Carbamazepine indications for use. Work on complex mechanisms. Principles of application and analogues

Carbamazepine tablets instructions

The instruction goes on sale with each package of the drug Carbamazepine; it covers all issues related to taking the tablets.

Form, composition, packaging

The dosage form of the drug is a tablet. Its color is white with a possible yellow tint, and its shape is flat and cylindrical. There is a mark for separation and chamfer. Concentration active substance carbamazepine is 200 milligrams per piece. The accompanying substances are suspensions (Tween-80) of polysorbate, potato starch, povidone, Aerosil, magnesium stearate and talc.

The tablets are supplied to the pharmacy chain in packs of thick cardboard, which contain 1,2, 3, 4 or 5 packages of cellular contour packs with a dozen pills each.

Storage period and conditions

The drug is stored for three years in dry and dark rooms. Room temperature. Children are not allowed.

Carbamazepine indications for use

Indications for prescription are certain diseases and conditions of the patient of a specific nature. Carbamazepine is recommended for use:

• for epilepsy (both for monotherapeutic measures and for integrated approach to treatment) for partial seizures of simple and complex nature, with mixed forms of epileptic seizure or tonic-clonic seizures, and their generalization can also be secondary, the patient may lose consciousness or do without it;
• when an acute manic state manifests itself in a patient during an exacerbation or when maintenance therapy is necessary, as well as in for preventive purposes in the presence of bipolar affective disorder or to reduce its clinical manifestations in severity;
• for alcohol withdrawal syndrome as a component of complex treatment;
• with severe neuralgia trigeminal nerve or neuralgia glossopharyngeal nerve idiopathic;
• with severe pain syndromes of diabetic neuropathy;
• with the development of polydipsia or polyuria of diabetes insipidus, the nature of which is neurohormonal.

Contraindications

The drug is not prescribed due to its contraindications in the following cases:

• with AV block;
• if the patient has a history of documented suppression of bone marrow hematopoiesis;
• with hepatic porphyria;
• if necessary, combine the use of Carbamazepine with antidepressants and another two weeks after stopping their use;
• for nursing mothers;
• in case of manifestations of hypersensitivity reactions to constituent components medicines.

It is allowed to prescribe the drug, but with extreme caution for those patients who have

• low white blood cell or platelet count;
• pregnancy;
• epileptic seizures, the form of which is mixed;
• refer to elderly age no category;
• increased VD;
• heart, kidney or liver failure;
• prostate hyperplasia;
• hypothyroidism;
• hyponatremia.

Carbamazepine instructions for use

Carbamazepine should be taken orally, without paying attention to food intake. Take small amounts of water.

Use of carbamazepine for the treatment of epilepsy

It is prescribed primarily as a monotherapeutic dose. If it is necessary to add carbamazepine to another antiepileptic treatment regimen, this must be done gradually. The drug should be started in small daily doses, which can be increased until the optimal effect of therapy occurs.

For an adult, you can start treatment with 100-200 mg / 2 r / day and gradually increase the dose to 400 mg / 2-3 r / day. The maximum you can take in one day is up to 2000 mg.

For a child under five years of age, treatment begins with doses of 20-60 mg/day, where it is allowed to increase the dosage every two days by 20-60 mg.

For a child over five years of age, the initial dose is 100 mg/day, with the dose increasing by 100 mg per week.

The dose for maintenance therapy for a child is 10-20 mg/kg of his body weight per day per 2-3 dose. In order to ensure accurate dosage, it is recommended that children be prescribed liquid forms drug for oral administration.

Use for identified neuralgia of the glossopharyngeal or trigeminal nerve

The initial dose of carbamazepine for treatment can be taken from 200 to 400 mg/day, after which the dosage can be increased to 600 or 800 mg until the pain stops. However, increase the dose gradually by no more than 200 mg per day. When the pain syndrome disappears, reduce the dose of the drug to the minimum effective dose.

