Finlepsinum 400 mg retard (50 tablets)
- $32.50
The instruction for medical use
of medicine
Finlepsinum 200 retard
Finlepsinum 400 retard
the Trade name
Finlepsinum 200 retard
Finlepsinum 400 retard
the International unlicensed
name Carbamazepine Dosage Form
of the Tablet of the prolonged action, 200 mg or 400 mg
Structure One tablet contains
active agent - carbamazepine of 200 mg or 400 mg,
excipients: the kopolimer (type B) dispersive, triacetin eudragit methacrylate 30D-ammonium RS (a glitserol triacetate), talc, the L 30D-55-methacrylic acid-ethyl acrylate a kopolimer eudragit (1:1) dispersive 30%, krospovidon, silicon colloidal anhydrous, magnesium stearate, cellulose microcrystalline.
The description
of the Tablet of white or yellowish color, round, in the form of a clover leaf with slanted edges, with a flat surface, with crosswise lines of a break on both parties and 4 notches on a side surface.
Pharmacotherapeutic group
Antiepileptic drugs. Derivatives of a karboksamid.
Carbamazepine.
The ATX N03AF01 code
the Pharmacological
Pharmacokinetics Absorption properties – slow, but full (meal significantly does not influence the speed and extent of absorption). After single dose of the tablet Cmax it is reached in 32 h. The average Cmax value of not changed active agent after single dose of 400 mg of carbamazepine is about 2.5 mkg/ml. Drug Css in plasma are reached in 1-2 weeks (speed of achievement depends on specific features of metabolism: an autoinduktion of fermental systems of a liver, heteroinduction by others, at the same time applied, HP) and also from a condition of the patient, a dose of drug and duration of treatment. Essential individual differences of Css values in therapeutic range are observed: at most of patients these values fluctuate from 4 to 12 mkg/ml (17-50 µmol/l). Concentration karbamazepin-10.11-epoxide (pharmacological an active metabolite) make about 30% of concentration of carbamazepine. Communication with proteins of plasma children – 55-59%, at adults have 70-80%. The seeming Vd – 0.8-1.9 l/kg. In cerebrospinal fluid and saliva the concentration proportional to amount of active agent, untied with proteins (20-30%) are created. Gets through a placental barrier. Concentration in breast milk makes 25-60% of that in plasma. It is metabolized in a liver, mainly on an epoxy way with formation of the main metabolites – active carbamazepine-10.11-epoxide and an inactive conjugate with glucuronic acid. The main isoenzyme providing carbamazepine biotransformation in carbamazepine - 10.11 epoxide, is P450 (CYPZA4) cytochrome. As a result of these metabolic reactions also the metabolite the 9th hydroxymethyl-10 – karbamoilakridan, having weak pharmacological activity is formed. Carbamazepine can induce own metabolism. T1/2 after intake of a single dose makes 60-100 h (on average about 70 h), at long reception of T1/2 decreases at the expense of an autoinduktion of fermental systems of a liver. After single dose of carbamazepine in 72% of the accepted dose also 28% with a stake are removed with urine, at the same time about 2% of the accepted dose are removed with urine in the form of not changed carbamazepine, about 1% - in the form of a 10.11-epoxy metabolite.
The data demonstrating that the pharmacokinetics of carbamazepine changes at patients of advanced age no.
The pharmacodynamics
the Antiepileptic means (derivative dibenzazepine) rendering also antidepressive, antipsychotic and antidiuretic action possesses analgeziruyushchy action at patients with neuralgia. The mechanism of action is connected with blockade of potentsialzavisimy natrium channels that leads to stabilization of a membrane of the overexcited neurons, inhibition of emergence of serial categories of neurons and decrease in synoptic carrying out impulses. Prevents repeated formation of Na+-dependent action potentials in the depolarized neurons. Reduces release of exciting neuromediator amino acid – a glutamate, raises a reduced convulsive threshold of central nervous system and, thus, reduces risk of development of an epileptic attack. Increases conductivity of K+, modulates potentsialzavisimy Sa + - channels that can make a contribution to anticonvulsant effect of drug. It is effective at the focal (partial) epileptic attacks (simple and complex) which are followed or not followed by secondary generalization, at generalized toniko-clonic epileptic attacks and also at a combination of the specified types of attacks (it is usually inefficient at small attacks – petit mal, absentias epileptica and myoclonic attacks). At patients with epilepsy (in particular at children and teenagers) positive influence on symptoms of uneasiness and depressions and also decrease in irritability and aggression is noted. Influence on cognitive function and psychomotor indicators depends on a dose. The beginning of anticonvulsant effect varies from several hours to several days (sometimes up to 1 month owing to a metabolism autoinduktion).
In an essential and secondary epileptiform neuralgia carbamazepine in most cases prevents emergence of painful attacks. Easing of pains in an epileptiform neuralgia is noted in 8 - 72 hours. At a syndrome of alcoholic abstinency raises a threshold of convulsive readiness which in this state is usually reduced, and reduces expressiveness of clinical manifestations of a syndrome (hyperexcitability, a tremor, disturbance of gait). Antipsychotic (anti-maniacal) action develops in 7-10 days, can be caused by oppression of metabolism of a dopamine and noradrenaline. The prolonged dosage form provides maintenance of more stable concentration of carbamazepine in blood at reception 1-2 times a day.
Indications
- epilepsy: partial attacks, both about idle time, and with difficult
symptomatology, big convulsive attacks, generally focal genesis (big attacks during sleep, diffusion big attacks), the mixed epilepsy forms
- an epileptiform neuralgia
- glossofaringealny neuralgia
- pains in diabetic neuropathy
- epileptiform spasms in multiple sclerosis, for example
epileptiform neuralgias, tonic spasms, a paroxysmal dysarthtia and
an ataxy, paroxysmal paresthesias and attacks of pain - prevention of convulsive attacks in an alcoholic abstinence
syndrome
- prevention of psychoses at manic-depressive states, hypochondriac depressions
the Route of administration and doses
Finlepsinum retard is appointed inside, individually, taking into account indications and a condition of the patient, in time or after a meal, washing down with enough water. It is possible to take a pill of the prolonged action after preliminary dissolution them in water as the property of the prolonged release of active ingredient after dissolution of a tablet in liquid remains.
In each separate case, treatment by Finlepsinum retard has to begin individually, depending on type and degree of gravity of a clinical picture, and further, the dose needs to be raised gradually for achievement of the most effective maintenance dose.
The daily dose usually is ranging from 400 up to 1200 mg which is distributed on 1-2 receptions a day. As a rule, the general daily dose should not exceed 1600 mg of carbamazepine.
A drug dose, optimum for the patient, especially at the combined treatment, define on the basis of carbamazepine level in blood plasma.
Experience shows that the therapeutic level of carbamazepine is 4-12 µг/мл.
In some cases the necessary dose can significantly differ from the recommended initial and maintenance dose (perhaps, because of the strengthened metabolism caused by enzyme induction or interaction with other drugs at the combined treatment).
