Carbamazepine

• Structure
• Release form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications to Carbamazepine use
• Contraindications
• Side effects
• Tablets Carbamazepine, application instruction (Way and dosage)
• Overdose
• Interaction
• Terms of sale
• Storage conditions
• Period of validity
• Special instructions
• With alcohol
• Analogs
• Responses

Structure

200 mg of active agent carbamazepine contain. Additional elements are: starch, povidone, talc, silicon dioxide, polysorbate and magnesium stearate.

Release form

The tableted form.

Pharmacological action

Antiepileptic means. Possesses psychotropic action.

Pharmacodynamics and pharmacokinetics

Active component is derivative dibenzazepine. Medicine renders anti-maniacal, normotimichesky, antidiuretic (at patients with not diabetes mellitus), anesthetic (at neuralgia) influences.

The principle of influence of a medicine is based on blockade of potentsialzavisimy natrium channels that causes inhibition of process of emergence of categories of neurons, stabilization of a membrane of neurons that productively leads to decrease in synoptic carrying out impulses.

Medicine interferes with repeated education sodium of dependent action potentials in structure of the depolarized neurons.

Carbamazepine leads to reduction of the released glutamate (neuromediator amino acid), allows to reduce risk of development of an epileptic seizure. At children, teenagers from epilepsy against reception medicinal means is noted positive dynamics in the relation expressiveness of a depression and uneasiness, and also aggression, irritability decreases.

Impact on psychomotor indicators, cognitive functions has dozozavisimy character, is variable in each case.

At an epileptiform neuralgia (essential, secondary) decrease in frequency of painful attacks is noted.

At post-herpetic neuralgia, at posttraumatic paresthesias, tabes Carbamazepine promotes simplification of a neurogenic pain.

At alcoholic abstinence medicine allows to reduce expressiveness of the main symptomatology (a tremor of extremities, a hyperexcitability, gait disturbances), raises a threshold of convulsive readiness.

At patients with a diabetes mellitus drug reduces feeling of heat, diuresis, leads to fast compensation of a water balance.

The anti-maniacal (antipsychotic) effect is registered in 7-10 days of therapy, develops as a result of oppression of a metabolism of noradrenaline, a dopamine.

Use of the prolonged forms of carbamazepine allows to reach stable concentration of the main substance in blood, without registration of "failures" and "peaks".

Indications to Carbamazepine use

From what tablets are used usually? Drug is appointed at epilepsy: the mixed forms of attacks, generalized forms of attacks accompanied with toniko-clonic spasms, partial attacks. Medicine is applied at idiopathic neuralgia of a glossopharyngeal nerve, at an epileptiform neuralgia at patients with multiple sclerosis, at an idiopathic epileptiform neuralgia.

What indications to use of Carbamazepine exist still? The medicine is recommended for use at acute maniacal states (a combination therapy with antipsychotic means, lithium drugs). Medicine is appointed at a diabetic neuropathy with painful symptomatology, at a syndrome of alcoholic abstinence (hyper excitability, spasms, uneasiness, sleep disorders), at faznoprotekayushchy affective frustration, at not diabetes mellitus of the central genesis, at a polydipsia of neurohormonal genesis, a polyuria.

Medicine appoint at psychotic frustration (psychoses, schizoaffective and affective a rasstroystvanarusheniye of functions of limbic system, panic frustration), at obsessivno-compulsive frustration, at a syndrome of Klyuvera-Byyusi, at senile dementia, a sonitus, a dysphoria, alarm, somatization, a chorea, a depression, at multiple sclerosis, back to tabes, stump neuralgias, a diabetic polyneuropathy, acute idiopathic neuritis, a gemifitsialny spasm, Ekbom's syndrome, posttraumatic neuralgia, a neuropathy, for prevention of migraine, at post-herpetic neuralgia.

Contraindications

Carbamazepine is not applied at an atrioventricular block, at an acute form of the "alternating" porphyria, disturbance of marrowy blood circulation (a leukopenia, anemia), at intolerance of the main substance, hypersensitivity to tricyclic antidepressants. At an asset alcoholism, the HSN dekompensirovanny form, insufficiency of bark of adrenal glands, a hypothyroidism, a hypopituitarism, ADG hypersecretion syndrome, at a cultivation hyponatremia, at oppression of a marrowy hemopoiesis, with the increased intraocular pressure, a prostate hyperplasia, at pathology of renal system the medicine is appointed with care, estimating possible risks.

Side effects of Carbamazepine

Expressiveness of side effect has dozozavisimy character.

Nervous system: accommodation paresis, headaches, an adynamy, an ataxy, dizzinesses, are seldom noted abnormally involuntary movements (tics, dystonia, a tremor), paresthesias, peripheral neuritis, choreoathetoid frustration, disturbances of the speech, oculomotor disturbances, orofastsialny dyskinesia, a nystagmus, paresis symptoms, a myasthenia.

Mental spheres: activation of psychosis, disorientation, excitement, agressive behavior, concern, loss of appetite, depression, visual hallucinations, auditory hallucinations. Allergic reactions: skin itch, erythrosis, small tortoiseshell, photosensitivity, Lyell's disease, Stephens-Johnson's syndrome.

Bodies of a hemopoiesis: aplastic anemia, leukocytosis, thrombocytopenia, reticulocytosis, hemolitic anemia, limfoadenopatiya. Digestive tract: pancreatitis, stomatitis, a glossitis, pain in epigastriums, disturbances of a chair, a liver failure, jaundice, granulematozny hepatitis, increase of enzymes of a liver.