Carbamazepine for alcohol withdrawal syndrome

On average, 200 mg of the drug is prescribed 3 times a day. If the case is severe, the dosage can be increased to 400 mg with the same frequency of administration for the first days of treatment. Also, at the beginning of therapy, Carbamazepine should be combined with drugs for detoxification, sedatives and sleeping pills.

In the treatment of polydipsia, polyuria and diabetes

On average, an adult is prescribed 200 mg/up to three times a day;

For children, the dose is calculated taking into account age and weight.

Diabetic neuropathy (for pain syndromes)

200 mg/up to 4 rubles per day.

In acute manic states or for support in bipolar affective disorders

The average daily recommended dose can range from 400 to 1600 mg/several doses. In case of exacerbation, the dosage should be quickly increased. When only maintenance therapy is needed, dose increases, if necessary, can be small and gradual.

Side effects

The drug Carbamazepine has a fairly extensive list of side effects. This information should be taken into account when prescribing medicine along with its contraindications.

Nervous system

Neuroleptic symptoms may develop malignant syndrome, dizziness, taste disturbances, signs of ataxia, paresis, feelings of fatigue and drowsiness. Headaches, paresthesia, diplopia, peripheral neuropathies cannot be excluded, and accommodation disturbance may occur. There have been complaints of tremor, choreoathetoid disorders, muscle dystonia, dysarthria, tics and nystagmus. Disturbances in ocular movement and the development of orofacial dyskinesia are not uncommon.

Mental disorders

In the form of hallucinations, increased psychosis, depressive states, agitation and disorientation. Possible development of anorexia, as well as various kinds anxiety and aggressive behavior.

Skin

There have been complaints about the development of exfoliative and allergic nature, patients experienced hair loss, sweating and acne. Urticaria may occur, accompanied by itching, erythroderma and systemic lupus erythematosus. Photosensitivity reactions, manifestations of erythema nodosum or multiforme, toxic epidermal necrolysis, purpura or skin pigmentation disorders have been observed.

Hematopoiesis

There have been cases of hemolytic, aplastic or megaloblastic anemia, as well as leukopenia and thrombocytopenia, reticulocytosis. Eosinophilia, folic acid deficiency, leukocytosis, and lymphadenopathy may occur. Agranulocytosis, variegated and late cutaneous porphyrias, as well as intermittent acute porphyrias, erythrocyte aplasia and pancytopenia cannot be excluded.

Hepatobiliary system

In the form of liver failure, hepatitis of any type, including mixed, jaundice.

Digestive system

In the form of vomiting and nausea, diarrhea or constipation, as well as the development of pancreatitis, glossitis, stomatitis. Dry mouth or pain in the peritoneal area may occur.

Allergic reaction

There have been cases of the development of multiorgan hypersensitivity, the type of which is delayed, accompanied by fever, vasculitis and skin rashes. Changes in liver function parameters are not excluded. The development of aseptic meningitis, as well as anaphylactic reactions and angioedema is possible.

Cardiovascular system

The development of intracardiac conduction disturbances, arrhythmia or bradycardia is possible. It is possible that blood pressure may fall or rise, fainting states, collapse, congestive cardiac failure. Thrombophlebitis or thromboembolism may occur.

Endocrine system

The development of swelling, weight gain and fluid retention were observed, plasma osmolarity decreased, and hyponatremia developed. There have been cases of water intoxication, which were accompanied by headaches, vomiting, neurological disorders or disorientation. There were cases of lethargy. There were increases in prolactin levels, which were often accompanied by phenomena such as gynecomastia or galactorrhea.

Genitourinary system

Patients complained of urinary retention or frequent toileting. Disorders of reproductive function developed, and spermatogenesis was disrupted. Cases of interstitial nephritis, renal failure, azotemia, albuminuria, oliguria and hematuria have been reported.

Sense organs

There were complaints from patients about visual and hearing disorders, as well as taste disturbances. The lens may become cloudy, VD may increase, and conjunctivitis may develop.

Muscles and bones

It is possible that muscle pain may develop, including cramps, as well as muscle weakness and arthralgia.

Respiratory system

Shortness of breath or fever, which are associated with the development of hypersensitivity reactions, as well as pneumonia.

