Tegretol CR tablets 200mg, no. 50

Epilepsy: large, focal, mixed (including large and focal) epileptic seizures.

Pain syndrome of predominantly neurogenic genesis, incl. essential neuralgia of the trigeminal nerve, neuralgia of the trigeminal nerve in multiple sclerosis, essential glossopharyngeal neuralgia.

Prevention of seizures in alcohol withdrawal syndrome.

Affective and schizoaffective psychoses (as a means of prevention).

Diabetic neuropathy with pain syndrome.

Diabetes insipidus of central origin, polyuria and polydipsia of neurohormonal nature.

Set individually. For oral administration for adults and adolescents 15 years of age and older, the initial dose is 100-400 mg. If necessary and taking into account the clinical effect, the dose is increased by no more than 200 mg / day with an interval of 1 week. The frequency of admission is 1-4 times / day. The maintenance dose is usually 600-1200 mg / day in divided doses. The duration of treatment depends on the indications, the effectiveness of treatment, the patient's response to therapy.

In children under 6 years of age, use 10-20 mg / kg / day in 2-3 divided doses; if necessary and taking into account tolerance, the dose is increased by no more than 100 mg / day with an interval of 1 week; the maintenance dose is usually 250-350 mg / day and does not exceed 400 mg / day. Children aged 6-12 years - 100 mg 2 times / day on the first day, then the dose is increased by 100 mg / day with an interval of 1 week. until the optimal effect is obtained; the maintenance dose is usually 400-800 mg / day.

Maximum doses: when taken orally for adults and adolescents 15 years of age and older - 1.2 g / day, for children - 1 g / day.

Sustained-release film-coated tablets

1 tab.

carbamazepine

Excipients: microcrystalline cellulose, sodium carmellose, polyacrylate dispersion 30% (Eudragit E 30 D), ethylcellulose aqueous dispersion, talc, colloidal anhydrous silicon dioxide, magnesium stearate.

• AV blockade,

• previous myelodepression,

• a history of intermittent porphyria,

• simultaneous administration of MAO inhibitors and lithium preparations,

• hypersensitivity to carbamazepine.

pharmachologic effect

Antiepileptic agent derived from tricyclic iminostilbene. It is believed that the anticonvulsant effect is associated with a decrease in the ability of neurons to maintain a high frequency of development of repeated action potentials through inactivation of sodium channels. In addition, inhibition of the release of neurotransmitters by blocking presynaptic sodium channels and the development of action potentials, which in turn reduces synaptic transmission, appears to be important.

It has a moderate antimanic, antipsychotic effect, as well as an analgesic effect for neurogenic pain. Mechanisms of action possibly involve GABA receptors, which may be associated with calcium channels; also, apparently, the effect of carbamazepine on the systems of modulators of neurotransmission.

The antidiuretic effect of carbamazepine may be associated with a hypothalamic effect on osmoreceptors, which is mediated through the secretion of ADH, and also due to a direct effect on the renal tubules.

Pharmacokinetics

After oral administration, carbamazepine is almost completely absorbed from the gastrointestinal tract. Plasma protein binding is 75%. It is an inducer of liver enzymes and stimulates its own metabolism.

T1 / 2 is 12-29 hours. 70% is excreted in the urine (in the form of inactive metabolites) and 30% in the feces.

Side effect

From the side of the central nervous system and peripheral nervous system: often - dizziness, ataxia, drowsiness; possible headache, diplopia, accommodation disturbances; rarely - involuntary movements, nystagmus; in some cases - oculomotor disorders, dysarthria, peripheral neuritis, paresthesias, muscle weakness, paresis symptoms, hallucinations, depression, fatigue, aggressive behavior, agitation, impaired consciousness, increased psychosis, taste disturbances, conjunctivitis, tinnitus, hyperacusis.

From the digestive system: nausea, increased GGT, increased alkaline phosphatase activity, vomiting, dry mouth; rarely - increased activity of transaminases, jaundice, cholestatic hepatitis, diarrhea or constipation; in some cases - decreased appetite, abdominal pain, glossitis, stomatitis.

From the side of the cardiovascular system: rarely - myocardial conduction disorders; in some cases - bradycardia, arrhythmias, AV block with syncope, collapse, heart failure, manifestations of coronary insufficiency, thrombophlebitis, thromboembolism.

From the hematopoietic system: leukopenia, eosinophilia, thrombocytopenia; rarely - leukocytosis; in some cases - agranulocytosis, aplastic anemia, erythrocytic aplasia, megaloblastic anemia, reticulocytosis, hemolytic anemia, granulomatous hepatitis.

From the side of metabolism: hyponatremia, fluid retention, edema, weight gain, decrease in plasma osmolality; in some cases - acute intermittent porphyria, folic acid deficiency; disorders of calcium metabolism, increased cholesterol and triglyceride levels.

From the endocrine system: gynecomastia or galactorrhea; rarely - dysfunction of the thyroid gland.

From the urinary system: rarely - renal dysfunction, interstitial nephritis and renal failure.

From the respiratory system: in some cases - dyspnea, pneumonitis or pneumonia.

Allergic reactions: skin rash, itching; rarely - lymphadenopathy, fever, hepatosplenomegaly, arthralgia.

