Carbamazepine таб. 0,2 No. 50

General characteristics. Structure:

Active ingredient: One tablet contains carbamazepine 0,2 g; excipients.

Pharmacological properties:

Pharmacodynamics. Carbamazepine possesses the expressed anticonvulsant (antiepileptic), moderate antidepressive (timoleptichesky) and normotimichesky influence. At epilepsy, along with positive dynamics of paroxysms, carbamazepine improves an emotional state and increases skill to communicate of patients with changes of the personality that promotes their social rehabilitation. Prevents or considerably reduces the frequency of epileptic seizures, leads to normalization of EEG. Carbamazepine has anapgeziruyushchy effect at epileptiform neuralgias, prevents development of paroxysmal pain. Analgetic effect of carbamazepine at trigeminal neuralgia is based on reduction of synoptic transfer in a trifacial kernel. The mechanism of anticonvulsant effect of carbamazepine is connected with restriction of spread of activation from certain zones of a cerebral cortex, with reduction of post-tetanic potentiation in a spinal cord, with reduction in the rate of carrying out on motor and sensory nerves, and also with nonspecific membrane stabilizing effect. Psychotropic effect of carbamazepine is implemented due to changes in transport of ions through a cellular membrane thanks to increase in activity of Na-K-Atfazy and braking of tsAMF. At the same time inhibitory influence of carbamazepine on neurotransfer in limbic system is not excluded. At not diabetes mellitus leads to bystry normalization (rekompensation) of a water balance.

Pharmacokinetics. Carbamazepine after hit in a stomach is rather slowly released from a tablet. Active ingredient in not changed form reaches peak concentration in a blood plasma in 4-24 hours after reception in a single dose. Therapeutic concentration of carbamazepine in plasma makes 5-12 mkg/ml. 70-80% of carbamazepine contact proteins of plasma. Degree of bioavailability makes 70-95%. The elimination half-life of not changed carbamazepine - 26-65 hours, at long reception owing to an autoinduktion of microsomal enzymes of a liver decreases till 16-24 o'clock. It Biotransformirutsya in a liver. The main metabolite - 10,11 epoxide which possesses antiepileptic action. It is removed with urine (72%) and with a stake (23%). Passes through placental and hematoencephalic barriers, gets into breast milk. Metabolism of carbamazepine is reduced at people of advanced age and at children.
Control of the level of carbamazepine is necessary with side effects, pregnancy and its simultaneous use with other anticonvulsant drugs and medicines of the accompanying therapy.

Indications to use:

Epilepsy (big convulsive attacks, the mixed epilepsy forms, focal attacks with simple or difficult symptomatology); prevention of attacks at an abstinence syndrome at patients with an alcoholism; neuralgia (a trifacial, glossofaringealny and post-herpetic neuralgia, neuralgia at diabetic polyneuropathy, acute idiopathic neuritis, a stump neuralgia); paroxysmal dysarthtia and ataxy, tonic attacks, paroxysmal paresthesia and attacks of pain; psychoses (maniac-depressive psychosis, the alarming agitated depression, catatonic excitement); acute alcoholic abstinence; central not partial not diabetes mellitus.

Route of administration and doses:

Carbamazepine is accepted inside during food. The adult for treatment of epilepsy at the beginning of a course appoint 0,2 g 1-2 times a day, the patient of advanced age - on 0,1 g (1/2 tablets) 1-2 times a day. Further a dose to 0,4 g 2-3 times a day before achievement of an optimum daily dose gradually increase 0,8-1,2 g. The maximum dose - 1,6 g/days.
To children dose at the rate of 10-20 mg/kg of body weight that makes for children of 4-12 months 0,1-0,2 g in days, 2-3 years - 0,2-0,3 g a day, 4-7 years - 0,3-0,5 g a day, 8-14 years-0,5-1,0 g a day, 15-18 years-0,8-1,2 g a day. The daily dose is divided into 2 receptions. At treatment of various neuralgia and pain syndromes carbamazepine accept 0,2-0,4 g which is divided into 2-3 receptions in a daily dose. The dose is gradually raised to disappearance of pain and appoint 0,2 g 3-4 times a day within 7-10 days. Further, after improvement of a condition of the patient, the dose is gradually reduced to supporting (minimum effective) which accept a long time. At an abstinence syndrome the average dose of carbamazepine makes 0,2 g 3 times a day. In hard cases within the first several days it is possible to raise a dose to 0,4 g 3 times a day and to combine reception of carbamazepine with sedative and hypnotic drugs (клометиазол, chlordiazepoxide). After weakening of an acute form treatment continuation by carbamazepine as the main therapeutic means up to disappearance of a pain syndrome is possible.
At use for treatment of not diabetes mellitus the average dose for adults makes 0,2 g 2-3 times a day, dosages for children - as at treatment of epilepsy.

