Prosulfin® (Prosulpin®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
Read on
Active substanceSulpirideSulpiride
Similar drugsTo uncover
  • Betamax
    pills inwards 
    GRINDEX, JSC     Latvia
  • BETAMAKS
    pills inwards 
    GRINDEX, JSC     Latvia
  • Prosulfin®
    pills inwards 
    PRO.MED.CS Prague as.     Czech Republic
  • Sulpiride
    pills inwards 
    ORGANICS, JSC     Russia
  • Sulpiride
    solution inwards 
    Rosemont Pharmaceuticals Ltd.     United Kingdom
  • Sulpiride
    solution w / m 
    ORGANICS, JSC     Russia
  • Sulpirid Belupo
    capsules inwards 
    Beluga, medicines and cosmetics.     Croatia
  • Eglonil®
    solution w / m 
    Sanofi-Aventis France     France
  • Eglonil®
    pills inwards 
    Sanofi-Aventis France     France
  • Eglonil®
    pills inwards 
    Sanofi-Aventis France     France
  • Eglonil®
    capsules inwards 
    Sanofi-Aventis France     France
    • Dosage form: & nbspPills.
    Composition:
    Composition per one tablet
    Active substance:
    Sulpiride 50 mg 200 mg
    Excipients:
    Potato starch 60.25 mg 54.00 mg
    Lactose Monohydrate 22,50 mg 22.00 mg
    Silica colloidal dioxide 7.50 mg 11.40 mg
    Gipromellose K4M 6.75 mg 3.30 mg
    Hypromellose K15M - 3.30 mg
    Magnesium stearate 2.00 mg 4.00 mg
    Talc 1.00 mg 2.00 mg
    Weight of tablet: 150.00 mg 300.00 mg
    Description:Round, flat tablets are white or almost white with a risk on one side.
    Pharmacotherapeutic group:Antipsychotic agent (antipsychotic).
    ATX: & nbsp

    N.05.A.L   Benzamides

    Pharmacodynamics:
    Sulpiride is an atypical neuroleptic from the group of substituted benzamides. Has moderate neuroleptic activity in combination with stimulating and thymoanaleptic (antidepressant) action.
    Neuroleptic effect is associated with dopamine-blocking action. Sulpiride blocks in the central nervous system (CNS) predominantly dopaminergic receptors of the limbic system, slightly affecting them in the neostriatic system.
    In addition, when taken in low doses sulpiride also has an activating CNS action, simulating a dopaminomimetic effect.
    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. The peripheral action of sulpiride is based on oppression of presynaptic receptors. With an increase in the content of dopamine in the central nervous system, the improvement in mood is associated with a decrease in the development of symptoms of depression. Sulpiride has no significant effect on adrenergic, cholinergic, serotonin, histamine, and GABA receptors.Stimulates the secretion of prolactin and has a central antiemetic effect (suppression of the vomiting center) due to blockade of dopamine D2 receptors in the trigger zone of the vomiting center.
    Pharmacokinetics:
    When administered to one tablet containing 200 mg of sulpiride, the maximum concentration of sulfiride in the blood plasma (Cmax) is reached after 3-6 hours, and is 0.73 mg / L and 0.25 mg / L with a single tablet containing 50 mg .
    The biological availability of medicinal forms intended for oral administration is about 25-35%, and is characterized by a significant individual variability. Sulpiride has linear kinetics after taking doses in the range of 50 mg to 300 mg. Sulpiride quickly diffuses into the tissues of the body: the volume of distribution in the equilibrium state is 0.94 l / kg.
    Binding to blood plasma proteins -approximately 40%; the drug penetrates into erythrocytes through passive diffusion, its concentration in blood plasma and erythrocytes are commensurable. The concentration of sulpiride in the cerebrospinal fluid is low, and averages about 13% (4-29%) of the serum concentration. Sulpiride quickly penetrates the liver and kidneys, more slowly - in the brain tissue (the main amount of the drug accumulates in the pituitary and hypothalamus). The concentration of sulpiride in the central nervous system is 2-5% of the concentration in the blood plasma. Sulpiride penetrates the placental barrier; a small amount appears in breast milk. In the human body sulpiride only to a small extent is metabolized and excreted by the kidneys by glomerular filtration in an almost unchanged form (92%), and the remainder is eliminated with excrement. The plasma half-life (T1 / 2) is 7 hours. With breast milk, 0.1% of the daily dose is excreted. The total plasma clearance of sulpiride reaches 90-210 ml / min, with renal clearance reaching a bit lower values ​​than the total plasma clearance.
