BETAMAX - instructions for use, doses, side effects, contraindications

Excipients: lactose monohydrate; methyl cellulose; starch potato; potato starch, dried; silicon dioxide colloidal, anhydrous; magnesium stearate; talc.

Description:

Round flat-cylindrical tablets of white or almost white color with a bevel.

Pharmacotherapeutic group:Antipsychotic agent (antipsychotic)

ATX: & nbsp

N.05.A.L Benzamides

Pharmacodynamics:

Sulpiride is an atypical antipsychotic agent (neuroleptic), it also has a stimulating, antidepressant and antiemetic effect.

The antipsychotic effect is due to the blockade of dopamine D2-receptor mesolimbic and mesocortical system. Antipsychotic effect manifests itself in doses of more than 600 mg / day, in doses up to 600 mg / day, the stimulating and antidepressant effect predominates.

Stimulates secretion of prolactin, does not significantly affect adrenergic, cholinergic, serotonin, histamine, and GABA receptors. Antiemetic effect due to blockade of dopamine D2 receptors of the trigger zone of the vomiting center. Peripheral action is based on oppression of presynaptic receptors. With peptic ulcer of the stomach and duodenum, having a selective effect on the hypothalamus, suppresses the excitation of the centers of the sympathetic nervous system and improves the blood supply of the stomach, increases the secretion of mucus in the stomach; accelerates the proliferation of granulation tissue, forms the regenerated epithelium, improves the proliferation of capillaries in tissues.

Pharmacokinetics:

After oral administration, the maximum plasma concentration is achieved in 3-6 hours and is 0.73 mg / l.Bioavailability of sulpiride for oral administration is 25-35%. The binding of sulpiride to plasma proteins is about 40%. Rapidly penetrates the liver and kidneys, more slowly - into the brain tissue (the main amount of the drug accumulates in the pituitary gland). The concentration of sulpiride in the central nervous system (CNS) is 2-5 % of the concentration in the plasma. Sulpiride is excreted in breast milk (0.1% of the daily dose).

Sulpiridum in the human body is not metabolized and is excreted virtually unchanged through the kidneys through glomerular filtration (92%). The total ground clearance is 126 ml / min. The half-life period (T1 / 2) is about 7 hours. This value is significantly increased in patients with moderate and severe renal disease insufficiency (up to 20-26 hours after intravenous administration). Such patients should lower the dose of sulpiride and / or increase the interval between taking the drug.

Indications:

Alarming conditions in adults (short-term symptomatic treatment with ineffectiveness of conventional methods of treatment).

Severe behavioral disorders (agitation, self-mutilation, stereotypy) in children older than 6 years, especially in combination with autism.

Contraindications:

- Hypersensitivity to sulpiride and / or excipients of the drug;

- Acute poisoning with alcohol, hypnotics, narcotic analgesics;

- Prolactin-dependent tumors (prolactinomas of the pituitary gland and breast cancer);

hyperprolactinemia;

- a known pheochromocytoma or a suspicion of it;

- acute porphyria:

- Congenital galactosemia, glucose-galactose malabsorption syndrome or lactase deficiency (due to the presence of lactose in the formulation);

- simultaneous application with levodopa, cabergoline, kinagolide and rotigotine;

- simultaneous application with mechitazine, citalopram and escitaloiram;

- the period of breastfeeding;

- Children under 6 years.

Carefully:

· In patients with a predisposition to the development of cardiac rhythm disorders due to the fact that sulpiride may cause lengthening of the interval QT and increase the risk of developing severe ventricular arrhythmias, including the development of ventricular arrhythmias such as pirouettes:

- with bradycardia less than 55 beats per minute;

- with violations of electrolyte balance, in particular with hypokalemia;

- with congenital lengthening of the interval QT;

- simultaneously receiving drugs that can cause a pronounced bradycardia (less than 55 beats per minute); hypokalemia; slowing of intracardiac conduction or lengthening of the interval QT (cm.sections "Interaction with other medicines", "Special instructions").

