Carbamazepine - instructions for use, analogs, testimonials and release forms (200 mg tablets) for the treatment of epilepsy and affective disorders in adults, children and pregnancy. Composition and interaction with alcohol

In this article, you can read the instructions for using the drug Carbamazepine. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Carbamazepine in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of carbamazepine in the presence of existing structural analogues.Use for the treatment of epilepsy and affective disorders in adults, children, as well as in pregnancy and lactation. Composition and interaction of the drug with alcohol.

Carbamazepine - antiepileptic agent (dibenzazepine derivative), which also has a normotime, antimanic, antidiuretic (in patients with diabetes insipidus) and analgesic (in patients with neuralgia).

The mechanism of action is associated with blockade of the potential of dependent Na channels, which leads to stabilization of the neuronal membrane, inhibition of the occurrence of serial discharges of neurons, and a decrease in synaptic impulses. Prevents the re-formation of Na-dependent action potentials in depolarized neurons. Reduces the release of the excitatory neurotransmitter amino acid glutamate, increases the reduced convulsive threshold, and so on. reduces the risk of developing an epileptic attack. Increases the conductivity for K, modulates the potential-dependent Ca channels, which can also cause the anticonvulsant effect of the drug. Corrects epileptic personality changes and, in the long run, improves the communicability of patients, contributes to their social rehabilitation.Can be prescribed as the main therapeutic drug and in combination with other anticonvulsant drugs. Effective in focal (partial) epileptic attacks (simple and complex), accompanied or not accompanied by secondary generalization, with generalized tonic-clonic epileptic seizures, and also with a combination of these types (usually ineffective in small seizures - petit mal, absences and myoclonic seizures) .

Patients with epilepsy (especially in children and adolescents) have a positive effect on the symptoms of anxiety and depression, as well as a decrease in irritability and aggressiveness. The effect on cognitive function and psychomotor parameters depends on the dose and is highly variable.

The onset of an anticonvulsant effect varies from a few hours to several days (sometimes up to 1 month due to autoinduction of metabolism). In the case of essential and secondary neuralgia of the trigeminal nerve, in most cases it prevents the occurrence of painful attacks. Effective for alleviating neurogenic pain in the dry spinal cord, post-traumatic paresthesia and postherpetic neuralgia.Relaxation of pain in trigeminal neuralgia is observed after 8-72 hours. With alcohol withdrawal syndrome, it increases the threshold of convulsive readiness (which is usually reduced in this condition) and reduces the severity of clinical manifestations of the syndrome (increased excitability, tremor, gait disturbance).

In patients with diabetes insipidus leads to rapid compensation of water balance, reduces diuresis and thirst.

Antipsychotic (antimanic) action develops after 7-10 days, may be due to oppression of the metabolism of dopamine and norepinephrine.

Composition

Carbamazepine + excipients.

Pharmacokinetics

Absorption - slow, but quite complete (eating does not affect the speed and degree of absorption). In the cerebrospinal fluid (further CSF) and saliva, concentrations are created in proportion to the amount of the active substance unbound with proteins (20-30%). Penetrates through the placental barrier. Concentration in breast milk is 25-60% of that in plasma. Metabolised in the liver, mainly along the epoxide route with the formation of the main metabolites: active - carbamazepine-10,11-epoxide and inactive conjugate with glucuronic acid.A low-active metabolite of 9-hydroxy-methyl-10-carbamoylacridan is also formed. Can induce own metabolism. The concentration of carbamazepine-10,11-epoxide is 30% of the concentration of carbamazepine.

It is excreted as inactive metabolites with urine (70%) and feces (30%). There is no evidence that the pharmacokinetics of carbamazepine change in elderly patients. Data on the pharmacokinetics of carbamazepine in patients with impaired renal or hepatic function are not yet sufficient.