    Indications:
    Tablets 50 mg:
    - severe behavioral disorders (agitation, self-mutilation, stereotypy) in children over the age of 6, especially in combination with autism syndrome;
    - anxious conditions in adults - short-term symptomatic treatment with ineffectiveness of conventional methods of treatment.

    Tablets 200 mg:
    - 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;
    - Prolactin-dependent tumors (prolactinomas of the pituitary gland and breast cancer);
    - hyperprolactinemia;
    - acute intoxication with alcohol, hypnotics, narcotic analgesics;
    - pheochromocytoma;
    - acute porphyria;
    - lactation period;
    - age to 18 years (for tablets 200 mg);
    - children's age till 6 years (for tablets 50 mg);
    - simultaneous reception with levodopa;
    - simultaneous use with dopamine receptor agonists (cabergoline, quinagolide, etc.), except for patients with Parkinson's disease;
    - simultaneous application with mechitazine, citalopram and escitalopram;
    - Congenital galactosemia, glucose-galactose malabsorption or lactase deficiency (due to the presence of lactose in the formulation).
    Carefully:
    - For patients:
    -with heart failure, stenocardia, arterial hypertension, severe bradycardia (less than 55 bpm);
    with congenital elongation of the QT interval;
    - with violations of electrolyte balance, in particular with hypokalemia;
    - at the same time taking drugs that can cause:
    - expressed bradycardia (less than 55 bpm): β-adrenoblockers: anaprilin, etc .; blockers of "slow" calcium channels: diltiazem and verapamil; clonidine; glycosides of digitalis;
    hypokalemia: hypokalemic diuretics; stimulant laxatives; intravenously administered amphotericin B; glucocorticoids; tetracosactide;
    - slowing of intracardiac conduction or lengthening 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 torsades de pointes: antiarrhythmic drugs of the IA class (quinidine, hydroquinidine, disopyramide) and antiarrhythmic drugs of III class (amiodarone, sotalol, dofetilide, ibutilide); some antipsychotics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, tiapride, pimozide, haloperidol, droperidol); other drugs, such as: bepridil, cisapride, difemanyl, administered intravenously erythromycin, misolastine administered intravenously wincamine, halofantrine, pentamidine, sparfloxacin. moxifloxacin; oral antibiotics (azithromycin, clarithromycin, roxithromycin) (see the sections "Interaction with other drugs", "Special instructions");
    -with a malignant neuroleptic syndrome in the anamnesis (see sections "Side effect", "Special instructions");
    -with aggressive behavior or excitation with impulsivity (simultaneous use of sedatives may be required);
    -in epilepsy or with convulsive seizures in the anamnesis (risk of lowering the threshold of convulsive readiness, see section "Special instructions");
    - with risk factors for stroke (see section "Special instructions");
    - with risk factors for venous thromboembolic complications (see section "Special instructions");
    - with Parkinson's disease (see sections "Special instructions", "Interaction with other medicinal products"); with intestinal obstruction.
    Precautions should also be observed when using sulfirid in patients:
    - the elderly (increased risk of sedation, orthostatic hypotension, extrapyramidal disorders);
    - elderly people with dementia (see section "Special instructions");
    - at a diabetes and at presence of risk factors of development of a diabetes (risk of development of a hyperglycaemia: the control of level of sugar in blood is required);
    - at a closed angle glaucoma;
    - with hyperplasia of the prostate;
    - with pyloric stenosis;
    - with retention of urine;
    - with renal failure (correction of the dosing regimen is required, see the sections "Dosing and Administration", "Special instructions");
    - at pregnancy (the limited experience of application, see sections "Application at pregnancy and in the period of thoracal feeding", "Special instructions");
    - while taking medications containing ethanol (see section "Interaction with other drugs").
    Pregnancy and lactation:
    Limited experience in the use of sulpiride by pregnant women has not revealed a teratogenic effect of sulpiride. In connection with the lack of clinical data on the use of the drug in pregnant women, taking sulpiride during pregnancy is not recommended.

    If sulpiride all the same it was used during pregnancy, it is necessary to carry out constant medical supervision of the state of newborns who underwent intrauterine exposure to sulpiride.In newborns born to mothers who have been treated with neuroleptics, especially during the third trimester of pregnancy, there is a risk of developing adverse reactions that vary in severity and duration after delivery, including extrapyramidal symptoms and / or withdrawal symptoms. They note the development of agitation, muscular hypertonicity, hypotension, tremor, drowsiness, respiratory distress, violation of the feeding process (see sections "Side effect", "Special instructions"). Sulpiride penetrates into breast milk. The use of the drug during breastfeeding is contraindicated (see section "Contraindications").
