When will it help?

When are Carbamazepine tablets prescribed? Indications for use include those with different types of symptoms (complex, simple). Can be used for generalized primary, secondary process, and mixed types. It is allowed to prescribe the drug for idiomatic neuralgia affecting the glossopharyngeal nerve. The medicine is recommended for the treatment of affective disorder, polydipsia. The medication is ineffective for polyuria in the case of diabetes insipidus. It is recommended to use tablets for withdrawal symptoms due to alcohol dependence. In case of polyneuropathy associated with diabetes, the medicine relieves pain.

The practice of using Carbamazepine for idiopathic trigeminal neuralgia is widespread. The drug is prescribed if neuralgia is caused by multiple sclerosis. The remedy can be used as a preventive measure if the likelihood of affective disturbance is assessed above average. The drug is effective for schizoaffective problems and depressive, manic psychosis.

When and how much?

Although the price of Carbamazepine is quite affordable (about one hundred rubles), this is not a reason to be careless about the drug dosage program. Do not use the product in excess, as this may cause undesirable consequences. The optimal program of use is chosen by the doctor based on the diagnosis and concomitant diseases. The tablets are used orally; the administration procedure does not depend on meals. It is necessary to take the drug with a small amount of pure liquid without additives.

Persons with epilepsy are well aware of the price of Carbamazepine, since the drug in question is prescribed very often for this diagnosis. It is recommended to use the medicine independently, if possible. First, the patient is prescribed a minimum dose per day, gradually increasing the amount, waiting for a pronounced effect. If the patient is already undergoing treatment for epilepsy, inclusion in the Carbamazepine program is allowed only in small doses. Previously used drugs are initially taken in the same dosages, but if necessary, the volumes are gradually adjusted.

Specific numbers

Adult patients with epilepsy are first prescribed 0.1-0.2 g once or twice a day for a day. The dosage is increased until a therapeutic effect is obtained. As a rule, 0.4 g of the product up to four times daily is sufficient. Do not use the medicine in quantities of more than two grams per day.

For three-year-old children, the drug is prescribed in an amount of 20-60 mg per day. The dosage is gradually increased. Volume adjustments are allowed every two days. The dose increase step is 20-60 mg.

Children over three years of age are initially recommended to take 0.1 g of the drug per day with a gradual increase in volume once a week. The dose increment is 0.1 g. The maintenance dosage usually varies around 110-120 mg per kilogram of weight. The daily dose is divided into several doses. For children under five years of age, 0.2-0.4 g, divided into two doses, is sufficient. Children under ten years of age are prescribed up to 0.6 g, divided into three doses, and for persons older and up to fifteen years of age inclusive, up to a gram per day is prescribed. The total volumes are divided into three portions.

In the case of trigeminal neuralgia, on the first day of treatment it is indicated to take 0.2-0.4 g, then the dose is increased until the pain stops. The dose increase step is 0.2 g per day. Usually, 0.4-0.8 g per day is enough for patients to relieve pain. Having achieved a pronounced effect, the dose is reduced until the desired result is maintained.

Features and diagnoses

If the reason for prescribing the drug is neurogenic pain, the patient is initially recommended to take 0.1 g of the drug twice a day, then the dose is increased. Maximum - 0.2 g per day. The volumes are increased until the pain is relieved. The maintenance dose varies between 0.2-1.2 g per day.

In case of advanced age and high sensitivity of the body, it is recommended to start therapy with 0.1 g twice a day.

In case of alcohol poisoning and withdrawal syndrome, the drug should be used three times daily, 0.2 g each. In severe cases, in the first days it is allowed to take 0.4 g three times. If withdrawal symptoms at the beginning of therapy manifest themselves with severe symptoms, “Carbamazepine” is combined with sedatives and sleeping pills .

For diabetes insipidus, Carbamazepine is usually prescribed in the amount of 0.2 g up to three times daily. Children are shown smaller doses, calculated by the doctor based on weight. If diabetes has caused neuropathy and pain, on average it is enough to take 0.2 g up to four times a day. To prevent exacerbation of affective disorder, schizoaffective psychosis, 0.6 g of the drug is prescribed four times a day.