Epilepsy
At treatment of epilepsy, Finlepsinum retard preferably has to be used in the form of monotherapy. Treatment has to take place under observation of the experienced expert. Upon transition to Finlepsinum retard the dose of earlier used antiepileptic drug has to decrease gradually. If the patient forgot to accept in due time the next dose of drug, it is necessary to accept the passed dose at once as soon as this omission became noticed, at the same time it is impossible to accept a double dose of drug.
Adults: the dosage has to be individually chosen for each patient. For definition of an optimum dose the monitoring of concentration of carbamazepine in plasma can be useful.
The initial recommended dose – 200-400 mg a day, then gradually raise a dose to achievement of optimum effect. A maintenance dose – 800-1200 mg a day which distributes on 1-2 receptions a day.
Children
the Initial dose for children from 6 to 15 years – 200 mg a day, then gradually increase a dose by 100 mg a day before achievement of optimum effect. For children the average maintenance dose makes 10-20 mg/kg of body weight/days. A maintenance dose for children of 6-10 years – 400-600 mg a day (in 2 receptions), for children of 11-15 years – 600-1000 mg a day (in 2 receptions). The following scheme of dosing is recommended:
An initial dose
the Maintenance dose
Adults
on 200-300 mg in the evening
on 200-600 mg in the morning
on 400-600 mg in the evening
Children from 6 to 10 years
on 200 mg in the evening
on 200 mg in the morning
on 200-400 mg in the evening
Children from 11 to 15 years
on 200 mg in the evening
on 200-400 mg in the morning
on 400-600 mg in the evening
In an epileptiform neuralgia and glossofaringealny neuralgia drug appoint 200-400 mg/days which is distributed on 2 receptions in an initial dose. The initial dose is raised to total disappearance of pains up to 400-800 mg/days which is accepted by 1-2 times a day. After that treatment can be continued using lower maintenance dose making 400 mg/days, distributed on 2 receptions. The patient of advanced age and sick, sensitive to carbamazepine, Finlepsinum retard is appointed in the initial dose making 200 mg of 1 times a day.
At a pain syndrome in diabetic neuropathy the average daily dose makes 200 mg in the morning and 400 mg in the evening. In exceptional cases it is possible to appoint up to 1.2 g/days (on 600 mg 2 times a day).
In epileptiform spasms in multiple sclerosis the average daily dose makes 400-800 mg, distributed on 2 receptions.
Prevention of development of convulsive attacks in an alcoholic abstinence syndrome (in the conditions of a hospital)
the Average daily dose makes 600 mg (200 mg in the morning, 400 mg in the evening).
In hard cases in the first days it is possible to raise a dose to 600 mg 2 times a day. Finlepsinum retard should not be combined with sedative and hypnotic means. If necessary Finlepsinum retard can be combined with other substances applied to treatment of alcoholic abstinency. During treatment it is regularly necessary to control carbamazepine content in blood plasma. Due to the development of side effects from central and the autonomic nervous system for the patient establish careful observation in the conditions of a hospital.
For prevention of psychoses drug appoint 200-400 mg/days in a dose. If necessary this dose can be raised to 800 mg/days which is distributed on 2 receptions. Duration of treatment changes depending on a case and is defined by the attending physician.
Antiepileptic treatment always is long-term. At treatment of epilepsy, such questions as stabilization and duration of treatment by Finlepsinum retard have to be solved individually experienced expert. The decision on reduction of a dose and the termination of administration of drug should not be accepted before at the patient attacks within two or three years stop.
For the termination of treatment it is necessary to reduce gradually a dose within a year or two years under control of EEG. At children at decrease in a daily dose of drug it is necessary to consider increase in body weight with age.
At treatment of neuralgia the continuation of treatment within several weeks with reception of a maintenance dose, for belief in absence of pain is enough. Carefully reducing a dose, it is necessary to find out whether there occurred spontaneous regression of symptoms of a disease. When resuming attacks of pain, treatment continues to be carried out using the previous maintenance dose.
Duration of treatment of pain in diabetic neuropathy and epileptiform spasms in multiple sclerosis same, as well as in neuralgia.
Treatment of patients with an alcoholic abstinence syndrome the drug Finlepsinum retard is stopped, gradually reducing a dose for 7-10 days.
Prevention of manic-depressive phases long.
Duration of therapy depends on a case and is defined by the attending physician.
Side effects
from the central nervous system:
Often - dizziness, an ataxy, drowsiness, the general weakness, a headache, paresis, accommodations,
Sometimes - abnormal involuntary movements (for example, a tremor," flitting" a tremor – asterixis, dystonia, tics), a nystagmus,
is rare - hallucinations (visual or acoustical), a depression, a loss of appetite, concern, agressive behavior, psychomotor excitement, a disorientation, activation of psychosis, orofatsialny dyskinesia, oculomotor disturbances, disturbances of the speech (for example, a dysarthtia or the muffled speech), horeatetoidny disorders, peripheral neuritis, paresthesias, muscle weakness and symptoms of paresis. A carbamazepine role as the drug causing or contributing to the development of a malignant antipsychotic syndrome, especially when it is appointed together with neuroleptics, remains obscure.
Allergic reactions:
Often - a small tortoiseshell,
Sometimes - an erythrosis, multiorgan delayed-type hypersensitivity reactions with fever, skin rashes, a vasculitis (including a knotty erythema as manifestation of a skin vasculitis), the limfoadenopatiya, signs reminding a lymphoma, arthralgias, a leukopenia, an eosinophilia, a gepatosplenomegaliya and changed by indicators of function of a liver (the specified manifestations meet in various combinations). Also other bodies can be involved (for example, lungs, kidneys, a pancreas, a myocardium, a large intestine), anaphylactoid reaction, a Quincke's disease, an allergic pneumonitis or eosinophilic pneumonia are possible aseptic meningitis with a myoclonus and a peripheral eosinophilia. At emergence of the allergic reactions stated above the use of drug has to be stopped.
Seldom - a volchanopodobny syndrome, an itching, skins, a mnogoformny exudative erythema (including Stephens-Johnson's syndrome), a toxic epidermal necrolysis (Lyell's disease), photosensitivity.
From bodies of a hemopoiesis:
Often - a leukopenia, thrombocytopenia, an eosinophilia,
it is rare - a leukocytosis, a limfoadenopatiya, deficiency of folic acid, an agranulocytosis, aplastic anemia, a true erythrocyte aplasia, megaloblastny anemia, the sharp "alternating" porphyria, a reticulocytosis, hemolytic anemia, a splenomegaly.
From digestive system:
Often - nausea, vomiting, dryness in a mouth increase in activity of a gammaglutamiltransferaza (owing to induction of this enzyme in a liver), increase in activity of alkaline phosphatase.
Sometimes - increase in activity "hepatic" transminaz, diarrhea or a constipation, abdominal pains.
