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.
Pharmacodynamics and pharmacokinetics
The active component is a derivative of dibenzazepine . The drug has antimanic, normothymic, antidiuretic (in patients with diabetes insipidus ), analgesic (for neuralgia ) effects.
The principle of action of the drug is based on the blockade of voltage-gated sodium channels, which causes inhibition of the process of occurrence of neuronal discharges, stabilization of the neuron membrane, which effectively leads to a decrease in synaptic conduction of impulses.
The drug prevents the re-formation of sodium-dependent action potentials in the structure of depolarized neurons.
Carbamazepine leads to a decrease in the release of glutamate (a neurotransmitter amino acid), which reduces the risk of developing an epileptic seizure . In children and adolescents with epilepsy , while taking the drug, there is a positive trend in the severity of depression and anxiety, as well as a decrease in aggressiveness and irritability.
The effect on psychomotor indicators and cognitive functions is dose-dependent and variable in each specific case.
With trigeminal neuralgia (essential, secondary), there is a decrease in the frequency of pain attacks.
For postherpetic neuralgia , post-traumatic paresthesia , tabes of the spinal cord - Carbamazepine helps relieve neurogenic pain.
During alcohol withdrawal, the drug can reduce the severity of the main symptoms (tremor of the limbs, increased excitability, gait disturbances), and increases the threshold of convulsive readiness.
In patients with diabetes mellitus, the drug reduces the feeling of heat, diuresis, and leads to rapid compensation of water balance.
The antimanic (antipsychotic) effect is registered after 7-10 days of therapy and develops as a result of inhibition of the metabolism of norepinephrine and dopamine .
The use of prolonged forms of carbamazepine makes it possible to achieve a stable concentration of the main substance in the blood, without recording “dips” and “peaks”.
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.
Indications for use of Carbamazepine
What are the tablets commonly used for? The drug is prescribed for epilepsy: mixed forms of seizures, generalized forms of seizures accompanied by tonic-clonic seizures, partial seizures .
The drug is used for idiopathic neuralgia of the glossopharyngeal nerve , for trigeminal neuralgia in patients with multiple sclerosis, for idiopathic trigeminal neuralgia.
What other indications for the use of Carbamazepine exist? The medication is recommended for use in acute manic states (combination therapy with antipsychotics, lithium preparations). The medicine is prescribed for diabetic neuropathy with painful symptoms, alcohol withdrawal syndrome (hyperexcitability, convulsions, anxiety, sleep disturbances), phasic affective disorders, diabetes insipidus of central origin, polydipsia of neurohormonal origin, polyuria.
The drug is prescribed for psychotic disorders (psychosis, schizoaffective and affective disorders, dysfunction of the limbic system, panic disorders), obsessive-compulsive disorders, Kluver-Bucy syndrome , senile dementia, tinnitus, dysphoria , anxiety, somatization, chorea, depression , for multiple sclerosis, tabes dorsalis, phantom pain, diabetic polyneuropathy , acute idiopathic neuritis, hemificial spasm, Ekbom's syndrome, post-traumatic neuralgia, neuropathy, for the prevention of migraine, for postherpetic neuralgia.
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 shows a relatively low level of effectiveness in the case of a minor myoclonic attack or absence seizure.
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.
Contraindications
Carbamazepine is not used for atrioventricular block, acute form of “intermittent” porphyria, impaired bone marrow circulation (leukopenia, anemia), intolerance to the main substance, hypersensitivity to tricyclic antidepressants . In case of active alcoholism, decompensated form of CHF, adrenal insufficiency, hypothyroidism , hypopituitarism , ADH hypersecretion syndrome, dilution hyponatremia, suppression of bone marrow hematopoiesis, increased intraocular pressure, prostatic hyperplasia, and pathology of the renal system, the medication is prescribed with caution, evaluating possible risks.
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 patient a course of Carbamazepine, is obliged to inform about possible dangers. The patient is usually advised to undergo antenatal diagnosis.
Side effects of Carbamazepine
The severity of the side effect is dose-dependent.