If an acute manic state or bipolar disorder is diagnosed, the patient should use 0.4-1.6 g of the drug per day. In acute conditions, it is necessary to quickly increase the dosage. As part of maintenance treatment, the volumes are increased gradually so that the substance is better tolerated by the body.

Adverse events

Side effects of Carbamazepine include a number of reactions from the central nervous system. Some people experience headaches, dizziness and sleepiness. Sometimes patients note weakness, tremors and paresis, dyskinesia and weakness of muscle tissue. There is a possibility of neuritis, dysarthria, tics, and nystagmus. It is noted that some hallucinated, became depressed, lost appetite, became anxious and became aggressive during treatment. There is a possibility of disorientation, exacerbation of psychosis, and excessive agitation.

Side effects of Carbamazepine include an allergic reaction. There is a possibility of developing increased sensitivity in several internal organs at once. In a minimal percentage of cases, the drug provoked aseptic meningitis, anaphylactic response, Quincke's edema, shortness of breath and fever, and pneumonia. Possible negative effects on the hematopoietic system, deterioration of stool, and gastrointestinal activity. Some people have dry mouth, stomach pain, and inflammation of the tongue. The activity of liver enzymes may increase. There is a risk of cardiac dysfunction, thrombophlebitis, collapse, and fainting. In the case of ischemia, there is a danger of exacerbation of the condition.

Is it possible or not?

As can be seen from the instructions, the contraindications for taking Carbamazepine tablets are hypersensitivity to the active component of the drug, as well as other drugs with similar chemical qualities. Tricyclic antidepressants, for example, belong to this category. Do not use the composition if you are allergic to the auxiliary ingredients. The substance is not used against the background of acute porphyria. Carbamazepine is contraindicated in persons taking MAOIs, as well as those who completed such a course less than two weeks ago. Carbamazepine is prohibited for those who have impaired hematopoietic bone marrow function or an atrioventricular block. The drug is not prescribed to pregnant and lactating women.

Carbamazepine should be used extremely carefully if a sodium deficiency is detected, if the hematopoietic function of the bone marrow was previously suppressed under the influence of drugs. Use the product with caution if you are an elderly person. The restrictions are associated with prostatic hyperplasia, severe heart failure, and impaired functioning of the kidneys and liver, which are often found in such patients. In case of increased pressure inside the eye, Carbamazepine is used only if it is possible to regularly check the patient’s condition.

Is there an alternative?

Analogues of Carbamazepine tablets include the following drugs:

• "Tegretol".
• "Finlepsin".

The choice in favor of a specific name must be agreed with the attending physician. It is strictly not recommended to replace the drug with an alternative one on your own. Such self-will can cause the ineffectiveness of the drug program and undesirable consequences for the body.

Features of use

Regarding the compatibility of Carbamazepine and alcohol. It is strictly forbidden to drink alcohol during treatment. This is associated with an increased risk of developing adverse reactions and a sharp deterioration in the patient’s condition, which is not always predictable. When using Carbamazepine as part of the treatment of alcohol withdrawal syndrome, the doctor will pay special attention to these limitations and risks associated with neglecting the basic rule of treatment.

There is a possibility of pregnancy during the period when the patient is being treated with Carbamazepine. In this case, as well as when deciding whether to take the drug if conception has already occurred, it is necessary to evaluate what the obvious advantages of the therapeutic course are and the possible risks associated with bearing a child. It is especially important to correctly assess the situation in the first trimester. As observations have shown, if a mother has epilepsy, then her unborn child has an increased likelihood of developing defects.

Carbamazepine can induce abnormal development processes in the body. Similar features are inherent in all other medications effective for epilepsy. There are several known cases of children being born with developmental defects and diseases. A doctor, when offering a course of Carbamazepine to a patient, is obliged to inform about possible dangers. The patient is usually advised to undergo antenatal diagnosis.

