Finlepsin retard 200 mg, 50 tablets, extended release

Pharmacological properties of the drug Finlepsin retard

Pharmacodynamics . Anticonvulsant, derivative of tricyclic iminostilbene. It has a moderate antidepressant and normothymic effect. The therapeutic effect is primarily due to the inhibition of synaptic transmission of excitation, and thereby reducing the spread of convulsive attacks. At higher concentrations, carbamazepine causes a decrease in post-tetanic potentiation. Reduces pain in trigeminal neuralgia. This effect is due to inhibition of synaptic transmission of stimulation in the spinal nucleus of the trigeminal nerve. Pharmacokinetics. After oral administration, carbamazepine is absorbed slowly and almost completely. The half-life is 8.5 hours and has a wide range (approximately 1.72–12 hours). After a single dose, the maximum concentration of carbamazepine in the blood plasma in adults is achieved after 4-16 hours (very rarely - after 35 hours), in children - after approximately 4-6 hours. The concentration of carbamazepine in the blood plasma is not linearly dependent on the dose and at When used in higher doses, the plasma concentration curve has the appearance of a plateau. When using extended-release tablets, a lower concentration of carbamazepine in the blood plasma is achieved than when using regular tablets. Equilibrium concentration is achieved after 2–8 days. There is no close correlation between the dose of carbamazepine and steady-state plasma concentrations. Regarding the therapeutic and toxic concentrations of carbamazepine in the blood plasma, it is indicated that attacks may disappear when its level in the blood plasma is 4–12 μg/ml. Concentrations of the drug in blood plasma exceeding 20 mcg/ml worsen the picture of the disease. The drug, with a concentration of the active substance in the blood plasma of 5–18 mcg/ml, eliminates pain in trigeminal neuralgia. 70–80% of carbamazepine is bound to plasma proteins. The portion of carbamazepine not bound to proteins remains constant at a concentration of 50 μg/ml. 48–53% of the pharmacologically active metabolite carbamazepine-10, 11-epoxide is bound to plasma proteins. The concentration of carbamazepine in the cerebrospinal fluid is 33% of the concentration in the blood plasma. Carbamazepine crosses the placental barrier and is excreted into breast milk. After taking a single dose, carbamazepine is eliminated from the blood plasma with a half-life of 36 hours. With prolonged treatment, the half-life is reduced by 50% due to the induction of microsomal liver enzymes. In healthy people, the total plasma clearance is approximately 19.8 ml/h/kg body weight, in patients with monotherapy - approximately 54.6 ml/h/kg, in patients with combination treatment - approximately 113.3 ml/h/kg . After a single oral dose of carbamazepine, 72% of the dose in the form of metabolites is excreted from the body by the kidneys. The remaining 28% is excreted along with feces, partially unchanged. Only 2–3% of the substance excreted in the urine is unchanged carbamazepine.

Indications for use of the drug Finlepsin retard

• epilepsy: partial seizures with elementary symptoms (Jacksonian seizures); partial seizures with complex symptoms (psychomotor seizures); grand mal epileptic seizures, in particular of a focal nature (nocturnal epilepsy, diffuse epilepsy); mixed forms of epilepsy;
• trigeminal neuralgia;
• Genuine glossopharyngeal neuralgia;
• pain from diabetic neuropathy;
• non-epileptic seizures in patients with multiple sclerosis, such as trigeminal neuralgia, tonic seizures, paroxysmal dysarthria and ataxia, paroxysmal paresthesia and attacks of pain;
• prevention of the development of convulsive attacks during alcohol withdrawal syndrome;
• Prevention of manic-depressive phases when lithium therapy is ineffective, when patients experience rapid phase changes while taking lithium or when lithium use is contraindicated.

