Beta max.

General characteristics. Structure:

Active ingredient: 50 mg, 100 mg or 200 mg of Sulpiridum.

Excipients: povidone, magnesium stearate, кросповидон, starch corn, cellulose microcrystallic.

Cover: dye of Opadray white 33G28707 (gipromelloza, lactoses monohydrate, macrogoal 3000, titanium dioxide, triacetin), karnaubsky wax.

Means with antipsychotic means.

Pharmacological properties:

Pharmacodynamics. Sulpiridum - atypical antipsychotic means (neuroleptic), renders also stimulating, antidepressive and antiemetic action. Antipsychotic action is caused by blockade of dopamine 02 receptors of mesolimbic and mesocortical system. Antipsychotic action is shown in doses more than 600 mg/days, in doses to 600 mg/days the stimulating and antidepressive action prevails.

Stimulates prolactin secretion, does not make considerable impact on adrenerg чес Kia, cholinergic, serotoninovy, histamine and GAMK receptors.

Antiemetic action is caused by blockade dopamine D2 receptors of a trigger zone of the emetic center. Peripheral action is based on oppression of presynaptic receptors.

At a peptic ulcer of a stomach and duodenum, having the selection effect on a hypothalamus, suppresses excitement of the centers of a sympathetic nervous system and improves blood supply of a stomach, increases secretion of slime in a stomach; accelerates proliferation of granulyatsionny fabric, creates the regenerated epithelium, improves proliferation of capillaries in fabrics.

Pharmacokinetics: After oral administration the maximum concentration in plasma are reached in 1,5-3 hours. Bioavailability of Sulpiridum at intake - 27%. Linkng of Sulpiridum with proteins of plasma makes less than 40%. Quickly gets into a liver and kidneys, more slowly - into brain tissues (the main amount of drug collects in a hypophysis). Concentration of Sulpiridum in the central nervous system makes 2 - 5% of concentration in plasma.

Sulpiridum is allocated with breast milk (0,1% of a daily dose).

Sulpiridum in a human body is not exposed to metabolism and is removed practically in not changed look through kidneys by glomerular filtering (92%). The general clearance - 126 ml/min. The elimination half-life makes about 7 hours. This size considerably increases at patients with a moderate and heavy renal failure (till 20 - 26 o'clock after intravenous administration). Such patients should lower a dose of Sulpiridum and/or to increase an interval between administration of drug.

Indications to use:

Beta max. should be accepted strictly on doctor's orders.
As monotherapy or in combination with other psychotropic drugs:

- acute and chronic schizophrenia;

- acute delirious states;

- depressions of various etiology;

- neurosises;

- dizziness of various etiology (vertebro-basilar insufficiency, vestibular neuritis, Menyer's disease, craniocereberal injury, average otitis);

- migraine;

- auxiliary therapy at a peptic ulcer of a stomach, duodenum and an irritable colon.

Route of administration and doses:

Accept inside in the first half of day (till 16-00), irrespective of meal, washing down with a small amount of liquid.

Acute and chronic schizophrenia, acute delirious psychosis: initial doses of the drug Beta max. depend on a clinical picture of a disease and make 600 - 1200 mg the day divided into several receptions; maintenance doses - 300 - 800 mg a day. The maximum recommended daily dose - 1600 mg.

Depression: from 150 - 200 mg to 600 mg the day divided into several receptions.

Neurosises: on 400-600 mg the day divided into several receptions.

Dizziness: 150 - 200 mg a day, at serious conditions a dose it is possible to increase to 300 - 400 mg. Duration of treatment has to be not less than 14 days.

Migraine: on 100 - 300 mg of drug a day.

Auxiliary therapy at a peptic ulcer of a stomach and duodenum, an irritable colon: on 150 mg of the drug Beta max. a day in 3 receptions, within 4-6 weeks.

Doses at patients with a renal failure: because Sulpiridum is brought out of an organism preferential through kidneys, it is recommended to reduce a dose of the drug Beta max. and/or to increase an interval between introduction of separate doses of drug depending on indicators of clearance of creatinine: at Cl of creatinine of 30-60 ml/min. the dose makes 70% from standard or by 1,5 times the interval between receptions increases; at Cl of creatinine of 10-30 ml/min. — 50% or twice; less than 10 ml/min. — 34% or by 3 times (a dose decline or increase in an interval between receptions respectively).

Doses for patients of advanced age: the initial dose of the drug Beta max. has to make ¼ - ½ doses for adults.

At pregnancy appoint low doses and it is not long.

Features of use:

At emergence during treatment of a hyperthermia drug should be cancelled (the hyperthermia is a sign of development of an antipsychotic malignant syndrome).

At purpose of drug at patients with epilepsy before an initiation of treatment it is necessary to conduct preliminary clinical and electrophysiologic survey as drug reduces a threshold of convulsive activity. At simultaneous treatment with the medicines increasing risk of development of ventricular arrhythmias regular control of an ECG is recommended.

Lengthening of a QT interval - dozozavisimy effect. The use of ethanol against the background of administration of drug is contraindicated.

During the period pregnancy Sulpiridum is appointed in cases when the doctor, having estimated a ratio of advantage and risk for the pregnant woman and a fruit, makes the decision that use of drug is necessary. At the same time it is recommended to limit a dose and duration of a course of treatment, as far as possible. Drug is contraindicated in the period of a lactation.