· In patients with a history of malignant neuroleptic syndrome (see the sections "Side effect", "Special instructions"),

· In elderly patients (increased risk of sedation, orthostatic hypotension, extrapyramidal disorders).

· Aggressive behavior or agitation with impulsivity (simultaneous use of sedatives may be required).

· In elderly patients with dementia (see section "Special instructions").

· In patients with risk factors for stroke (see section "Special instructions").

· In patients with Parkinson's disease (see section "Special instructions").

· In patients with risk factors for venous thromboembolic complications (see section "Special instructions").

· In diabetes mellitus and in the presence of risk factors for the development of diabetes mellitus (the risk of developing hyperglycemia, control of glucose in the blood is required);

· In pregnancy (limited experience of use) (see section "Pregnancy and the period of breastfeeding").

· With renal failure (correction of the dosing regimen is required,See section "Dosing and Administration").

· With epilepsy or convulsive fits in the anamnesis (the risk of lowering the threshold of convulsive alertness) (see section "Special instructions").

· With the simultaneous use of drugs containing ethanol (see section "Interaction with other drugs").

· Against the background of therapy with neuroleptics, including BETAMAX, leukopenia, neutropenia and agranulocytosis were noted. The development of unexplained infections or fever may be signs of blood disorders, which requires the immediate implementation of hematological studies.

· Patients who have a history of glaucoma, intestinal obstruction, congenital stenosis of the digestive tract, delayed urination or prostatic hyperplasia (since the drug has m-cholinoblocking properties).

· In patients (especially elderly patients) with arterial hypertension due to the risk of hypertensive crisis (patients should be under medical supervision).

Pregnancy and lactation:

Experiments on animals have not revealed a teratogenic effect.The person has very limited clinical data on the intake of sulpiride during pregnancy.

Due to the limited experience of taking the drug by pregnant women, the use of sulpiride during pregnancy is not recommended.

Newborns who were exposed to intrauterine exposure to antipsychotics during the third trimester of pregnancy, including BETAMAX, are at risk of developing unwanted reactions after birth, including extrapyramidal symptoms or withdrawal, which may vary in severity and duration (see "Side effect" "). There have been reports of agitation, muscle hypertension, muscle hypotension, tremor, drowsiness, respiratory distress, or eating disorders. Therefore, newborns should be under constant medical supervision.

Breastfeeding period

Sulpirid penetrates into the human breast milk. Therefore, breast-feeding during treatment with sulpiride is not recommended.

Dosing and Administration:

Apply inside, not liquid, squeezed a small amount of liquid, regardless of food intake.

In all cases, the minimum effective dose should be used. If the patient's clinical condition allows, treatment should begin with low doses.

The minimum effective dose is selected by gradually increasing the dose until the desired effect is achieved.

It is not recommended to apply the drug in the afternoon (after 16 hours) due to the possible activating action of the drug.

Disturbing conditions in adults: the daily dose is from 50 mg to 150 mg within 4 weeks as much as possible.

Severe behavioral disorders in children older than 6 years: the initial dose is 1-2 mg / kg / day, if necessary, it is possible to increase the dose to 5 mg / kg / day. Daily intake of the drug is divided into 2-3 identical doses. The maximum daily dose for children and adolescents should not exceed 10 mg / kg of body weight.

Doses for elderly patients

The initial dose of sulpiride should be ¼ - ½ dose for adults.

Doses for patients with impaired renal function

Due to sulpiride is excreted from the body mainly through the kidneys, it is recommended to reduce the dose and / or increase the interval between taking individual doses depending on the creatinine clearance: at a clearance of 30-60 ml / min, the dose should be reduced by 30%and intervals between doses of the drug should be increased by 1.5 times; at a clearance of 10-30 ml / min, the dose should be reduced by a factor of 2, and the intervals between doses should be increased 2-fold; with a clearance of less than 10 ml / min, the dose should be reduced by 70%, and the intervals between doses should be increased 3 times.

