Effect of the medicine. Pharmacodynamics. Derivative a karboksamida that is appointed as anticonvulsant and analgezivny drug at an epileptiform neuralgia.
Antivascular action is found in a suspension or reduction of frequency of attacks and contributes to normalization of pathological changes on EEG. The carbapin shows sedative and myorelaxation action. In the presence of an epileptiform neuralgia analgetic effect of carbamazepine is based on reduction of synoptic transmission in a trifacial kernel. Drug has anti-maniacal action.
Pharmacokinetics. After internal use carbamazepine is quickly soaked up and gets in the most part of body tissues. The maximum concentration in a blood plasma after peroral use of 400 mg of drug is reached in 6-7 hours. Carbamazepine gets through a placenta, a blood-brain barrier and it is found in maternal milk. Linkng with proteins of a blood plasma makes 78%. Carbamazepine is almost completely metabolized in a liver with formation of a number of metabolites, one with which (10, 11-epoksid) shows anticonvulsant activity. Only 2% of carbamazepine are removed with urine in a steady-state condition.
At children excretion is raised that can be the drive for recalculation of a dose on higher.
Indications to use. Epilepsy (for prevention of generalized epileptic seizures - "grand mal", epilepsy with and without disturbance of consciousness, the mixed epilepsy forms, for treatment of such forms of epilepsy that are followed by disturbance of mentality and changes of EEG);
for treatment of an epileptiform neuralgia;
abstinence syndrome at patients on an alcoholism;
diabetic neuropathy which is followed by pain;
Way of use and dose. The general day dose is divided into several single doses which are appointed with food or after food, with a small amount of liquid. In need of a tablet it is possible to divide into smaller doses.
For adults the initial dose makes Karbapina 100-200 mg which is appointed by 1-2 times a day. The dose is gradually raised to 800-1200 mg, and in certain cases it is equal to 1600-2000 mg a day.
For children the dose is appointed depending on age: 4-12 months – 100-200 mg a day; 2-3 years – 200-300 mg a day; 4-7 years – 300-500 mg a day; 8-14 years – 0, 5-1, 0 g a day. In youthful age the daily dose makes 600-1000mg. Noted doses divide into 2 receptions.
It is possible to appoint a carbapin along with other anticonvulsants.
The initial dose of drug makes 200-400 mg, in 2-3 receptions which is gradually increased before disappearance of pain. Usually appoint 200 mg, 3 - 4 times a day, within 7-10 days.
It is recommended to patient of advanced age to appoint lower initial dose of drug - on 100 mg, 2 times a day.
Side effect. Dizziness, drowsiness, a depression, activation to psychosis, a diplopia, disturbance of accommodation, opacification of a kristallik, a sonitus, decrease in flavoring feelings, disturbances of the speech, AV blockade, intersticial nephrite, osteomalacy, disturbance of sexual functions, nausea, skin rash are possible. In some cases - a headache, dryness in a mouth, it is very rare - a lock, a diarrhea, a joint pain and muscles, perspiration, loss of appetite, a hair loss.
Allergic reactions, leukopenia, thrombocytopenia, agranulocytosis, aplastic anemia, it is very rare - congestive hepatitis and exfoliative dermatitis.
Are possible: an ataxy, involuntary muscular contractions, a nystagmus, an abnormal liver function, a liquid delay in an organism, a generalized limfoadenopatiya, pulmonary insufficiency.
The majority of symptoms have a temporality, arise most often in an initiation of treatment and disappear after use of drug in several days.
Contraindications. Hypersensitivity to drug (including to tricyclic antidepressants);
severe forms of heart diseases (atrioventricular block);
blood diseases, disturbance of a marrowy hemopoiesis;
heavy dysfunctions of a liver and kidneys;
disturbance of formation of porphyrine, that is the acute alternating porphyria;
pregnancy (I trimester), lactation period.
Overdose. At overdose the dysarthtia, a nystagmus, an ataxy, spasms, a hypothermia, breath braking, a fluid lungs, tachycardia, a cardiac standstill, dizziness, hallucinations, drowsiness, a coma, a stupor, nausea, vomiting, irritability, orientation disturbance, a tremor, the involuntary movements, pathological reflexes, erubescence, cyanosis, an ischuria, hypotonia or a hypertension are observed. The leukocytosis, a glycosuria and a ketonuria, an oliguria or an anury, a hyponatremia, a hyperglycemia, AV blockade is sometimes observed. In these cases it is necessary to cause vomiting or a gastric lavage. Appoint enterosorbents, laxatives and diuretics. There is no specific antidote. Therapy is symptomatic.
Features of use. With care appoint drug pregnant, sick with a renal failure and a liver, with heart diseases, diuresis disturbance, the patient with glaucoma and mentally sick with opacification of consciousness or irritability.
If necessary purpose of drug in the period of a lactation it is necessary to resolve an issue about an opportunity a suspension of chest feeding (gets into mother's milk).
At women who at the same time apply Karbapin and oral contraceptives uterine bleedings are possible. The sudden suspension of treatment by Karbapin can entail an epilepsy attack therefore it is necessary to appoint barbiturates. When carrying out surgical interventions (an exodontia inclusive) it is necessary to warn the doctor about drug use. It is necessary to avoid alcohol intake.
To children till 6 years Karbapin's appointment only for vital need in connection with high risk of emergence of side effects is possible. To children who cannot swallow a tablet – to crush it and to drink dates with some drink.
Before and during treatment necessary control of blood tests and urine.
Interaction with other medicines. At simultaneous use of Karbapin with anticonvulsant drugs, such as Phenytoinum, Phenobarbitonum and Primidonum, decrease in their concentration in blood serum is noted, hour of half-decay of Phenytoinum decreases;
simultaneous use of carbamazepine with erythromycin, an isoniazid, verapamil, diltiazem, dextropropoxyphene, viloksaziny and Cimetidinum can bring to increase of concentration of carbamazepine and development of the toxic phenomena. Carbamazepine leads to decrease in time of half-decay of doxycycline;
co-administration of MAO inhibitors, lithium drugs is not recommended;
reduces activity of corticosteroids, estrogensoderzhashchy contraceptives, quinidine, cardiac glycosides;
against treatment the risk of disturbances of bone formation increases.
Conditions and periods of storage. To store at a temperature from 15 to 25 °C, in protected from light and moisture and the place, unavailable to children. A drug period of validity – 3 years.