Cardiovascular system: an ischemic heart disease aggravation, aggravation of a current of HSN, an atrioventricular block with faints, bradycardia, instability of a blood pressure, disturbance of endocardiac conductivity, arrhythmia, a thromboembolic syndrome, thrombophlebitis. Metabolism, endocrine system: a giperprolaktinemiya, decrease in level of L-thyroxine, a hyponatremia, increase in body weight, puffiness, a liquid delay in an organism, a hypercholesterolemia, osteomalacy.

Urinogenital system: the speeded-up urination, disturbances in work to renal system, intersticial nephrite, decrease in a potentiality, a hamaturia, an oliguria, an albuminuria. Musculoskeletal system: spasms, mialgiya, arthralgia.

Sense bodys: change of perception of height of a sound, gipoakuziya, hyperacusia, sonitus, hearing disorder, conjunctivitis, cataract, disturbance of flavoring perception. Increase of sweating, an acne, purple, an alopecia, disturbance of a xanthopathy, a hirsutism is also possible.

Tablets Carbamazepine, application instruction (Way and dosage)

Drug is accepted inside, washing down with enough water. Tablets of long action (Carbamazepine Retard) do not chew, swallow entirely, twice a day.

At epilepsy medicine is appointed whenever possible as monotherapy. Treatment is recommended to be begun with small doses with gradual increase in a dosage that allows to achieve optimum result. The initial dosage for adults makes 100-200 mg 1-2 times a day, gradually the quantity of a medicine is increased.

Epileptiform neuralgia: the first day of therapy – 200-400 mg, with gradual increase to 400-800 mg a day, then gradually cancel the drug Carbamazepine.

The initial dosage at a pain syndrome of neurogenic genesis makes 100 mg twice a day, with increase of a dose each 12 hours before achievement of easing of pain. The supporting dosage makes 200-1200 mg a day, is counted on several receptions.

The average dosage at a syndrome of alcoholic abstinence makes 200 mg three times a day, at a serious condition the dose is increased to 400 mg three times a day.

In the first days of therapy it is recommended to appoint in addition chlordiazepoxide, klometiazol and other sedative hypnagogues.

At not diabetes mellitus appoint adult 200 mg 2-3 times a day.

At a diabetic neuropathy with a pain syndrome appoint 200 mg 2-4 times a day.

Prevention of schizoaffective and affective psychoses: 600 mg on 3-4 receptions a day.

The daily dose at bipolar, affective disorders, maniacal states leaves 400-1600 mg.

The application instruction Acre Carbamazepine is similar.

Overdose

It is shown by disturbances in work of respiratory, cardiovascular and nervous systems.

Sense bodys, nervous system: dysarthtia, unconscious states, disorientation, nystagmus, hyporeflexia, myoclonus, psychomotor frustration, spasms, mydriasis, hypothermia, disturbances of visual perception, hallucination, drowsiness, excitement.

Cardiovascular system: cardiac standstill, disturbance of intra ventricular conductivity, tachycardia, instability of arterial pressure.

Also the fluid lungs, respiratory depression, vomiting, nausea, decrease in motility of a large intestine, a delay of evacuation of food from a stomach, a hyponatremia, a liquid delay, an anury, an oliugriya, a metabolic acidosis, a hyperglycemia is noted.

The specific antidote is not developed. Treatment of overdose carry out posindromny.

Interaction

The metabolism of drug is carried out by means of CYP3A4 cytochrome. At co-administration with inhibitors of this cytochrome increase of its concentration is noted, and, respectively, expressiveness of side effects amplifies. Inductors of cytochrome accelerate metabolic processes, reduce the level of concentration of a medicine in blood, reducing expressiveness of its therapeutic influence.

Concentration of drug in blood is increased: Nikotinamid, Verapamil, Cimetidinum, fluvoksamin, Fluoxetine, Viloksazin, Dextropropoxyphene, Felodipin, Diltiazem, acetazoleamide, Desipramine, Danazol, Trefenadin, macroleads (troleandomitsin, Klaritromitsin, Dzhozamitsin, Erythromycin), azoles (Flukonazol, Itrakonazol, Ketokonazol), ritonavir, propoxyhair dryer, isoniazid, Loratadin.

Phenobarbital, Cisplatinum, Rifampicin, Theophylline, Fensuksimid, Metsuksimid, Primidonum, Phenytoinum, valproic acid, Valpromid, Clonazepam, Doxorubicine, Cisplatinum — also increase concentration of a medicine in blood.

Terms of sale

The recipe is necessary.

Storage conditions

In the place, dry, dark, unavailable to children, at a temperature no more than 25 degrees Celsius.

Period of validity

No more than three years.

Special instructions

Monotherapy of patients with epilepsy begins with small dosages with gradual accumulation of amount of drug for achievement of desirable effect. At a combination therapy determination of concentration of carbamazepine in plasma for selection of an optimum dosage is reasonable. At sharp cancellation of medicine epileptic attacks often are registered. In need of cancellation of carbamazepine of the patient try to transfer to other antiepileptic medicine. During therapy control over indicators of work of hepatic system, a condition of blood is required. At Carbamazepine the weak anticholinergic effect is noted that demands a constant control over an indicator of intraocular pressure. Medicine is capable to reduce productivity of oral contraceptives that demands use of additional methods for protection against pregnancy.

MNN: Carbamazepine.

Carbamazepine and alcohol

Drug is used for treatment of an abstinence syndrome after alcohol intake. Improves an emotional condition of the person. However, this treatment should be applied only in a hospital, and it is not recommended to use together these two means to avoid excessive stimulation of a nervous system.