Sulpirid Belupo (Sulpirid Belupo)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceSulpirideSulpiride
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    • Dosage form: & nbspCapsules.
    Composition:
    capsules 50 mg: one capsule contains
    active substance sulpiride 50 mg;
    Excipients: corn starch -31.0 mg, lactose monohydrate 29.0 mg, corn pregelatinized starch-7.2 mg, magnesium stearate-2.8 mg; capsule [titanium dioxide - 2%, gelatin - up to 100.0%].
    capsules 200 mg: one capsule contains
    active substance sulpiride 200 mg;
    Excipients: corn starch - 112.0 mg, lactose monohydrate -83.0 mg, magnesium stearate - 5.0 mg; lid capsule [titanium dioxide - 2%, gelatin - up to 100.0%], capsule body [indigocarmine FD & C blue 2 - 0.11%, titanium dioxide -1.10%, gelatin - up to 100.0%].
    Description:
    ATX: & nbsp

    N.05.A.L   Benzamides

    Pharmacodynamics:Sulpiride - an atypical neuroleptic from the group of substituted benzamides, has a moderate neuroleptic activity in combination with stimulating and thymoanaleptic (antidepressant) action. Neuroleptic effect is associated with antidophaminergic action. In the central nervous system (CNS) sulpiride blocks predominantly dopaminergic receptors of the limbic system, the effect on the neostriatic system is negligible. Has an antipsychotic effect and causes a small number of side effects. The peripheral action of sulpiride is based on oppression of presynaptic receptors. An increase in the amount of dopamine in the central nervous system is associated with an improvement in mood, with a decrease in the development of symptoms of depression.
    Antipsychotic effect of sulpiride is manifested in doses of more than 600 mg per day, in doses up to 600 mg per day, a stimulating and antidepressant effect predominates. Sulpiride has no significant effect on adrenergic, cholinergic, serotonin, histamine, and gamma-aminobutyric acid receptors (GABA receptors).
    Sulpiride stimulates the secretion of prolactin and has a central antiemetic effect (suppression of the vomiting center)
    Pharmacokinetics:
    Suction
    After oral administration, the maximum concentration of sulpiride in the plasma is reached after 3-6 hours. Bioavailability is 25-35% and is characterized by significant individual variability. The pharmacokinetics of sulpiride remain linear in the dosage range of 50 mg to 300 mg. Simultaneous intake of sulpiride with food reduces absorption by 30%.
    Distribution
    Sulpiride is rapidly distributed into tissues, the volume of distribution in the equilibrium state is 0.94 l / kg. Binding to plasma proteins is approximately 40%. Small amounts of sulpiride are excreted in breast milk and penetrate the placental barrier.
    Metabolism
    In the human body sulpiride poorly metabolized.
    Excretion
    It is excreted mainly by the kidneys in the unmodified form by glomerular filtration. The total clearance is 126 ml / min. The half-life of the drug from the plasma is 7 hours.

