Benzonal

General characteristics. Structure:

Active ingredient: 100 mg of petrolbarbital (benzonal).

Excipients: potato starch, povidone, (polyvinylpirrolidone low-molecular medical), methyl cellulose, stearic acid.

Pharmacological properties:

Pharmacodynamics. Petrolbarbital belongs to derivatives of barbituric acid which is a basis of many hypnotic drugs, narcotic and anticonvulsants. Prepayorata of this group render anestetichesky, somnolent, sedative and protivosuyodorozhny effects. Barbiturates contact barbituratny receptors. What in turn exponentiates effects of GAMK (piperidic acid) and strengthens a flow of ions of chlorine through a neuron membrane, leading to its partial giyoperpolyarization and decrease in permeability. As a barbituratny receptor рас­положен near receptors of benzodiazepines and GAMK, barbiturates strengthen interaction of these connections with their receptors. Barbiturates cause the general oppression of functions of the central nervous system.

Petrolbarbital - antiepileptic means, has practically no snoyotvorny effect. Pharmacological action is caused by a metabolite - fenoyobarbitaly which strengthens brake GAMK-ergichesky influences in a tsentralyyony nervous system, especially in a thalamus, the ascending activating retikulyaryony formation of a brainstem at the level of internuncial neurons. Reducing a pronitsayeyomost of membranes of nerve fibrils for Na + (a sodium ion), reduces distribution of impulses from the center of epileptic activity. The effect occurs in 20-60 min. after oral administration. Petrolbarbital is the inductor of microsomal enzymes of a liver, reduces concentration of bilirubin in blood serum.

Pharmacokinetics. Absorption: petrolbarbital is quickly soaked up in a stomach. The maximum kontsenyotration in blood is reached in 1-3 hours after reception. Steady concentration in blood is established for the 3rd day. Therapeutic concentration in a blood plasma of 15-45 mg/l.

Distribution: communication with proteins of plasma - weak. It is evenly distributed in various bodies and fabrics. Creates high concentration in a brain, peyochen and kidneys. Gets through gistogematichesky barriers and into breast milk.

Metabolism: petrolbarbital in an organism is quickly metabolized mikrosomal-by ny enzymes of a liver, releasing phenobarbital which renders protivo-epileptic effect.

Removal: an elimination half-life (T 1/2) - 3-4 days. It is removed by kidneys, both in a neizyomenenny look, and in the form of metabolites.

Indications to use:

Convulsive syndrome, epilepsy of various genesis, all types of attacks.

- partial attacks;

- for the second time generalized attacks;

- toniko-clonic attacks;

- myoclonic attacks;

- attacks at Lennox-Gasto's syndrome;

- infantile spasms.

Route of administration and doses:

Inside, after food, 3 times a day. The dosing mode individual also naznachayotsya by the doctor. Treatment is begun with a single dose of a single dose. In 2-3 days gradually increase a dose before achievement of clinical effect (decrease in a chasyotota or complete cessation of attacks). Course of treatment continuous and dlitelyyony, not less than 2 years.

Single dose - 100 - 150 - 200 mg; the highest single dose of 300 mg, the highest daily doyoza - 800 mg.

For children of 7-10 years one-time - 50-100 mg, daily - 150-300 mg; 11-14 years razoyovy - 100 mg, daily - 300-400 mg; the highest single dose for children of the senior vozrasyot - 150 mg; the highest daily - 450 mg.

For children 7 years of a tablet with a dosage of 100 mg are younger are not used.

Features of use:

Pregnancy and lactation. Due to the penetration through a placental barrier and in breast milk does not sleyodut to use drug during pregnancy and a lactation. For the period of treatment не­обходимо to stop feeding by a breast.

- The withdrawal - resuming or utyazheleyony attacks is characteristic of barbiturates at the termination of administration of drugs. Upon transition to treatment by Benzonal at the patients who were earlier accepting other barbiturates the sleep disorder which is eliminated with appointment for night of phenobarbital (50 - 100 mg) or other somnolent medicines is possible. Now treatment of patients with epilepsy is begun with other antiepileptic means (valproic acid, carbamazepine, etc.) having less vyrazhenyony side effects. Petrolbarbital is appointed if these means not of an efyofektivna, are more often as a part of a combination therapy.