Name:
Carbamazepine
INN:
Carbamazepine
ATX code: N03AF01.

Analogues: Finlepsin

Pharmacotherapeutic group:

Antiepileptic drug.

Compound

One tablet contains

active substance:

carbamazepine - 200 mg,

Excipients: microcrystalline cellulose, sodium starch glycolate, povidone, magnesium stearate, sodium lauryl sulfate.

pharmachologic effect

Anticonvulsant, tricyclic iminostilbene derivative. The anticonvulsant effect is associated with a decrease in the ability of neurons to maintain a high frequency of repeated action potentials through inactivation of sodium channels. Carbamazepine also has a moderate antimanic, antipsychotic effect, as well as an analgesic effect for neurogenic pain. The mechanisms of action may involve gamma-aminobutyric acid receptors, which may be coupled to calcium channels; The effect of carbamazepine on neurotransmission modulator systems also appears to be important. The antidiuretic effect of Carbamazepine is associated with a hypothalamic effect on osmoreceptors, which is mediated through the secretion of antidiuretic hormone, as well as a direct effect on the renal tubules. It prevents attacks of trigeminal neuralgia, reduces the severity of clinical manifestations of alcohol withdrawal and reduces convulsive activity. In diabetes insipidus, it reduces diuresis and thirst.

Pharmacokinetics

Absorbed slowly from the gastrointestinal tract. Almost completely metabolized. Maximum plasma concentration occurs after 8-12 hours. Binds to blood proteins by 70-80%. In the cerebrospinal fluid and saliva, concentrations are created in proportion to the proportion of the active substance not bound to proteins (20-30%). The half-life is 30-40 hours, with long-term use it decreases to 10-20 hours. Penetrates into breast milk (25-60% of plasma levels) and through the placental barrier. Biotransforms in the liver with the formation of several metabolites. Excreted in small quantities in breast milk. The onset of anticonvulsant action varies from several hours to several days (sometimes up to 1 month). The antineuralgic effect develops after 8-72 hours, the antimanic effect - after 7-10 days.

Indications for use

epilepsy: partial seizures with elementary symptoms (focal seizures); partial seizures with complex symptoms (psychomotor seizures); grand mal seizures, mainly of focal origin (grand mal seizures during sleep, diffuse grand mal seizures); mixed forms of epilepsy;

trigeminal neuralgia;

paroxysmal pain of unknown cause arising on one side of the root of the tongue, pharynx and soft palate (genuine glossopharyngeal neuralgia);

pain due to damage to peripheral nerves due to diabetes mellitus (pain due to diabetic neuropathy);

epileptiform convulsions in multiple sclerosis, such as spasms of the facial muscles in trigeminal neuralgia, tonic convulsions, paroxysmal speech and movement disorders (paroxysmal dysarthria and ataxia), discomfort (paroxysmal paresthesia) and attacks of pain;

prevention of the development of convulsive seizures during alcohol withdrawal syndrome;

psychoses (mainly in manic-depressive states, hypochondriacal depression). Secondary prevention of affective and schizoaffective psychoses.

Directions for use and doses

Inside, during or after meals, with a small amount of liquid

Contraindications

• Atrioventricular block;
• Treatment with MAO inhibitors for 14 days before starting treatment with carbamazepine;
• Liver failure;
• Acute recurrent porphyria.

Side effect

Carbamazepine is an antiepileptic drug that causes the fewest side effects. However, in some cases, ataxia, dizziness, accommodation disorders, drowsiness, dry mouth, and diarrhea develop.

Allergic reactions (rash, Stevens-Johnson syndrome), hair loss, leukopenia are possible. Rarely, especially in older people, cardiac conduction disorders, hematological changes, cholestatic hepatitis, edema and weight gain may occur, and in some cases an increase in seizures may occur. All these reactions are indications for discontinuation of the drug. In the elderly, especially at the beginning of treatment, confusion may occur, which usually resolves spontaneously after 1-2 weeks or after reducing the dose.