Laboratory indicators

Development of hypogammaglobulinemia.

Overdose

An overdose should be treated with targeted symptomatic therapy, since its symptoms can manifest themselves in various body systems. First of all, you should rinse your stomach and make an appointment activated carbon to avoid recurrence of intoxication symptoms. The victim should be hospitalized.

Symptoms of an overdose may include the following:

• From the nervous system

Its functions may be significantly suppressed, up to the development of coma, and the development of disorientation, agitation and hallucinations may occur. Also signs of overdose are “fog” before the eyes, drowsiness and nystagmus. The development of dysarthria, dyskinesia and ataxia is also possible. One should expect manifestations of hyperreflexia, which may give way to hyporeflexia, as well as seizures and psychomotor disorders. The development of mydriasis, myoclonus and hypothermia is characteristic.

• From the respiratory system

Breathing may be depressed and pulmonary edema may develop.

• From the cardiovascular system

It is possible to change blood pressure levels, both falling and increasing, developing tachycardia and impaired cardiac conduction, up to cardiac arrest.

• From the digestive system

Manifested by vomiting, decreased intestinal motility and retention of stomach contents.

• From the urinary system

In the form of urinary fluid retention, anuria or oliguria.

• Laboratory data

The development of metabolic acidosis, hyperglycemia, and hyponatremia may be detected.

Drug interactions

It should be taken into account that the combination of the drug Carbamazepine with medications that affect the CYP 3A4 isoenzyme, in the case of simultaneous administration with an isoenzyme inhibitor, helps to increase its concentration in the blood plasma, and in the case of combination with an inducer, to decrease it.

Among the medications that lead to an increase in the plasma concentration of Carbamazepine are drugs from the group of macrolide antibiotics, dextroproxifene, danazol, ibuprofen, azoles, fluoxetine, nefazodone and others. Also, combination with loratadine, isoniazid, terfenadine, omeprazole, viral protease inhibitors in the treatment of HIV infection and many other drugs of the corresponding pharmacological groups will lead to an increase in the concentration of the drug.

Among medical supplies, which lead to a decrease in the plasma concentration of Carbamazepine, we can note the drugs phenobarbital, felbamate, oxarbazepine, phenytoin and others similar action. Drugs can also be included here. plant origin with St. John's wort and valproic acid in the composition.

When prescribing a medication for treatment, it is necessary to take into account some of its combinations that it forms when taken with other medications.

• Isoniazid can enhance the hepatotoxicity of Carbamazepine;
• Levetirocetam increases toxicity;
• Lithium preparations and neuroleptic drugs (thioridazine, haloperidol) increase the incidence of adverse neurological reactions;
• Diuretics (furosemide, hydrochlorothiazide) develop hyponatremia accompanied by clinical manifestations;
• Non-depolarizing muscle relaxants may conflict with carbamazepine, which may require increasing the dosage of the muscle relaxant to avoid cessation of its effect.
• Grapefruit juice significantly increases the concentration of the active substance of the drug in the blood plasma.

Additional instructions

Before starting treatment and periodically during the therapy period, the patient needs blood, urine and intraocular pressure tests.

Taking Carbamazepine is not compatible with drinking alcohol, since this drug can lead to an increase in the inhibitory effect of alcohol on the central nervous system.

During treatment, the patient must refrain from driving vehicles any kind. He should also limit his activities in relation to complex mechanisms and those areas of activity that involve increased attention and speed of response.

Carbamazepine analogues

Analogues of the medical drug Carbamazepine are mainly presented in tablet form. Among them, the following drugs are especially popular: Finlepsin, Tegretol, Finlepsin retard, Tegretol CR. Their cost ranges from 250 to 350 rubles per package.

Carbamazepine price

The cost of a package of Carbamazepine is significantly lower than its analogues and ranges from 45 to 60 rubles in online pharmacies subject to self-pickup.

Carbamazepine reviews

The drug as a whole has good reviews, with the exception of some who did not want to try the drug, not so much questioning its effectiveness as fearing a wide range of side effects that are indicated in its instructions.