    Indications:
    Capsules 50 mg
    - anxious 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 with autism syndrome.
    Capsules 200 mg
    - acute psychotic disorders.
    - chronic psychotic disorders (schizophrenia, chronic non-schizophrenic delusions: paranoid nonsense, chronic hallucinatory psychosis).
    Contraindications:
    - Hypersensitivity to sulpiride or excipients of the drug
    - Children under 6 years (for capsules 50 mg)
    - Children under the age of 14 (for capsules 200 mg)
    - Prolactin-dependent tumors (prolactinomas of the pituitary gland and breast cancer)
    - Hyperprolactinemia
    - Pheochromocytoma or suspicion of pheochromocytoma
    - Acute intoxication with alcohol, hypnotics, narcotic analgesics
    - Breastfeeding period
    - Congenital galactosemia, glucose / galactose malabsorption syndrome or lactase deficiency (due to the presence of lactose in the formulation)
    - Simultaneous reception of levodopa (see the section "Interaction with other medicinal products")
    - Simultaneous administration of mechitazine, cabergoline, quinagolide, rotigotine, citalopram and escitalopram (cf.section "Interaction with other
    medicinal preparations ")
    Carefully:
    - In patients with a predisposition to the development of cardiac arrhythmias
    - with bradycardia less than 55 beats per minute;
    - with violations of electrolyte balance, in particular with hypokalemia;
    - with congenital lengthening of QT interval;
    - simultaneously receiving drugs that can cause a pronounced bradycardia (less than 55 beats per minute); hypokalemia; slowing of intracardiac conduction or prolongation of the QT interval, since sulpiride can cause prolongation of the QT interval and increase the risk of developing severe ventricular rhythm disturbances, including the development of pirouette ventricular tachycardia (see the sections "Interaction with other medicinal products", "Special instructions").
    - In patients with malignant neuroleptic syndrome in anemia (see the sections "Side effect", "Special instructions").
    - In the elderly (increased risk of sedation, orthostatic hypotension, extrapyramidal disorders).
    - Aggressive behavior or excitation 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 thromboembolism (see section "Special instructions").
    - With diabetes and in the presence of risk factors for the development of diabetes mellitus (the risk of hyperglycemia, blood sugar control is required).
    - In pregnancy (limited experience of use) (see section "Application during pregnancy and during breastfeeding").
    - With epilepsy or convulsive fits in the anamnesis (risk of lowering the threshold of convulsive alertness) (see section "Special instructions").
    - In case of renal insufficiency (correction of dosing regimen is required) (see section "Dosage and Administration").
    - With the simultaneous use of medicines containing ethanol (see section "Interaction with other medicinal products-
    mi ").
    - Against the background of therapy with neuroleptics, including the preparation of Sulpirid Belupo, there were leukopenia, neutropenia and agranulocytosis. Develop unexplained infections or increasebody temperature can be signs of blood disorders, which requires immediate hematological studies.
    - Patients with a history of glaucoma, intestinal obstruction, congenital stenosis of the digestive tract, delay in urination or prostatic hyperplasia (because 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).
    - When used in children, care should be taken because the efficacy and safety of sulpiride in this category of patients have not been adequately studied.
    Pregnancy and lactation:
    Experiments on animals have not revealed a teratogenic effect. There are very limited clinical data on the use of sulpiride by pregnant women, so the appointment of sulpiride to pregnant women is not recommended. Newborns, who during the third trimester of pregnancy were subjected to intrauterine exposure to antipsychotics,are at a high risk of developing adverse reactions, including extrapyramidal symptoms or withdrawal syndrome, which may differ in severity and duration (see "Side effect" section).
    There have been reported cases of agitation, muscle hypertension, muscle hypotension, tremor, drowsiness, respiratory distress or eating disorders, so newborns should be under constant medical supervision.
    Sulpirid penetrates into breast milk, so breastfeeding during treatment sulpiride should be discontinued.
    Dosing and Administration:
    Inside, before eating, squeezed a small amount of liquid. The daily dose is divided into several doses. It is not recommended to take the drug in the afternoon (after 16 hours) due to the increase in the level of wakefulness. In all cases, use the minimum effective dose of the drug. 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.
    Adults
    Short-term symptomatic treatment with ineffectiveness of conventional methods of treatment: The daily dose is 50 to 150 mg for no more than 4 weeks.
    Acute psychotic disorders, chronic psychotic disorders (schizophrenia, chronic non-schizophrenic delusions): The daily dose is 200-400 mg of sulpiride twice a day. If necessary, the dose may be increased to 1200 mg twice daily (the highest recommended dose is 2,400 mg).
    Children over 6 years old
    Severe behavioral disorders (agitation, self-mutilation, stereotypy), especially with autism syndrome: The daily dose is 5-10 mg / kg body weight.
    Doses for the elderly
    The initial dose of sulpiride should be 1/4 - 1/2 dose for adults.
    Doses in patients with impaired renal function
    Due to sulpiride is excreted from the body mainly through the kidneys, it is recommended to reduce the dose of sulpiride and / or increase the interval between taking individual doses of the drug depending on the creatinine clearance values:

    Clearance of the

    Dose

    Increase

    tin

    sulpi-

    Inter-

    (ml / min)

    a

    between

    compared

    receptions

    with

    sulpiri-

    standard-

    Yes

    (%)