    Dosing and Administration:
    Inside, washed down with a small amount of water, 1-3 times a day, regardless of food intake.
    In all cases, the minimum effective dose of the drug should be given. If the patient's clinical condition allows, treatment should begin with low doses. The minimum effective dose of the drug 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 mg to 1000 mg.It is not recommended to take the drug in the afternoon (after 16 hours) due to the possible activating action of the drug.
    50 mg tablets
    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.
    Disturbing conditions in adults: the daily dose is from 50 mg to 150 mg for 4 weeks as much as possible.
    Tablets 200 mg
    Acute and chronic psychotic disorders: the daily dose is from 200 mg to 1000 mg, divided into several doses.
    Doses for elderly patients: the initial dose should be 1 / 4-1 / 2 doses for adults.
    Doses for patients with impaired renal function: due to the fact that up to 92% of sulpiride is excreted from the body mainly through the kidneys, it is recommended to reduce the dose of sulpiride and / or to increase the interval between taking individual doses of the drug depending on the creatinine clearance (CC) values. When QC is 30-60 ml / min, the dose of sulpiride should be reduced by 30%and intervals between the methods of the drug increase by 1.5 times; with KK 10-30 ml / min dose of sulpiride should be reduced by 50%, and the intervals between doses of the drug to increase by 2 times; with CC less than 10 ml / min, the dose of sulpiride should be reduced by 70%, and the intervals between doses of the drug should be increased 3 times.
    Side effects:
    Adverse events that develop as a result of sulpiride. are similar to undesirable phenomena caused by other neuroleptics, but their frequency of development is less.
    From the cardiovascular system:
    Hypertension, hypotension (with high doses), orthostatic hypotension; prolongation of the QT interval, ventricular arrhythmias, such as torsades de pointes, and ventricular tachycardia, which can lead to ventricular fibrillation or cardiac arrest, sudden death; venous thromboembolic complications, including pulmonary embolism, sometimes fatal, deep vein thrombosis (see section "Special instructions").
    From the central nervous system: sedation, drowsiness, insomnia; extrapyramidal disorders and related disorders: symptoms of parkinsonism with the manifestation of tremor, hypokinesia (bradykinesia, amyemia), muscular hypertonia,vegetative disorders (hypersalivation, excessive sweating); acute dyskinesia (spasmodic torticollis, spasm of chewing musculature, oculogic crisis, trism), dystonia, akathisia. These symptoms are usually reversed with simultaneous administration of m-cholinoblocking antiparkinsonian drugs; tardive dyskinesia, characterized by stereotyped involuntary rhythmic movements, mainly of the tongue and / or facial muscles (as well as after taking other antipsychotics with long courses of treatment for more than 3 months), while the use of m-holinoblocking antiparkinsonian drugs is not effective or can cause worsening of symptoms; convulsions.
    From the endocrine system: hyperprolactinemia.
    From the genitals and mammary glands: disorders associated with hyperprolactinemia (galactorrhea, amenorrhea, gynecomastia, breast enlargement, breast tenderness, orgasmic and erectile dysfunction).
    From the side of metabolism and nutrition: hyperglycemia, weight gain.
    From the digestive system: dry mouth, constipation.
    From the immune system: allergic reactions.
    From the side of the blood and lymphatic system: leukopenia, neutropenia, agranulocytosis.
    On the part of the organs of vision: blurred vision.
    From the liver and bile ducts: Cholestatic hepatitis, increased activity of microsomal liver enzymes (especially transaminases).
    Pregnancy, postpartum and perinatal conditions: withdrawal syndrome in newborns who were born from mothers who received therapy with neuroleptics during the third trimester of pregnancy.
    Other: malignant neuroleptic syndrome (CNS), which is a fatal complication, and the occurrence of which is possible with the use of any antipsychotics (see sections "With caution", "Special instructions").
    Overdose:
    The experience of an overdose of sulpiride is limited. In case of overdose or poisoning, it is necessary to take into account the possibility of combined intoxication associated with the simultaneous administration of sulpiride with other medications. To date, cases of intoxication after taking one dose in a volume of 1-3 g of sulpiride are described.The following symptoms were registered: anxiety, impaired consciousness, extrapyramidal syndrome. After taking 3-7 g, they noted agitation, confusion, development of extrapyramidal disorders. Doses in excess of 7 g, in some cases caused someone and a sharp drop in blood pressure. Treatment
    Due to the absence of a specific antidote, symptomatic and supportive therapy should be used with careful and constant monitoring of respiratory and cardiac activity (risk of prolongation of the QT interval), which should continue until the patient fully recovers.