Indications

• epilepsy (excluding absence, myoclonic or flaccid seizures) - partial seizures with complex and simple symptoms, primary and secondary generalized forms of seizures with tonic-clonic convulsions, mixed forms of seizures (monotherapy or in combination with other anticonvulsant drugs);
• idiopathic neuralgia of the trigeminal nerve;
• neuralgia of the trigeminal nerve with multiple sclerosis;
• idiopathic glossopharyngeal neuralgia;
• alcohol withdrawal syndrome;
• treatment of affective disorders;
• polydipsia and polyuria in diabetes insipidus;
• pain syndrome in diabetic polyneuropathy;
• prevention of phase-related affective disorders (manic-depressive psychosis, schizoaffective disorder, etc.).

Forms of release

Tablets 200 mg.

Instructions for use and dosage

Inside, regardless of food intake, along with a small amount of liquid.

Epilepsy. Whenever possible, carbamazepine should be given as monotherapy. Treatment begins with the application of a small daily dose, which is then slowly increased until an optimal effect is achieved.

The addition of carbamazepine to already conducted antiepileptic therapy should be carried out gradually, at the same time the dosages of the medicines used are not changed or, if necessary, corrected.

For adults, the initial dose is 100-200 mg 1-2 times a day. Then the dose is slowly increased to achieve the optimal therapeutic effect (usually 400 mg 2-3 times a day, maximum - 1.6-2 g per day).

Children from 3 years old - at an initial dose of 20-60 mg per day, gradually increasing by 20-60 mg every other day.

In children older than 3 years - in the initial dose of 100 mg per day, the dose is increased gradually, every week by 100 mg. Supportive doses: 10-20 mg / kg per day (in several doses): for 4-5 years - 200-400 mg (in 1-2 doses), 6-10 years - 400-600 mg (in 2-3 doses ), for 11-15 years - 600-1000 mg (in 2-3 administrations).

With neuralgia of the trigeminal nerve, on the first day, 200-400 mg per day is prescribed, gradually increasing by no more than 200 mg per day until the pain ceases (an average of 400-800 mg per day), and then reduced to the minimum effective dose.

In the pain syndrome of neurogenic origin, the initial dose is 100 mg twice a day on the first day, then increase the dose by no more than 200 mg per day, if necessary, increasing it by 100 mg every 12 hours until the pain decreases. The maintenance dose is 200-1200 mg per day in several doses.

In the treatment of elderly patients and patients with hypersensitivity, the initial dose is 100 mg 2 times a day.

Alcohol abstinence syndrome: the average dose is 200 mg 3 times a day; in severe cases during the first few days the dose can be increased to 400 mg 3 times a day. At the beginning of treatment for severe manifestations of abstinence it is recommended to appoint in combination with sedative-hypnotic drugs (clomethiazole, chlordiazepoxide).

Non-diabetes mellitus: the average dose for adults is 200 mg 2-3 times a day. In children, the dose should be reduced in accordance with the age and body weight of the child.

Diabetic neuropathy, accompanied by pain: the average dose is 200 mg 2-4 times a day.In the prevention of relapses affective and schizoaffective psychoses - 600 mg per day in 3-4 reception.

In acute manic states and affective (bipolar) disorders, daily doses of 400-1600 mg. The average daily dose is 400-600 mg (in 2-3 doses). In acute manic state, the dose is increased rapidly, with maintenance therapy of affective disorders - gradually (to improve tolerability).

