Instructions Sulpiride capsules 100 mg No. 24
Composition
active ingredient: sulpiride;
1 capsule contains 50 mg or 100 mg of sulpiride;
excipients: colloidal anhydrous silicon dioxide, corn starch, lactose monohydrate, magnesium stearate;
hard gelatin capsule for 50 mg: gelatin, titanium dioxide (E 171);
hard gelatin capsule for 100 mg: gelatin, titanium dioxide (E 171), quinoline yellow (E 104), iron oxide red (E 172).
Dosage form
The capsules are hard.
Main physicochemical properties:
50 mg capsules: cylindrical capsules with semicircular edges, number 3, white, filled with white or cream-colored powder;
100 mg capsules: cylindrical capsules with semicircular edges, number 3, yellow, filled with white or cream-colored powder.
Pharmacotherapeutic group
Antipsychotics. Benzamides. ATX code N05A L01.
Pharmacological properties
Pharmacodynamics
Sulpiride belongs to the group of substituted benzamides, whose activity is structurally different from phenothiazines, butyrophenones, and thioxanthenes.
In terms of behavior and biochemical composition, sulpiride shares with these classical neuroleptics certain properties that indicate antagonism of the brain dopamine receptor. These differences include the lack of catalepsy at doses active in other behavioral tests, the absence of effect on the turnover of noradrenaline or serotonin (5HT), a slight anticholinesterase activity, and the absence of effect on muscarinic receptor or gamma-aminobutyric acid receptor binding. One of the characteristics of sulpiride is its bimodal activity, since it has properties of both an antidepressant and a neuroleptic. Improvement of mood is observed after a few days of treatment, and then the pronounced symptoms of schizophrenia disappear. The sedative effect and the absence of emotional reactions usually associated with classical neuroleptics of the phenothiazine or butyrophenone type are not a characteristic feature of sulpiride therapy.
The therapeutic effect during the treatment of schizophrenia is observed 8-12 weeks after the start of treatment.
Sulpiride activates the secretion of prolactin. The active substance improves mucus secretion and blood supply to the mucous membrane of the stomach and duodenum.
Sulpiride also exhibits antiemetic effects.
Pharmacokinetics
Sulpiride is slowly absorbed from the gastrointestinal tract. The presence of food reduces absorption by 30%. Bioavailability is low (27-34%) and depends on individual differences. The active substance quickly enters the tissues; only a small amount of it penetrates the blood-brain barrier. The maximum concentration in the blood plasma is reached 3-6 hours after oral administration. Protein binding is about 40%, the volume of distribution is from 1 to 2.7 l/kg. The half-life from the blood plasma is about 8 hours. In patients with severe renal impairment, it is prolonged to 20-26 hours after intravenous administration. A small amount of the active substance penetrates into breast milk. It is excreted with urine and feces mainly in unchanged form.
Indication
Short-term symptomatic treatment of anxiety disorders in adults when conventional therapeutic measures have failed.
Serious behavioral disorders (agitation, self-harm, stereotypy) in children aged 6 years and older, especially in patients with autistic syndromes.
Contraindication
· Hypersensitivity to sulpiride or any of the excipients of the drug.
Known or suspected diagnosis of pheochromocytoma.
Acute porphyria.
Concomitant prolactin-dependent tumors (e.g., prolactin-secreting pituitary adenoma (prolactinoma) and breast cancer).
Concomitant use with non-antiparkinsonian dopamine agonists (cabergoline, rotigotine and quinagolide), combinations with levodopa or antiparkinsonian drugs (including ropinorole), combinations with mecitazine, citalopram and escitalopram (see section "Interaction with other medicinal products and other types of interactions").
Interaction with other medicinal products and other types of interactions
Sedatives
It should be remembered that many drugs or substances can have an additive inhibitory effect on the central nervous system and lead to a decrease in mental activity. These drugs include morphine derivatives (analgesics, cough suppressants and replacement therapy), neuroleptics, barbiturates, benzodiazepines, non-benzodiazepine anxiolytics (such as meprobamate), hypnotics, sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), sedative H1-antihistamines, centrally acting antihypertensives, baclofen and thalidomide.
Drugs that may cause the development of paroxysmal ventricular tachycardia (torsades de pointes)
This serious cardiac arrhythmia can be caused by a number of drugs, with or without antiarrhythmic activity. Precipitating factors include hypokalemia and bradycardia or the presence of congenital or acquired QT prolongation.