Use of the drug Finlepsin retard

Treatment with Finlepsin retard is started carefully, the drug is prescribed in low doses individually for each patient, depending on the type and severity of the disease. The dose is then gradually increased until the most effective maintenance dose is achieved. The optimal dose of the drug for the patient, especially in combination therapy, is determined by its level in the blood plasma. According to accumulated experience, the therapeutic concentration of the drug Finlepsin retard in blood plasma is 4–12 μg/ml. Replacing one antiepileptic drug with Finlepsin retard should be done gradually, reducing the dose of the previously used drug. If possible, the antiepileptic drug is used only for monotherapy. Treatment is carried out under the supervision of a doctor. The generally accepted dose range is 400–1200 mg of Finlepsin retard per day in 1–2 doses. Exceeding the total daily dose of 1200 mg does not make sense. The maximum daily dose should not exceed 1600 mg because higher doses may cause an increase in side effects. In some cases, the dose required for treatment may differ significantly from the recommended initial and maintenance dose (for example, due to accelerated metabolism due to the induction of microsomal liver enzymes or due to drug interactions during combination therapy). Unless otherwise prescribed, follow this indicative regimen for using the drug. Antiepileptic treatment The initial adult dose of 200–400 mg carbamazepine is slowly increased to a maintenance dose of 800–1200 mg carbamazepine. The following dosage regimen is recommended: Adults: initial daily dose - 200-300 mg in the evening, maintenance dose daily - 200-600 mg in the morning, 400-600 mg in the evening. Children aged 6-10 years - initial daily dose - 200 mg in the evening, maintenance dose daily - 200 mg in the morning, 200-400 mg in the evening. Children aged 11-15 years - initial daily dose - 200 mg in the evening, maintenance dose daily - 200-400 mg in the morning, 400-600 mg in the evening. Indication : due to the lack of experience in using the drug in children under 6 years of age, Finlepsin retard delayed release is not prescribed to patients in this age category. The maintenance dose of carbamazepine for children is on average 10–20 mg/kg body weight per day. Trigeminal neuralgia, genuine glossopharyngeal neuralgia The initial dose for adults - 200-400 mg of carbamazepine - is gradually increased until a daily dose of 400-800 mg of carbamazepine is reached, which is taken 1-2 times a day until the pain completely disappears. After this, in some patients, treatment can be continued using the drug at a lower maintenance dose that prevents pain attacks - 400 mg of carbamazepine once a day. For elderly patients, the initial dose of Finlepsin retard is 200 mg of carbamazepine 1 time per day. Pain in diabetic neuropathy The average daily dose is 600 mg of carbamazepine (200 mg in the morning and 400 mg in the evening. In exceptional cases, Finlepsin retard can be prescribed at a dose of 600 mg 2 times a day (corresponding to 1200 mg of carbamazepine). Prevention of the development of convulsive attacks during alcohol withdrawal syndrome The average daily dose is 200 mg in the morning, in the evening 400 mg is prescribed (corresponding to 600 mg of carbamazepine). In severe cases in the first days, the dose can be increased to 600 mg 2 times a day (corresponding to 1200 mg of carbamazepine). Non-epileptic seizures in patients with multiple sclerosis The average daily dose is 200–400 mg 2 times a day (corresponding to 400–800 mg of carbamazepine) .Prevention of manic-depressive states The initial dose, which, as a rule, is also a maintenance dose, is 200–400 mg of carbamazepine per day (take 1 once a day). If necessary, this dose can be increased to 800 mg of carbamazepine 1 time per day. For patients with severe cardiovascular diseases, liver and kidney damage, as well as for the elderly, the drug is prescribed in lower doses. Extended-release tablets have a longitudinal notch and are taken during or after meals with a sufficient amount of liquid (for example, a glass of water). Long-acting tablets can be used after dissolving them in water (in the form of a suspension). The prolonged effect persists even after dissolving the tablet in water. The duration of use depends on the indication and the patient’s individual response to the drug. Treatment for epilepsy takes a long time. The question of transferring the patient to Finlepsin retard, the duration of use and its discontinuation in each particular case is decided by the doctor. In general, the dose of the drug can be reduced or completely stopped treatment no earlier than after 2-3 years of absence of attacks. Therapy is stopped, gradually reducing the dose of the drug over 1–2 years. In this case, in children it is necessary to take into account the increase in body weight. The encephalogram indicators should not deteriorate. In the treatment of neuralgia, the use of the drug Finlepsin retard in a maintenance dose sufficient to eliminate pain for several weeks was effective. By carefully reducing the dose, it is necessary to determine whether spontaneous remission of the symptoms of the disease has occurred. When painful attacks resume, treatment is continued using the previous maintenance dose. The duration of treatment for pain relief in diabetic neuropathy and epileptiform seizures in multiple sclerosis is the same as for neuralgia. Treatment of patients with alcohol withdrawal syndrome with Finlepsin retard is stopped, gradually reducing the dose over 7-10 days. Prevention of manic-depressive phases is long-term. The duration of therapy depends on the case and is determined by the doctor conducting the treatment.

Finlepsin® retard

The drug should be used only under regular medical supervision.

Monotherapy for epilepsy begins with the administration of the drug in low doses, gradually increasing them until the desired therapeutic effect is achieved.

In some cases, treatment with antiepileptic drugs was accompanied by the occurrence of suicide attempts/suicidal intentions. This was also confirmed in a meta-analysis of randomized clinical trials using antiepileptic drugs. Since the mechanism of suicide attempts when using antiepileptic drugs is not known, their occurrence cannot be excluded during treatment with Finlepsin® retard. Patients and staff should be warned to monitor for suicidal thoughts/behavior and to seek immediate medical attention if symptoms occur.

It is advisable to determine the concentration of carbamazepine in plasma in order to select the optimal dose, especially in combination therapy. In some cases, the dose required for treatment may deviate significantly from the recommended initial and maintenance dose, for example, due to accelerated metabolism due to the induction of microsomal liver enzymes or as a result of drug interactions during combination therapy.

The drug Finlepsin® retard should not be combined with sedative-hypnotics. If necessary, it can be combined with other substances used to treat alcohol withdrawal.

When transferring a patient to carbamazepine, the dose of the previously prescribed antiepileptic drug should be gradually reduced until it is completely discontinued. Sudden cessation of carbamazepine may trigger epileptic seizures. If it is necessary to abruptly interrupt treatment, the patient should be transferred to another antiepileptic drug under the cover of the drug indicated in such cases (for example, diazepam IV or rectally, or phenytoin IV).

Several cases of vomiting, diarrhea and/or decreased nutrition, convulsions and/or respiratory depression have been described in newborns whose mothers took carbamazepine concomitantly with other anticonvulsants (these reactions may represent neonatal withdrawal syndrome).

It should be borne in mind that carbamazepine may adversely affect the reliability of oral contraceptives, therefore women of reproductive age during treatment should use alternative methods of birth control (intermenstrual bleeding in women is likely when using oral contraceptives simultaneously).

Before prescribing carbamazepine and during treatment, monitoring of liver function parameters is necessary, especially in patients with a history of liver disease, as well as in the elderly. If existing liver dysfunction worsens or active liver disease develops, the drug should be discontinued immediately. Before starting treatment, it is necessary to conduct a blood picture study (including platelet count, reticulocyte count), iron level in the blood serum, general urinalysis, urea level in the blood, EEG, determination of the concentration of electrolytes in the serum; blood (and periodically during treatment, as hyponatremia may develop). Subsequently, these indicators should be monitored weekly during the first month of treatment and then monthly.

In most cases, a transient or persistent decrease in the number of platelets and/or leukocytes is not a precursor to the onset of aplastic anemia or agranulocytosis. However, before starting treatment, and periodically during treatment, clinical blood tests should be performed, including platelet counts and possibly reticulocyte counts, and serum iron levels should be determined. Non-progressive asymptomatic leukopenia does not require discontinuation, however, treatment should be discontinued if progressive leukopenia or leukopenia accompanied by clinical symptoms of an infectious disease occurs.