Seldom - a glossitis, an ulitis, stomatitis, pancreatitis, hepatitis of cholestatic, parenchymatous (hepatocellular) type, jaundice, granulematozny hepatitis, a liver failure.
From warmly vascular system:
Seldom - disturbances of intracardial conductivity, decrease or increase in arterial blood pressure, bradycardia, arrhythmias, atrioventricular block with faints, collapse, aggravation or development of chronic heart failure, exacerbation of coronary heart disease (including emergence or increase of attacks of stenocardia), thrombophlebitis, a thromboembolic syndrome.
From an endocrine system and a metabolism:
Often - hypostases, a liquid delay, increase in body weight, a hyponatremia (decrease in osmolarity of plasma owing to the effect similar to effect of antidiuretic hormone that in rare instances leads to the hyponatremia of cultivation which is followed by a lethargy, vomiting, a headache, a disorientation and neurologic disturbances),
it is rare - increase in concentration of prolactin (can be followed by a galactorrhoea and a gynecomastia), decrease in concentration of L-thyroxine and increase in concentration of thyroid stimulating hormone (usually is not followed by clinical manifestations), disturbances of kalitsiyevofosforny exchange in a bone tissue (decrease in concentration of Ca2 + and 25-IT-cholecalciferol in blood plasma), osteomalacy, a hypercholesterolemia (including cholesterol of lipoproteins of high density), a gipertriglitseridemiya and a hyperadenosis, a hirsutism.
From an urinogenital system: Seldom - interstitial nephrite, a renal failure, a renal failure (for example, an albuminuria, a hamaturia, an oliguria, increase an urea/azotemia), the speeded-up urination, an ischuria, decrease in potency.
From the musculoskeletal system:
Seldom - an arthralgia, myalgia or spasms
from sense bodys: Seldom - disturbance of flavoring feelings, increase in intraocular pressure, a cataract, conjunctivitis, hearing disorder, including sonitus, a hyperacusia, a gipoakuziya, changes of perception of height of a sound.
Other: disturbances of xanthopathy, purple, acne, perspiration, alopecia.
Contraindications
- a combination with inhibitors of a monoaminooxidase (MAO), intake
of MAO inhibitors it is necessary to stop a minimum in 2 weeks prior to prescribing
of carbamazepine
- a concomitant use of drugs of lithium
- a concomitant use of a vorikonazol
- disturbance of a marrowy hemopoiesis (anemia, a leukopenia)
- disturbances of conductivity (atrioventricular block)
- hypersensitivity to acting and
to excipients, tricyclic antidepressants
- the sharp alternating porphyria (including in the anamnesis)
- absentias epileptica
- heavy dysfunctions of heart, liver and kidneys
- sodium exchange disturbance
- children's age up to 6 years
With care:
- dekompensirovanny chronic heart failure, a cultivation hyponatremia (syndrome of hypersecretion of ADG, a hypopituitarism, a hypothyroidism, insufficiency of bark of adrenal glands), insufficiency of a funtion of a liver and kidneys, patients of advanced age, active alcoholism (oppression of central nervous system amplifies, carbamazepine metabolism amplifies), oppression of a marrowy hemopoiesis against the background of drug intake (in the anamnesis), a prostate hyperplasia, increase in intraocular pressure, a combination with sedative sleeping medicines.
Co-administration of carbamazepine with CYP inhibitors 3A4 can lead medicinal interactions to increase in its concentration in blood plasma and to development of side reactions. Combined use of inductors CYP 3A4 can lead to carbamazepine metabolism acceleration, decrease in its concentration in blood plasma and to reduction of therapeutic effect, on the contrary, their cancellation can reduce the speed of biotransformation of carbamazepine and lead to increase in its concentration.
Raise a carbamazepine kontsetration in plasma verapamil, diltiazem, felodipin, dextropropoxyphene, viloksazin, fluoxetine, fluvoksamin, Cimetidinum, acetazoleamide, danazol, desipramine, niacinamide (at adults, only in high doses), macroleads (erythromycin, dzhozamitsin, klaritromitsin, troleandomitsin), azoles (itrakonazol, ketokonazol, flukonazol), terfenadin, loratadin, the isoniazid, the propoxyhair dryer, grapefruit juice, inhibitors of virus protease used at therapy of HIV infection (for example, ritonavir) – is required correction of the mode of dosing or monitoring of concentration of carbamazepine in plasma.
Felmabat reduces concentration of carbamazepine in plasma and increases concentration of carbamazepine – 10.11 – epoxide, at the same time perhaps simultaneous decrease in concentration in felbamat serum.
Concentration of carbamazepine is reduced by phenobarbital, Phenytoinum, Primidonum, metsuksimid, fensuksimid, theophylline, rifampicin, Cisplatinum, doxorubicine, it is possible: clonazepam, valpromid, valproic acid, okskarbazepin and the vegetable drugs containing a St. John's wort made a hole (Hypericum perforatum). There is a possibility of replacement by valproic acid and Primidonum of carbamazepine from communication with proteins of plasma and increase in concentration pharmacological of an active metabolite (carbamazepine-10.11-epoxide). At the combined use of Finlepsinum with valproic acid in exceptional cases there can come the coma and confusion of consciousness.
Izotretinoin changes bioavailability and/or clearance of carbamazepine and carbamazepine-10.11-epoxide (monitoring of a kontsetration of carbamazepine in plasma is necessary). Carbamazepine can reduce concentration in plasma (to reduce or even completely to level effects) and correction of doses of the following drugs can be required: a klobazama, clonazepam, digoxin, Ethosuximidum, Primidonum, valproic acid, an alprazolam, glucocorticosteroids (Prednisolonum, dexamethasone), cyclosporine, tetracyclines (doxycycline), a haloperidol, methadone, the oral drugs containing estrogen and/or progesterone (selection of alternative methods of contraception), theophylline, oral anticoagulants (warfarin, a fenprokumon, a dikumarol), a lamotridzhina, the topiramat, tricyclic antidepressants (Imipraminum, amitriptyline, a nortriptilin, a klomipramin), clozapine, the felbamat, a tiagabin, an okskarbazepin, inhibitors of the proteases applied at therapy of HIV infection (an indinavir, a ritonavir, a sakvinovir), blockers of calcium channels (group of digidropiridon, for example felodipin is necessary), an itrakonazola, left thyroxine, midazolam, olanzapine, a prazikvantel, a risperidon, a tramadol, a tsiprazidon. There is a possibility of increase or decrease in level of Phenytoinum in blood plasma against the background of carbamazepine and increase in level of Mephenytoinum. At simultaneous use of carbamazepine and drugs of lithium, neurotoxic influences of both active agents can amplify.
Tetracyclines can weaken therapeutic effect of carbamazepine. At combined use with paracetamol the risk of its toxic influence on a liver increases and the therapeutic effectiveness (paracetamol metabolism acceleration) decreases.