This interaction occurs with erythromycin, dolasetron, spiramycin, and vincamine, only in dosage forms for intravenous administration.
Concomitant administration of two drugs that can cause paroxysmal ventricular tachycardia (those that cause torsades de pointes) is generally contraindicated. However, methadone and some other drugs are exceptions: antiparasitic drugs (halofantrine, lumefantrine, pentamidine) - they are not advisable to combine with other drugs that can cause paroxysmal ventricular tachycardia of the "pirouette" type (torsades de pointes); neuroleptics that can cause the development of paroxysmal ventricular tachycardia of the "pirouette" type (torsades de pointes) are also not advisable, but not contraindicated, to combine with other drugs that can cause the development of paroxysmal ventricular tachycardia of the "pirouette" type (torsades de pointes).
Contraindicated combinations
Citalopram, escitalopram
Increased risk of developing ventricular arrhythmias, especially polymorphic ventricular tachycardia.
Dopamine receptor agonists not for the treatment of Parkinson's disease (cabergoline, quinagolide, rotigotine)
There is mutual antagonism between dopamine agonists and neuroleptics.
Levodopa and antiparkinsonian drugs (including ropinorole)
There is mutual antagonism between levodopa, antiparkinsonian drugs (amantadine, apomorphine, bromocriptine, entacapone, lisuride, pergolide, piribedil, pramipexole, ropinorole, rasagiline, selegiline) and neuroleptics.
Dopamine agonists may cause or exacerbate psychiatric disorders. If neuroleptics are required in patients with Parkinson's disease treated with dopamine agonists, the dose of dopamine agonists should be gradually reduced (abrupt withdrawal puts the patient at risk of neuroleptic malignant syndrome), as concomitant use is contraindicated.
Increased risk of developing ventricular arrhythmias, especially polymorphic ventricular tachycardia.
Mechitazine
Increased risk of developing ventricular arrhythmias, especially polymorphic ventricular tachycardia.
Unwanted combinations
Antiparasitic drugs that may induce torsades de pointes (halofantrine, lumefantrine, pentamidine). Due to increased risk of ventricular arrhythmias, particularly torsades de pointes.
If possible, treatment with azole antifungals should be discontinued. If concomitant treatment cannot be avoided, the QT interval should be checked before starting treatment and ECG should be monitored during treatment.
Other drugs that may cause torsades de pointes include class Ia (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, dronedarone, sotalol, dofetilide, ibutilide) antiarrhythmic drugs and other drugs such as bepridil, cisapride, diphemanil, dolasetron, intravenous erythromycin, mizolastine, intravenous vincamine, levofloxacin, prucalopride, toramiphen, moxifloxacin, intravenous spiramycin.
High risk of ventricular arrhythmias, particularly torsades de pointes.
Other neuroleptics that can cause the development of paroxysmal ventricular tachycardia of the "pirouette" type (torsades de pointes) (amisulpride, chlorpromazine, cyamemazine, droperidol, flupentixol, fluphenazine, haloperidol, levomepromazine, pimozide, pipotiazide, sertindole, sulpiride, sultopride, tiapride, veralipride, zuclopenthixol)
High risk of ventricular arrhythmias, in particular paroxysmal ventricular tachycardia of the "pirouette" type (torsades de pointes).
Ethanol
Potentiation of the sedative effects of neuroleptics.
Patients should avoid drinking alcoholic beverages or medications that contain alcohol.
Methadone
Increased risk of ventricular arrhythmias, in particular torsades de pointes.
Combinations requiring caution
Azithromycin
Increased risk of ventricular arrhythmias, especially polymorphic ventricular tachycardia. ECG and clinical monitoring are necessary during concomitant use.
Beta-blockers used in heart failure (bisoprolol, carvedilol, metoprolol, nebivolol) - increased risk of ventricular arrhythmias, in particular torsades de pointes. Clinical monitoring and ECG control are necessary.
Drugs that cause bradycardia (including class Ia antiarrhythmic drugs, beta-blockers, some class III antiarrhythmic drugs, some calcium channel blockers (diltiazem, verapamil, clonidine, guanfacine), digitalis glycosides, pilocarpine, anticholinesterase drugs) - increased risk of developing ventricular arrhythmias, in particular paroxysmal ventricular tachycardia of the "pirouette" type (torsades de pointes). Clinical monitoring and ECG control are necessary.