Carbamazepine should be discontinued immediately if hypersensitivity reactions or symptoms suggestive of Stevens-Johnson syndrome or Lyell's syndrome occur. Mild skin reactions (isolated macular or maculopapular rash) usually disappear within a few days or weeks, even with continued treatment or after reducing the dose of the drug (the patient should be under medical supervision at this time).

When using the drug, one should take into account the possibility of activation of latent psychoses, and in elderly patients - the possibility of developing disorientation or psychomotor agitation.

Possible disturbances in male fertility and/or disturbances in spermatogenesis (the relationship between these disturbances and the use of carbamazepine has not yet been established).

The patient should be informed about possible early signs of toxic reactions from the hematopoietic system, liver and dermatological reactions and the need to immediately consult a doctor in the event of such undesirable reactions as fever, sore throat, rash, ulceration of the oral mucosa, causeless bruising , hemorrhages in the form of petechiae or purpura.

Before starting treatment, it is recommended to conduct an ophthalmological examination, including examination of the fundus with a slit lamp and, if necessary, measurement of intraocular pressure. When prescribing the drug to patients with increased intraocular pressure, constant monitoring is necessary.

Patients with severe diseases of the cardiovascular system, liver and kidney damage, as well as elderly people are prescribed the drug in lower doses.

Although the relationship between carbamazepine dose, carbamazepine concentration and clinical efficacy or tolerability is very small, regular determination of carbamazepine plasma concentrations is also useful when there is a sharp increase in the frequency of attacks; to check the patient’s regularity of taking the drug; during pregnancy; when treating children or adolescents; if there is a suspicion of impaired absorption of the drug; if toxic reactions are suspected if the patient is taking several medications.

While using the drug, it is recommended to stop drinking alcohol.

Contraindications to the use of the drug Finlepsin retard

• bone marrow damage, suppression of bone marrow function in the patient's medical history;
• AV block;
• known hypersensitivity to carbamazepine, tricyclic antidepressants or other components of the drug;
• acute intermittent porphyria;
• concomitant treatment with an MAO inhibitor;
• concomitant treatment with voriconazole, as it may cause treatment failure;
• children under 6 years of age.

In the following cases, Finlepsin retard should be prescribed only after a thorough study of the potential benefits of using the drug compared to the likely risks:

• any current or past diseases of the hematopoietic system, any reactions from the blood system to other medications in the patient’s history;
• disturbance of sodium metabolism;
• serious functional disorders of the heart, liver and kidneys;
• myotonic dystrophy, since with this disorder there is often a disturbance in cardiac conduction.

Side effects of the drug Finlepsin retard

The side effects that were observed occurred more frequently with combination treatment than with monotherapy. Depending on the dose and mainly at the beginning of treatment, certain side effects may occur. In general, they disappear on their own after 8–14 days or after a temporary dose reduction. From the central nervous system and psyche Confusion, drowsiness, dizziness, fatigue, impaired coordination of movements (cerebellar ataxia) and headache may often occur. Elderly patients may experience confusion and restlessness. In isolated cases, depressive mood, aggressive behavior, slowness of thinking, decreased motivation, as well as perception disorders (hallucinations) and tinnitus are noted. When treated with Finlepsin retard, latent psychoses may become more active. Rarely, involuntary movements such as large-scale tremors, muscle contractions, or nystagmus occur. In addition, in elderly patients with brain damage, involuntary movements in the maxillofacial area may occur in the form of grimacing (maxillofacial dyskinesia), rotational movements (choreoathetosis), neuroleptic malignant syndrome, and polyneuropathy. Isolated cases of speech impairment, false sensations, muscle weakness, neuritis (peripheral neuritis), as well as paralysis of the lower limbs (paresis) and taste disturbances have been reported. On the part of the organ of vision In some cases, inflammation of the mucous membrane of the eye (conjunctivitis) occurs, sometimes developing into visual disturbances (impaired accommodation, double vision, blurred images), increased intraocular pressure. There have been reports of cases of lens opacity. Retinotoxicity was detected in 2 patients after prolonged therapy with carbamazepine. After stopping carbamazepine, the severity of these phenomena decreased significantly. From the organ of hearing: Decreased hearing, increased auditory perception, impaired perception of pitch. From the musculoskeletal system In isolated cases, arthralgia, myalgia, and muscle spasms were noted. These phenomena disappeared after stopping the drug. On the skin There have been reports of cases of allergic reactions from the skin with or without fever, for example, urticaria, pruritus, sometimes large lamellar or scaly inflammation of the skin (exfoliative dermatitis, erythroderma), Lyell's syndrome, photosensitivity, exudative erythema multiforme, erythema nodosum, Stevens syndrome - Johnson), petechial hemorrhages in the skin and disseminated lupus erythematosus). In isolated cases, hair loss (alopecia) and sweating (diaphoresis), changes in skin pigmentation, acne, hirsutism and vasculitis were noted. From the circulatory and lymphatic system When treated with Finlepsin retard, hemogram disorders may occur: leukocytosis, eosinophilia or leukopenia, thrombocytopenia. According to the literature, the most common form of leukopenia occurs benign (transient in approximately 10% of cases, and permanent in 2% of cases). There are isolated cases of blood diseases, sometimes life-threatening, such as agranulocytosis, aplastic anemia along with other forms of anemia (hemolytic, megaloblastic), reticulocytosis, pancytopenia, erythrocyte aplasia, as well as enlargement of the spleen and lymph nodes. As a rule, this occurs in the first 4 months of treatment. From the gastrointestinal tract Sometimes - loss of appetite, dry mouth, nausea and vomiting, rarely diarrhea or constipation. Isolated cases of abdominal pain and inflammation of the mucous membrane of the nasopharynx (stomatitis, gingivitis, glossitis) are known. There are indications in the literature that carbamazepine can sometimes cause pancreatitis. From the liver and gallbladder Sometimes changes in liver function test parameters are noted, in some cases jaundice occurs, in isolated cases - various forms of hepatitis (cholestatic, hepatocellular, granulomatous, mixed). In isolated cases, acute hepatitis with liver failure developed in the first few months against the background of allergic manifestations. Hormonal and water-salt metabolism Individual cases of enlarged mammary glands in men (gynecomastia) and spontaneous leakage of milk from the mammary glands in women (galactorrhea) have been reported. Finlepsin retard can affect indicators of thyroid function (triiodothyronine, thyroxine, thyroid-stimulating hormone and free thyroxine), especially when combined with other antiepileptic drugs. The most common side effect was hyponatremia, sometimes accompanied by fluid retention, weight gain, and decreased plasma osmotic concentration. In very rare cases, this has resulted in water intoxication with vomiting, headache, confusion, drowsiness and other neurological disorders. Individual cases of edema and weight gain have been observed. Finlepsin retard may reduce serum calcium levels. In isolated cases, this leads to softening of the bones (osteomalacia). In extremely rare cases, cholesterol levels may increase, including HDL cholesterol and TG, as well as free cortisol in the blood serum. Carbamazepine may reduce serum folate levels. A decrease in serum vitamin B12 levels and an increase in homocysteine ​​levels have also been reported under the influence of carbamazepine. In two cases, acute intermittent porphyria occurred. On the part of the respiratory system, isolated disorders have been described, which were accompanied by fever, shortness of breath (dyspnea), inflammation and the development of pulmonary fibrosis. From the genitourinary system Rarely, renal dysfunction occurs, which is manifested by proteinuria, hematuria, oliguria, interstitial nephritis, in isolated cases they develop into renal failure. Perhaps these disorders are due to the drug's own antidiuretic effect. Sometimes dysuria, polakiuria and urinary retention occur. In addition, there are known cases of sexual disorders, such as impotence, decreased libido, and impaired spermatogenesis. From the cardiovascular system Very rarely, mainly in elderly people or in patients with impaired heart function, bradycardia, cardiac arrhythmias, congestive heart failure, circulatory collapse, as well as worsening of coronary heart disease may occur. Disturbances in the conduction of excitation in the myocardium (AV blockade) are rarely observed, which is occasionally accompanied by fainting conditions. In addition, in some cases, significant fluctuations in blood pressure are detected. A drop in blood pressure mainly occurs when the drug is used in high doses. Vasculitis, thrombophlebitis and thromboembolism were also observed. Hypersensitivity reactions Rarely, delayed-type hypersensitivity reactions to the drug develop, accompanied by fever, skin rash, swollen lymph nodes, joint pain, leukocytosis, enlarged liver and spleen, changes in liver function tests, with involvement of other organs, such as the lungs, kidneys, pancreas and myocardium. In isolated cases, an acute generalized reaction and aseptic meningitis with manifestations of myoclonus, eosinophilia, anaphylactic reactions and angioedema were observed.