- With care it is necessary to apply at the patients abusing lekaryostvenny means or at instructions in the anamnesis on a medicinal zaviyosimost; at abnormal liver functions, acute or constant pains, nayorusheniye of function of kidneys, diseases of the respiratory organs which are followed by an asthma or obstruction of respiratory tracts, especially at the asthmatic status.

- At prolonged use damage of a liver is possible.

- The patients having hypersensitivity to one of barbiyoturat can have hypersensitivity to other barbiturates.

- It is not necessary to apply petrolbarbital along with griseofulvin. At simultaneous use monitoring of concentration of derivatives of hydantoin in a blood plasma is necessary.

- Development of medicinal dependence is possible. Weak intoxication of a barbiyoturatama, acute or chronic, reminds alcoholic intoxication. Simyoptoma include block, a diskoordination, difficulties in myshleyoniya, bad memory, a hypophrasia and understanding, disturbance of criticism, races - a tormazhivaniye of sexual aggressive impulses, narrowing of range of a vniyomaniye, emotional lability and a point of the main personal lines that in an effect can lead to development of suicide behavior. During treatment not to allow alcohol intake.

Influence on ability to manage vehicles and mechanisms. During treatment delay of speed of psychomotor reactions is observed. It is necessary to refrain from potentially dangerous types of activity, treyobuyushchy the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the central nervous system: drowsiness, slackness, delay of psiyokhichesky reactions, block, a headache, an ataxy, a nystagmus, difficulties of the speech (in these cases dose adjustment or purpose of caffeine is required).

From system of a hemopoiesis: thrombocytopenia, anemia.

From cardiovascular system: lowering of arterial pressure, thrombophlebitis.

Others: accustoming, medicinal dependence, syndrome of "cancellation", deterioration in appetite, allergic reactions, bronchospasm.

If any of the side effects specified in the instruction are aggravated, or you noticed any other side effects which are not specified in the instruction, report about it to the doctor.

Interaction with other medicines:

Strengthens effect of narcotic analgetics, medicines for the general anesthesia, neuroleptics, tranquilizers, tricyclic antidepressants, ethanol, hypnagogues, reduces - paracetamol, anticoagulants, tetracyclines, griseofulvin, glucocorticosteroids, mineralokortikoid, cardiac glycosides, quinidine, vitamin D, xanthines.

Contraindications:

Heavy renal failures and/or a liver, a chronic cordial nedostayotochnost of the II-IV functional class on NYHA, a porphyria, anemia, bronchial asthma, respiratory insufficiency, a diabetes mellitus, a thyrotoxicosis, nadpochechniyokovy insufficiency, hyperkinesias, depressions (with suicide attempts), hypersensitivity to petrolbarbital. Children up to 7 years.

Overdose:

Symptoms: oppression of functions of the central nervous system (drowsiness, a sight ukhudyosheniye, an ataxy, a dysarthtia, a nystagmus) up to a coma, oppression дыхательно­го the center, a lowering of arterial pressure, a renal failure, a headache, the expressed weakness, increase or fall of temperature of a body, excitement, narrowing of pupils, takhi-or bradycardia, cyanosis, hemorrhages in places a davleyoniya, a fluid lungs. At chronic intoxication - irritability, easing of ability to critical evaluation, a sleep disorder, confusion of consciousness.

Treatment: a gastric lavage, reception of absorbent carbon, the symptomatic and resuscitation therapy directed to recovery and maintenance of function of respiratory and cardiovascular system, the central nervous system, a pecheyona, kidneys.

Storage conditions:

According to rules of storage of strong substances. In the place protected from light at a temperature not above 25 °C. To store in the places unavailable to children. A period of validity - 4 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 100 mg. On 10 tablets in a blister strip packaging from a film poliyovinilkhloridny and a foil of aluminum or flexible packaging on the basis of an alyuminiyeyovy foil. 1, 2 or 5 blister strip packagings with the instruction on a primeneyoniya in a pack from a cardboard.