Co-administration of carbamazepine with fenotiaziny, Pimozidum, thioxanthenes, molindony, a haloperidol, Maprotilinum, clozapine and tricyclic antidepressants leads to strengthening of the oppressing action on the central nervous system and to easing of anticonvulsant effect of carbamazepine. Monoamine oxidase inhibitors increase risk of developing hyperpyrexial crises, hypertensive crises, spasms, death (before prescribing of carbamazepine monoamine oxidase inhibitors have to be cancelled, at least, in 2 weeks or if the clinical situation, even for bigger term allows).
Co-administration with diuretics (hydrochlorothiazide, furosemide) can lead to the hyponatremia which is followed by clinical manifestations. Weakens effects of not depolarizing muscle relaxants (pankuroniya). In case of use of such combination there can be a need of increase in a dose of muscle relaxants, at the same time careful monitoring of a condition of the patient in connection with a possibility of faster cancellation of muscle relaxants is necessary. Carbamazepine reduces tolerance of ethanol. Myelotoxic medicines strengthen manifestations of a gematotoksichnost of drug.
Accelerates metabolism of indirect anticoagulants, hormonal contraceptive drugs, folic acid, prazikvantet, can strengthen elimination of hormones of a thyroid gland.
Accelerates metabolism of anesthetics (an enfluran, a halothane, Ftorotanum) and increases risk of development of hepatotoxic effects, strengthens formation of nefrotoksichny metabolites of a metoksifluran. Strengthens hepatotoxic action of an isoniazid.
The special
indications Monoterapiyu of epilepsy begin with purpose of a low initial dose, gradually raising it to achievement of desirable therapeutic effect.
At selection of an optimum dose it is reasonable to define concentration of carbamazepine in blood plasma, in particular at combination therapy.
In some cases the optimum dose can deviate considerably the recommended initial and maintenance dose, for example, in connection with induction of microsomal enzymes of a liver or because of interactions at combination therapy.
Finlepsinum retard should not be combined with sedative and hypnotic means. In need of it it is possible to combine with other substances applied to treatment of alcoholic abstinency. During treatment it is regularly necessary to control carbamazepine content in blood plasma. Due to the development of side effects from central and the autonomic nervous system for patients establish careful observation in the conditions of a hospital. At conversion of the patient to carbamazepine it is necessary to reduce gradually a dose of earlier appointed antiepileptic means up to its full cancellation. The sudden termination of intake of carbamazepine can provoke epileptic attacks. If it is necessary to interrupt sharply treatment, it is necessary to transfer the patient to other antiepileptic means under cover of the drug shown in such cases (for example, the diazepam entered intravenously or rektalno or Phenytoinum entered intravenously).
It is described several cases of vomiting, diarrhea and/or subnutrition, a spasm and/or respiratory depressions at newborns whose mothers accepted carbamazepine along with other anticonvulsant drugs (perhaps, these reactions represent manifestations at newborns of a withdrawal). Before prescribing of carbamazepine and in the course of treatment the research of function of a liver, especially at patients in whose anamnesis there are data on liver diseases and also for patients of advanced age is necessary. In case of strengthening of already being available abnormal liver functions or at appearance of an active disease of a liver, drug should be cancelled immediately. Before an initiation of treatment it is necessary to conduct blood picture researches (including calculation of thrombocytes, reticulocytes), iron level in serum of blood, the general analysis of urine, urea level in blood, the electroencephalogram, definition of concentration of electrolytes in blood serum (and periodically during treatment since development of a hyponatremia is possible). Subsequently these indicators should be controlled within the first month of treatment weekly, and then monthly.
In most cases passing or permanent decrease in number of thrombocytes and/or leukocytes are not harbingers of the beginning of aplastic anemia or agranulocytosis. Nevertheless, before an initiation of treatment and also periodically in the course of treatment it is necessary to carry out complete blood count tests, including calculation of number of thrombocytes and, perhaps, reticulocytes and also to determine iron level in blood serum. Not progressing symptomless leukopenia does not demand cancellation, however, treatment should be stopped at emergence of the progressing leukopenia or the leukopenia which is followed by clinical symptoms of an infectious disease. Carbamazepine has to be immediately cancelled at the emergence of reactions of hypersensitivity or symptoms demonstrating development of a syndrome of Stephens-Johnson or a Lyell's disease. Mild skin reactions (the isolated makulezny or makulopapulezny dieback) usually take place within several days or weeks even at continuation of treatment or after a drug dose decline (the patient has to be under fixed observation of the doctor at this time).
It is necessary to take into account a possibility of activation latentno of the proceeding psychoses, and at advanced age – a possibility of development of a disorientation or psychomotor excitement. Disturbances of male fertility and/or disturbance of a spermatogenesis are possible, however the interrelation of these disturbances with intake of carbamazepine is not established yet. Appearance of intermenstrual bleedings at simultaneous use of oral contraceptives is possible. Carbamazepine can negatively affect reliability of oral contraceptive drugs therefore women of reproductive age during treatment should apply alternative methods of protection from pregnancy. Carbamazepine has to be applied only under medical observation.
It is necessary to inform patients information on precursory symptoms of toxicity and also on symptoms from integuments and a liver. The patient is informed on need to see immediately a doctor in case of such undesirable reactions as fever, sore throat, rash, an ulceration of a mucous oral cavity, causeless developing of bruises, hemorrhages in the form of petechias or a purpura.
Before an initiation of treatment it is recommended to perform ophthalmologic examination, including a research of an eyeground and measurement of intraocular pressure. In case of prescribing of drug the patients with increase in intraocular pressure need constant control of this indicator.
The patient with a serious cardiovascular illness, damages of a liver and kidneys and also to elderly people appoint lower doses of drug. Though the interrelation between a carbamazepine dose, its concentration and clinical performance or shipping is very insignificant, nevertheless, regular determination of level of carbamazepine can be useful in the following situations: at sharp increase in frequency of attacks to check whether the patient takes the drug properly, during pregnancy, at treatment of children or teenagers, at suspicion for drug absorption disturbances, at suspicion on development of toxic reactions if the patient accepts several medicines.
During treatment Finlepsinum retardy is recommended to refrain from alcohol intake.
Carbamazepine it is necessary to appoint pregnancy and the period of a lactation during pregnancy only after careful weighing of benefits and risks. Women of childbearing age need to explain about need of planning and control of pregnancy. Whenever possible, women of childbearing age should appoint carbamazepine as monotherapy as at combination therapy with other anti-epileptic means the risk of congenital defects increases.
In case of approach of pregnancy during treatment by carbamazepine or emergence of need for treatment by carbamazepine during pregnancy, the attending physician has to weigh carefully potential advantage of use of drug in comparison with possible to risks for a fruit, especially, in the first trimester of pregnancy. It is necessary to appoint a minimal effective dose and to carry out monitoring of concentration of drug in blood plasma. It is impossible to stop treatment at all, without having consulted with the doctor as epileptic seizures can threaten health, both mother, and the child.