Application during pregnancy and lactation

If it is necessary to use it during pregnancy (especially in the first trimester) and during lactation, the expected benefits of treatment for the mother and the risk for the fetus or child should be carefully weighed. In this case, carbamazepine is recommended to be used only as monotherapy in the minimum effective doses.

Women of childbearing age are advised to use non-hormonal contraception during treatment with carbamazepine.

Application for violations of liver function

Use with caution in severe liver dysfunction.

Application for impaired renal function

Use with caution in severe renal impairment.

Application in children

Use with caution in children.

Use in elderly patients

Use with caution in elderly patients.

special instructions

Carbamazepine is not used for atypical or generalized minor epileptic seizures, myoclonic or atonic epileptic seizures. Should not be used to relieve common pain; as a prophylactic agent during long periods of remission of trigeminal neuralgia.

Use with caution in concomitant diseases of the cardiovascular system, severe liver and / or kidney dysfunction, diabetes mellitus, increased intraocular pressure, with indications of a history of hematological reactions to the use of other drugs, hyponatremia, urinary retention, hypersensitivity to tricyclic antidepressants , with indications in the history of interruption of the course of treatment with carbamazepine, as well as children and elderly patients.

Treatment should be carried out under the supervision of a physician. With long-term treatment, it is necessary to monitor the blood picture, the functional state of the liver and kidneys, the concentration of electrolytes in the blood plasma, and conduct an ophthalmological examination. Periodic determination of the level of carbamazepine in blood plasma is recommended to monitor the effectiveness and safety of treatment.

At least 2 weeks before starting therapy with carbamazepine, it is necessary to discontinue treatment with MAO inhibitors.

Avoid drinking alcohol during treatment.

Influence on the ability to drive vehicles and use mechanisms

During treatment, one should refrain from engaging in potentially hazardous activities that require increased attention, speed of psychomotor reactions.

Drug interactions

With the simultaneous use of inhibitors of the isoenzyme CYP3A4, an increase in the concentration of carbamazepine in the blood plasma is possible.

With the simultaneous use of inducers of the CYP3A4 isoenzyme system, it is possible to accelerate the metabolism of carbamazepine, decrease its concentration in blood plasma, and decrease the therapeutic effect.

With the simultaneous use of carbamazepine stimulates the metabolism of anticoagulants, folic acid.

With simultaneous use with valproic acid, it is possible to reduce the concentration of carbamazepine and a significant decrease in the concentration of valproic acid in the blood plasma. This increases the concentration of the carbamazepine metabolite - carbamazepine epoxide (probably due to inhibition of its conversion to carbamazepine-10,11-trans-diol), which also has anticonvulsant activity, therefore the effects of this interaction can be leveled, but more often side reactions occur - blurred vision, dizziness, vomiting, weakness, nystagmus. With the simultaneous use of valproic acid and carbamazepine, a hepatotoxic effect may develop (apparently due to the formation of a minor metabolite of valproic acid, which has a hepatotoxic effect).

With the simultaneous use of valpromide reduces the metabolism in the liver of carbamazepine and its metabolite carbamazepine-epoxide due to inhibition of the enzyme epoxide hydrolase. The specified metabolite has anticonvulsant activity, but with a significant increase in plasma concentration, it can have a toxic effect.

With simultaneous use with verapamil, diltiazem, isoniazid, dextropropoxyphene, viloxazine, fluoxetine, fluvoxamine, cimetidine, acetazolamide, danazol, desipramine, nicotinamide (in adults, only in high doses), erythromycin, troleandamycin, clarythromycin; with azoles (including with itraconazole, ketoconazole, fluconazole), terfenadine, loratadine, it is possible to increase the concentration of carbamazepine in the blood plasma with the risk of side effects (dizziness, drowsiness, ataxia, diplopia).

With simultaneous use with hexamidine, the anticonvulsant effect of carbamazepine is weakened; with hydrochlorothiazide, furosemide - a decrease in the sodium content in the blood is possible; with hormonal contraceptives - the weakening of the effect of contraceptives and the development of acyclic bleeding is possible.

With simultaneous use with thyroid hormones, it is possible to increase the elimination of thyroid hormones; with clonazepam - an increase in the clearance of clonazepam and a decrease in the clearance of carbamazepine are possible; with lithium preparations - mutual enhancement of neurotoxic action is possible.

With simultaneous use with primidone, it is possible to reduce the concentration of carbamazepine in the blood plasma. There are reports that primidone can increase the plasma concentration of a pharmacologically active metabolite, carbamazepine-10,11-epoxide.

With simultaneous use with ritonavir, it is possible to increase the side effects of carbamazepine; with sertraline - a decrease in the concentration of sertraline is possible; with theophylline, rifampicin, cisplatin, doxorubicin - a decrease in the concentration of carbamazepine in the blood plasma is possible; with tetracycline - the effects of carbamazepine may be weakened.

With simultaneous use with felbamate, a decrease in the concentration of carbamazepine in the blood plasma is possible, but an increase in the concentration of the active metabolite of carbamazepine-epoxide, while a decrease in the plasma concentration of felbamate is possible.

With simultaneous use with phenytoin, phenobarbital, the concentration of carbamazepine in the blood plasma decreases. Mutual weakening of the anticonvulsant action is possible, and in rare cases - its enhancement.