Carbamazepine

Carbamazepine – drug with psychotropic, antiepileptic action.

Form of release and structure

Carbamazepine is produced in the form of tablets (on 10, 15, 25 pieces in blister strip packagings, on 1-5 packagings in a cardboard pack; on 20, 30 pieces in blister strip packagings, on 1, 2, 5, 10 packagings in a cardboard pack; on 20, 30, 40, 50, 100 pieces in bank, after 1 bank in a cardboard pack).

Is a part of 1 tablet:

• Active agent: carbamazepine – 200 mg;
• Auxiliary components: talc – 3,1 mg, K30 povidone – 14,4 mg, colloid silicon dioxide (aerosil) – 0,96 mg, polysorbate of 80 - 1,6 mg, potato starch – 96,64 mg, magnesium stearate – 3,1 mg.

Indications to use

• Epilepsy (except sluggish or myoclonic attacks, absentias epileptica) – for the second time and initially generalized forms of attacks which are followed by toniko-clonic spasms, partial attacks with simple and difficult symptomatology, the mixed forms of attacks (monotherapy or in a combination with other drugs with anticonvulsant action);
• Polyuria and polydipsia at not diabetes mellitus, a pain syndrome at diabetic polyneuropathy, an epileptiform neuralgia at multiple sclerosis, an idiopathic epileptiform neuralgia, an alcoholic abstinence syndrome, idiopathic glossopalatine neuralgia, affective frustration;
• Faznoprotekayushchy affective disturbances, including schizoaffective disorders, maniac-depressive psychosis, etc. (prevention).

Contraindications

• Atrioventricular block;
• Disturbance of a marrowy hemopoiesis;
• The acute alternating porphyria (including instructions in the anamnesis);
• Concomitant use with monoamine oxidase inhibitors and for 14 days after their cancellation;
• Pregnancy and period of a lactation;
• Hypersensitivity to drug components, and also to similar to active agent medicines (tricyclic antidepressants) in the chemical relation.

Carbamazepine should be applied with care along with alcohol intake, to elderly patients, and also the patients with the expressed heart failure, a cultivation hyponatremia raised by the intraocular pressure, oppression of a marrowy hemopoiesis against the background of reception of medicines (in the anamnesis), a prostate hyperplasia, a liver failure, a chronic renal failure.

Route of administration and dosage

Carbamazepine is accepted inside, washing down with a small amount of liquid. A pill can be taken irrespective of meal.

At treatment of epilepsy, in cases when it is possible, drug is appointed in the form of monotherapy. Administration of drug is begun with a small daily dose which is gradually increased further to optimum.

If antiepileptic therapy is already carried out, Carbamazepine needs to be attached gradually (depending on indications, doses of the medicines applied at the same time can be adjusted).

The initial adult dose makes 100-200 mg 1-2 times a day. In need of it slowly increase before achievement of optimum medical effect (as a rule, up to 400 mg 2-3 times a day). The maximum daily dose – 1600-2000 mg.

To children appoint the following mode of dosing:

• Up to 5 years: an initial daily dose – 20-60 mg, every other day gradually increase a dose by 20-60 mg;
• Of 5 years: an initial daily dose – 100 mg, every week gradually increase a dose by 100 mg.

Maintenance dose – 10-20 mg/kg a day for 2-3 receptions (to provide exact dosing at children up to 5 years it is necessary to apply liquid peroral dosage forms of drug to children).

According to other indications Carbamazepine is appointed:

• Epileptiform neuralgia: in the first day – 200-400 mg a day; the dose is gradually increased before the termination of a pain syndrome, but it is no more than on 200 mg a day (an average daily dose – 400-800 mg), then reduce to a minimal effective dose;
• Pain syndrome of neurogenic genesis: in the first day – 100 mg 2 times a day; before easing of pains the dose is increased no more than by 200 mg a day (increase on 100 mg is possible each 12 hours). The supporting daily dose – 200-1200 mg (in stages);
• The diabetic neuropathy which is followed by pains: an average dose – 200 mg 2-4 times a day. For prevention of a recurrence of schizoaffective and affective psychoses – 600 mg a day in 3-4 receptions;
• Not diabetes mellitus: an average adult dose – 200 mg 2-3 times a day. To children Carbamazepine is appointed according to the body weight and age of the child;
• Syndrome of alcoholic abstinence: an average dose – 200 mg 3 times a day; at a heavy current during the first several days it is possible to increase a single dose to 400 mg. At the beginning of therapy at the heavy phenomena of abstinence simultaneous use with medicines with sedative and somnolent action is recommended (klometiazoly, chlordiazepoxide);
• Acute maniacal states and affective (bipolar) frustration: a daily dose – 400-1600 mg (on average drug is accepted on 400-600 mg in 2-3 receptions). At acute disease the dose is increased quickly, at a maintenance therapy of affective frustration – gradually (for portability improvement).