As well as in a case with other antikonvulsant, it was reported about razlichn
to Develop
of medicine
Finlepsinum 200 retard
Finlepsinum 400 retard
the Trade name
Finlepsinum 200 retard
Finlepsinum 400 retard
the International unlicensed
name Carbamazepine Dosage Form
of the Tablet of the prolonged action, 200 mg or 400 mg
Structure One tablet contains
active agent - carbamazepine of 200 mg or 400 mg,
excipients: the kopolimer (type B) dispersive, triacetin eudragit methacrylate 30D-ammonium RS (a glitserol triacetate), talc, the L 30D-55-methacrylic acid-ethyl acrylate a kopolimer eudragit (1:1) dispersive 30%, krospovidon, silicon colloidal anhydrous, magnesium stearate, cellulose microcrystalline.
The description
of the Tablet of white or yellowish color, round, in the form of a clover leaf with slanted edges, with a flat surface, with crosswise lines of a break on both parties and 4 notches on a side surface.
Pharmacotherapeutic group
Antiepileptic drugs. Derivatives of a karboksamid.
Carbamazepine.
The ATX N03AF01 code
the Pharmacological
Pharmacokinetics Absorption properties – slow, but full (meal significantly does not influence the speed and extent of absorption). After single dose of the tablet Cmax it is reached in 32 h. The average Cmax value of not changed active agent after single dose of 400 mg of carbamazepine is about 2.5 mkg/ml. Drug Css in plasma are reached in 1-2 weeks (speed of achievement depends on specific features of metabolism: an autoinduktion of fermental systems of a liver, heteroinduction by others, at the same time applied, HP) and also from a condition of the patient, a dose of drug and duration of treatment. Essential individual differences of Css values in therapeutic range are observed: at most of patients these values fluctuate from 4 to 12 mkg/ml (17-50 µmol/l). Concentration karbamazepin-10.11-epoxide (pharmacological an active metabolite) make about 30% of concentration of carbamazepine. Communication with proteins of plasma children – 55-59%, at adults have 70-80%. The seeming Vd – 0.8-1.9 l/kg. In cerebrospinal fluid and saliva the concentration proportional to amount of active agent, untied with proteins (20-30%) are created. Gets through a placental barrier. Concentration in breast milk makes 25-60% of that in plasma. It is metabolized in a liver, mainly on an epoxy way with formation of the main metabolites – active carbamazepine-10.11-epoxide and an inactive conjugate with glucuronic acid. The main isoenzyme providing carbamazepine biotransformation in carbamazepine - 10.11 epoxide, is P450 (CYPZA4) cytochrome. As a result of these metabolic reactions also the metabolite the 9th hydroxymethyl-10 – karbamoilakridan, having weak pharmacological activity is formed. Carbamazepine can induce own metabolism. T1/2 after intake of a single dose makes 60-100 h (on average about 70 h), at long reception of T1/2 decreases at the expense of an autoinduktion of fermental systems of a liver. After single dose of carbamazepine in 72% of the accepted dose also 28% with a stake are removed with urine, at the same time about 2% of the accepted dose are removed with urine in the form of not changed carbamazepine, about 1% - in the form of a 10.11-epoxy metabolite.
The data demonstrating that the pharmacokinetics of carbamazepine changes at patients of advanced age no.
The pharmacodynamics
the Antiepileptic means (derivative dibenzazepine) rendering also antidepressive, antipsychotic and antidiuretic action possesses analgeziruyushchy action at patients with neuralgia. The mechanism of action is connected with blockade of potentsialzavisimy natrium channels that leads to stabilization of a membrane of the overexcited neurons, inhibition of emergence of serial categories of neurons and decrease in synoptic carrying out impulses. Prevents repeated formation of Na+-dependent action potentials in the depolarized neurons. Reduces release of exciting neuromediator amino acid – a glutamate, raises a reduced convulsive threshold of central nervous system and, thus, reduces risk of development of an epileptic attack. Increases conductivity of K+, modulates potentsialzavisimy Sa + - channels that can make a contribution to anticonvulsant effect of drug. It is effective at the focal (partial) epileptic attacks (simple and complex) which are followed or not followed by secondary generalization, at generalized toniko-clonic epileptic attacks and also at a combination of the specified types of attacks (it is usually inefficient at small attacks – petit mal, absentias epileptica and myoclonic attacks). At patients with epilepsy (in particular at children and teenagers) positive influence on symptoms of uneasiness and depressions and also decrease in irritability and aggression is noted. Influence on cognitive function and psychomotor indicators depends on a dose. The beginning of anticonvulsant effect varies from several hours to several days (sometimes up to 1 month owing to a metabolism autoinduktion).
In an essential and secondary epileptiform neuralgia carbamazepine in most cases prevents emergence of painful attacks. Easing of pains in an epileptiform neuralgia is noted in 8 - 72 hours. At a syndrome of alcoholic abstinency raises a threshold of convulsive readiness which in this state is usually reduced, and reduces expressiveness of clinical manifestations of a syndrome (hyperexcitability, a tremor, disturbance of gait). Antipsychotic (anti-maniacal) action develops in 7-10 days, can be caused by oppression of metabolism of a dopamine and noradrenaline. The prolonged dosage form provides maintenance of more stable concentration of carbamazepine in blood at reception 1-2 times a day.
Indications
- epilepsy: partial attacks, both about idle time, and with difficult
symptomatology, big convulsive attacks, generally focal genesis (big attacks during sleep, diffusion big attacks), the mixed epilepsy forms
- an epileptiform neuralgia
- glossofaringealny neuralgia
- pains in diabetic neuropathy
- epileptiform spasms in multiple sclerosis, for example
epileptiform neuralgias, tonic spasms, a paroxysmal dysarthtia and
an ataxy, paroxysmal paresthesias and attacks of pain - prevention of convulsive attacks in an alcoholic abstinence
syndrome
- prevention of psychoses at manic-depressive states, hypochondriac depressions
the Route of administration and doses
Finlepsinum retard is appointed inside, individually, taking into account indications and a condition of the patient, in time or after a meal, washing down with enough water. It is possible to take a pill of the prolonged action after preliminary dissolution them in water as the property of the prolonged release of active ingredient after dissolution of a tablet in liquid remains.
In each separate case, treatment by Finlepsinum retard has to begin individually, depending on type and degree of gravity of a clinical picture, and further, the dose needs to be raised gradually for achievement of the most effective maintenance dose.
The daily dose usually is ranging from 400 up to 1200 mg which is distributed on 1-2 receptions a day. As a rule, the general daily dose should not exceed 1600 mg of carbamazepine.
A drug dose, optimum for the patient, especially at the combined treatment, define on the basis of carbamazepine level in blood plasma.
Experience shows that the therapeutic level of carbamazepine is 4-12 µг/мл.
In some cases the necessary dose can significantly differ from the recommended initial and maintenance dose (perhaps, because of the strengthened metabolism caused by enzyme induction or interaction with other drugs at the combined treatment).