    30-60 ml / min

    70

    1.5 times

    10-30 ml / min

    50

    2 times

    less than 10 ml / min

    30

    3 times
    Side effects:
    To indicate the frequency of side effects, the following classification is used, according to WHO: very often (> 1/10), often (> 1/100 and <1/10), infrequently (> 1/1000 and <1/100), rarely (> 1/10000 and <1/1000), very rarely (<1/10000), the frequency is unknown (can not be calculated from available data).
    The undesirable phenomena that develop as a result of the use of sulpiride are similar to undesirable phenomena caused by other psychotropic agents, but the frequency of their development is, in general, less.
    From the endocrine system: often: hyperprolactinemia.
    From the liver and bile ducts: often: increased activity of "liver" enzymes.
    From the nervous system: often: sedation, 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 is unknown: malignant neuroleptic syndrome, hypokinesia, tardive dyskinesia (after taking for more than 3 months,as well as when taking other neuroleptics, while taking antiparkinsonian drugs is ineffective or can provoke an increase in symptoms), seizures.
    From the cardiovascular system: infrequently: orthostatic hypotension; rarely: ventricular arrhythmias, ventricular fibrillation, ventricular tachycardia; frequency is unknown: prolongation of the QT interval, pirouette ventricular tachycardia, cardiac arrest, sudden death, venous thromboembolic complications, including pulmonary embolism and deep vein thrombosis, sometimes fatal; increase in blood pressure (see section "Special instructions").
    From the genitals and mammary glands: infrequently: enlargement of mammary glands, amenorrhea, orgasmic dysfunction, erectile dysfunction; often: soreness of the mammary glands, galactorrhea; frequency is unknown: gynecomastia.
    From the skin and subcutaneous tissues: often: maculopapular rash.
    Common violations: often: increase in body weight.
    From the side of the blood and lymphatic system: infrequently: leukopenia; frequency is unknown: neutropenia, agranulocytosis.
    From the side of the psyche: often: insomnia.
    From the gastrointestinal tract: infrequently: hypersalivation.
    From the immune system: frequency is unknown: anaphylactic reactions (hives, shortness of breath, excessive decrease
    arterial pressure, anaphylactic shock).
    From the side of the musculoskeletal and connective tissue: frequency is unknown: torticollis, trismus.
    Pregnancy, postpartum period and perinatal condition: frequency is unknown: the syndrome of "withdrawal" of the drug in newborns (see the section "Application during pregnancy and during breastfeeding").

    Overdose:
    Symptoms
    Experience with an overdose of sulpiride is limited. Specific symptoms are absent. There may be: dyskinesia with spastic torticollis, protruding tongue and trismus. Some patients have parkinsonism and coma syndrome. Sulpiride partially excreted in hemodialysis.
    Treatment
    Due to the absence of a specific antidote, symptomatic and supportive therapy should be used with careful monitoring of respiratory function and continuous monitoring of cardiac activity (risk of QT interval prolongation and development of ventricular arrhythmias), which should continue until the patient recovers completely.With the development of a pronounced extrapyramidal syndrome, anticholinergics are prescribed.

    Interaction:
    Contraindicated combinations

    - With levodopa: mutual antagonism of the effects of levodopa and neuroleptics.

    - With cabergoline, quinagolide, rotigotine: mutual antagonism between dopamine receptor agonists and neuroleptics.

    - With mechitazine, citalopram and escitalopram: increased risk of violations of the ventricular rhythm, in particular pirouette-ventricular arrhythmia.

    Unrecommended combinations

    - With ethanol: Ethanol increases the sedative effect of antipsychotics, so you should avoid drinking alcohol and medications containing ethanol.

    - With drugs that can prolong the QT interval or cause pirouette ventricular tachycardia:

    - drugs that cause bradycardia, such as beta-blockers; blocking the number of heartbeats blockers of "slow" calcium channels (verapamil, diltiazem); clonidine, guanfacine; cardiac glycosides;

    - drugs that cause hypokalemia, such as potassium-releasing diuretics; stimulating intestinal peristalsis laxatives; amphotericin B for intravenous administration;glucocorticosteroids; tetracosactide (before taking sulpiride hypokalemia should be adjusted);

    - antiarrhythmic drugs IA class (quinidine, disopyramide);

    - antiarrhythmic drugs of III class (amiodarone, sotalol);

    - other drugs such as pimozide; sultopride; haloperidol; thioridazine; methadone; antidepressants, imipramine derivatives; lithium preparations; beprideil; cisapride; intravenously administered erythromycin; intravenously administered wincamine; halofantrine; pentamidine; sparfloxacin.

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

    Interactions that need to be taken into account

    - With antihypertensive drugs: additive hypotensive effect, increased risk of orthostatic hypotension.

    - With drugs that depress the function of the central nervous system (narcotic analgesics, H1-histamine receptor blockers with sedative action, barbiturates, benzodiazepines and other anxiolytics; clonidine and other antihypertensive drugs of central action): possibly cumulative oppression of the central nervous system and decreased response.

    - With antacids and sucralfate: when combined, they reduce the absorption of sulpiride; when combined use of sulpiride and antacids or sucralfate requires at least a two-hour break between their intake.