To the elderly patient and patients with hypersensitivity Carbamazepine in an initial dose 2 times a day usually appoint 100 mg.

Side effects

During use of Carbamazepine development of the following side effects is possible:

• Central nervous system: ataxy, dizziness, general weakness, drowsiness, oculomotor disturbances, headache, nystagmus, accommodation paresis, tics, tremor, orofatsialny dyskinesia, choreoathetoid frustration, peripheral neuritis, dysarthtia, paresthesias, paresis, muscular weakness;
• Cardiovascular system: decrease or increase in arterial pressure, disturbance of endocardiac conductivity, a collapse, bradycardia, arrhythmias, an atrioventricular block with faints, development or aggravation of congestive heart failure, an exacerbation of coronary heart disease (including increase or emergence of attacks of stenocardia), a thromboembolic syndrome, thrombophlebitis;
• Alimentary system: dryness in a mouth, vomiting, nausea, a lock or diarrhea, an abdominal pain, stomatitis, a glossitis, pancreatitis;
• Urinogenital system: a renal failure, intersticial nephrite, a renal failure (a hamaturia, an albuminuria, an oliguria, azotemia/increase in urea), an ischuria, the speeded-up urination, impotences/disorders of sexual function;
• Endocrine system and metabolism: a hyponatremia, increase in body weight, hypostases, increase in level of prolactin (it is possible along with development of a galactorrhoea and gynecomastia); L-thyroxine lowering of the level (free T4, TZ) and increase in level of thyritropic hormone (as a rule, is not followed by clinical manifestations), osteomalacy, disturbances of calcium-phosphorus exchange in a bone tissue (decrease in concentration of 25-IT-cholecalciferol and the ionized calcium form in a blood plasma), a gipertriglitseridemiya, a hypercholesterolemia;
• Musculoskeletal system: arthralgia, spasms, mialgiya;
• Liver: increase in activity gamma глутамилтрансферазы (as a rule, has no clinical value), increase in activity of an alkaline phosphatase and "hepatic" transaminases, hepatitis (granulematozny, the mixed, cholestatic or parenchymatous (hepatocellular) type), a liver failure;
• Bodies of a hemopoiesis: thrombocytopenia, a leukopenia, a leukocytosis, an eosinophilia, a lymphadenopathy, aplastic anemia, the acute alternating porphyria, an agranulocytosis, megaloblastichesky anemia, a true erythrocyte aplasia, hemolitic anemia, a reticulocytosis;
• Sense bodys: changes of perception of height of a sound, a phacoscotasmus, disturbances of flavoring feelings, conjunctivitis, hypo - or a hyperacusia;
• Mental sphere: concern, hallucinations, appetite loss, depression, agressive behavior, disorientation, excitement, activation of psychosis;
• Allergic reactions: volchanochnopodobny syndrome, exfoliative dermatitis, small tortoiseshell, Stephens-Johnson's syndrome, erythrosis, toxic epidermal necrolysis, photosensitivity, knotty and multiformny erythema. Multiorgan reactions of hypersensitivity of the slowed-down type with the vasculitis, fever, a lymphadenopathy, skin rashes, an eosinophilia reminding a lymphoma the signs, a leukopenia, arthralgias changed by indicators of function of a liver and a gepatosplenomegaliya are possible (the specified manifestations can meet in various combinations). Involvement and other bodies, for example, of kidneys, lungs, a myocardium, a pancreas, a large intestine is possible. Very seldom – aseptic meningitis with a myoclonus, a Quincke's disease, anaphylactic reaction, the reactions of hypersensitivity of lungs which are characterized by short wind, fever, a pneumonitis or pneumonia;
• Others: purpura, disturbances of a xanthopathy, perspiration, acne, alopecia.

Special instructions

Before use of Carbamazepine it is necessary to conduct examination: the general analysis of urine and blood (including calculation of reticulocytes, thrombocytes), determination of level of iron, concentration of urea and electrolytes in blood serum. Further these indicators need to be controlled weekly for the first month of treatment, and then – once a month.