Pregnancy and breastfeeding

There is some evidence of a teratogenic effect on the fetus. The use of the drug during pregnancy requires especially careful monitoring.

Side effects that occur in a child during breastfeeding: lethargy (rarely) and decreased appetite.

Precautionary measures

Before starting and during therapy, regular blood (cellular elements) and urine tests and monitoring of liver function indicators are recommended. Prescribe with caution if there is a history of heart, liver, kidney diseases, hematological disorders, increased intraocular pressure, latent psychosis, agitation, diseases characterized by seizures, in old age, transport drivers and people working with machinery. Women are advised to take additional folic acid (before or during pregnancy); In order to prevent increased bleeding in the last weeks of pregnancy and in newborns, vitamin K can be used.

Interaction with other drugs

Carbamazepine stimulates the metabolism of cyclosporine, ethosuximide, felodipine and warfarin, which leads to a reduction in the duration of action of these drugs. Danazol, dextropropoxyphene, erythromycin, isoniazid and verapamil inhibit the metabolism of carbamazepine, which may result in unexpectedly strong effects or side effects of carbamazepine. In some patients, diltiazem reduces the metabolism of carbamazepine, which leads to an increase in its concentration in the blood plasma. Barbiturates accelerate the elimination of carbamazepine. Cisplatin and doxorubicin reduce the absorption of carbamazepine and reduce its plasma levels.

Overdose

Symptoms:

disorientation, drowsiness, agitation, hallucinations, blurred vision, nystagmus, ataxia, convulsions, myoclonus, respiratory depression, pulmonary edema, tachycardia, cardiac arrest accompanied by loss of consciousness, decreased colonic motility, hyponatremia, hyperglycemia, possible metabolic acidosis.

Treatment:

gastric lavage, administration of activated charcoal and saline laxative, forced diuresis. To maintain airway patency - artificial respiration and (or) use of oxygen. It is necessary to anticipate a re-intensification of symptomatic overdose on the 2nd and 3rd day after its onset, which is associated with the slow absorption of the drug.

Package

30 or 50 tablets in plastic cases or in polymer jars for packaging medicines.

10 tablets in a blister pack.

Pencil case, jar, 3 or 5 blisters along with an insert in secondary packaging.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25ºС.

Keep out of the reach of children.

Best before date - 3 years.

Manufacturer:

LLC "Farmland"

Carbamazepine is a derivative of dibenzoazepine and has antiepileptic, neurotropic, psychotropic and antidiuretic effects.

Pharmacological properties

As an antiepileptic drug, it stabilizes the membranes of overexcited neurons, suppresses serial discharges of neurons and reduces the synaptic transmission of excitatory impulses. This effect is achieved presumably by blocking sodium channels, thereby preventing the re-occurrence of sodium-dependent action potentials in depolarized neurons. Reduces the release of the neurotransmitter glutamate. The psychotropic effect of carbamazepine is apparently due to inhibition of the metabolism of dogamine and norepinephrine.

Reduces the frequency of attacks, anxiety, depression, irritability and aggressiveness in patients with epilepsy. The effect on cognitive function in patients with epilepsy is variable. Prevents the appearance of paroxysmal pain due to neuralgia. In case of alcohol withdrawal syndrome, it increases the threshold of convulsive readiness, reduces increased nervous excitability, tremor, and gait disturbances. Used to treat affective disorders as an antipsychotic and mood stabilizer. In diabetes insipidus, it reduces diuresis and thirst.

Pharmacokinetics

Absorption is slow, but quite complete (the intake of food does not significantly affect the speed and degree of absorption). After a single dose, Cmax in blood plasma is achieved after 12 hours.

Equilibrium concentrations of the drug in plasma are achieved after 1-2 weeks. Among patients, there are significant individual differences in the value of equilibrium concentrations in the therapeutic range. The connection with blood plasma proteins is 70-80%. The concentration of unchanged carbamazepine in the cerebrospinal fluid and saliva is proportional to the amount of active substance not bound to proteins (20-30%). The concentration in breast milk is 25-60% of that in plasma. Penetrates through the placental barrier.