Valentina: I recently became acquainted with the drug on the recommendation of a neurologist. Lately I have problems sleeping and nervous overstrain. The examination is still ongoing, but the doctor advised me to take Carbamazepine as help. Miracle. Just half a tablet gave me the opportunity to sleep about twenty hours of undisturbed sleep. I hope the body will go into recovery mode. However, I realized that an overdose of these pills is fraught with serious consequences, so I would not recommend taking them without a prescription.

Nina: I was treating neuralgia and was very disappointed in the drug at the very beginning of taking it. I stopped drinking it and started looking for analogues. There are too many side effects that attacked me almost from the first day of treatment. I don’t really want to list them, the headache alone is worth it! I can’t say that the pills are not effective therapeutically, but I have never encountered so many side effects anywhere and I don’t want to experience them further on myself.

Love: The pills turned out to be our salvation. The drug is good as an anticonvulsant even for children, although you need to be very careful with dosing. My son has been suffering from seizures almost since birth, and we use Carbamazepine to save ourselves all the time. No side effects were noticed and there is no addiction. We drink as recommended by the doctor in tiny doses. She also took it for a short time depressed state. The effect is positive. I recommend. Good remedy of course, as prescribed by the doctor.

According to statistics, about 80% of the world's population suffers from seizures. They appear as a result of stress, muscle strain, circulatory disorders or disease nervous system body. Cramps can be mild or severe. IN mild form There may be a slight tingling sensation in the affected area, and severe cases- a so-called epileptic seizure. Find out about the anticonvulsant drug Carbamazepine - instructions for use, composition of the drug, doses for effective treatment.

What is Carbamazepine

Carbamazepine tablets are an antiepileptic and anticonvulsant drug. The medicine is used for seizures and focal psychomotor epilepsy. The action of the active substance carbamazepine is aimed at eliminating pain in the patient, which will reduce the risk of recurrent seizures. The product should be used only as prescribed by a doctor.

Compound

Carbamazepine is structurally similar to antidepressants such as imipramine. The active substance of the drug is carbamazepine at a dosage of 200 mg. Excipients in the composition:

• starch (81 mg);
• colloidal silicon dioxide (17 mg);
• talc (3 mg);
• magnesium stearate (3 mg);
• PVP (14 mg);
• polysorbate (3 mg);
• acid.

Release form

Flat-cylindrical tablets are available in white or yellowish color in blister packs. There is an insert - instructions for Carbamazepine. The drug can be sold in the form of syrup. The medication is available only with a prescription. The release form of the medicine is different:

• small cell packaging of 10-25 pcs.;
• medium contour pack of 30 pcs.;
• large polymer jar of 20-100 pieces.

Mechanism of action

Action this drug: in the process of metabolism, the patient’s body produces carbamazepine from the main substance, which provides antiepileptic properties even when taking the usual dose. The inhibitor suppresses seizures, delays their manifestation, without causing any harm. general condition person. The substance can be taken even by small children; it does not interfere with the development of children. The dosage, divided into several doses, is calculated as follows:

• 20 mg/kg body weight (with increasing dose by 20-50 mg daily) – up to 5 years;
• 100 mg (with the addition of 100 mg daily) – from 5 years and older.

In addition, Carbamazepine reduces the conductivity of calcium channels to the desired level, reducing the effect of proteins, and this leads to inhibition of the uptake of high concentrations of catecholamine hormones. As a result, carbamazepine suppresses epileptic seizures and ensures the elimination of affective disorders that accompany epilepsy. The period of accumulation of the maximum concentration of the substance is 4-24 hours, elimination is several days.

