Betamax - instructions for use, dose, side effects, contraindications

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 receptors of the 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 action is due to blockade of dopamine D2 receptors in 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 reached after 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 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:

Acute psychotic disorders.

Chronic psychotic disorders (schizophrenia, chronic non-schizophrenic delusional states: paranoid nonsense, chronic hallucinatory psychosis).

Contraindications:

Hypersensitivity to sulpiride and / or excipients of the drug; acute alcohol poisoning, hypnotics,

narcotic analgesics; Prolactin-dependent tumors (prolactinomas of the pituitary gland and breast cancer); hyperprolactinemia; known pheochromocytoma or suspected 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 escitalopram; the period of breastfeeding; children's age till 18 years.

Carefully:

In patients with predisposition to the development of cardiac arrhythmias (with bradycardia less than 55 beats per minute; with violation of electrolyte balance, in particular with hypokalemia; with congenital lengthening of the QT interval; simultaneously receiving drugs that can cause pronounced bradycardia (less than 55 beats per minute), hypokalemia, slowing of intracardiac conduction or prolongation of the QT interval, since sulpiride may cause prolongation of the QT interval and increase the risk of developing severe ventricular arrhythmias, including the development of ventricular arrhythmias such as pirouettes);

in patients with a malignant neuroleptic syndrome in the anamnesis;

in the elderly (increased risk of sedation, orthostatic hypotension, extrapyramidal disorders); in the elderly with dementia;

aggressive behavior or excitation with impulsivity (can simultaneous use of sedatives);

in patients with risk factors for stroke;

in patients with Parkinson's disease;

in patients with risk factors for development thromboembolism, leukopenia, neutropenia, agranulocytosis;

in patients with intestinal obstruction;

at a diabetes and at presence of risk factors of development of a diabetes mellitus (risk of developing hyperglycemia, requires monitoring of blood sugar levels);

during pregnancy (limited experience of use);

with renal failure (correction of the dosing regimen is required);

with epilepsy or a convulsive fit in the anamnesis (risk of lowering the threshold of convulsive readiness);

with the simultaneous use of medicines containing ethanol.

Pregnancy and lactation:Experiments on animals and limited experience with the use of sulpiride by pregnant women have not revealed a teratogenic effect. Due to the limited data on the intake of the drug by pregnant women, the use of sulpiride during pregnancy is not recommended. If sulpiride still used during pregnancy, newborns should be monitored taking into account the safety profile of sulpiride. In humans sulpiride penetrates into breast milk, so the use of sulpiride during breastfeeding is contraindicated.

Dosing and Administration:BETAMAKS tablets are intended only for admission to adults. Is taken orally, without chewing, squeezed with 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.The daily dose is divided into several receptions and ranges from 200 to 1000 mg. It is not recommended to apply the drug in the afternoon (after 16 hours) due to the possible activating action of the drug.

Doses for the elderly

The initial dose of sulpiride should be 1 / 4-1 / 2 doses for adults.

Doses in patients with impaired renal function

Due to sulpiride is excreted primarily 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 the intervals between doses 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:

Undesirable effects caused by sulpiride are similar to undesirable phenomena caused by other neuroleptics, but their frequency of development is less.

From the nervous system: sedation, drowsiness, insomnia; Extrapyramidal disorders and related disorders, including:Parkinsonism (tremor, muscle hypertonia, hypokinesia and hypersalivation), acute dyskinesia and muscular dystonia (spasm, torticollis, oculogic crisis, trism), akathisia - these symptoms usually undergo a reverse development with simultaneous admission anticholinergic antiparkinsonian means; tardive dyskinesia, characterized by stereotyped involuntary rhythmic movements, mainly of the tongue and / or facial muscles (as well as after taking other neuroleptics for more than 3 months after ingestion, with anti-Parkinsonics not effective or may cause symptoms); convulsions; malignant neuroleptic syndrome, which is a potentially fatal complication and whose occurrence is possible with any neuroleptics.