Finlepsin retard, 50 pcs., 200 mg, extended-release tablets

When assessing the frequency of occurrence of various adverse reactions, the following gradations were used: very often - 10% or more, often - 1-10%, sometimes - 0.1-1%, rarely - 0.01-0.1%, very rarely - less 0.01%.

The development of adverse reactions from the central nervous system may be a consequence of a relative overdose of the drug or significant fluctuations in the concentration of carbamazepine in the blood plasma.

From the side of the central nervous system: often - dizziness, ataxia, drowsiness, general weakness, headache, accommodation paresis; sometimes - abnormal involuntary movements (for example, tremor, “fluttering” tremor - asterixis, dystonia, tics); nystagmus; rarely - hallucinations (visual or auditory), depression, loss of appetite, anxiety, aggressive behavior, psychomotor agitation, disorientation, activation of psychosis, orofacial dyskinesia, oculomotor disorders, speech disorders (for example, dysarthria or slurred speech), choreoathetoid disorders, peripheral neuritis, paresthesia, muscle weakness and symptoms of paresis. The role of the drug in the development of neuroleptic malignant syndrome, especially in combination with antipsychotics, remains unclear.

Allergic reactions: often - urticaria; sometimes - erythroderma, multiorgan delayed-type hypersensitivity reactions with fever, skin rashes, vasculitis (including erythema nodosum as a manifestation of cutaneous vasculitis), lymphadenopathy, signs resembling lymphoma, arthralgia, leukopenia, eosinophilia, hepatosplenomegaly and altered liver function tests (these manifestations occur in various combinations). Other organs may also be involved (eg, lung, kidney, pancreas, myocardium, colon), aseptic meningitis with myoclonus and peripheral eosinophilia, anaphylactoid reaction, angioedema, hypersensitivity pneumonitis, or eosinophilic pneumonia. If the above allergic reactions occur, the use of the drug should be discontinued, rare - lupus-like syndrome, skin itching, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), photosensitivity.

From the hematopoietic organs: often - leukopenia, thrombocytopenia, eosinophilia; rarely - leukocytosis, lymphadenopathy, folic acid deficiency, agranulocytosis, aplastic anemia, true erythrocyte aplasia, metal regional anemia, acute intermittent porphyria, reticulocytosis, hemolytic anemia, splenomegaly.

From the digestive system: often - nausea, vomiting, dry mouth, increased activity of gamma-glutamyl transferase (due to the induction of this enzyme in the liver), which usually has no clinical significance, increased activity of alkaline phosphatase; sometimes - increased activity of liver transaminases, diarrhea or constipation, abdominal pain; rarely - glossitis, gingivitis, stomatitis, pancreatitis, cholestatic, parenchymal (hepatocellular) type hepatitis, jaundice, granulomatous hepatitis, liver failure.