Indications for use

The medication is prescribed for the treatment of diseases such as:

• leukopenia (decrease in white blood cells);
• neuralgia (including chronic, trigeminal and glossopharyngeal nerve);
• abstinence (in in this case they use the “blockade” method, that is, they do not allow addicts to take drugs);
• epilepsy (attacks are accompanied by convulsions, foam at the mouth and other signs);
• alcoholic withdrawal syndrome(convulsions, anxiety, hyperexcitability, insomnia);
• diabetes insipidus;
• psychological disorders;
• aggressive behavior patients with brain lesions;
• Kluver-Bucy syndrome, dysphoria, tinnitus, obsessive-compulsive disorder;
• for pain syndromes of neurogenic origin (Guillain-Barre syndrome);
• for the prevention of headaches and migraines.

Instructions for use of Carbamazepine

The patient is given a small daily dose of the medicine and gradually increases it each time to desired effect. If Carbamazepine is prescribed, the instructions for use for epilepsy are as follows:

• Adults – 2 times a day, 150 mg. IN next appointment the dose is increased to 350 mg.
• For children 4 years of age, the initial dose on the first day is 40 mg per day. Every other day, to enhance the effect, the child’s dose can be increased to 50 mg. Children five years of age and older should take 100 mg once daily. Every week, if necessary, the dose is increased by 100 mg.
• From the age of six - 0.5 g 3 times a day, and after 11 years the dose changes and the child needs to take 1 g of the substance.

Other reception options:

1. For trigeminal neuralgia, give 400 mg per day, increasing the amount by no more than 150 mg per day until it disappears discomfort. Then the dose is reduced to the minimum.
2. For alcohol withdrawal syndrome, take 0.2 g 2 times a day. In severe cases, the dose is increased to 350 mg.
3. Adults with diabetes insipidus should take 0.2 mg 2 times a day. Children are given a dose according to their weight and age. For acute affective disorders, you should take 1.5 g per day. The average dose is 550 mg 2-3 times a day.

The annotation of the drug indicates only average dosages. Full instructions The instructions for use can be found in the package insert of the medicine, and the treatment regimen can be found from the doctor. Other instructions:

• The tablets are taken regardless of meals, washed down with water.
• The drug should not be chewed, but swallowed whole.
• In some cases, the doctor may increase the dose.

Side effects

The development of side effects is possible with an overdose of the drug or significant fluctuations in plasma concentrations of carbamazepine. Headache, tic, speech impairment, and symptoms of paresis are observed. The drug can affect the human psyche, causing hallucinations, depression, anxiety, agitation, disorientation, and decreased appetite. The drug can cause urticaria, sometimes erythroderma. Rarely, a reaction in the form of hypersensitivity with fever and rash is observed.

Leukopenia, thrombocytopenia, and less commonly leukocytosis are often observed. Abdominal discomfort, dry mouth, vomiting, stomatitis or pancreatitis may occur. Swelling and weight gain also occur. Very rarely there is a decrease in potency and urinary retention. Myalgia, convulsions, impaired taste perception, conjunctivitis, tinnitus, and hearing changes are rarely observed. At intensive care observe:

• heart function;
• temperature;
• condition of the kidneys, bladder.

Contraindications

Carbamazepine should be taken carefully during pregnancy and under medical supervision. If you are hypersensitive to carbamazepine or other components of the drug, the drug should not be used. The medication is prohibited for disorders of bone marrow hematopoiesis, while taking inhibitors. People should take the drug with caution:

• aged;
• with active alcohol addiction;
• with renal failure;
• with increased intraocular pressure.

Interaction

Compatibility with other drugs is good, most do not affect the function of the product. Many drugs (Tramadol, Methadone, Doxycycline) can reduce their therapeutic effect or become toxic and damage the liver (like Paracetamol, the anti-tuberculosis drug Isoniazid). Plasma concentrations of carbamazepine can be increased by:

• Verapamil;
• Viloxazine;
• Nicotinamide;
• Danazol;
• Acetanazole.

Increases concentration also grapefruit juice, Ritonavir. There is evidence that the concentration of metabolites Phenytoin, Clonazepam, Rifampicin and Primidone reduces. Tricyclic antidepressants and oral anticoagulants are compatible with the substance. Concomitant use of carbamazepine with diuretics leads to hyponatremia.