Metabolized in the liver, mainly along the epoxide pathway with the formation of metabolites: active - carbamazepine-10,11-epoxide and low-active - 9-hydroxy-methyl-10 carbamoylacridan. The main isoenzyme that ensures the biotransformation of carbamazepine into carbamazepine-10,11-epoxide is the cytochrome P450 3A4 isoenzyme. The content of carbamazepine-10,11-epoxide is about 30% of the plasma level of carbamazepine. The biotransformation of carbamazepine-10,11-epoxide into carbamazepine-10,11-transdiol occurs with the help of the microsomal enzyme epoxide hydrolase. Another pathway of carbamazepine metabolism is the formation of various monohydroxylated derivatives, as well as N-glucuronides.

T1/2 after a single dose averages about 36 hours (ranges from 25 to 65 hours), after repeated doses - 16-24 hours. In patients receiving additional antiepileptic drugs that induce liver enzymes, an average of 9-10 hours. It is excreted primarily as inactive metabolites in urine (approximately 70%) and feces (approximately 30%). About 2% is excreted in the urine as unchanged carbamazepine and 1% as carbamazepine-10,11-epoxide.

In children, due to the faster elimination of carbamazepine, higher doses of the drug per kg of body weight may be required compared to adults.

There is no evidence that the pharmacokinetics of carbamazepine changes in elderly patients.

There are no data on the pharmacokinetics of carbamazepine in patients with impaired renal or hepatic function.

Indications for use

Indications for use of the drug Carbamazepine are: epilepsy (monotherapy or as part of complex therapy): complex and simple partial seizures (with or without loss of consciousness) with or without secondary generalization, as well as generalized tonic-clonic seizures. Mixed forms of epileptic seizures; acute manic states and maintenance therapy of bipolar affective disorders to prevent exacerbations or reduce the severity of clinical manifestations; in complex therapy of alcohol withdrawal syndrome; trigeminal neuralgia (idiopathic, with multiple sclerosis), idiopathic neuralgia of the glossopharyngeal nerve; pain syndrome in diabetic neuropathy; polyuria and polydipsia of neurohormonal nature in diabetes insipidus.

Mode of application

Carbamazepine take orally, regardless of food intake, with a small amount of liquid.

Epilepsy: Whenever possible, carbamazepine should be prescribed as monotherapy. Treatment begins with a small daily dose, which is subsequently slowly increased until the optimal effect is achieved. The addition of carbamazepine to existing antiepileptic therapy should be carried out gradually.

For adults, the initial dose is 100-200 mg 1-2 times a day. Then the dose is slowly increased to 400 mg 2-3 times a day. The maximum daily dose is 2000 mg.

For children under 5 years of age, the initial dose is 20-60 mg/day, increasing by 20-60 mg every two days. In children over 5 years of age, the initial dose is 100 mg/day, followed by an increase of 100 mg/week. The maintenance dose for children is 10-20 mg/kg body weight/day in 2-3 doses. To ensure accurate dosing, liquid oral dosage forms of carbamazepine must be used in children under 5 years of age.

Neuralgia of the trigeminal or glossopharyngeal nerves: initial dose 200-400 mg/day, then the dose is gradually increased by no more than 200 mg per day until the pain stops (on average, up to 600-800 mg), then reduced to the minimum effective dose. When treating elderly patients, the initial dose is 100 mg 2 times a day.

Alcohol withdrawal syndrome: average dose - 200 mg 3 times a day. In severe cases, in the first days, the dose can be increased to 400 mg 3 times a day. At the beginning of treatment for severe withdrawal symptoms, it is prescribed in combination with detoxification therapy, sedatives and hypnotics.

Polyuria and polydipsia in diabetes insipidus: the average dose for adults is 200 mg 2-3 times a day. In children, the dose is selected taking into account body weight and age.

Pain syndrome in diabetic neuropathy: 200 mg 2-4 times/day.