From the cardiovascular system: rarely - intracardiac conduction disorders; decrease or increase in blood pressure, bradycardia, arrhythmias, atrioventricular block with fainting, collapse, worsening or development of chronic heart failure, exacerbation of coronary heart disease (including the appearance or increased frequency of angina attacks), thrombophlebitis, thromboembolic syndrome.

From the endocrine system and metabolism: often - edema, fluid retention, weight gain, hyponatremia (decrease in plasma osmolarity due to an effect similar to the action of antidiuretic hormone, which in rare cases leads to dilution hyponatremia, accompanied by lethargy, vomiting, headache, disorientation and neurological disorders); rarely - increased concentration of prolactin (may be accompanied by galactorrhea and gynecomastia); a decrease in the concentration of L-thyroxine and an increase in the concentration of thyroid-stimulating hormone (usually not accompanied by clinical manifestations); disorders of calcium-phosphorus metabolism in bone tissue (decrease in the concentration of Ca2+ and 25-OH-cholecalciferol in the blood plasma): osteomalacia, hypercholesterolemia (including high-density lipoprotein cholesterol), hypertriglyceridemia and enlarged lymph nodes, hirsutism.

From the genitourinary system: rarely - interstitial nephritis, renal failure, impaired renal function (for example, albuminuria, hematuria, oliguria, increased urea/azotemia), frequent urination, urinary retention, decreased potency.

From the musculoskeletal system: rarely - arthralgia, myalgia or convulsions.

From the senses: rarely - taste disturbances, increased intraocular pressure; clouding of the lens, conjunctivitis; hearing impairment, incl. tinnitus, hyperacusis, hypoacusia, changes in the perception of pitch.

Other: skin pigmentation disorders, purpura, acne, sweating, alopecia.

Special instructions for the use of the drug Finlepsin retard

Since Finlepsin retard can provoke new or intensify existing special forms of seizures (so-called absence seizures), it is not recommended for use in patients with such forms of seizures. Finlepsin retard should not be used simultaneously with MAO inhibitors. Therapy with MAO inhibitors is stopped no later than 14 days before starting treatment with Finlepsin retard. For elderly patients, Finlepsin retard is prescribed in lower doses. Due to the possible occurrence of side effects, as well as hypersensitivity reactions to the drug, it is recommended (especially with prolonged use) to periodically monitor the hemogram and check the function of the liver and kidneys. This is done before the start of treatment, then during the 1st month of treatment - once a week, and after that - once a month. After the first 6 months of therapy, this control is carried out 2–4 times a year. In the following cases, careful monitoring of the patient's condition is necessary: ​​fever, infections, skin rash, general weakness, sore throat, ulcers on the oral mucosa, easy appearance of hematomas, increased levels of liver transaminases, decreased leukocytes 3000/mm3 and granulocytes below 1500/mm3, decreased platelets below 125,000/mm3, an increase in the level of iron in the blood serum over 150 mcg%, a decrease in reticulocytes below 0.3% = 20,000/mm. Carbamazepine should be discontinued if the red blood cell count decreases below 4 million/mm3, with petechial or purpuric hemorrhages, hematocrit decreases below 32%, hemoglobin decreases below 11 g%, leukocytes decreases below 2000/mm3, granulocytes below 1000/mm3 and platelets below 80 000 mm3, for symptomatic hematopoietic disorders. You should also regularly monitor the concentration of the drug Finlepsin retard and other antiepileptic drugs in the blood plasma during combination therapy and, if necessary, reduce the daily dose. Termination of therapy with Finlepsin retard in patients with epilepsy and transferring them to other antiepileptic drugs is not carried out suddenly, but by gradually reducing its dose. In patients with glaucoma, intraocular pressure is regularly monitored. It is necessary to take into account that the side effects of the drug Finlepsin retard can be similar to withdrawal symptoms in alcoholism. If, in exceptional cases, for the prevention of manic-depressive phases when only lithium preparations are insufficiently effective, Finlepsin retard is prescribed in combination with them, in order to prevent unwanted interactions, it is necessary to ensure that a certain concentration of carbamazepine in the blood plasma (8 mcg/ml) is not exceeded, the lithium content is maintained in the low therapeutic range (0.3–0.8 mEq/L), treatment with antipsychotics was carried out more than 8 weeks ago, and do not allow it to be carried out simultaneously. If a patient develops symptoms such as fever, sore throat or allergic skin reactions in the form of a skin rash with swollen lymph nodes or flu-like symptoms during treatment with Finlepsin retard, a blood test is necessary. If serious allergic reactions are detected, the use of Finlepsin retard should be stopped immediately. Finlepsin retard should not be combined with sedative-hypnotics. However, according to clinical requirements, if necessary, Finlepsin retard can be combined with other substances used to treat alcohol withdrawal. During therapy, it is necessary to regularly monitor the content of the drug Finlepsin retard in the blood plasma. Due to the development of side effects from the central nervous system and the autonomic nervous system, patients are carefully monitored. During treatment with carbamazepine, patients should avoid exposure to the sun to prevent the risk of photosensitivity. When switching from the immediate release dosage form to Finlepsin retard extended release tablets, ensure that an equivalent serum level of carbamazepine is achieved. Simultaneous administration of carbamazepine with grapefruit juice leads to an increase in the level of carbamazepine in the blood plasma, therefore Finlepsin retard should not be taken with grapefruit juice. Use during pregnancy and lactation The use of the drug during pregnancy in patients with epilepsy requires special attention. If a woman receiving Finlepsin retard has established or is planning a pregnancy, or during pregnancy there is a need to use the drug, the potential benefits of using the drug should be carefully weighed against the potential risk (especially in the first trimester of pregnancy). If possible, Finlepsin retard should be prescribed to women of reproductive age as monotherapy, since the incidence of congenital malformations in children whose mothers received combination therapy with antiepileptic drugs is higher than in children whose mothers received monotherapy. It is recommended to prescribe the drug in the minimum effective doses and monitor the level of carbamazepine in the blood plasma. Patients should be informed of the possible increased risk of developing birth defects and should be given the opportunity for antenatal screening. It is known that folic acid deficiency may develop during pregnancy. Antiepileptic drugs may increase folic acid deficiency. This may lead to an increased incidence of birth defects in children whose mothers receive antiepileptic therapy. Therefore, supplemental use of folic acid before and during pregnancy is recommended. Carbamazepine passes into breast milk. The benefits of breastfeeding against the potential for long-term side effects in infants must be carefully weighed. Women receiving Finlepsin retard can breastfeed, provided that the baby is monitored for the development of possible adverse reactions (for example, excessive drowsiness, allergic skin reactions). Children. Due to the high content of active substance and insufficient experience with the use of extended-release tablets, Finlepsin retard should not be prescribed to children under 6 years of age. The ability to influence the reaction rate when driving vehicles or working with other mechanisms Due to side effects on the central nervous system, in particular dizziness, drowsiness and fatigue that occur at the beginning of treatment, after increasing the dose or when using a combination with other drugs acting on the central nervous system, Finlepsin retard, even when used correctly, can affect the response of patients (regardless of the effect on the underlying disease), significantly impairing the ability to drive vehicles and operate complex machinery. This effect is enhanced when combined with alcohol. While using the drug, you should not drive vehicles or operate other machinery.