Analogs

Akrikhin, Zeptol, Carbalepsin, Tegretol, Mazepin, Stazepin and Finlepsin are considered analogues of this drug. Carbamazepine substitute Zeptol has a price of 175 rubles. Its advantages are considered to be high bioavailability and a choice of release forms. As with the prescription of the drug itself, any substitute drug should be used only after consultation with your doctor.

The drug was created in the 50s of the twentieth century. Since then, scientists have created many drugs that compete with it in properties, but Carbamazepine, side effects that should not be ignored, continues to occupy leading place among anticonvulsants. The Japanese were the first to notice something else important property drug - relief from manic syndrome, bipolar disorder And acute forms schizophrenia. In the period from 70-90. There have been quite a few studies that have proven this. Following Japan, the rest of the world adopted this, and today Carbamazepine is effectively used for both epilepsy syndromes and acute mental disorders.

When to receive?

Carbamazepine not only helps with cramps, but is also an excellent pain reliever and is recommended in the following cases:

• To prevent psycho-emotional diseases;
• Alcohol withdrawal;
• Epilepsy in any manifestations;
• Painful diabetic neuropathy;
• Trigeminal neuralgia;
• Manic syndrome.

Experts in the field of psychiatry also insist on the effectiveness of the drug for aggressiveness, psychosis, schizophrenia and transformations of brain tissue. Laboratory experiments to determine the effectiveness of these specific diseases have not been carried out; here we can rely solely on clinical researches doctors.

In epileptics, this medicine reduces the risk of seizures by increasing the threshold convulsive readiness. Psychiatrists use Carbamazepine as a rehabilitation drug for socially maladjusted patients.

For teenagers, the drug is useful because it reduces the level of aggressiveness, depression and nervousness. The effect of the medicine is individual. It is forbidden to indulge in self-medication and prescribe it for yourself or a child yourself.

Principles of application and analogues

The drug has a unique effect on our body. Based on this, self-medication with this medicine is contraindicated; it can only be taken with the prescription of a specialist.

Compliance following rules strictly required upon admission:

1. So as not to cause negative effects the drug, you need to take it carefully following the instructions and regimens prescribed by your doctor;
2. Before starting treatment with Carbamazepine, perform a liver examination. If during the course you feel a deterioration in your liver condition, you need to stop taking the medication immediately;
3. The state of your intraocular pressure is important. Carbamazepine activates greater production of ocular secretion. If you had problems with intraocular pressure before taking the drug, there is a risk of vision loss.

Carbamazepine has a number of analogues in properties and therapeutic actions. The most common are considered Carbapine, Tegretol, Mazepine and Carbamazepine Nycomed. Doctors and patients claim that the effects of the drugs are similar to the original Carbamazepine.

Carbamazepine not an antidepressant and doesn't cure everything mental disorders, and its use requires constant supervision by a specialist and regular testing.

How to use? Permissible doses

Carbamazepine is available in tablets, which already indicates that they are taken orally. They should be drunk before or after meals. It is also possible to take the medicine while eating, then you need to take the tablets with a significant amount of liquid.

People with epilepsy are not advised to take other medications while being treated with carbamazepine.

The dose of the drug is increased gradually from the first day of administration to the dose required for treatment. If carbamazepine is administered with other drugs, this recommendation remains valid. The dosage of other medications does not change.

Exact doses:

Overdose and side effects

Symptoms of overdose include:

1. Loss of coordination;
2. Drowsiness;
3. Memory loss;
4. Sudden loss of orientation;
5. Weakness;
6. Hallucinations;
7. Coma.

An overdose is extremely life-threatening.

Overdose symptoms:

• Arrhythmia of the eyeballs, foggy veil, unnatural dilation of the pupils;
• Sensation of muscle twitching, impaired speech intelligibility;
• Sudden surges in pressure, tachycardia, cardiac arrest.

If symptoms of overdose are noticed, you must immediate hospitalization. If this is not possible, it is necessary to rinse and take activated carbon.

Do not increase the dose on your own. If you experience symptoms of side effects, contact your doctor immediately.