Clarithromycin
Potassium-sparing drugs (potassium-sparing diuretics, including in combination, stimulant laxatives, glucocorticoids, tetracosactide and amphotericin for intravenous use) - increased risk of developing ventricular arrhythmias, in particular paroxysmal ventricular tachycardia of the "pirouette" type (torsades de pointes).
Before administration, correction of existing hypokalemia should be performed and clinical monitoring and control of electrolytes and ECG should be performed.
Lithium preparations
Risk of neuropsychiatric signs suggestive of neuroleptic malignant syndrome or lithium poisoning.
It is necessary to regularly monitor the clinical picture and laboratory test results, especially at the beginning of concomitant use.
Roxithromycin
Increased risk of ventricular arrhythmias, especially polymorphic ventricular tachycardia. ECG and clinical monitoring are necessary during concomitant use.
Sucralfate
Reduced absorption of sulpiride in the gastrointestinal tract.
There should be a certain time interval (more than
2 hours if possible).
Topical gastrointestinal agents, antacids, and activated charcoal
Reduced absorption of sulpiride in the gastrointestinal tract.
There should be a certain time interval (more than
2 hours if possible).
Combinations that should be prescribed taking into account interactions
Antihypertensives
Increased risk of arterial hypotension, particularly postural.
Beta-blockers (except esmolol, sotalol and beta-blockers used in heart failure) - vasodilator effect and risk of arterial hypotension, in particular postural (additive effect).
Other sedatives
More pronounced inhibition of central nervous system function. Due to impaired ability to concentrate, driving vehicles and working with other mechanisms may be dangerous.
Nitrates, nitrites and related drugs
Increased risk of arterial hypotension, particularly postural.
Sulpiride may reduce the effectiveness of ropinorole.
Application features
In some patients, sulpiride may cause motor agitation. When symptoms of aggression or an excited phase occur, small doses of the drug may exacerbate them. Patients with symptoms of hypomania should be monitored. Patients with aggressive behavior or agitation with impulsivity may take sulpiride with sedatives.
Except in special cases, this medicine should not be prescribed to patients with Parkinson's disease.
Extrapyramidal disorders and motor agitation (akathisia) may occur in a small number of patients. Dosage reduction or administration of antiparkinsonian drugs may be necessary.
Acute withdrawal syndrome, including nausea, vomiting, sweating and insomnia, has been reported following abrupt discontinuation of neuroleptics. Recurrence of psychotic symptoms may also occur. Involuntary movements such as akathisia, dystonia and dyskinesia have been reported. Therefore, gradual withdrawal of the drug is recommended.
Sulpiride causes only minor changes in the EEG, and while neuroleptics may lower the epileptogenic threshold, this impairment has not been assessed with the drug. It is recommended that the drug be prescribed with caution to patients with unstable epilepsy, and patients with a history of epilepsy should be monitored during treatment with sulpiride.
Patients requiring sulpiride and receiving anticonvulsant therapy do not need to change the dose of the anticonvulsant. Muscle cramps have been reported in patients without a history of epilepsy.
Since hyperglycemia may develop with the use of atypical antipsychotics, appropriate monitoring of blood glucose levels should be carried out at the beginning of treatment with sulpiride in individuals who have diabetes or have risk factors for developing diabetes.
As with other drugs that are primarily excreted by the kidneys, dosage reduction and increased monitoring are recommended in patients with renal insufficiency; in cases of severe renal insufficiency, intermittent courses of treatment are advisable.
During treatment with sulpiride, it is necessary to monitor patients with epilepsy more closely, since sulpiride may lower the seizure threshold, elderly patients who are more prone to developing postural hypotension, sedation and extrapyramidal effects of the drug, and patients who have a history of seizures after treatment with sulpiride (see section "Side effects").
Leukopenia, neutropenia and agranulocytosis have been reported with antipsychotics, including sulpiride. Unexplained infections or fever may indicate blood dyscrasias and require immediate laboratory blood testing.
It is recommended to avoid the use of sulpiride in patients with acute porphyria.
Potentially fatal neuroleptic malignant syndrome
Signs of autonomic dysfunction, such as sweating and changes in blood pressure, may develop before the onset of hyperthermia and are early warning symptoms.
Although this effect of neuroleptics may be idiosyncratic in nature, risk factors such as dehydration and organic brain damage may be present.