Nervous system: accommodation paresis, headaches, asthenia, ataxia, dizziness, rarely observed abnormal involuntary movements (tics, dystonia, tremor), paresthesia, peripheral neuritis , choreoathetoid disorders, speech disorders, oculomotor disorders, orofacial dyskinesias, nystagmus, symptoms of paresis, myasthenia gravis.
Mental areas: activation of psychosis, disorientation , agitation, aggressive behavior, anxiety, decreased appetite, depression, visual hallucinations, auditory hallucinations . Allergic reactions: skin itching, erythroderma, urticaria , photosensitivity, Lyell's syndrome, Stevens-Johnson syndrome.
Hematopoietic organs: aplastic anemia , leukocytosis, thrombocytopenia, reticulocytosis, hemolytic anemia, lymphadenopathy. Digestive tract: pancreatitis , stomatitis , glossitis , epigastric pain, stool disorders, liver failure, jaundice, granulomatous hepatitis, increased liver enzymes.
Cardiovascular system: exacerbation of coronary artery disease, worsening of CHF, atrioventricular block with fainting, bradycardia, instability of blood pressure, impaired intracardiac conduction, arrhythmia, thromboembolic syndrome , thrombophlebitis. Metabolism, endocrine system: hyperprolactinemia , decreased L-thyroxine levels, hyponatremia, weight gain, swelling, fluid retention in the body, hypercholesterolemia, osteomalacia.
Genitourinary system: frequent urination, disturbances in the renal system, interstitial nephritis, decreased potency, hematuria, oliguria, albuminuria . Musculoskeletal system: convulsions, myalgia, arthralgia.
Sense organs: changes in the perception of pitch, hypoacusia, hyperacusia, tinnitus, hearing impairment, conjunctivitis, lens opacification, impaired taste perception. Increased sweating, acne , purpura, alopecia, skin pigmentation disorders, and hirsutism are also possible.
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.
Carbamazepine tablets, instructions for use (Method and dosage)
The drug is taken orally with a sufficient amount of water. Long-acting tablets (Carbamazepine Retard) are not chewed, swallowed whole, twice a day.
For epilepsy, the drug is prescribed, whenever possible, as monotherapy. It is recommended to start treatment with small doses with a gradual increase in dosage, which allows you to achieve optimal results. The initial dosage for adults is 100-200 mg 1-2 times a day, gradually increasing the amount of medication.
Trigeminal neuralgia: the first day of therapy – 200-400 mg, with a gradual increase to 400-800 mg per day, then the drug Carbamazepine is gradually discontinued.
The initial dosage for pain syndrome of neurogenic origin is 100 mg twice a day, with an increase in dose every 12 hours until pain subsides. The maintenance dosage is 200-1200 mg per day, divided into several doses.
The average dosage for alcohol withdrawal syndrome is 200 mg three times a day; in severe cases, the dose is increased to 400 mg three times a day.
In the first days of therapy, it is recommended to additionally prescribe chlordiazepoxide, clomethiazole and other sedative-hypnotics.
For diabetes insipidus, adults are prescribed 200 mg 2-3 times a day.
For diabetic neuropathy with pain, 200 mg is prescribed 2-4 times a day.
Prevention of schizoaffective and affective psychoses: 600 mg for 3-4 doses per day.
The daily dose for bipolar, affective disorders, manic states is 400-1600 mg.
Instructions for use of Carbamazepine Acri are similar.
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.
Overdose
It manifests itself as disturbances in the functioning of the respiratory, cardiovascular and nervous systems.
Sense organs, nervous system: dysarthria , fainting, disorientation, nystagmus, hyporeflexia, myoclonus, psychomotor disorders, convulsions, mydriasis, hypothermia , visual disturbances, hallucinations, drowsiness, agitation.
Cardiovascular system: cardiac arrest, intraventricular conduction disturbance, tachycardia, blood pressure .
Pulmonary edema, respiratory depression, vomiting, nausea, decreased colonic motility, delayed evacuation of food from the stomach, hyponatremia , fluid retention, anuria , oliugria, metabolic acidosis , hyperglycemia are also noted.
A specific antidote has not been developed. Treatment of overdose is carried out syndromic.