    With the development of a pronounced extrapyramidal syndrome, we designate holin-blocking drugs (biperidene).
    Ulpirid is partially excreted in hemodialysis.
    Interaction:
    Contraindicated combinations
    - with levodopa
    Mutual antagonism of the effects of levodopa and neuroleptics.
    - with dopamine receptor agonists (cabergoline, quinagolide, etc.).
    In exceptional cases, sulpiride It 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,should gradually reduce the doses of the latter until complete cancellation (the abrupt withdrawal of dopaminergic drugs may increase the risk of the patient's ZNS).
    Not recommended combinations
    - with ethanol
    Ethanol enhances the sedative effect of neuroleptics. Avoid taking alcoholic beverages and medications containing ethanol.
    - with drugs that can extend the QT interval or cause a ventricular torsades de pointes tachycardia:
    - Bradycardia-mediated drugs, such as β-blockers; blocking the number of heartbeats blockers of "slow" calcium channels (verapamil, diltiazem); clonidine, guanfacine; cardiac glycosides;
    - causing hypokalemia drugs, such as potassium-withdrawing diuretics; stimulating intestinal peristalsis laxatives; intravenously administered amphotericin B; glucocorticoid steroids; tetracosactide (before the use of sulpiride, hypokalemia should be corrected);
    - antiarrhythmic drugs IA class (quinidine, hydroquinidine, disopyramide);
    - antiarrhythmic drugs of III class (amiodarone, sotalol, dofetilide, ibutilide);
    - antidepressants, imipramine derivatives (desmethylimipramine, chlorimipramine, etc.);
    - some antipsychotics (thioridazine, sultopride, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, tiapride, haloperidol, droperidol, pimozide);
    - other drugs such as methadone, bepridil, cisapride, difemanyl, misolastine administered intravenously erythromycin, administered intravenously wincamine; halofantrine, pentamidine, sparfloxacin, moxifloxacin; oral antibiotics (azithromycin, clarithromycin, roxithromycin).
    If patients can not avoid the simultaneous appointment of these drugs with sulpiride, then patients need to establish a thorough clinical, laboratory (control of electrolyte blood composition) and electrocardiologic monitoring.
    Combinations that should be taken into account
    - with antihypertensive drugs
    Additive hypotensive effect and increased risk of orthostatic hypotension.
    - with drugs that depress the central nervous system (CNS): narcotic analgesics, antidepressants (citalopram, escitalopram), antitussive drugs; barbiturates; benzodiazepines and other anxiolytics; hypnotics, blockers of H1-histamine receptors with sedative effect; clonidine and other antihypertensive drugs of central action
    Perhaps cumulative inhibition of the central nervous system and a decrease in response.
    - lithium preparations
    Increase the risk of extrapyramidal disorders.
    - with sucralphate and antacid preparations containing Mg2 and / or Al3 +
    With simultaneous use reduce the bioavailability of sulpiride. Sulpiride should be prescribed two hours before they are taken.
    - with ropinirole
    Mutual antagonism.
    Special instructions:
    Malignant neuroleptic syndrome
    Malignant neuroleptic syndrome is characterized by pallor, hyperthermia, muscle rigidity, dysfunction of the autonomic nervous system, impaired consciousness. Signs of autonomic nervous system dysfunction, such as increased sweating, 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 the development of the ZNS remains unclear: it is assumed that its mechanism is played by the blockade of dopamine receptors in the striatum and 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 cause a dose-dependent lengthening of the QT interval. This effect increases the risk of developing severe ventricular arrhythmias, such as ventricular pirouette torsades de pointes.
    Before starting therapy with neuroleptics, you need to make sure that there are no risk factors predisposing to the development of severe cardiac arrhythmias, such as: a bradycardia with a heart rate of less than 55 beats per minute; slowing of intracardiac conduction, congenital prolongation of the QT interval, or prolongation of the QT interval associated with simultaneous use of other drugs extending the QT interval; violation of electrolyte metabolism: hypomagnesemia, and especially,hypokalemia - should be adjusted; In addition, such patients need to ensure a constant monitoring of the electrolyte content in the blood, ECG monitoring and constant medical supervision. Patients with the above risk factors for the need for sulpiride should be used with caution (see the sections "With caution", "Side effect").
    Extrapyramidal syndrome
    In extrapyramidal syndrome caused by neuroleptics, m-cholinoblocking drugs should be prescribed, and not dopaminergic agonists (see section "Interaction with other drugs").