Side effects:

Classification of adverse reactions (HP) according to the frequency of development, according to the recommendations of the World Health Organization: very often (≥10%); often (≥1% and <10%); infrequently (≥0.1% and <1%); rarely (≥0.01% and <0.1%); very rarely (<0.01%); frequency is unknown (based on the available data it is impossible to estimate the frequency of HP development).

HP, caused by sulpiride, is similar to HP of other antipsychotics, but their frequency of development is generally less.

Heart Disease

Rarely: ventricular arrhythmias, ventricular fibrillation, ventricular tachycardia.

Frequency unknown: prolongation of the QT interval, ventricular pirouette tachycardia, cardiac arrest, sudden death.

Vascular disorders

Infrequently: orthostatic hypotension.

Frequency unknown: venous thromboembolic complications. Including thromboembolism of the pulmonary artery and deep vein thrombosis, sometimes fatal, increased blood pressure (see Fig.section "Special instructions").

Disorders from the endocrine system

Often: hyperprolactinemia.

General disorders

Often: increase in body weight.

Disturbances from the liver and bile ducts

Often: increased activity of "liver" enzymes.

Disturbances from the nervous system

Often: sedation or drowsiness, extrapyramidal disorders (these symptoms are usually reversible after the administration of antiparkinsonian drugs), parkinsonism, tremor, akathisia.

Infrequently: muscular hypertonia, dyskinesia, muscular dystonia.

Rarely: oculogic crisis.

Frequency unknown: malignant neuroleptic syndrome, hypokinesia, tardive dyskinesia (as with all antipsychotics for more than 3 months, while taking antiparkinsonian drugs is ineffective or can provoke an increase in symptoms), seizures.

Violations of the genitals and mammary glands

Often: morbidity of the mammary glands, galactorrhea.

Infrequently: increase of mammary glands, amenorrhea, orgasmic dysfunction (violations of orgasm), erectile dysfunction.

Frequency unknown: gynecomastia.

Disturbances from the skin and subcutaneous tissues

Often: maculopapular rash.

Violations of the blood and lymphatic system

Infrequently: leukopenia.

Frequency unknown: neutropenia, agranulocytosis.

Pregnancy, postpartum and perinatal conditions

Frequency unknown: extrapyramidal symptoms, the syndrome of "cancellation" in newborns (see the section "Pregnancy and the period of breastfeeding").

Immune system disorders

Frequency unknown: anaphylactic reactions (hives, shortness of breath, excessive lowering of blood pressure, anaphylactic shock).

Mental disturbance

Often: Insomnia.

Frequency unknown: confusion.

Disorders from the gastrointestinal tract

Infrequently: hypersalivation.

Disturbances from musculoskeletal and connective tissue

Frequency unknown: torticollis, trismus.

Disorders from the metabolism and nutrition

Frequency unknown: hyponatremia, syndrome of inadequate secretion of antidiuretic hormone.

Overdose:

Symptoms

Experience with an overdose of sulpiride is limited. Specific symptoms are absent,can be observed: dyskinesia with spastic torticollis, protruding tongue and trismus. In some patients - a life-threatening syndrome of parkinsonism and coma. Sulpiride partially excreted in hemodialysis.

Treatment. Due to the lack of a specific antidote, symptomatic and supportive therapy should be used, with careful monitoring of respiratory function and continuous monitoring of cardiac activity (the risk of lengthening the interval QT and the development of ventricular arrhythmias), which should continue until the patient's complete recovery, with the development of a pronounced extrapyramidal syndrome, m-cholinoblocking drugs are prescribed.

Interaction:

Contraindicated combinations

- With levodopa

Mutual antagonism of the effects of levodopa and neuroleptics.

- With dopamine receptor agonists (cabergoline, quinagolide, ropinirole, rotigotine)

Mutual antagonism between dopamine receptor agonists and neuroleptics (see "Contraindications", "Special instructions").

Unrecommended combinations

- With ethanol

Ethanol enhances the sedative effect of neuroleptics. Avoid taking alcoholic beverages and medicines containing ethanol.