At purpose of Carbamazepine patients with the increased intraocular pressure need periodically to control it.

Therapy should be stopped at development of the progressing leukopenia or leukopenia which is followed by clinical symptoms of an infectious disease (not progressing symptomless leukopenia of cancellation of Carbamazepine does not demand).

During therapy it is necessary to be careful at control of motor transport and performance of other potentially dangerous types of the works demanding the increased concentration of attention and bystry psychomotor reactions.

Medicinal interaction

At simultaneous use of Carbamazepine with some medicines there can be undesirable effects:

• CYP3A4 inhibitors: increase in concentration of carbamazepine in a blood plasma;
• Dextropropoxyphene, verapamil, фелодипин, diltiazem, вилоксазин, fluoxetine, флувоксамин, desipramine, Cimetidinum, даназол, acetazoleamide, niacinamide (only in high doses at adults); macroleads (джозамицин, erythromycin, кларитромицин, тролеандомицин); azoles (кетоконазол, итраконазол, флуконазол), лоратадин, терфенадин, the isoniazid, grapefruit juice, the propoxyhair dryer applied at therapy of HIV inhibitors of virus protease: increase in concentration of carbamazepine in a blood plasma;
• Felbamat, фенсуксимид, phenobarbital, Primidonum, Phenytoinum, метсуксимид, theophylline, Cisplatinum, rifampicin, doxorubicine, it is possible: вальпромид, clonazepam, valproic acid, окскарбазепин and vegetable drugs with the maintenance of a St. John's Wort of made a hole (Hypericum perforatum): decrease in concentration of carbamazepine in a blood plasma;
• Valproic acid and Primidonum: replacement of carbamazepine from communication with proteins of plasma and increase in concentration pharmacological an active metabolite (carbamazepine-10,11-epoxide);
• Izotretinoin: change of bioavailability and/or clearance of carbamazepine and carbamazepine-10,11-epoxide (control of concentration in a blood plasma is necessary);
• Klobazam, clonazepam, Primidonum, an Ethosuximidum, to alprazola, valproic acid, glucocorticosteroids (Prednisolonum, dexamethasone), a haloperidol, cyclosporine, doxycycline, methadone, peroral drugs with the content of progesterone and/or estrogen (it is necessary to pick up alternative methods of contraception), theophylline, peroral anticoagulants (фенпрокумон, warfarin, дикумарол), топирамат, ламотриджин, tricyclic antidepressants (Imipraminum, нортриптилин, amitriptyline, кломипрамин), фелбамат, clozapine, тиагабин, inhibitors of proteases which are applied at treatment of HIV infection (ритонавир, индинавир, саквинавир), окскарбазепин, итраконазол, blockers of calcium channels (group of digidropiridon, for example, фелодипин), midazolam, left thyroxine, a praziquantel, олазапин, рисперидон, трамадол, ципразидон: decrease in their concentration in plasma (reduction or even full leveling of their effects, correction of the applied doses can be required);
• Phenytoinum: increase or decrease in its level in a blood plasma;
• Mephenytoinum: increase (in rare instances) of its level in a blood plasma;
• Paracetamol: increase in risk of its toxic impact on a liver and decrease in a therapeutic effectiveness (paracetamol metabolism acceleration);
• Fenotiazin, Pimozidum, thioxanthenes, молиндон, haloperidol, Maprotilinum, clozapine and tricyclic antidepressants: strengthening of the oppressing action on the central nervous system and easing of anticonvulsant effect of carbamazepine;
• Diuretics (furosemide, hydrochlorothiazide): development of the hyponatremia which is followed by clinical manifestations;
• Not depolarizing muscle relaxants (pankuroniya): decrease in their effects;
• Ethanol: decrease in its portability;
• Indirect anticoagulants, hormonal contraceptive drugs, folic acid: metabolism acceleration;
• Means for the general anesthesia (энфлуран, a halothane, Ftorotanum): acceleration of metabolism with increase in risk of development of gepatoksichny effects;
• Metoksifluran: strengthening of formation of nefrotoksichny metabolites;
• Isoniazid: strengthening of a hepatotoxic action.

Terms and storage conditions

To store in protected from light, the place, dry, unavailable to children, at a temperature up to 25 °C.

Period of validity – 2 years.