Side effect

• dizziness;
• ataxia;
• drowsiness;
• general weakness;
• headache;
• tics;
• nystagmus;
• oculomotor disorders;
• peripheral neuritis;
• paresthesia;
• muscle weakness and paresis;
• hallucinations;
• depression;
• loss of appetite;
• anxiety;
• aggressive behavior;
• excitation;
• disorientation;
• activation of psychosis;
• hives;
• exfoliative dermatitis;
• erythroderma;
• lupus-like syndrome;
• Stevens-Johnson syndrome;
• photosensitivity;
• multiform and erythema nodosum;
• aseptic meningitis with myoclonus;
• anaphylactic reaction;
• angioedema;
• reactions of hypersensitivity from the lungs, characterized by fever, dyspnea, pneumonitis or pneumonia;
• leukopenia, thrombocytopenia, eosinophilia, leukocytosis, lymphadenopathy, agranulocytosis, aplastic anemia;
• nausea, vomiting;
• dry mouth;
• diarrhea or constipation;
• abdominal pain;
• glossitis;
• stomatitis;
• pancreatitis;
• violations of intracardiac conduction;
• decrease or increase in blood pressure;
• bradycardia;
• arrhythmias;
• atrioventricular blockade with syncope;
• collapse;
• aggravation or development of congestive heart failure;
• exacerbation of ischemic heart disease (including the appearance or increased frequency of angina attacks);
• thrombophlebitis;
• thromboembolic syndrome;
• edema;
• increase in body weight;
• increased prolactin levels (may be accompanied by galactorrhea and gynecomastia);
• hypercholesterolemia and hypertriglyceridemia;
• interstitial nephritis;
• kidney failure;
• impaired renal function (albuminuria, hematuria, oliguria, increased urea / azotemia);
• frequent urination;
• retention of urine;
• disorders of sexual function / impotence;
• arthralgia;
• violation of taste;
• cataract;
• conjunctivitis;
• changes in perception of pitch;
• disorders of skin pigmentation;
• purpura;
• acne;
• sweating;
• alopecia.

Contraindications

• hypersensitivity to carbamazepine and chemically similar medicinal products (tricyclic antidepressants) or to any other component of the drug;
• acute intermittent porphyria (including in the anamnesis);
• simultaneous administration of monoamine oxidase inhibitors (hereinafter MAO inhibitors) and within 2 weeks after their cancellation;
• violation of bone marrow hematopoiesis;
• atrioventricular block;
• pregnancy;
• lactation period.

Application in pregnancy and lactation

When pregnancy occurs (when deciding whether to prescribe carbamazepine during pregnancy), it is necessary to carefully compare the expected benefits of therapy and its possible complications, especially in the first 3 months of pregnancy. It is known that children born to mothers with epilepsy are predisposed to violations of intrauterine development, including malformations.

Carbamazepine, like all other antiepileptic drugs, can increase the risk of these disorders. There are isolated reports of cases of congenital diseases and malformations, including non-vertebral arches (spina bifida), hypospadias.Patients should be provided with information on the possibility of increasing the risk of malformations and the ability to undergo antenatal diagnostics.

Antiepileptic drugs increase the deficiency of folic acid, often observed during pregnancy, which can contribute to an increase in the frequency of birth defects in children (before and during pregnancy an additional folic acid supplement is recommended). In order to prevent increased bleeding in newborns, in the last weeks of pregnancy, as well as newborns, vitamin K1 is recommended.

Carbamazepine penetrates into breast milk, it is necessary to compare the benefits and possible undesirable consequences of breastfeeding in conditions of continuing therapy. Mothers taking carbamazepine can breast-feed their children, provided that a child is observed to develop possible adverse reactions (eg, severe drowsiness, allergic skin reactions).

Use in children

The use is possible in children older than 3 years according to the dosing regimen.

special instructions

Before starting treatment, it is necessary to perform a general blood test (including platelet count, reticulocyte count), a general urine test, determine the level of iron, the concentration of electrolytes and urea in the blood serum. Subsequently, these indicators should be monitored during the first month of treatment on a weekly basis, and then on a monthly basis. When appointing patients with increased intraocular pressure, its periodic monitoring is necessary. Non-progressive asymptomatic leukopenia does not require withdrawal, however, treatment should be discontinued if progressive leukopenia or leukopenia occurs, accompanied by clinical symptoms of an infectious disease.

Information about the possible effect of a drug for medical use on the ability to manage vehicles, mechanisms. During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Drug Interactions

Carbamazepine enhances the activity of microsomal liver enzymes and can reduce the effectiveness of drugs metabolized in the liver.Simultaneous administration of carbamazepine with inhibitors of CYP3A4 may lead to an increase in its concentration in the blood plasma. Co-administration with CYP3A4 inducers can lead to an acceleration of the metabolism of carbamazepine and a decrease in its concentration in the blood plasma; on the contrary, their removal can reduce the rate of biotransformation of carbamazepine and lead to an increase in its concentration.