Finlepsin retard, 400 mg, extended-release tablets, 50 pcs.

Inside

, during or after meals, with plenty of liquid. For ease of use, the tablet (as well as half or a quarter of it) can be pre-dissolved in water or juice, because the property of prolonged release of the active substance after dissolving the tablet in the liquid is preserved. The range of doses used is 400–1200 mg/day, divided into 1–2 doses per day.

The maximum daily dose should not exceed 1600 mg.

Epilepsy

Where possible, Finlepsin® retard 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 the drug Finlepsin® retard to already ongoing antiepileptic therapy should be carried out gradually, while the doses of the drugs used are not changed or, if necessary, adjusted. If the patient forgot to take the next dose of the drug in a timely manner, the missed dose should be taken as soon as this omission became noticed, and a double dose of the drug should not be taken.

Adults.

The initial dose is 200–400 mg/day, then the dose is gradually increased until the optimal effect is achieved. Maintenance dose: 800–1200 mg/day, divided into 1–2 doses per day.

Children.

The initial dose for children from 6 to 15 years is 200 mg/day, then the dose is gradually increased by 100 mg/day until the optimal effect is achieved. Maintenance doses for children 6–10 years old: 400–600 mg/day (in 2 doses); for children 11–15 years old - 600–1000 mg/day (in 2 doses).

The following dosage regimen is recommended:

The duration of use depends on the indication and the patient's individual response to treatment. The decision to transfer the patient to Finlepsin® retard, the duration of its use and discontinuation of treatment is made by the doctor individually. The possibility of reducing the drug dose or stopping treatment is considered after a 2-3 year period of complete seizure freedom.

Treatment is stopped, gradually reducing the dose of the drug over 1–2 years, under EEG monitoring. In children, when reducing the daily dose of the drug, the increase in body weight with age should be taken into account.

Trigeminal neuralgia, idiopathic glossopharyngeal neuralgia

The initial dose is 200–400 mg/day, divided into 2 doses. The initial dose is increased until pain disappears completely, on average to 400–800 mg/day. After this, in a certain part of patients, treatment can be continued with a lower maintenance dose of 400 mg.

For elderly patients and patients sensitive to carbamazepine, Finlepsin® retard is prescribed at an initial dose of 200 mg 1 time per day.

Pain due to diabetic neuropathy

The average daily dose is 200 mg in the morning and 400 mg in the evening. In exceptional cases, Finlepsin® retard can be prescribed at a dose of 600 mg 2 times a day.

Treatment of alcohol withdrawal in a hospital setting

The average daily dose is 600 mg (200 mg in the morning and 400 mg in the evening). In severe cases, in the first days the dose can be increased to 1200 mg/day, divided into 2 doses.

If necessary, Finlepsin® retard can be combined with other substances used to treat alcohol withdrawal, except sedative-hypnotics.

During treatment, it is necessary to regularly monitor the content of carbamazepine in the blood plasma.

Due to the possible development of side effects from the central and autonomic nervous system, patients are closely monitored in a hospital setting.

Epileptiform seizures in multiple sclerosis

The average daily dose is 200–400 mg 2 times a day.

Treatment and prevention of psychosis

The initial and maintenance doses are usually the same - 200–400 mg/day. If necessary, the dose can be increased to 400 mg 2 times a day.

Interactions of the drug Finlepsin retard

Cytochrome P450 ZA4 (CYP ZA4) is the main enzyme that catalyzes the formation of the active metabolite carbamazepine-10, 11-epoxide. The simultaneous use of CYP3A4 inhibitors may cause an increase in the concentration of carbamazepine in the blood plasma, which in turn can lead to the development of adverse reactions. Concomitant use of CYP3A4 inducers may increase the metabolism of carbamazepine, leading to a potential decrease in carbamazepine serum concentrations and its therapeutic effect. Similarly, discontinuation of the CYP3A4 inducer may decrease the rate of carbamazepine metabolism, resulting in increased plasma levels of carbamazepine. Carbamazepine is a powerful inducer of CYP3A4, and therefore can reduce the concentration of other drugs in the blood plasma, which are predominantly metabolized by inducing their metabolism. Drugs that increase the level of carbamazepine in the blood plasma. Since an increase in the level of carbamazenin in the blood plasma can lead to adverse reactions, the dosage of the drug must be adjusted and/or monitored its level in the blood plasma when used simultaneously with the following drugs:

• macrolide antibiotics: erythromycin, troleandomycin, yosamycin, clarithromycin;
• anti-tuberculosis drugs: isoniazid;
• affecting the cardiovascular system: verapamil, diltiazem; - carbonic anhydrase inhibitors: acetazolamide;
• antidepressants: viloxazine, fluoxetine, nefazodone, desipramine and fluvoxamine, trazodone;
• antifungals: itraconazole, ketoconazole, fluconazole;
• antihistamines: terfenadine, loratadine;
• drugs for the treatment of gastrointestinal diseases: cimetidine;
• antiviral drugs: ritonavir.