Epilepsy
At treatment of epilepsy, Finlepsinum retard preferably has to be used in the form of monotherapy. Treatment has to take place under observation of the experienced expert. Upon transition to Finlepsinum retard the dose of earlier used antiepileptic drug has to decrease gradually. If the patient forgot to accept in due time the next dose of drug, it is necessary to accept the passed dose at once as soon as this omission became noticed, at the same time it is impossible to accept a double dose of drug.
Adults: the dosage has to be individually chosen for each patient. For definition of an optimum dose the monitoring of concentration of carbamazepine in plasma can be useful.
The initial recommended dose – 200-400 mg a day, then gradually raise a dose to achievement of optimum effect. A maintenance dose – 800-1200 mg a day which distributes on 1-2 receptions a day.
Children
the Initial dose for children from 6 to 15 years – 200 mg a day, then gradually increase a dose by 100 mg a day before achievement of optimum effect. For children the average maintenance dose makes 10-20 mg/kg of body weight/days. A maintenance dose for children of 6-10 years – 400-600 mg a day (in 2 receptions), for children of 11-15 years – 600-1000 mg a day (in 2 receptions). The following scheme of dosing is recommended:
An initial dose
the Maintenance dose
Adults
on 200-300 mg in the evening
on 200-600 mg in the morning
on 400-600 mg in the evening
Children from 6 to 10 years
on 200 mg in the evening
on 200 mg in the morning
on 200-400 mg in the evening
Children from 11 to 15 years
on 200 mg in the evening
on 200-400 mg in the morning
on 400-600 mg in the evening
In an epileptiform neuralgia and glossofaringealny neuralgia drug appoint 200-400 mg/days which is distributed on 2 receptions in an initial dose. The initial dose is raised to total disappearance of pains up to 400-800 mg/days which is accepted by 1-2 times a day. After that treatment can be continued using lower maintenance dose making 400 mg/days, distributed on 2 receptions. The patient of advanced age and sick, sensitive to carbamazepine, Finlepsinum retard is appointed in the initial dose making 200 mg of 1 times a day.
At a pain syndrome in diabetic neuropathy the average daily dose makes 200 mg in the morning and 400 mg in the evening. In exceptional cases it is possible to appoint up to 1.2 g/days (on 600 mg 2 times a day).
In epileptiform spasms in multiple sclerosis the average daily dose makes 400-800 mg, distributed on 2 receptions.
Prevention of development of convulsive attacks in an alcoholic abstinence syndrome (in the conditions of a hospital)
the Average daily dose makes 600 mg (200 mg in the morning, 400 mg in the evening).
In hard cases in the first days it is possible to raise a dose to 600 mg 2 times a day. Finlepsinum retard should not be combined with sedative and hypnotic means. If necessary Finlepsinum retard can be combined with other substances applied to treatment of alcoholic abstinency. During treatment it is regularly necessary to control carbamazepine content in blood plasma. Due to the development of side effects from central and the autonomic nervous system for the patient establish careful observation in the conditions of a hospital.
For prevention of psychoses drug appoint 200-400 mg/days in a dose. If necessary this dose can be raised to 800 mg/days which is distributed on 2 receptions. Duration of treatment changes depending on a case and is defined by the attending physician.
Antiepileptic treatment always is long-term. At treatment of epilepsy, such questions as stabilization and duration of treatment by Finlepsinum retard have to be solved individually experienced expert. The decision on reduction of a dose and the termination of administration of drug should not be accepted before at the patient attacks within two or three years stop.
For the termination of treatment it is necessary to reduce gradually a dose within a year or two years under control of EEG. At children at decrease in a daily dose of drug it is necessary to consider increase in body weight with age.
At treatment of neuralgia the continuation of treatment within several weeks with reception of a maintenance dose, for belief in absence of pain is enough. Carefully reducing a dose, it is necessary to find out whether there occurred spontaneous regression of symptoms of a disease. When resuming attacks of pain, treatment continues to be carried out using the previous maintenance dose.
Duration of treatment of pain in diabetic neuropathy and epileptiform spasms in multiple sclerosis same, as well as in neuralgia.
Treatment of patients with an alcoholic abstinence syndrome the drug Finlepsinum retard is stopped, gradually reducing a dose for 7-10 days.
Prevention of manic-depressive phases long.
Duration of therapy depends on a case and is defined by the attending physician.
Side effects
from the central nervous system:
Often - dizziness, an ataxy, drowsiness, the general weakness, a headache, paresis, accommodations,
Sometimes - abnormal involuntary movements (for example, a tremor," flitting" a tremor – asterixis, dystonia, tics), a nystagmus,
is rare - hallucinations (visual or acoustical), a depression, a loss of appetite, concern, agressive behavior, psychomotor excitement, a disorientation, activation of psychosis, orofatsialny dyskinesia, oculomotor disturbances, disturbances of the speech (for example, a dysarthtia or the muffled speech), horeatetoidny disorders, peripheral neuritis, paresthesias, muscle weakness and symptoms of paresis. A carbamazepine role as the drug causing or contributing to the development of a malignant antipsychotic syndrome, especially when it is appointed together with neuroleptics, remains obscure.
Allergic reactions:
Often - a small tortoiseshell,
Sometimes - an erythrosis, multiorgan delayed-type hypersensitivity reactions with fever, skin rashes, a vasculitis (including a knotty erythema as manifestation of a skin vasculitis), the limfoadenopatiya, signs reminding a lymphoma, arthralgias, a leukopenia, an eosinophilia, a gepatosplenomegaliya and changed by indicators of function of a liver (the specified manifestations meet in various combinations). Also other bodies can be involved (for example, lungs, kidneys, a pancreas, a myocardium, a large intestine), anaphylactoid reaction, a Quincke's disease, an allergic pneumonitis or eosinophilic pneumonia are possible aseptic meningitis with a myoclonus and a peripheral eosinophilia. At emergence of the allergic reactions stated above the use of drug has to be stopped.
Seldom - a volchanopodobny syndrome, an itching, skins, a mnogoformny exudative erythema (including Stephens-Johnson's syndrome), a toxic epidermal necrolysis (Lyell's disease), photosensitivity.
From bodies of a hemopoiesis:
Often - a leukopenia, thrombocytopenia, an eosinophilia,
it is rare - a leukocytosis, a limfoadenopatiya, deficiency of folic acid, an agranulocytosis, aplastic anemia, a true erythrocyte aplasia, megaloblastny anemia, the sharp "alternating" porphyria, a reticulocytosis, hemolytic anemia, a splenomegaly.
From digestive system:
Often - nausea, vomiting, dryness in a mouth increase in activity of a gammaglutamiltransferaza (owing to induction of this enzyme in a liver), increase in activity of alkaline phosphatase.
Sometimes - increase in activity "hepatic" transminaz, diarrhea or a constipation, abdominal pains.