QT prolongation
Sulpiride may cause QT prolongation. This increases the risk of serious ventricular arrhythmias, including torsades de pointes, which is more common in patients with bradycardia, hypokalemia, and congenital or acquired QT prolongation (when sulpiride is taken concomitantly with a drug that prolongs the QT interval).
Therefore, before administering the drug and if the clinical situation allows, patients should be checked for risk factors that may contribute to the development of this type of arrhythmia: bradycardia less than 55 beats per minute, hypokalemia, congenital prolongation of the QT interval, concomitant treatment with a drug that can cause severe bradycardia (less than 55 beats per minute), hypokalemia, slowing of intracardiac conduction or prolongation of the QT interval (see sections "Contraindications" and "Interaction with other medicinal products and other types of interactions").
Except in urgent cases, it is recommended that an ECG be performed during the initial assessment of patients who require treatment with a neuroleptic drug. The drug should not be taken concurrently with other neuroleptics.
Stroke
An increased risk of stroke has been reported in elderly patients with dementia treated with certain atypical antipsychotics. The mechanism of this increased risk is unknown. An increased risk cannot be excluded when taken with other antipsychotics or in other patient groups. Sulpiride should be used with caution in patients with risk factors for stroke.
Elderly patients with dementia
The risk of death is increased among elderly patients with dementia-related psychosis who are treated with antipsychotics.
Although the causes of deaths with atypical antipsychotics varied, the majority were due to cardiovascular disease (e.g., heart failure, sudden death) or infections (e.g., pneumonia).
Treatment with standard antipsychotics has been reported to increase mortality, as has been the case with atypical antipsychotics.
The respective role of antipsychotic medication and patient characteristics in increasing mortality rates remains uncertain.
Venous thromboembolism
Fatal cases of venous thromboembolism (VTE) have been reported with antipsychotic drugs. Since patients taking antipsychotics often have acquired risk factors for VTE, these factors should be identified and preventive measures taken before and during treatment with sulpiride.
It is not recommended to take the drug together with alcohol, levodopa, lithium, antiparkinsonian dopamine agonists, antiparasitic agents that can cause torsades de pointes, methadone, other neuroleptics and drugs that can cause torsades de pointes (see "Interaction with other medicinal products and other types of interactions").
Sulpiride has an anticholinergic effect, so it should be used with caution in patients with glaucoma, intestinal obstruction, congenital gastrointestinal stenosis, urinary retention, and a history of prostatic hyperplasia.
Sulpiride should be used with caution in patients with a predisposition to hypertension, especially elderly patients, due to the risk of hypertensive crisis.
When using the drug even at low doses, the risk of developing tardive dyskinesia should be considered, particularly in elderly patients.
Sulpiride should not be taken late at night due to the possibility of sleep disturbances.
This medicinal product contains lactose and is therefore not recommended for use in patients with galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption syndrome (rare hereditary disease).
Use during pregnancy or breastfeeding
Pregnancy. In animals, a decrease in fertility was observed, which is associated with the pharmacological properties of sulpiride (prolactin-mediated effect). Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development and/or postnatal development. Very limited data on effects on pregnancy are available in humans. In almost all cases of fetal or neonatal malformations reported in the context of sulpiride use during pregnancy, alternative explanations are considered to be more likely. Therefore, due to limited experience, sulpiride is not recommended during pregnancy. When antipsychotics, including sulpiride, are used during the third trimester of pregnancy, there is a risk of adverse reactions, in particular extrapyramidal syndrome and withdrawal syndrome (with varying degrees of severity and duration), in which the severity and duration of adverse reactions in newborns after delivery may vary. Agitation, hypertension, hypotension, tremor, drowsiness, respiratory distress syndrome, and feeding disturbances have been reported. Therefore, close monitoring of the newborn is necessary.
Breastfeeding: Since sulpiride is found in breast milk, breastfeeding is not recommended during treatment.
Ability to influence reaction speed when driving vehicles or other mechanisms
Patients, especially those who drive or operate machinery, should be warned that the use of this medicinal product may cause drowsiness (see section "Adverse reactions").
While using the drug, it is contraindicated to drive vehicles and work with other mechanisms.
Method of administration and doses
For oral use.
The minimum effective dose should always be prescribed. If the patient's clinical condition permits, treatment should be initiated at a low dose, followed by gradual dose titration.