Side effects are demonstrated in the form of severe drowsiness, severe headache, taste bud disturbances, aggression, vomiting, dizziness, chronic fatigue, depression, nausea, dry mouth. If there is an individual intolerance to the components of the drug, an allergy appears.

Contraindications for use and interactions with other medications

Despite such a large and frightening list of side effects, in the lion's share of cases it is tolerated without problems. With minor changes in well-being, the problem can be solved by reducing the dose and adjusting the treatment regimen.

Who is contraindicated to take Carbamazepine:

1. People with atrioventricular block;
2. In the presence of hepatic porphyria;
3. During and breastfeeding;
4. Taking MAO inhibitors.

Be sure to notify your doctor about all medications you are taking at this time. Some drugs increase the risk of overdose. An example of such drugs: Fluoxetine, Erythromecin, Nicotinamide, etc.

When taking oral contraceptives with hormones, there is a possibility of uterine bleeding.

Alcohol intake is contraindicated; it increases the patient's state of depression.

The general trend of taking Carbamazepine is quite productive. Doctors have been successfully using it in treatment for more than half a century. Side effects, although wide in the range of damage, occur rarely enough to safely take it when prescribed by a specialist.

Video about self-correction of psychosomatic conditions

In this video you will learn how and why to take Carbamazepine:

Gross formula

Pharmacological group of the substance Carbamazepine

Nosological classification (ICD-10)

CAS Code

Characteristics of the substance Carbamazepine

White or almost white crystalline powder. Practically insoluble in water, soluble in ethanol and acetone. Molecular mass 236,27.

Pharmacology

Blocks sodium channels hyperactive membranes nerve cells, reduces the influence of excitatory neurotransmitter amino acids (glutamate, aspartate), enhances inhibitory (GABAergic) processes and interaction with central adenosine receptors. Antimanic properties are due to inhibition of the metabolism of dopamine and norepinephrine. Anticonvulsant effect occurs in partial and generalized seizures (grand mal). Effective (especially in children and adolescents) for relieving symptoms of anxiety and depression, as well as reducing irritability and aggressiveness (epilepsy). Prevents attacks of trigeminal neuralgia, reduces the severity of clinical manifestations of alcohol withdrawal (including agitation, tremor, gait disturbances) and reduces seizure activity. In diabetes insipidus, it reduces diuresis and thirst.

Absorbed into the gastrointestinal tract, although slowly, but almost completely; food does not affect the rate and extent of absorption. C max with a single dose of a regular tablet is achieved after 12 hours. With a single or repeated administration of retard tablets, C max (25% less than after a regular tablet) is observed within 24 hours. The retard form allows you to reduce daily fluctuations in plasma levels (determined after 1 -2 weeks) without changing the minimum value of the equilibrium concentration. Bioavailability when taking retard tablets is 15% lower than after using other drugs. dosage forms. Binding to blood proteins is 70-80%. IN cerebrospinal fluid and saliva, concentrations are created in proportion to the proportion of the active substance not bound to proteins (20-30%). Penetrates into breast milk (25-60% of plasma levels) and through the placental barrier. The apparent volume of distribution is 0.8-1.9 l/kg. It is biotransformed in the liver (mainly via the epoxide pathway) with the formation of several metabolites - the 10,11-trans-diol derivative and its conjugates with glucuronic acid, monohydroxylated derivatives, as well as N-glucuronides. T 1/2 - 25-65 hours, at long-term use- 8-29 hours (due to induction of metabolic enzymes); in patients taking inducers of the monooxygenase system (phenytoin, phenobarbital), T1/2 is 8-10 hours. After a single oral dose of 400 mg 72% dose taken excreted by the kidneys and 28% through the intestines. In urine, 2% of unchanged carbamazepine, 1% of active (10,11-epoxide derivative) and about 30% of other metabolites are determined. In children, excretion is accelerated (higher doses based on body weight may be required). 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.

Use of the substance Carbamazepine

Epilepsy (excluding petit mal), manic states, prevention of manic-depressive disorders, alcohol withdrawal, neuralgia of the trigeminal and glossopharyngeal nerves, diabetic neuropathy.