Seldom - a glossitis, an ulitis, stomatitis, pancreatitis, hepatitis of cholestatic, parenchymatous (hepatocellular) type, jaundice, granulematozny hepatitis, a liver failure.
From warmly vascular system:
Seldom - disturbances of intracardial conductivity, decrease or increase in arterial blood pressure, bradycardia, arrhythmias, atrioventricular block with faints, collapse, aggravation or development of chronic heart failure, exacerbation of coronary heart disease (including emergence or increase of attacks of stenocardia), thrombophlebitis, a thromboembolic syndrome.
From an endocrine system and a metabolism:
Often - hypostases, a liquid delay, increase in body weight, a hyponatremia (decrease in osmolarity of plasma owing to the effect similar to effect of antidiuretic hormone that in rare instances leads to the hyponatremia of cultivation which is followed by a lethargy, vomiting, a headache, a disorientation and neurologic disturbances),
it is rare - increase in concentration of prolactin (can be followed by a galactorrhoea and a gynecomastia), decrease in concentration of L-thyroxine and increase in concentration of thyroid stimulating hormone (usually is not followed by clinical manifestations), disturbances of kalitsiyevofosforny exchange in a bone tissue (decrease in concentration of Ca2 + and 25-IT-cholecalciferol in blood plasma), osteomalacy, a hypercholesterolemia (including cholesterol of lipoproteins of high density), a gipertriglitseridemiya and a hyperadenosis, a hirsutism.
From an urinogenital system: Seldom - interstitial nephrite, a renal failure, a renal failure (for example, an albuminuria, a hamaturia, an oliguria, increase an urea/azotemia), the speeded-up urination, an ischuria, decrease in potency.
From the musculoskeletal system:
Seldom - an arthralgia, myalgia or spasms
from sense bodys: Seldom - disturbance of flavoring feelings, increase in intraocular pressure, a cataract, conjunctivitis, hearing disorder, including sonitus, a hyperacusia, a gipoakuziya, changes of perception of height of a sound.
Other: disturbances of xanthopathy, purple, acne, perspiration, alopecia.
Contraindications
- a combination with inhibitors of a monoaminooxidase (MAO), intake
of MAO inhibitors it is necessary to stop a minimum in 2 weeks prior to prescribing
of carbamazepine
- a concomitant use of drugs of lithium
- a concomitant use of a vorikonazol
- disturbance of a marrowy hemopoiesis (anemia, a leukopenia)
- disturbances of conductivity (atrioventricular block)
- hypersensitivity to acting and
to excipients, tricyclic antidepressants
- the sharp alternating porphyria (including in the anamnesis)
- absentias epileptica
- heavy dysfunctions of heart, liver and kidneys
- sodium exchange disturbance
- children's age up to 6 years
With care:
- dekompensirovanny chronic heart failure, a cultivation hyponatremia (syndrome of hypersecretion of ADG, a hypopituitarism, a hypothyroidism, insufficiency of bark of adrenal glands), insufficiency of a funtion of a liver and kidneys, patients of advanced age, active alcoholism (oppression of central nervous system amplifies, carbamazepine metabolism amplifies), oppression of a marrowy hemopoiesis against the background of drug intake (in the anamnesis), a prostate hyperplasia, increase in intraocular pressure, a combination with sedative sleeping medicines.
Co-administration of carbamazepine with CYP inhibitors 3A4 can lead medicinal interactions to increase in its concentration in blood plasma and to development of side reactions. Combined use of inductors CYP 3A4 can lead to carbamazepine metabolism acceleration, decrease in its concentration in blood plasma and to reduction of therapeutic effect, on the contrary, their cancellation can reduce the speed of biotransformation of carbamazepine and lead to increase in its concentration.
Raise a carbamazepine kontsetration in plasma verapamil, diltiazem, felodipin, dextropropoxyphene, viloksazin, fluoxetine, fluvoksamin, Cimetidinum, acetazoleamide, danazol, desipramine, niacinamide (at adults, only in high doses), macroleads (erythromycin, dzhozamitsin, klaritromitsin, troleandomitsin), azoles (itrakonazol, ketokonazol, flukonazol), terfenadin, loratadin, the isoniazid, the propoxyhair dryer, grapefruit juice, inhibitors of virus protease used at therapy of HIV infection (for example, ritonavir) – is required correction of the mode of dosing or monitoring of concentration of carbamazepine in plasma.
Felmabat reduces concentration of carbamazepine in plasma and increases concentration of carbamazepine – 10.11 – epoxide, at the same time perhaps simultaneous decrease in concentration in felbamat serum.
Concentration of carbamazepine is reduced by phenobarbital, Phenytoinum, Primidonum, metsuksimid, fensuksimid, theophylline, rifampicin, Cisplatinum, doxorubicine, it is possible: clonazepam, valpromid, valproic acid, okskarbazepin and the vegetable drugs containing a St. John's wort made a hole (Hypericum perforatum). There is a possibility of replacement by valproic acid and Primidonum of carbamazepine from communication with proteins of plasma and increase in concentration pharmacological of an active metabolite (carbamazepine-10.11-epoxide). At the combined use of Finlepsinum with valproic acid in exceptional cases there can come the coma and confusion of consciousness.
Izotretinoin changes bioavailability and/or clearance of carbamazepine and carbamazepine-10.11-epoxide (monitoring of a kontsetration of carbamazepine in plasma is necessary). Carbamazepine can reduce concentration in plasma (to reduce or even completely to level effects) and correction of doses of the following drugs can be required: a klobazama, clonazepam, digoxin, Ethosuximidum, Primidonum, valproic acid, an alprazolam, glucocorticosteroids (Prednisolonum, dexamethasone), cyclosporine, tetracyclines (doxycycline), a haloperidol, methadone, the oral drugs containing estrogen and/or progesterone (selection of alternative methods of contraception), theophylline, oral anticoagulants (warfarin, a fenprokumon, a dikumarol), a lamotridzhina, the topiramat, tricyclic antidepressants (Imipraminum, amitriptyline, a nortriptilin, a klomipramin), clozapine, the felbamat, a tiagabin, an okskarbazepin, inhibitors of the proteases applied at therapy of HIV infection (an indinavir, a ritonavir, a sakvinovir), blockers of calcium channels (group of digidropiridon, for example felodipin is necessary), an itrakonazola, left thyroxine, midazolam, olanzapine, a prazikvantel, a risperidon, a tramadol, a tsiprazidon. There is a possibility of increase or decrease in level of Phenytoinum in blood plasma against the background of carbamazepine and increase in level of Mephenytoinum. At simultaneous use of carbamazepine and drugs of lithium, neurotoxic influences of both active agents can amplify.
Tetracyclines can weaken therapeutic effect of carbamazepine. At combined use with paracetamol the risk of its toxic influence on a liver increases and the therapeutic effectiveness (paracetamol metabolism acceleration) decreases.