Increase the concentration of carbamazepine in plasma: verapamil, diltiazem, felodipine, dextropropoxyphene, viloxazine, fluoxetine, fluvoxamine, cimetidine, acetazolamide, danazol, desipramine, nicotinamide (in adults, only in high doses); macrolides (erythromycin, josamycin, clarithromycin, troleandomycin); azoles (itraconazole, ketoconazole, fluconazole), terfenadine, loratadine, isoniazid, propoxyphene, grapefruit juice, viral protease inhibitors used in HIV therapy. Felbamate reduces the concentration of carbamazepine in plasma and increases the concentration of carbamazepine-10,11-epoxide, while a simultaneous decrease in serum felbamate concentration is possible. The concentration of carbamazepine is reduced by phenobarbital, phenytoin, primidone, metsuksimid, fensuksimid, theophylline, rifampicin, cisplastin, doxirubicin, possibly: clonazepam,valprromide, valproic acid, oxcarbazepine and herbal preparations containing St. John's wort (Hypericum perforatum). There are reports of the possibility of displacing valproic acid and primidone carbamazepine from plasma protein binding and increasing the concentration of pharmacologically active metabolite (carbamazepine-10,11-epoxide). Isotretinoin changes the bioavailability and / or clearance of carbamazepine and carbamazepine-10,11-epoxide (carbamazepine concentration in the plasma is monitored). Carbamazepine can reduce plasma concentrations (reduce or even completely eliminate effects) and require correction of the doses of the following drugs: clobazam, clonazepam, ethosuximide, primidon, valproic acid, alprazolam, glucocorticosteroids (prednisolone, dexamethasone), cyclosporine, doxycycline, haloperidol, methadone, oral preparations containing estrogens and / or Progesterone (a selection of alternative methods of contraception), theophylline, oral anticoagulants (warfarin, fenprokumona, dicumarol), la otridzhina, topiramate, tricyclic antidepressants (imipramine, amitriptyline, nortriptyline, clomipramine), clozapine, felbamate, tiagabine, oxcarbazepine,protease inhibitors used in HIV therapy (indinavir, ritonavir, saquinovir), calcium channel blockers (digidropiridonov group, e.g., felodipine), itraconazole, levothyroxine, midazolam, olazapina, praziquantel, risperidone, Tramadol ziprasidone. It has been reported that in patients receiving carbamazepine phenytoin plasma levels may either rise or fall, and mephenytoin level - increase (in rare cases). Carbamazepine when combined with Paracetamol increases the risk of its toxic effect on the liver and reduces therapeutic effectiveness (acceleration of the metabolism of paracetamol). The simultaneous appointment of carbamazepine with phenothiazines, pimozide, thioxanthenes, molindone, haloperidol, maprotiline, clozapine and tricyclic antidepressants leads to increased inhibitory action on the central nervous system and weaken the anticonvulsant effect of carbamazepine. Simultaneous administration with diuretics (hydrochlorothiazide, furosemide) can lead to hyponatremia, accompanied by clinical manifestations. Reduces the effects of nondepolarizing muscle relaxants (pancuronium). Reduces the tolerance of ethanol (alcohol).Accelerates the metabolism of indirect anticoagulants, hormonal contraceptives, folic acid; prazikvantela, can enhance the elimination of thyroid hormones. Accelerates the metabolism of funds for general anesthesia (enflurane, halothane, ftorotan) with an increased risk of hepatotoxic effects; enhances the formation of nephrotoxic metabolites of methoxyflurane. Enhances the hepatotoxic effect of isoniazid.

Analogues of the drug Carbamazepine

Structural analogs for the active substance:

• Actinerval;
• Apo Carbamazepine;
• Zagreton;
• Zeptol;
• Carbaleptin retard;
• Carbamazepine Nycomed;
• Carbamazepine Acry;
• Carbamazepine Ferein;
• Carbapine;
• Carbasan retard;
• Mazepine;
• Stasepine;
• Storilate;
• Tegretol;
• Tegretol CR;
• Finlepsin;
• Finlepsin retard;
• Epial.

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