N20 carbamazepine 0,2g
Producer: LLC Pharmaceutical Company Zdorovye Ukraine
Code of automatic telephone exchange: N03A F01
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
International and chemical names: carbamazepine, 5H-dibenz-[b, f] - azepine-5-karboksamid;
main physical and chemical properties: tablets of color, white or white with a creamy shade; structure: one tablet contains carbamazepine 0,2 g; excipients: starch potato or corn, polyvinylpirrolidone low-molecular medical, calcium stearate, aerosil.
Pharmacological properties:
Carbamazepine participates in processes of mediator exchange, possesses M-cholinolytic and adrenergic action. Lowers amplitude of potentials in sensitive kernels back and a diencephalon. Carbamazepine possesses the expressed anticonvulsant (antiepileptic) and 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 analgeziruyushchy 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 Na4 – K+ - Atfaza and to reduction of the tsAMF level. 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 hydrogen balance.
Pharmacokinetics. It is well soaked up in digestive tract. Carbamazepine after oral administration is rather slowly absorbed in the alimentary system. 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. Gets through biological barriers and from blood gets to various bodies and body tissues. Degree of bioavailability makes from 70 to 95%. The elimination half-life of not changed carbamazepine after reception in a single dose is in limits of 20-65 hours, averaging 36 hours. At long reception owing to an autoinduktion of microsomal enzymes of a liver time of semi-removal decreases till 16-24 o'clock. It is removed with urine and a stake. With urine in not changed look about 25% of the dose of drug getting into a stomach are removed. Carbamazepine biotransformirutsya in a liver to 10,11 epoxide, dihydrocarbamazepine and other metabolites. Epoxide possesses the antiepileptic action making 1/3 from inherent in carbamazepine. Carbamazepine and its active metabolite gets through a placenta. Metabolism of carbamazepine is weakened at people of advanced age and 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. At patients with epilepsy the elimination half-life of drug decreases till 10-12 o'clock.
Indications to use:
Carbamazepine is applied at psychomotor epilepsy, big and small attacks, at a combination of big attacks with psychomotor manifestations, at local forms of epilepsy.
Carbamazepine is also shown at primary and vtorichnogeneralizirovanny forms of attacks with a toniko-clonic component.
Drug is used and as adjuvant together with the specific medicines appointed for therapy of generalizirovanny forms of attacks (absentia epileptica type).
Carbamazepine is applied at the essential and caused by multiple sclerosis epileptiform neuralgia, essential glosofaringialny neuralgia.
Appoint for treatment of the penetrating pain in case of a spinal sukhota and a pain syndrome of peripheral diabetic neuropathy.
Carbamazepine can be choice drug in treatment of painful twitching.
Carbamazepine is shown at an abstinence syndrome at patients with an alcoholism (as a part of a combination therapy).
Besides, carbamazepine is applied at not diabetes mellitus of any origin, a polydipsia and a polyuria of neurohormonal genesis.
Route of administration and doses:
Carbamazepine is accepted inside during food. The adult for treatment of epilepsy in the beginning of a course appoint on 1 tablet (0,2 g) 1-2 times a day, the patient of advanced age - 1/2 tablets (0,1 g) 1-2 times a day. Further the dose is gradually increased to 2 tablets (0,4 g) by 2-3 times a day, that is before achievement of an optimum daily dose within 0,8-1,2 g (4-6 tablets). The maximum daily dose should not exceed 1,2 g.
To children carbamazepine is dosed depending on age at the rate of 10-20 mg/kg of body weight that makes for children of 4-12 months 1/2 - 1 tablet (0,1-0,2 g) a day, 2-3 years – 1-1,5 tablets (0,2-0,3 g) a day, 4-7 years – 1,5-2,5 tablets (0,3-0,5 g) a day, 8-14 years – 2,5-5 tablets (0,5-1,0 g) a day, 15-18 years – 4-6 tablets (0,8-1,2 g) a day. The appointed doses usually divide into 2 receptions.
At treatment of various neuralgia and pain syndromes carbamazepine is accepted in the daily dose making 1-2 tablets (0,2-0,4 g) which is divided into 2-3 receptions. The dose is gradually raised to disappearance of pain and appointed on 1 tablet (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 1 tablet (0,2 g) 3 times a day. In hard cases within the first several days it is possible to raise a dose to 2 tablets (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 1 tablet (0,2 g) 2-3 times a day, for children of a dose, similar as at treatment of epilepsy.
Features of use:
Treatment by carbamazepine needs to 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 or epilepsy.
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 attentively 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, nausea, skin rash, a headache, a xerostomia, diarrhea, a lock, an arthralgia, a mialgiya, a fotosensebilization, a hyperhidrosis, anorexia, an alopecia, sexual disturbances, allergic reactions, a leukopenia, thrombocytopenia, an agranulocytosis, aplastic anemia are possible; cholestatic hepatitis and exfoliative dermatitis develop exclusively seldom, but development of such phenomena demands the immediate termination of therapy, carrying out the appropriate medical measures and transition to other antiepileptic drug.
At purpose of carbamazepine the involuntary movements, a liquid delay in an organism, an abnormal liver function, a generalized lymphadenopathy, pulmonary insufficiency can appear.
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 with a 12-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.
Dipheninum lowers concentration of carbamazepine in a blood plasma.
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, bronchial asthma.
Overdose:
Dizziness, drowsiness, nausea, vomiting, hypererethism, irritability, 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 place, dry, unavailable to children, at a temperature not above 25 °C.
Period of validity - 2 years.
Issue conditions:
According to the recipe
Packaging:
Tablets on 0,2 g No. 20, No. 30, No. 20х3 in blister strip packagings.