Sulpiride should be taken at least 1 hour before or 2 hours after a meal, as the presence of food in the stomach reduces the absorption of the drug by 30%.
Sulpiride should not be taken simultaneously with antacids or sucralfate (there should be a certain time interval between the administration of these agents and sulpiride - more than 2 hours, if possible).
Adults: Short-term symptomatic treatment of anxiety disorders in cases where conventional therapeutic measures have failed: daily dose is 50-150 mg for no more than 4 weeks.
Children aged 6 years and over. Serious behavioural disturbances (agitation/anxiety, self-harm, stereotypy), especially in patients with autistic syndromes:
5 mg/kg body weight per day (if necessary, this dose can be increased to 10 mg/kg body weight per day). For children, another dosage form is more suitable - oral solution.
Elderly patients: use the usual doses as for adult patients. Reduce the dose in the presence of impaired renal function (according to the doctor's recommendation).
Patients with renal impairment: For this group of patients, doses should be adjusted according to the degree of renal impairment, the dose should be reduced or the interval between doses should be extended.
Children
Since the efficacy and safety of sulpiride in children have not been fully studied, it should be used with caution (see section "Method of administration and dosage"). Due to the effect of the drug on cognitive abilities, it is recommended to conduct an annual clinical examination to assess learning ability. The dose of the drug should be adjusted periodically, based on the clinical status of the child.
The use of hard capsules is contraindicated in children under 6 years of age, as it may lead to airway obstruction.
Overdose
Experience with overdose of sulpiride is limited. Dyskinetic manifestations with spasmodic torticollis, tongue protrusion and trismus may occur. Some patients may develop life-threatening parkinsonism or even coma.
Sulpiride is partially removed by hemodialysis. There is no specific antidote for sulpiride.
Treatment should be symptomatic: resuscitation with careful monitoring of cardiac and respiratory function (risk of QT prolongation and ventricular arrhythmias), which should be continued until the patient recovers completely. In case of severe extrapyramidal syndrome, anticholinergic drugs should be administered.
Adverse reactions
From the blood and lymphatic system: leukopenia, neutropenia, agranulocytosis.
Cardiovascular: orthostatic hypotension, increased blood pressure, QT prolongation, ventricular arrhythmias such as ventricular flutter, torsades de pointes, and ventricular tachycardia, which may result in ventricular fibrillation or cardiac arrest, sudden death.
Cases of venous thromboembolism, including fatal cases of pulmonary embolism and deep vein thrombosis, have been reported with the use of antipsychotics.
On the part of the endocrine system: transient hyperprolactinemia (which disappears after discontinuation of treatment), which may lead to amenorrhea, galactorrhea, gynecomastia, impotence, frigidity, breast enlargement and breast pain.
From the side of the central nervous system: early dyskinesia (spastic torticollis, oculogyric crises, trismus), which decreases with the use of anticholinergic antiparkinsonian drugs.
Extrapyramidal symptoms and related disorders:
− parkinsonism and related symptoms: tremor, hypertension, hypokinesia, hypersalivation;
− akinetic symptoms, accompanied or not accompanied by hypertonicity and partially relieved by the use of anticholinergic antiparkinsonian agents;
− hyperkinetic-hypertonic, excitable motor activity;
− akathisia.
Tardive dyskinesia, characterized by involuntary rhythmic movements, particularly of the tongue and/or face, which can occur with long-term treatment with all neuroleptics; in this case, anticholinergic antiparkinsonian drugs are ineffective and may exacerbate clinical manifestations.
Sedative effect or drowsiness.
There were reports of insomnia and confusion.
Convulsions (see section "Special warnings and precautions for use").
Potentially fatal neuroleptic malignant syndrome (see section "Special warnings and precautions for use").
Skin and subcutaneous tissue disorders: maculopapular rash, urticaria.
Immune system disorders: anaphylactic reactions, shortness of breath and anaphylactic shock.
General disorders: weight gain, hypersensitivity reactions.
Conditions during pregnancy, postpartum and perinatal periods: withdrawal syndrome in newborns.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 ºС in a place inaccessible to children.
Packaging
12 capsules in a blister, 2 blisters in a box.
Vacation category
According to the recipe.
Producer
Teva Operations Poland LLC.
Location of the manufacturer and its business address
80 Mogilska Street, 31-546 Krakow, Poland.