Other substances: nicotinamide (in adults and only in high doses). Elevated levels of carbamazepine-10, 11-epoxide in blood plasma can cause dizziness, fatigue, unsteadiness of gait, and diplopia. The dosage of carbamazepine in the event of these symptoms should be adjusted accordingly and/or the level of the drug in the blood plasma should be monitored if Finlepsin retard is taken simultaneously with the following drugs: loxapine, quetiapine, primedone, progabide, valproic acid, valpromide. Effect of the drug Finlepsin retard on plasma levels when used in combination with other drugs Carbamazepine can reduce the levels of certain drugs in the blood plasma and reduce or neutralize their effects. Therefore, their dose must be adjusted according to clinical need. This applies to the following drugs:

• other anticonvulsants: for example, clonazepam, ethosuximide, felbamate, primidom, lamotrigine, oxcarbazepine, tiagabine, topiramate, valproic acid. Under the influence of carbamazepine, the concentration of phenytoin in the blood plasma may increase or decrease. In exceptional cases, this can cause confusion and even coma;
• benzodiazepines: alprazolam, clobazam;
• typical antipsychotics: (haloperidol, bromperidol) and atypical antipsychotics (clozapine, olanzapine, risperidone, quetiapine);
• tricyclic antidepressants: for example imipramine, amitriptyline, nortriptyline, clomipramine;
• tetracyclic drugs: for example doxycycline;
• azole-type antifungals: for example, voriconazole, itraconazole, since antifungals may cause ineffective treatment;
• anthelmintic drugs: praziquantel;
• antiviral drugs: indinavir;
• analgesics, anti-inflammatory drugs: methadone, paracetamol, tramadol;
• antibiotics: doxycycline;
• anxiolytics: midazolam, alprazolam;
• GCS (for example, prednisolone, dexamethasone), cyclosporines, tacrolimus;
• anticoagulants (eg warfarin, phenprocoumon, dicumarol);
• hormonal contraceptives.

In patients taking hormonal contraceptives, the effectiveness of contraception may decrease and intermenstrual bleeding may suddenly begin. Therefore, it is necessary to take oral contraceptives containing more than 50 mg of estrogen, or the use of other, non-hormonal methods of contraception can be recommended. Drugs that reduce the level of carbamazepine in the blood plasma. It may be necessary to adjust the dose of the drug when used in combination with the following drugs: - other anticonvulsants: phenobarbital, phenytoin, primidone, felbamate, methsuximide; - anti-tuberculosis drugs: rifampicin; - bronchodilators or anti-asthma drugs: theophylline, aminophylline; — antitumor drugs: doxorubicin, cisplatin; - other: preparations containing St. John's wort (Hypericum perforatum). Combinations of drugs that require separate consideration The combined use of lithium with carbamazepine may enhance the neurotoxic effect of both drugs. Therefore, it is necessary to carefully monitor serum levels of both substances. Patients should not take concomitant antipsychotics during the 8-week run-in period before prescribing carbamazepine, nor during treatment with carbamazepine. The following symptoms of neurotoxicity should be observed: unsteadiness of gait, ataxia, horizontal nystagmus, increased muscle proprioceptive reflexes, muscle twitching (muscle fasciculation). Information has been published in the literature that in patients taking carbamazepine in combination with antipsychotics, the risk of neuroleptic malignant syndrome and erythema maligna was increased. The combined use of Finlepsin retard with most diuretics (hydrochlorothiazide, furosemide) can cause symptomatic hyponatremia. Under the influence of Finlepsin retard, the effectiveness of muscle relaxants (for example, pancuronium bromide) may decrease. Therefore, patients taking muscle relaxants should be monitored and, if necessary, the dose of these drugs should be increased. In cases where Finlepsin retard is taken in combination with isotretinoin (an anti-acne drug), it is necessary to monitor the level of carbamazepine in the blood plasma. Carbamazepine may increase the excretion of thyroid hormone, resulting in an increased need for this hormone in patients with hypothyroidism. Therefore, at the beginning and at the end of treatment with Finlepsin retard, it is necessary to determine indicators of thyroid function in patients receiving hormone replacement therapy. If necessary, adjust the dose of the thyroid hormone drug. Thyroid function may change, especially when carbamazepine is combined with other anticonvulsants (in particular phenobarbital). Carbamazepine appears to accelerate the metabolism of zotepine.

Finlepsin® retard

When selecting the optimal dose, it is advisable to determine the concentration of carbamazepine in the blood plasma, especially during combination therapy. In some cases, the optimal dose may deviate significantly from the recommended initial and maintenance dose, for example, due to the induction of microsomal liver enzymes or due to interactions during combination therapy.

Finlepsin® retard should not be combined with sedative-hypnotics. If necessary, it can be combined with other substances used to treat alcohol withdrawal. During treatment, it is necessary to regularly monitor the content of carbamazepine in the blood plasma. Due to the development of side effects from the central and autonomic nervous system, patients are closely monitored in a hospital setting. When transferring a patient to carbamazepine, the dose of the previously prescribed antiepileptic drug should be gradually reduced until it is completely discontinued. Sudden cessation of carbamazepine may trigger epileptic seizures. If it is necessary to abruptly interrupt treatment, the patient should be transferred to another antiepileptic drug under the cover of the drug indicated in such cases (for example, diazepam administered intravenously or rectally, or phenytoin administered intravenously).