Acute manic states and maintenance therapy of bipolar affective disorders: daily dose 400-1600 mg (average daily dose 200-600 mg) for 2-3 doses/day. In acute cases, the dose is increased quickly enough. During maintenance therapy, dose increases should be gradual and small.

Side effects

Nervous system disorders: dizziness, ataxia, drowsiness, fatigue, headache, diplopia, accommodation disturbances, tremor, muscular dystonia, tics, nystagmus, orofacial dyskinesia, oculomotor disorders, dysarthria, choreoathetoid disorders, peripheral neuropathy, paresthesia, paresis, taste disturbances, neuroleptic malignant syndrome.

Mental disorders: hallucinations (visual or auditory), depression, anorexia, anxiety, aggressive behavior, agitation, disorientation, increased psychosis.

On the part of the skin and its appendages: allergic dermatitis, urticaria, exfoliative dermatitis, erythroderma, systemic lupus erythematosus, itching, Stevens-Johnson syndrome, toxic epidermal necrolysis, photosensitivity reactions, erythema multiforme and nodosum, skin pigmentation disorders, purpura, acne, sweating, hair loss.

Rare cases of hirsutism have been reported, but the causal relationship of this complication to the drug remains unclear.

From the hematopoietic system: leukopenia, thrombocytopenia, eosinophilia, leukocytosis, lymphadenopathy, folic acid deficiency, agranulocytosis, aplastic anemia, pancytopenia, anemia, true erythrocyte aplasia, megaloblastic anemia, variegated porphyria, porphyria cutanea tarda, acute intermittent porphyria, recurrent ticulocytosis, hemolytic anemia .

From the hepatobiliary system: increased levels of GGT, alkaline phosphatase, transaminases; hepatitis (cholestatic, parenchymal (hepatocellular) or mixed type), jaundice, granulomatous hepatitis, liver failure.

From the gastrointestinal tract: nausea, vomiting, dry mouth, diarrhea, constipation, abdominal pain, glossitis, stomatitis, pancreatitis.

Hypersensitivity reactions: multiorgan delayed-type hypersensitivity with fever, skin rash, vasculitis, lymphadenopathy, arthralgia, leukopenia, eosinophilia, hepatosplenomegaly and altered liver function tests (these manifestations occur in various combinations). Other organs may also be involved (lungs, kidneys, pancreas, myocardium, colon). Aseptic meningitis with myoclonus and eosinophilia; anaphylactic reaction, angioedema.

From the cardiovascular system: intracardiac conduction disorders; decrease or increase in blood pressure, bradycardia, arrhythmia, AV block with fainting, collapse, congestive heart failure, worsening of coronary heart disease, thrombophlebitis, thromboembolism.

From the endocrine system and metabolism: edema, fluid retention, weight gain, hyponatremia and a decrease in plasma osmolarity due to an effect similar to the action of antidiuretic hormone, which in rare cases leads to water intoxication (dilution hyponatremia), accompanied by lethargy, vomiting, headache pain, disorientation and neurological disorders; increased prolactin levels, accompanied or not accompanied by galactorrhea, gynecomastia; decreased concentrations of triiodothyronine and thyroxine, increased concentrations of thyroid-stimulating hormone, which is usually not accompanied by clinical manifestations; disorders of bone tissue metabolism (decrease in the concentration of calcium and 25-hydroxycolecalciferol in the blood plasma), which leads to osteomalacia; increased concentrations of cholesterol, including high-density lipoprotein cholesterol and triglycerides.

From the genitourinary system: interstitial nephritis, renal failure, albuminuria, hematuria, oliguria, azotemia, frequent urination, urinary retention, sexual function disorders, spermatogenesis disorders.

From the senses: disturbances in taste, clouding of the lens, increased intraocular pressure, conjunctivitis; hearing disorders.

From the musculoskeletal system: arthralgia, muscle pain, muscle weakness, cramps.

From the respiratory system: hypersensitivity reactions characterized by fever, shortness of breath, pneumonitis or pneumonia.

Changes in laboratory results: hypogammaglobulinemia.