    Stroke
    In randomized clinical trials comparing the effects of some atypical antipsychotics with placebo 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 psychosis associated with dementia, in the treatment with antipsychotic drugs, there was an increase (1.6-1.7 times) in the risk of death, in most cases associated with cardiovascular (heart failure, sudden death) or infectious diseases (pneumonia ). An analysis of 17 placebo-controlled studies showed that the risk of death in elderly patients with dementia who received atypical antipsychotics is 4.5%, and 2.6% with placebo. Comparative studies have confirmed that treatment with both atypical and typical antipsychotics can 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 not clear.
    Venous thromboembolic complications
    When using antipsychotic drugs, there have been cases of venous thromboembolic complications, including pulmonary embolism, sometimes fatal; deep vein thrombosis. Therefore, all possible risk factors for venous thromboembolic complications must be identified beforebeginning and during drug therapy; it is also necessary to take appropriate preventive measures (see the section "With caution").
    Patients with epilepsy
    Due to the fact that antipsychotics can lower the epileptogenic threshold, in the appointment of sulpiride, patients with epilepsy should be provided with strict medical supervision.
    Patients with Parkinson's disease receiving dopaminergic agonists
    In exceptional cases, sulpiride should not be prescribed to patients suffering from Parkinson's disease. If there is an urgent need for treatment with neuroleptics in patients with Parkinson's disease receiving dopaminergic agonists, a gradual reduction in the doses of the latter should be undertaken until complete withdrawal. Abrupt withdrawal of dopaminergic drugs may increase the risk of developing a patient's CNS (see sections "With caution", "Interaction with other drugs").
    Leukopenia, neutropenia, agranulocytosis
    With prolonged use of antipsychotics, it is recommended to regularly monitor the composition of peripheral blood, especially if a fever occurs or an infection of an unexplained etiology is established (the possibility of developing leukopenia and agranulocytosis).In case of significant hematological changes in the peripheral blood, treatment with sulfirid should be stopped.
    Patients with impaired renal function
    In patients with impaired renal function, reduced doses of sulpiride should be used (see section "Method of administration and dose").
    Patients with diabetes mellitus or with risk factors for the development of diabetes mellitus.
    Since there is information about the development of hyperglycemia in patients taking atypical antipsychotics, patients with an established diagnosis of diabetes mellitus or risk factors for its development who are prescribed sulfide therapy should monitor blood sugar levels.
    The use of alcohol or the use of medications containing alcohol, during treatment with sulpiride is strictly prohibited.
    It should be borne in mind that sulpiride when used simultaneously with general stimulating substances (eg anorectics, some anti-asthmatic drugs), can cause anxiety, neurosis, excitability and insomnia.
    Special precautions should be observed when prescribing sulpiride to young women with unsteady menstrual cycles.
    It is recommended to conduct constant medical supervision of the condition of newborns who underwent intrauterine exposure to sulpiride. In newborns, there is a risk of developing unwanted reactions involving extrapyramidal symptoms and / or withdrawal symptoms.
    Attention Deficit Hyperactivity Disorder (or without it)
    It should be taken into account that in connection with the influence of sulpiride on cognitive processes in children, it is necessary to monitor the child's ability to learn annually. It is necessary to regularly adjust the dose of the drug taking into account the clinical state of the child.
    The preparation contains lactose. For patients with rare hereditary disorders, including galactose intolerance, insufficiency of lactase or impaired absorption of glucose-galactose, the use of this drug is not recommended.
    Effect on the ability to drive transp. cf. and fur:Due to the sedative effect of the preparation, it should avoid the implementation of potentially dangerous activities during the period of its application, which require an increased concentration of attention and speed of psychomotor reactions (vehicle management, work with moving mechanisms, etc.).
    Form release / dosage:Tablets 50 mg, 200 mg.
    Packaging:For 10 tablets in PVC / al. blister. Three blisters together with instructions for use in a cardboard box.
    Storage conditions:In dry, dark place at a temperature of 15-25 ° C. Keep out of the reach of children!
    Shelf life:
    4 years.
    Do not use after the expiration date!
    Terms of leave from pharmacies:On prescription
    Registration number:П N015244 / 01
    Date of registration:31.10.2008
    The owner of the registration certificate:PRO.MED.CS Prague as.PRO.MED.CS Prague as. Czech Republic
    Manufacturer: & nbsp
    Representation: & nbspPRO.MED.CS Prague as. PRO.MED.CS Prague as. Czech Republic
    Information update date: & nbsp28.08.2015
    Illustrated instructions
      Instructions
      Up