- With drugs that can lengthen the interval QT or cause the development of ventricular tachycardia such as "pirouette":

- drugs that cause bradycardia: beta-blockers; blocking the heart rate blockers of "slow" calcium channels (verapamil, diltiazem); clonidine, guanfacine, cardiac glycosides;

- drugs that cause hypokalemia: diuretics that reduce the concentration of potassium in the blood: laxatives that stimulate intestinal motility: amphotericin B for intravenous use, glucocorticosteroids: tetracosactide (before the use of sulpiride, hypokalemia should be corrected);

- antiarrhythmic drugs IA class, such as quinidine, disopyramide;

- antiarrhythmic drugs III class, such as amiodarone, sotalol, dofetelide, ibutilide;

- other drugs such as pimozide; amisulpride; sultopride; tiapride; haloperidol; thioridazine; methadone: chlorpromazine; droperidol; cyamemazine; pipotiazine; sertindole; levomepromazine; antidepressants, imipramine derivatives; lithium preparations; beprideil; cisapride; intravenously administered erythromycin; intravenously administered wincamine, administered intravenously spiramycin; moxifloxacin; levofloxacin; misolastine; difemanyl; halofantrine; pentamidine; lumefantrine; sparfloxacin, azithromycin, clarithromycin, roxithromycin

selective serotonin reuptake inhibitors (citalopram, escitalopram).

If patients can not avoid the simultaneous administration of these drugs with sulpiride, then patients should conduct a thorough clinical, laboratory (control of electrolyte blood composition) and electrocardiographic observation.

Interaction, which should be taken into account

- With antihypertensive drugs, nitrates and nitrate derivatives Additive hypotensive effect, increased risk of orthostatic hypotension.

- With drugs that depress the function of the central nervous system: morphine derivatives (analgesics, antitussives); blockers H1-gistaminovyh receptors with sedative effect; barbiturates; benzodiazepines and other anxiolytics; hypnotics; antidepressants with sedative effect (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine); antihypertensive agents of central action clonidine and other antihypertensive drugs of central action); baclofen; thalidomide.

Perhaps a marked increase in the inhibitory effect of the central nervous system and a decrease in the psychomotor response.

- FROM antacids and sucralfate

With simultaneous use, the absorption of sulpiride is reduced. Therefore, with the simultaneous use of sulpiride and antacids or sucralfate, at least a two-hour break between their intake is required.

- FROM lithium preparations

The risk of extrapyramidal side effects increases. When the first symptoms of neurotoxicity should stop taking both drugs.

Special instructions:

Malignant neuroleptic syndrome

Malignant neuroleptic syndrome, which is a potentially lethal complication, and whose occurrence is possible with any neuroleptics, is characterized by pallor, hyperthermia, rigidity of muscles, dysfunction of the autonomic nervous system, impaired consciousness. Signs of dysfunction of the autonomic nervous system, such as increased sweating and lability of blood pressure and pulse may precede the onset hyperthermia and are early warning signs. In the case of an unexplained increase in body temperature, treatment with sulpiride should be stopped. The genesis of malignant neuroleptic syndrome remains unclear. It is assumed that its mechanism is played by the blockade of dopamine receptors in the striatum and the hypothalamus, and congenital predisposition (idiosyncrasy) is also not excluded. The development of the syndrome can contribute to intercurrent infection, dehydration or organic brain damage.

Interval lengthening QT

Sulpiride can cause lengthening of the interval QT. It is known that this effect increases the risk of developing severe ventricular arrhythmias, such as ventricular pirouette tachycardia (see "Side effect" section).

Before using the drug, if the patient's condition allows, it is necessary to exclude the presence of factors predisposing to the development of these severe rhythm disturbances (bradycardia less than 55 beats per minute, hypokalemia, hypomagnesemia, inhibition of intraventricular conduction and congenital elongated interval QT or lengthening the interval QT when using other drugs that extend the interval QT) (see the sections "With caution", "Side effect").

Patients with the above risk factors should be careful when sulpiride is needed. Hypokalemia and hypomagnesemia should be adjusted before the drug is started; In addition, medical supervision and constant monitoring of the electrolytes in the blood and ECG should be provided.