Co-administration of carbamazepine with fenotiaziny, Pimozidum, thioxanthenes, molindony, a haloperidol, Maprotilinum, clozapine and tricyclic antidepressants leads to strengthening of the oppressing action on the central nervous system and to easing of anticonvulsant effect of carbamazepine. Monoamine oxidase inhibitors increase risk of developing hyperpyrexial crises, hypertensive crises, spasms, death (before prescribing of carbamazepine monoamine oxidase inhibitors have to be cancelled, at least, in 2 weeks or if the clinical situation, even for bigger term allows).
Co-administration with diuretics (hydrochlorothiazide, furosemide) can lead to the hyponatremia which is followed by clinical manifestations. Weakens effects of not depolarizing muscle relaxants (pankuroniya). In case of use of such combination there can be a need of increase in a dose of muscle relaxants, at the same time careful monitoring of a condition of the patient in connection with a possibility of faster cancellation of muscle relaxants is necessary. Carbamazepine reduces tolerance of ethanol. Myelotoxic medicines strengthen manifestations of a gematotoksichnost of drug.
Accelerates metabolism of indirect anticoagulants, hormonal contraceptive drugs, folic acid, prazikvantet, can strengthen elimination of hormones of a thyroid gland.
Accelerates metabolism of anesthetics (an enfluran, a halothane, Ftorotanum) and increases risk of development of hepatotoxic effects, strengthens formation of nefrotoksichny metabolites of a metoksifluran. Strengthens hepatotoxic action of an isoniazid.
The special
indications Monoterapiyu of epilepsy begin with purpose of a low initial dose, gradually raising it to achievement of desirable therapeutic effect.
At selection of an optimum dose it is reasonable to define concentration of carbamazepine in blood plasma, in particular at combination therapy.
In some cases the optimum dose can deviate considerably the recommended initial and maintenance dose, for example, in connection with induction of microsomal enzymes of a liver or because of interactions at combination therapy.
Finlepsinum retard should not be combined with sedative and hypnotic means. In need of it it is possible to combine with other substances applied to treatment of alcoholic abstinency. During treatment it is regularly necessary to control carbamazepine content in blood plasma. Due to the development of side effects from central and the autonomic nervous system for patients establish careful observation in the conditions of a hospital. At conversion of the patient to carbamazepine it is necessary to reduce gradually a dose of earlier appointed antiepileptic means up to its full cancellation. The sudden termination of intake of carbamazepine can provoke epileptic attacks. If it is necessary to interrupt sharply treatment, it is necessary to transfer the patient to other antiepileptic means under cover of the drug shown in such cases (for example, the diazepam entered intravenously or rektalno or Phenytoinum entered intravenously).
It is described several cases of vomiting, diarrhea and/or subnutrition, a spasm and/or respiratory depressions at newborns whose mothers accepted carbamazepine along with other anticonvulsant drugs (perhaps, these reactions represent manifestations at newborns of a withdrawal). Before prescribing of carbamazepine and in the course of treatment the research of function of a liver, especially at patients in whose anamnesis there are data on liver diseases and also for patients of advanced age is necessary. In case of strengthening of already being available abnormal liver functions or at appearance of an active disease of a liver, drug should be cancelled immediately. Before an initiation of treatment it is necessary to conduct blood picture researches (including calculation of thrombocytes, reticulocytes), iron level in serum of blood, the general analysis of urine, urea level in blood, the electroencephalogram, definition of concentration of electrolytes in blood serum (and periodically during treatment since development of a hyponatremia is possible). Subsequently these indicators should be controlled within the first month of treatment weekly, and then monthly.
In most cases passing or permanent decrease in number of thrombocytes and/or leukocytes are not harbingers of the beginning of aplastic anemia or agranulocytosis. Nevertheless, before an initiation of treatment and also periodically in the course of treatment it is necessary to carry out complete blood count tests, including calculation of number of thrombocytes and, perhaps, reticulocytes and also to determine iron level in blood serum. Not progressing symptomless leukopenia does not demand cancellation, however, treatment should be stopped at emergence of the progressing leukopenia or the leukopenia which is followed by clinical symptoms of an infectious disease. Carbamazepine has to be immediately cancelled at the emergence of reactions of hypersensitivity or symptoms demonstrating development of a syndrome of Stephens-Johnson or a Lyell's disease. Mild skin reactions (the isolated makulezny or makulopapulezny dieback) usually take place within several days or weeks even at continuation of treatment or after a drug dose decline (the patient has to be under fixed observation of the doctor at this time).
It is necessary to take into account a possibility of activation latentno of the proceeding psychoses, and at advanced age – a possibility of development of a disorientation or psychomotor excitement. Disturbances of male fertility and/or disturbance of a spermatogenesis are possible, however the interrelation of these disturbances with intake of carbamazepine is not established yet. Appearance of intermenstrual bleedings at simultaneous use of oral contraceptives is possible. Carbamazepine can negatively affect reliability of oral contraceptive drugs therefore women of reproductive age during treatment should apply alternative methods of protection from pregnancy. Carbamazepine has to be applied only under medical observation.
It is necessary to inform patients information on precursory symptoms of toxicity and also on symptoms from integuments and a liver. The patient is informed on need to see immediately a doctor in case of such undesirable reactions as fever, sore throat, rash, an ulceration of a mucous oral cavity, causeless developing of bruises, hemorrhages in the form of petechias or a purpura.
Before an initiation of treatment it is recommended to perform ophthalmologic examination, including a research of an eyeground and measurement of intraocular pressure. In case of prescribing of drug the patients with increase in intraocular pressure need constant control of this indicator.
The patient with a serious cardiovascular illness, damages of a liver and kidneys and also to elderly people appoint lower doses of drug. Though the interrelation between a carbamazepine dose, its concentration and clinical performance or shipping is very insignificant, nevertheless, regular determination of level of carbamazepine can be useful in the following situations: at sharp increase in frequency of attacks to check whether the patient takes the drug properly, during pregnancy, at treatment of children or teenagers, at suspicion for drug absorption disturbances, at suspicion on development of toxic reactions if the patient accepts several medicines.
During treatment Finlepsinum retardy is recommended to refrain from alcohol intake.
Carbamazepine it is necessary to appoint pregnancy and the period of a lactation during pregnancy only after careful weighing of benefits and risks. Women of childbearing age need to explain about need of planning and control of pregnancy. Whenever possible, women of childbearing age should appoint carbamazepine as monotherapy as at combination therapy with other anti-epileptic means the risk of congenital defects increases.
In case of approach of pregnancy during treatment by carbamazepine or emergence of need for treatment by carbamazepine during pregnancy, the attending physician has to weigh carefully potential advantage of use of drug in comparison with possible to risks for a fruit, especially, in the first trimester of pregnancy. It is necessary to appoint a minimal effective dose and to carry out monitoring of concentration of drug in blood plasma. It is impossible to stop treatment at all, without having consulted with the doctor as epileptic seizures can threaten health, both mother, and the child.
As well as in a case with other antikonvulsant, it was reported about razlichn
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