With care appoint at such sluchayakhyakh: epilepsy, arterial hypertension, a dysmenorrhea, a serious illness of heart, stenocardia, a liver failure, a malignant antipsychotic syndrome in the anamnesis, glaucoma, a prostate hyperplasia, an ischuria, advanced age.

It is necessary to observe precautionary measures at purpose of Sulpiridum to patients with a renal failure as to 95% of Sulpiridum it is removed through kidneys. These patients are recommended to reduce a drug dose.

It is also necessary to observe precautionary measures at purpose of Sulpiridum the patient with parkinsonism, to young women with an irregular menstrual cycle.

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions

Side effects:

The undesirable phenomena developing as a result of reception of Sulpiridum are similar to the undesirable phenomena, the caused other psychotropic drugs, but the frequency of their development, generally is less.

From endocrine system: development of a reversible giperprolaktinemiya most of which frequent manifestations are a galactorrhoea, disturbance of a menstrual cycle is possible, is more rare - a gynecomastia, impotence and frigidity. During treatment the increased perspiration, increase in body weight can be noted by Sulpiridum.

From the alimentary system: dryness in a mouth, heartburn, nausea, vomiting, locks, increase in activity of hepatic transaminases and the alkaline phosphatase (AP).

From the central nervous system (CNS): an extrapyramidal syndrome (usually meets at purpose of doses higher than 400 mg/days), a tremor, early and late dyskinesia (a spastic wryneck, oculomotor disturbances, a spasm of chewing muscles), an akathisia (disturbance of a pose of rest), sleeplessness, drowsiness, uneasiness, irritability, excitement, frustration of a dream, a headache, a malignant antipsychotic syndrome (pallor of integuments, vegetative frustration, a hyperthermia). At development of a hyperthermia drug should be cancelled!

From cardiovascular system: increase in the arterial pressure (AP), is rare - decrease in the ABP, orthostatic hypotension, dizziness, tachycardia, lengthening QT йнтервала, seldom, arrhythmia like "torsade de pointes".
Allergic reactions: skin rash, eczematic rashes, an itch are possible. Sight: visual acuity disturbances.

Interaction with other medicines:

At simultaneous use: with a levodopa efficiency of Sulpiridum decreases; with hypotensive medicines - their hypotensive action amplifies and the risk of development of orthostatic hypotension increases. With medicines, the oppressing TsNS (narcotic analgetics, somnolent and anxiolytic medicines (tranquilizers), a clonidine, antibechic medicines of the central action), their oppressing action amplifies.

Sukralfat, the antacids containing ^{Mg2 +} and/or ^A13+ reduce bioavailability of Sulpiridum by 20 - 40%.

Antagonism with agonists of dofaminergichesky receptors (амантадин, Apomorphinum, Bromocriptinum, каберголин, энтакапон, лизурид, перголид, piribedit, прамипексол, кинаголид, рошпшрол) and neuroleptics.

At the extrapyramidal syndrome induced by neuroleptics do not apply agonists of dofaminergichesky receptors, and use anticholinergic medicines.

In need of treatment of patients with Parkinson's disease against the background of use of agonists of dofaminergichesky receptors, the dose of the last should be lowered gradually to full cancellation (sharp cancellation can lead to development of a malignant antipsychotic syndrome).

At simultaneous use with sultopridy the risk of development of ventricular arrhythmias increases (including a ciliary arrhythmia).

The risk of development of ventricular arrhythmias like "torsade de pointes" increases at simultaneous use: - with antiarrhythmic Ia medicines of a class (quinidine, hydroquinidine, Disopyramidum) and the III class (Amiodaronum, соталол, dofetit, ибутилид), some neuroleptics (thioridazine, Chlorpromazinum, levomepromazinum, трифлуоперазин, циамемазин, амисульприд, тиаприд, a haloperidol, Droperidolum, Pimozidum);

- with the medicines causing bradycardia (diltiazem, verapamil, beta-blockers, a clonidine, гуанфацин, foxglove drugs, donepezil, ривастигмин, такрин, an ambenoniya chloride, Galantaminum, pyridostigmine, not awns гмин);

- with the medicines causing a hypopotassemia (kaliyvyvodyashchy diuretics, some laxatives, Amphotericinum In intravenously, glucocorticosteroids, тетракозактид);

- with others (including bepridit, цизаприд, difemanit, erythromycin intravenously, мизоластин, Vincaminum intravenously, галофантрин, pentamidine, спарфлоксацин, moxifloxacin).

Contraindications:

• Acute alcoholic poisoning, hypnagogues, narcotic analgetics;
• hypersensitivity to drug components;
• maniacal psychosis;
• convulsive attacks;
• Parkinson's disease;
• pheochromocytoma;
• prolaktinzavisimy tumors (including breast cancer);
• giperprolaktinemiya;
• affective frustration, agressive behavior;
• idiopathic hypertensia 2-3 stages;
• breastfeeding period;
• children up to 18 years.

Overdose:

Symptoms: dyskinesia (spasm of chewing muscles, spastic wryneck), extrapyramidal disturbances. In some cases - the expressed parkinsonism, a coma.

Treatment: symptomatic. Holinoblokatora of the central action.

Storage conditions:

In the dry place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 30 tablets in a bottle from plastic with the pressed-down cover and control of the first opening. On 1 bottle together with the application instruction in a pack from a cardboard.