Interaction
Metabolism of the drug is carried out using cytochrome CYP3A4 . When administered simultaneously with inhibitors of this cytochrome, an increase in its concentration is observed, and, accordingly, the severity of side effects increases. Cytochrome inducers accelerate metabolic processes, reduce the level of drug concentration in the blood, reducing the severity of its therapeutic effect.
The concentration of the drug in the blood increases: Nicotinamide , Verapamil , Cimetidine , fluvoxamine , Fluoxetine , Viloxazine , Dextropropoxyphene , Felodipine , Diltiazem , acetazolamide , Desipramine , Danazol , Trefenadine , macrolides ( troleandomycin , Clarithromycin , Josamycin , Erythromycin cin ), azoles ( Fluconazole , Itraconazole , Ketoconazole ), ritonavir , propoxyphene , isoniazid , Loratadine .
Phenobarbital , Cisplatin , Rifampicin , Theophylline , Primidone , Phenytoin , valproic acid , Valpromide , Doxorubicin , Cisplatin - reduce the concentration of the drug in the blood.
When the drug is combined with maprotiline psychosis and confusion may occur .
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.
special instructions
Monotherapy for patients with epilepsy begins with small dosages with a gradual increase in the amount of the drug to achieve the desired effect. In combination therapy, it is advisable to determine the plasma concentration of carbamazepine to select the optimal dosage. When the drug is abruptly discontinued, epileptic seizures . If it is necessary to discontinue carbamazepine, they try to transfer the patient to another antiepileptic drug. During therapy, monitoring of the performance of the liver system and blood condition is required. Carbamazepine has a weak anticholinergic effect , which requires constant monitoring of intraocular pressure. The drug can reduce the effectiveness of oral contraceptives, which requires the use of additional methods to protect against pregnancy.
MNN: Carbamazepine.
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.
Reviews of Carbamazepine
There are few reviews on forums about the drug used for medicinal purposes. Basically, opinions are left on the effect of the drug as a drug.
When a medicine is used in the treatment of various types of depressive conditions and mental disorders, opinions are expressed about its weak effectiveness in comparison with more modern analogues, which at the same time have fewer side effects. In the treatment of trigeminal neuralgia, the medication is considered ineffective.
Insomnia may also be a consequence of using the drug.
Reviews of Carbamazepine Acri are similar.
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.
Carbamazepine price, where to buy
The price of Carbamazepine is 55 rubles per package of 50 tablets of 200 mg.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Carbamazepine tablets 0.2g 50 pcs. JSC Obolenskoe farm.
enterprise 205 rub. order
Pharmacy Dialogue
- Carbamazepine tablets 200 mg No. 40 Alsi Pharm
73 rub. order
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Pharmacy24
- Carbamazepine-Astrapharm 200 mg N20 tablets TOV Astrapharm, Ukraine
21 UAH order - Carbamazepine-FS 200 mg No. 50 tablets Pharma Start TOV, Ukraine
35 UAH order
- Carbamazepine-Darnitsa 0.2 g No. 20 tablets PrAT” Pharmaceutical company “Darnitsa”, Ukraine
17 UAH order
- Carbamazepine-FS 200 mg No. 20 tablets Pharma Start TOV, Ukraine
18 UAH order
- Carbamazepine 200 mg N20 tablets PrAT "Technolog", Uman, Cherkasy region, Ukraine
18 UAH order
PaniPharmacy
- Carbamazepine tablet 0.2g No. 20
18 UAH order
- CARBAMAZEPINE tablets Carbamazepine tablets. 200 mg No. 20 Ukraine, Health LLC
18 UAH order
- CARBAMAZEPINE tablets Carbamazepine tablets. 0.2g No. 50 Ukraine, Tekhnolog ChAO
38 UAH order
- Carbamazepine tablets Carbamazepine tablets. 0.2g No. 20 Ukraine, Darnitsa ChAO
21 UAH order
- CARBAMAZEPINE tablets Carbamazepine-FS tablet. 200 mg No. 20 Ukraine, Pharma Start LLC
22 UAH order
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Technical information
The 200 mg of carbamazepine contained in 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.