From the cardiovascular system: orthostatic hypotension; arterial hypertension, arterial hypotension (when taking large doses); the prolongation of the QT interval and the occurrence of ventricular arrhythmias such as ventricular pirouette tachycardia, ventricular tachycardia,which can lead to the development of ventricular fibrillation or cardiac arrest, sudden death; thromboembolism, including pulmonary embolism (sometimes fatal) and deep vein thrombosis.

From the organs of hematopoiesis and lymphatic system: agranulocytosis, leukopenia, neutropenia.

From the digestive system: dry mouth, constipation.

On the part of the organs of vision: blurred vision.

From the liver and bile ducts: jaundice, increased activity of microsomal liver enzymes.

From the endocrine system: hyperprolactinemia.

From the immune system: hypersensitivity (pigmentation, urticaria, maculopapular rash, exfoliative dermatitis, photosensitivity reactions).

From the genitals and mammary glands: disorders associated with hyperprolactinaemia (galactorrhea,

amenorrhea, gynecomastia, breast enlargement, breast tenderness, orgasmic dysfunction and erectile dysfunction).

From the side of metabolism and nutrition: hyperglycemia, weight gain.

Pregnancy, postpartum period and condition of newborns: withdrawal syndrome in newborns whose mothers used antipsychotics during the third trimester of pregnancy.

With the sudden discontinuation of sulpiride, the development of withdrawal syndrome is possible, which is accompanied by the following symptoms: nausea, vomiting, increased sweating, insomnia, repetition of psychotic symptoms, voluntary movements (akathisia, dystonia, dyskinesia). Therefore, when discontinuing the use of sulpiride, doses should be reduced gradually.

Overdose:

Symptoms. Experience with an overdose of sulpiride is limited. Specific symptoms are absent, can be observed: dyskinesia with a specific torticollis, protruding tongue and trismus. In some patients, the syndrome of Parkinsonism and coma.

Treatment. Due to the absence of a specific antidote, symptomatic and supportive therapy should be used, with careful monitoring of respiratory function and constant monitoring of cardiac activity (risk of prolongation of the QT interval), which should continue until the patient fully recovered, with the development of a pronounced extrapyramidal syndrome, m-holin-blocking facilities

(biperidene). Sulpiride partially excreted in hemodialysis.

Interaction:

Contraindicated combinations: with levodopa, agonists of dopamine receptors (cabergoline, kinagolide and rotigotine) in connection with the mutual antagonism of effects.

Not recommended combinations: with ethanol (ethanol enhances the sedative effect of antipsychotics, so you should avoid taking alcoholic beverages and medicines containing ethanol); with drugs that can prolong the QT interval or cause a ventricular tachycardia such as "pirouette" (beta-blockers, verapamil, diltiazem, clonidine, guanfacine, digitalis preparations, potassium-deducing diuretics, laxatives, stimulating intestinal peristalsis, amphotericin B for intravenous administration, glucocorticosteroids, tetracosactide, Class IA antiarrhythmics, such as quinidine, disopyramide, antiarrhythmic drugs of the III class, such as amiodarone, sotalol, other drugs such as pimozide, sultopride, haloperidol, thioridazine, methadone, antidepressants, imipramine derivatives, lithium preparations, bepridil, cisapride administered intravenously erythromycin and wincamine, halofantrine, pentamidine, sparfloxacin, oral antibiotics (azithromycin, clarithromycin, roxithromycin)).

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

Interactions that need to be taken into account: with antihypertensive means (additive hypotensive effect, increased risk of orthostatic hypotension); with drugs that depress the function of the central nervous system (narcotic analgesics, antihistamines drugs, antidepressants (citalopram, escitalopram), H1-histamine receptor blockers with sedative action (mechitazine), barbiturates, benzodiazepines and other anxiolytics, clonidine and other antihypertensive agents of central action), since it is possible cumulative inhibition of the CNS and a decrease in the response; with antacids and sucralfate (reduce the absorption of sulpiride, requires at least a two-hour break between applications); with ropinirole (mutual antagonism); with lithium preparations (increase the risk of extrapyramidal disorders).