Contraindications

Hypersensitivity (including to tricyclic antidepressants), AV blockade, myelosuppression or acute porphyria in history.

Use during pregnancy and breastfeeding

Side effects of the substance Carbamazepine

Dizziness, agitation, hallucinations, depression, aggressive behavior, activation of psychosis, headache, diplopia, accommodation disturbances, lens opacification, nystagmus, conjunctivitis, tinnitus, change taste sensations, speech disorders (dysarthria, slurred speech), abnormal involuntary movements, peripheral neuritis, paresthesia, muscle weakness and symptoms of paresis, AV block, congestive heart failure, hyper- or hypotension, thromboembolism, renal dysfunction, interstitial nephritis, nausea, vomiting, increased levels of liver enzymes, jaundice, hepatitis, osteomalacia, sexual dysfunction, moderate leukopenia, thrombocytopenia, hematopoietic disorders, hyponatremia, multiorgan delayed-type hypersensitivity reactions, exfoliative dermatitis, lupus-like syndrome ( skin rash, urticaria, hyperthermia, sore throat, joint pain, weakness), Stevens-Johnson syndrome, Lyell, anaphylactic reactions.

Interaction

Incompatible with MAO inhibitors. Increases the hepatotoxicity of isoniazid. Reduces the effects of anticoagulants, anticonvulsants (hydantoin derivatives or succinimides), barbiturates, clonazepam, primidone, valproic acid. Phenothiazines, pimozide, thioxanthenes increase CNS depression; cimetidine, clarithromycin, diltiazem, verapamil, erythromycin, propoxyphene reduce metabolism (increases the risk toxic effect). Reduces the activity of corticosteroids, estrogens and estrogen-containing drugs oral contraceptives, quinidine, cardiac glycosides (induction of metabolism). In the presence of carbonic anhydrase inhibitors, the risk of osteogenesis disorders increases.

Overdose

Symptoms: disorientation, drowsiness, agitation, hallucinations and coma, blurred vision, dysarthria, nystagmus, ataxia, dyskinesia, hyper-/hyporeflexia, convulsions, myoclonus, hypothermia; respiratory depression, pulmonary edema; tachycardia, hypo-/hypertension, cardiac arrest accompanied by loss of consciousness; vomiting, decreased colonic motility; fluid retention, oliguria or anuria, changes in laboratory parameters: hyponatremia, possible metabolic acidosis, hyperglycemia, increased muscle fraction of creatinine phosphokinase.

Treatment: induction of vomiting or gastric lavage, administration of activated charcoal and saline laxative, forced diuresis. To maintain airway patency - tracheal intubation, artificial respiration and/or use of oxygen. In case of hypotension or shock - plasma expanders, dopamine or dobutamine; in case of seizures - administration of benzodiazepines (diazepam) or other anticonvulsants (in children, increased respiratory depression is possible; with the development of hyponatremia - fluid restriction, careful intravenous infusion isotonic solution sodium chloride. When combined severe poisoning with renal failure, renal dialysis is indicated. There is no specific antidote. It is necessary to anticipate a re-intensification of the symptoms of overdose on the 2nd and 3rd day after its onset, which is associated with the slow absorption of the drug.

Routes of administration

Inside.

Precautions for the substance Carbamazepine

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 or kidney diseases, hematological disorders, increased intraocular pressure, latent psychoses, inadequate response to external stimuli, agitation, diseases characterized by mixed convulsions, in old age, drivers of vehicles and persons operating the machinery. Treatment should not be stopped suddenly. Additional intake is recommended for women folic acid(before or during pregnancy); in order to prevent increased bleeding in last weeks During pregnancy and in newborns, vitamin K can be used.

Interactions with other active ingredients

Trade names

1 tablet contains:

active substance: carbamazepine 200 mg;

Excipients: ludipress (lactose monohydrate, povidone, crospovidone), magnesium stearate, calcium stearate monohydrate, potato starch.

N.03.A.F.01 Carbamazepine