Contraindications

Contraindications to the use of the drug Carbamazepine are: V-blockade; history of suppression of bone marrow hematopoiesis; hepatic porphyrias; simultaneous use of MAO inhibitors and for 2 weeks after their discontinuation; breastfeeding period; hypersensitivity to any of the components of the drug or chemically similar drugs (tricyclic antidepressants).

Use with caution when: low levels of leukocytes or platelets; mixed forms of epileptic seizures, including absence seizures; in old age; with heart, liver or kidney failure; increased intraocular pressure; dilution hyponatremia; hypothyroidism; prostatic hyperplasia; pregnancy (increased risk of developing intrauterine development disorders, including malformations).

Pregnancy

The use of the drug is contraindicated Carbamazepine during pregnancy.

Interaction with other drugs

Simultaneous use Carbamazepine with inhibitors of the CYP3A4 isoenzyme may lead to increased plasma concentrations of carbamazepine. The combined use of inducers of the CYP 3 A 4 isoenzyme may lead to an acceleration of the metabolism of carbamazepine and a possible decrease in its plasma concentration. Withdrawal of concomitantly taken inducers of the CYP 3A4 isoenzyme may reduce the rate of biotransformation of carbamazepine and lead to an increase in the level of carbamazepine in the blood plasma. When used simultaneously with drugs metabolized by the CYP 3A4 isoenzyme, induction of metabolism and a decrease in their concentration in plasma is possible.

Drugs that may increase plasma concentrations of carbamazepine or carbamazepine-10,11-epoxide: dextropropoxyphene, ibuprofen, danazol, macrolide antibiotics (eg, erythromycin, troleandomycin, josamycin, clarithromycin), fluoxetine, fluvoxamine, nefazodone, paroxetine, trazodone, viloxazine, stiripentol, vigabatrin, azoles (eg, itraconazole, ketoconazole, fluconazole, voriconazole), loratadine, terfenadine, loxapine, olanzapine, quetiapine, isoniazid, viral protease inhibitors for HIV therapy (eg, ritonavir), acetazolamide, verapamil, diltiazem, omeprazole , oxybutynin, dantrolene, ticlopidine, nicotinamide (in adults, only in high doses), possibly cimetidine, desipramine, primidone, valproic acid.

Drugs that may reduce plasma concentrations of carbamazepine: felbamate, methsuximide, oxcarbazepine, phenobarbital, fensuximide, phenytoin, fosphenytoin, primidone, progabide, theophylline, aminophylline, isotretinoin, rifampicin, cisplatin, doxorubicin; herbal preparations containing St. John's wort and, although data are conflicting, possibly also clonazepam, valproic acid or valpromide.

Effect of carbamazepine on plasma concentrations of drugs used as concomitant therapy: Carbamazepine can reduce plasma concentrations or reduce or even completely neutralize the effects of the following drugs: methadone, paracetamol, antipyrine, tramadol, doxycycline, oral anticoagulants (warfarin, phenprocoumon, dicumarol, acenocoumarol), bupropion, citalopram, trazodone, tricyclic antidepressants (imipramine, amitriptyline, nortriptyline, clomipramine), clobazam, clonazepam, ethosuximide, felbamate, lamotrigine, oxcarbazepine, primidone, tiagabine, topiramate, valproic acid, zonisamide, itraconazole, p raziquantel, imatinib, clozapine, haloperidol, bromperidol, olanzapine, quetiapine, risperidone, ziprasidone, used in the treatment of HIV infection (indinavir, ritonavir, saquinavir), alprazolam; midazolam, theophylline, calcium channel blockers of the dihydropyridine group (for example, felodipine), digoxin, oral contraceptives (selection of alternative methods of contraception is necessary), glucocorticosteroids (for example, prednisolone, dexamethasone); cyclosporine, everolimus, levothyroxine sodium, estrogens and/or progesterone.

There are reports that while taking carbamazepine, the level of phenytoin in the blood plasma may either increase or decrease, and the level of mephenytoin may increase (in rare cases).