Several cases of vomiting, diarrhea and/or decreased nutrition, convulsions and/or respiratory depression have been described in newborns whose mothers took carbamazepine concomitantly with other anticonvulsants (these reactions may represent neonatal withdrawal syndrome). Before prescribing carbamazepine and during treatment, liver function testing is necessary, especially in patients with a history of liver disease, as well as in elderly patients. If existing liver dysfunction worsens or active liver disease develops, the drug should be discontinued immediately. Before starting treatment, it is necessary to conduct a study of the blood picture (including counting platelets, reticulocytes), iron level in the blood serum, general urine analysis, urea level in the blood, electroencephalogram, determination of the concentration of electrolytes in the blood serum (and periodically during treatment, because hyponatremia may develop). Subsequently, these indicators should be monitored weekly during the first month of treatment and then monthly.

In most cases, a transient or persistent decrease in the number of platelets and/or leukocytes is not a precursor to the onset of aplastic anemia or agranulocytosis. However, before starting treatment, and periodically during treatment, clinical blood tests should be performed, including platelet counts and possibly reticulocyte counts, and serum iron levels should be determined. Non-progressive asymptomatic leukopenia does not require discontinuation, however, treatment should be discontinued if progressive leukopenia or leukopenia accompanied by clinical symptoms of an infectious disease occurs. Carbamazepine should be discontinued immediately if hypersensitivity reactions or symptoms suggestive of Stevens-Johnson syndrome or Lyell's syndrome occur. Mild skin reactions (isolated macular or maculopapular exanthema) usually disappear within a few days or weeks, even with continued treatment or after reducing the dose of the drug (the patient should be under close medical supervision at this time).

The possibility of activation of latent psychoses should be taken into account, and in elderly patients, the possibility of developing disorientation or psychomotor agitation.

In some cases, treatment with antiepileptic drugs was accompanied by the occurrence of suicide attempts/suicidal intentions. This was also confirmed in a meta-analysis of randomized clinical trials using antiepileptic drugs. Since the mechanism of suicide attempts when using antiepileptic drugs is not known, their occurrence cannot be ruled out when treating patients with Finlepsin® retard. Patients and staff should be warned to monitor for suicidal thoughts/behavior and to seek immediate medical attention if symptoms occur.

Male fertility and/or spermatogenesis disorders are possible, but the relationship between these disorders and carbamazepine has not yet been established.

Intermenstrual bleeding may occur with simultaneous use of oral contraceptives. Carbamazepine may adversely affect the reliability of oral contraceptives, so women of reproductive age should use alternative methods of birth control during treatment.

Carbamazepine should only be used under medical supervision. Patients should be informed of early signs of toxicity, as well as skin and liver symptoms. The patient is informed of the need to immediately consult a doctor in case of adverse reactions such as fever, sore throat, rash, ulceration of the oral mucosa, causeless bruising, hemorrhages in the form of petechiae or purpura.

Before starting treatment, it is recommended to conduct an ophthalmological examination, including fundus examination and measurement of intraocular pressure. If the drug is prescribed to patients with increased intraocular pressure, constant monitoring of this indicator is required.

Patients with severe cardiovascular diseases, liver and kidney damage, as well as elderly people are prescribed lower doses of the drug. Although the relationship between the dose of carbamazepine, its concentration and clinical efficacy or tolerability is very small, regular determination of carbamazepine levels may be useful in the following situations: with a sharp increase in the frequency of attacks; to check whether the patient is taking the drug properly; during pregnancy; when treating children or adolescents; if there is a suspicion of impaired absorption of the drug; if toxic reactions are suspected if the patient is taking several medications.

During treatment with Finlepsin® retard, it is recommended to refrain from drinking alcohol.

Overdose of the drug Finlepsin retard, symptoms and treatment

An overdose of the drug requires urgent medical intervention. The picture of an overdose of the drug Finlepsin retard is characterized by an increase in side effects such as trembling (tremor), convulsive seizures that occur when the brain is excited (tonic-clonic seizures), agitation, as well as impaired breathing and function of the cardiovascular system with often reduced (sometimes also elevated) blood pressure, tachycardia and conduction dysfunction (AV block, ECG changes), cardiac arrest, accompanied by loss of consciousness and respiratory depression. The following may occur: dizziness, ataxia, drowsiness, stupor, nausea, vomiting, agitation, confusion, involuntary movements, dilated pupils, nystagmus, flushing, urinary retention, cyanosis, opisthotonus, abnormal reflexes (weakening or strengthening of reflexes). In isolated cases, leukocytosis, leukopenia, neutropenia, glucosuria or acetonuria were observed. When assessing intoxication, it is necessary to take into account the possibility of multiple intoxication with other pharmacological drugs that could be used for suicidal purposes. Intoxication with carbamazepine occurs mainly when taken in very high doses from 4 to 10 g. The level of the drug in the blood plasma is more than 20 mcg/ml. People have survived after intentionally or accidentally taking high doses of carbamazepine that produced plasma concentrations of 38 mcg/mL. There is no specific antidote for the treatment of acute poisoning with Finlepsin retard. Treatment for overdose with Finlepsin retard is usually carried out depending on the severity of poisoning in a hospital setting. In case of overdose, treatment is symptomatic: if possible, quickly remove the toxic substance from the stomach by inducing vomiting and/or gastric lavage, as well as using activated charcoal and laxatives. For convulsive attacks, anticonvulsants may be used. It is not recommended to prescribe barbiturates due to respiratory depression, especially in children. Due to the high binding of carbamazepine to blood proteins, forced diuresis, as well as hemodialysis or peritoneal dialysis are ineffective