Except in cases of urgent intervention, patients who are required to be treated with antipsychotics are advised to assess the condition and remove the ECG.

Extrapyramidal syndrome

For extrapyramidal syndrome caused by neuroleptics, m-cholinoblocking drugs (rather than dopamine receptor agonists) should be prescribed (see section "Interaction with other drugs").

Stroke

In randomized clinical trials, compared with some atypical antipsychotics with placebo performed in elderly patients with dementia, there was a triple increase in the risk of developing cerebrovascular events. The mechanism of this risk is not known.It can not be ruled out that this risk increases with other neuroleptics or in other patient populations, so sulpiride should be used with caution in patients with risk factors for stroke.

Older patients with dementia

In elderly patients with psychoses associated with dementia, in the treatment of antipsychotic drugs, there was an increased risk of death. An analysis of 17 placebo-controlled trials (mean longer than 10 weeks) showed that the majority of patients who received atypical antipsychotics had a 1.6-1.7 times greater risk of death than patients receiving a placebo.

In a 10-week, placebo-controlled study, the incidence of fatal outcomes for atypical neuroleptics was 4.5% for these patients, and 2.6% for placebo. Although the causes of death in clinical studies with atypical antipsychotics varied, most of the causes of death were either cardiovascular (eg, heart failure, sudden death), or infectious (eg, pneumonia) by nature.Observational studies have confirmed that, like treating atypical antipsychotics, treatment with conventional antipsychotics can also increase mortality. The extent to which an increase in mortality may be due to an antipsychotic drug, rather than to certain features of patients, is unclear.

Venous thromboembolic complications

When using antipsychotic drugs, there have been cases of venous thromboembolic complications, sometimes lethal. therefore sulpiride should be used with caution in patients with risk factors for venous thromboembolic complications (see the sections "With caution", "Side effect").

Patients with epilepsy

Due to the fact that neuroleptics can lower the epileptogenic threshold, when sulpiride is prescribed to patients with epilepsy, the latter should be under strict medical supervision.

Patients with Parkinson's disease, receiving dopamine receptor agonists

In exceptional cases, this drug should not be used in patients with Parkinson's disease.If there is an urgent need for treatment with neuroleptics of patients with Parkinson's disease receiving dopamine receptor agonists, a gradual reduction in doses of the latter to complete cancellation should be made (the abrupt withdrawal of dopamine receptor agonists may increase the risk of developing a malignant neuroleptic syndrome in the patient) (see "With caution" "Interaction with other drugs").

Patients with impaired renal function

Lower doses should be used (see section "Method of administration and dose").

Patients with diabetes mellitus or with risk factors for diabetes mellitus As it has been reported on the development of hyperglycemia in patients taking atypical antipsychotics, patients with an established diagnosis of diabetes mellitus or with risk factors for its development, who are prescribed sulfide treatment, it is necessary to monitor the concentration of glucose in the blood.

The use of ethanol

Consumption of alcoholic beverages containing ethanol, or the use of medicinal products containing ethanol, during treatment with BETAMAX is strictly prohibited.

Effect on the ability to drive transp. cf. and fur:

During the treatment with BETAMAKS it is prohibited to drive vehicles and engage in other potentially hazardous activities requiring attention and speed of psychomotor reactions (since, even in recommended doses, the drug may cause sedation).

Form release / dosage:

Tablets 50 mg.

Packaging:

For 10 tablets in a planar cell packaging made of polyvinylchloride film and aluminum foil.

By 3 contour squares with instructions for use in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-004197

Date of registration:17.03.2017

Expiration Date:17.03.2022

The owner of the registration certificate:GRINDEX, JSC GRINDEX, JSC Latvia

Manufacturer: & nbsp

Grindeks, JSC Latvia

Representation: & nbspGrindeks Rus, Open CompanyGrindeks Rus, Open CompanyRussia

Information update date: & nbsp13.04.2017

Illustrated instructions

Instructions

BETAMAKS (Betamaks)