Features of use:

Treatment by carbamazepine should be begun with small doses, individually raising them to establishment of desirable therapeutic level.
Definition of concentration of drug in a blood plasma for selection of an optimum dose is desirable, especially at the joint therapy. At selection of a dose it is necessary to show special care concerning patients with cardiovascular diseases, abnormal liver functions and/or kidneys, and also in relation to patients of advanced age.
Before an initiation of treatment it is necessary to conduct researches of function of a liver and a picture of blood. Further these researches should be repeated periodically. During treatment by carbamazepine it is necessary to abstain from occupations such types of activity which require special attention, the speed of mental and motor reactions as drug can lower reactive ability.
Treatment by drug has to be carried out under observation of the doctor. If the expressed side effects demand drug withdrawal, it is necessary to consider that the sudden termination of therapy can lead to development of an attack.
In case of forced sudden phase-out of carbamazepine transfer of the patient into other antiepileptic means has to be carried out using barbiturates.
With care appoint carbamazepine at pregnancy: it is necessary to weigh carefully expected therapeutic effect and possible risk connected with administration of drug (especially in the first 3 months). Specified concerns as well the lactation period as active ingredient of drug gets into breast milk. However carbamazepine is considered as choice drug at the women of childbearing age forced to accept anticonvulsants and also as the safest concerning a fruit.
At women who at the same time accept carbamazepine and oral contraceptives uterine bleedings can develop.

Side effects:

Are usually expressed slightly, are most often noted at the beginning of therapy and disappear within several days. Dizziness, drowsiness, a headache, an agressive behavior, the involuntary movements, an arthralgia, a mialgiya, a fotosensebilization, bradycardia, arrhythmias, AV blockade, anorexia, nausea, diarrhea or a lock, an abnormal liver function, a leukopenia, thrombocytopenia, an agranulocytosis, aplastic anemia, a generalized lymphadenopathy, hypostases, renal failures, диспноэ, pulmonary insufficiency, an alopecia, a gynecomastia, sexual disturbances, allergic reactions, exfoliative dermatitis are possible. In most cases side effects disappear at a dose decline or temporary drug withdrawal.

Interaction with other medicines:

At simultaneous use of carbamazepine with such anticonvulsants as Phenytoinum, phenobarbital and Primidonum, decrease in their concentration in blood serum is noted. Carbamazepine reduces Phenytoinum half-life.
Co-administration of carbamazepine with erythromycin, an isoniazid, verapamil, diltiazem, dextropropoxyphene, viloksaziny and Cimetidinum can lead to increase in concentration of carbamazepine and development of toxic reactions.
Carbamazepine leads to reduction of an elimination half-life of doxycycline in this connection it is necessary to appoint doxycycline from 12 an hour interval.
Co-administration with warfarin leads to decrease in concentration of the last in a blood plasma and to reduction of the period of its semi-removal.
It is not necessary to appoint carbamazepine along with MAO inhibitors (the break between their appointment has to make not less than 2 weeks). At appointment or cancellation of carbamazepine it is necessary to change a dose of anticoagulants (according to clinical requirements).
During treatment by carbamazepine reliability of action of hormonal contraceptives can decrease. As carbamazepine, as well as other psychotropic medicines, can reduce tolerance to alcohol, during treatment drug recommends to abstain from the use of alcoholic drinks.

Contraindications:

Individual intolerance or hypersensitivity to carbamazepine and tricyclic antidepressants; atrioventricular block; marrow diseases; hematologic diseases; heavy abnormal liver functions, kidneys, cordial activity, sodium exchange; glaucoma; prostatitis.

Overdose:

Symptoms: dizziness, drowsiness, nausea, vomiting, hypererethism, irritability, a disorientation, the involuntary movements, hypo - and a hyperreflexia, a mydriasis, a dermahemia, an ischuria, arterial hypotonia or symptomatic hypotension. In certain cases overdoses of drug can develop a leukocytosis, a leukopenia, a glucosuria and a ketonuria.
Treatment: gastric lavage and symptomatic therapy.

Storage conditions:

In the dry, protected from light place at the room temperature. To store in the place, unavailable to children.

Period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 50 tablets in containers polymeric.