    - With azithromycin, clarithromycin, roxithromycin: increased risk of violations of the ventricular rhythm, in particular pirouette ventricular arrhythmia; when combined, clinical and electrocardiographic monitoring of the patient's condition is necessary.
    Special instructions:Malignant neuroleptic syndrome
    Malignant neuroleptic syndrome is characterized by pallor, hyperthermia, rigidity of muscles, dysfunction of the autonomic nervous system, impaired consciousness. Signs of autonomic nervous system dysfunction, such as increased sweating and lability of blood pressure and pulse, may precede the onset of hyperthermia and, therefore, be 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 not ruled out. The development of the syndrome can contribute to intercurrent infection, dehydration or organic brain damage.
    QT interval extension
    Sulpiride can induce prolongation of the QT interval. It is known that this effect increases the risk of developing severe ventricular arrhythmias, such as pirouette ventricular tachycardia (see section "Side effect").
    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, retardation of intraventricular conduction and congenital long QT interval or prolongation of the QT interval with other drugs, extending the interval
    QT) (see "With caution", "Side effect").
    Caution is necessary for patients with the above-listed risk factors for the use of sulpiride. Hypokalemia, hypomagnesemia should be corrected before starting the use of the drug, in addition, medical supervision and constant monitoring of the electrolytes in the blood and ECG should be provided. Except for cases of urgent intervention, patients who require treatment with neuroleptics are advised to assess the condition and removal of the ECG.
    Extrapyramidal syndrome
    In extrapyramidal syndrome caused by neuroleptics, m-cholinoblocking drugs (rather than dopamine receptor agonists) should be used (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 complications. The mechanism of this risk is unknown. 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 for placebo, -2.6%. Although the causes of death in clinical studies with atypical antipsychotics varied, most of the causes of death were either cardiovascular (cardiac failure, sudden death), or infectious (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 fatal. 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 using sulpiride in patients with epilepsy, the latter should be under strict medical supervision.
    Patients with Parkinson's disease receiving dopamine receptor 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 taking 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
    patient of a malignant neuroleptic syndrome) (see sections "With care", "Interaction with other medicinal preparations").
    Patients with impaired renal function
    Use reduced dosages (see section "Method of administration and dose").
    Patients with diabetes mellitus or risk factors for developing diabetes mellitus
    Since the reported development of hyperglycemia in patients taking atypical antipsychotics, patients with a diagnosed diabetes mellitus or risk factors for its development, who are prescribed sulfide treatment, it is necessary to monitor the concentration of glucose in the blood.
    Ethanol
    Consumption of alcoholic beverages containing ethanol, or the use of medications containing ethanol, during treatment with sulpiride is strictly prohibited.
    Use in children
    In connection with the influence of sulpiride on cognitive processes in children, it is necessary to monitor the ability to learn annually. It is necessary to regularly adjust the dose taking into account the clinical condition of the child.
    Leukopenia, neutropenia and agranulocytosis
    It was reported on the development of leukopenia, neutropenia and agranulocytosis with the use of antipsychotic drugs.Unexplained infections or fever may be a manifestation of blood disorders and require immediate hematologic examination.
    Lactose
    Do not apply the drug to patients with lactase deficiency, intolerance to galactose and glucose-galactose
    malabsorption.
    Effect on the ability to drive transp. cf. and fur:During treatment with the drug Sulpirid Belupo, it is prohibited to drive vehicles and work with mechanisms requiring increased attention.
    Form release / dosage:
    Capsules 50 mg, 200 mg.
    Packaging:
    Capsules 50 mg
    For 15 capsules in PVC / Al blister. 2 blisters together with instructions for use in a cardboard bundle.

    Capsules 200 mg
    For 12 capsules in a white polypropylene bottle with a screw-on double-layered lid that has protection from children (such as "push-open"), a ring to control the first opening and a stamped top. 1 bottle with instructions for use in a cardboard box.
    Storage conditions:Store at a temperature not exceeding 25 ° C. Keep out of the reach of children!
    Shelf life:4 years.
    Terms of leave from pharmacies:On prescription
    Registration number:P N009371
    Date of registration:01.07.2008
    The owner of the registration certificate:Beluga, medicines and cosmetics.Beluga, medicines and cosmetics. Croatia
    Manufacturer: & nbsp
    Representation: & nbspBeluga, medicines and cosmetics. Beluga, medicines and cosmetics. Croatia
    Information update date: & nbsp31.08.2015
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