Combinations to consider:

Increased hepatotoxicity caused by isoniazid is possible when used simultaneously with carbamazepine.

In the case of co-administration with levetiracetam, the toxic effect of carbamazepine may be enhanced.

The combined use of carbamazepine and lithium or metoclopramide, as well as carbamazepine and antipsychotic drugs (haloperidol, thioridazine) can lead to an increase in the frequency of adverse neurological reactions (in the case of the latter combination, even at therapeutic concentrations of active substances in the blood plasma).

The simultaneous use of carbamazepine with some diuretics (hydrochlorothiazide, furosemide) can lead to hyponatremia, accompanied by clinical manifestations.

Carbamazepine may antagonize the action of non-depolarizing muscle relaxants (eg, pancuronium bromide). If such a combination of drugs is used, it may be necessary to increase the dose of these muscle relaxants; Patients should be closely monitored as the effects of muscle relaxants may cease more quickly than expected.

Coadministration with grapefruit juice may increase plasma levels of carbamazepine.

Overdose

Overdose symptoms Carbamazepine:

• Central nervous system: depression of the functions of the central nervous system up to coma, disorientation, drowsiness, agitation, hallucinations, a feeling of “fog” before the eyes, dysarthria, nystagmus, ataxia, dyskinesia, hyperreflexia alternating with hyporeflexia, convulsions, psychomotor disorders, myoclonus, hypothermia, mydriasis;
• respiratory system: respiratory depression, pulmonary edema;
• cardiovascular system: tachycardia, decreased or increased blood pressure, cardiac conduction disturbances with widening of the QRS complex, cardiac arrest;
• digestive system: vomiting, delayed evacuation of food from the stomach, decreased colon motility;
• urinary system: urinary retention, oliguria or anuria, fluid retention, dilution hyponatremia;
• laboratory parameters: metabolic acidosis, hyperglycemia, increased muscle CPK fraction, hyponatremia.

Treatment: there is no specific antidote. Gastric lavage, administration of activated charcoal (late evacuation of gastric contents can lead to delayed absorption for 2-3 days and reappearance of intoxication symptoms), hospitalization, symptomatic therapy. Forced diuresis, hemodialysis and peritoneal dialysis are ineffective (dialysis is indicated for a combination of severe poisoning and renal failure). It is recommended to carry out hemosorption on carbon sorbents.

Storage conditions

Carbamazepine store out of reach of children, in a dry place, protected from light at a temperature not exceeding 25°C.

Shelf life - 3 years.

Release form

Carbamazepine- tablets of 0.2 g in packs of 30 and 100 pieces.

Compound

1 tablet contains: Carbamazepine 200 mg.

Excipients: potato starch - 80.5 mg, colloidal silicon dioxide (Aerosil) - 16.4 mg, talc - 3.1 mg, magnesium stearate - 3.1 mg, povidone (polyvinylpyrrolidone) - 14.4 mg, polysorbate (Tween-80) - 2.5 mg.

Additionally

Before starting treatment, as well as periodically during treatment, clinical blood tests (including counting the number of platelets, reticulocytes, and iron concentration in the blood serum), general urine tests and determination of the level of urea in the blood should be performed. The drug has weak anticholinergic activity. Therefore, when using the drug in patients with increased intraocular pressure, constant monitoring of this indicator is necessary. It is recommended to periodically determine the concentration of carbamazepine in the blood plasma in cases of increased frequency of epileptic seizures, in the treatment of children, in pregnant women, in the case of its use as part of complex therapy, or in the development of severe side effects. There are isolated reports of disturbances in male fertility and/or disturbances in spermatogenesis. However, the causal relationship of these disorders with taking the drug has not yet been proven. Cross-hypersensitivity reactions may occur between carbamazepine and phenytoin or oxcarbazepine. During therapy, it is necessary to stop drinking alcohol, since carbamazepine enhances the inhibitory effect of alcohol on the central nervous system. Influence on the ability to drive vehicles and operate machinery. During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

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