Special instructions:

Malignant neuroleptic syndrome (CNS)

ZNS is characterized by pallor, hyperthermia, rigidity of muscles, dysfunction of the autonomic nervous system, impaired consciousness. Signs of dysfunction of the autonomic nervous system (increased sweating and lability of blood pressure and pulse) may precede

offensive hyperthermia and, therefore, to be early, warning symptoms. In the case of an unexplained increase in body temperature, treatment with sulpiride should be stopped. The genesis of the development of the NSA 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 not included. Development of the NSA can be facilitated by intercurrent infection, dehydration or organic brain damage.

The elongation of the OT interval

Sulpiride can cause prolongation of the QT interval, which increases the risk of serious ventricular arrhythmias (ventricular pirouette tachycardia).

Before prescribing therapy with neuroleptics, if the patient's condition allows, it is necessary to exclude Availability factors predisposing to the development of these severe rhythm disturbances (bradycardia less than 55 beats per minute, hypokalemia, hypomagnesemia, slowing of intraventricular conduction and congenital elongated QT interval, or prolongation of the QT interval with the use of other drugs extending the QT interval). Patients with the above risk factors should be careful when sulpiride is needed. Hypokalemia should be adjusted before starting the drug, medical supervision, monitoring of blood electrolytes and ECG should be provided. Except for cases of urgent intervention, patients who require treatment with neuroleptics are advised to assess the condition and remove the ECG.

Extrapyramidal syndrome (EPS)

With EPS, caused by neuroleptics, should be prescribed anticholinergic drugs (rather than dopaminergic agonists).

Stroke

In elderly patients with dementia, a triple increase risk of 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 antipsychotic drugs there was an increase (1.6-1.7 times) of the risk of death in most cases due to heart failure or an infectious disease (pneumonia). When sulpiride was used, the risk of death in the elderly with dementia was 4.5%, with placebo 2.6%. As far as the increase in mortality is associated with the drug, and not with the characteristics of the patient itself is not clear.

Thromboembolism

With the use of antipsychotics, there have been cases of thromboembolism, sometimes fatal, so sulpiride should be used with caution in patients with risk factors for thromboembolism.

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 dopaminergic agonists

In exceptional cases, sulpiride 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 dopaminergic agonists, a gradual reduction of doses of the latter to complete cancellation should be made (a sharp cancellation of dopaminergic drugs may lead to ZNS).

Patients with impaired renal function

Lower doses should be used.

Patients with diabetes mellitus or with risk factors for diabetes mellitus

Since it was reported on the development of hyperglycemia in patients taking atypical antipsychotics, patients with an established diagnosis of diabetes mellitus or risk factors for its development, which begins treatment with sulpiride, it is necessary to monitor the level of sugar in the blood. The use of alcohol or the use of medications containing alcohol during the treatment with sulpiride is strictly prohibited.

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

Due to sulpiride has a sedative effect, it causes drowsiness and can slow down the psychomotor reactions, during the period of its use, risk-related work should be avoided, which requires dexterity and quick response (working with technical devices,management of vehicles, etc.).

Form release / dosage:

Tablets, film-coated, 50 mg, 100 mg and 200 mg.

Packaging:

For 30 tablets in a vial of plastic with a pressurized lid and control of the first autopsy.

1 bottle with instructions for use in a pack of cardboard.

Storage conditions:

Store in a dry place at a temperature of no higher than 25 ° C.

Keep out of the reach of children!

Shelf life:

2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N012795 / 01

Date of registration:21.06.2010

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

Manufacturer: & nbsp

GRINDEX, AO Latvia

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

Information update date: & nbsp26.08.2015

Illustrated instructions

Instructions

Betamax (Betamaks)