Instructions for Eglonil capsules 50 mg blister No. 30
Composition
active ingredient: sulpiride;
1 capsule contains sulpiride 50 mg;
excipients: lactose monohydrate, methylcellulose, talc, magnesium stearate, capsule shell: gelatin, titanium dioxide (E 171).
Dosage form
Capsules.
Main physicochemical properties: opaque white or almost white capsules No. 4 containing creamy white powder.
Pharmacotherapeutic group
Antipsychotics. ATX code N05A L01.
Pharmacological properties
Pharmacodynamics
Sulpiride acts on dopaminergic neurotransmission in the brain as a dopaminomimetic, thereby exerting an activating effect at low doses. At higher doses, sulpiride also reduces productive symptoms.
Pharmacokinetics
After oral administration of one 50 mg capsule, peak plasma concentrations of sulpiride (0.25 mg/l) are reached after 3-6 hours.
The bioavailability of oral dosage forms is 25-35% with wide individual fluctuations; sulpiride has a linear pharmacokinetic profile after administration in doses from 50 to 300 mg.
Sulpiride is rapidly distributed in body tissues: the apparent volume of distribution at steady state is 0.94 l/kg. Plasma protein binding is 40%.
Sulpiride is found in small amounts in breast milk and can cross the placental barrier.
Sulpiride is practically not metabolized in the human body.
Sulpiride is excreted mainly by the kidneys by glomerular filtration. Its renal clearance is 126 ml/min. The plasma half-life is 7 hours.
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 (see section "Composition").
Prolactin-dependent tumors (e.g. prolactin-secreting pituitary adenoma (prolactinoma) and breast cancer).
Known or suspected diagnosis of pheochromocytoma.
Acute porphyria.
Combinations with dopamine receptor agonists not for the treatment of Parkinson's disease (cabergoline, quinagolide), citalopram and escitalopram, hydroxyzine, domperidone and piperazine (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 additive CNS depressant effects and lead to decreased mental performance. These drugs include morphine derivatives (analgesics, antitussives and substitution 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 (see "Potassium-sparing drugs") and bradycardia (see "Bradycardia-inducing drugs") or the presence of congenital or acquired QT prolongation.
These include, in particular, antiarrhythmic drugs of classes Ia and III and some neuroleptics. This effect is also induced by other drugs that do not belong to these classes.
Dolasetron, erythromycin, spiramycin, and vincamine only enter into this interaction in dosage forms for intravenous administration.
Concomitant administration of two "torsadogenic" (those that cause torsades de pointes) drugs is generally contraindicated.
However, some of these drugs are exceptions, as their use cannot be avoided. Therefore, they are simply not recommended for use in combination with drugs that can induce torsades de pointes. This applies to methadone, antiparasitic drugs (chloroquine, halofantrine, lumefantrine, pentamidine) and neuroleptics.
However, these exceptions do not include citalopram, domperidone, and escitalopram: their use with all drugs that can induce torsades de pointes is contraindicated.
Contraindicated combinations (see section "Contraindications").
Citalopram, escitalopram
Increased risk of developing ventricular arrhythmias, especially torsades de pointes.
Dopamine receptor agonists are not for the treatment of Parkinson's disease (cabergoline, quinagolide).
There is mutual antagonism between dopamine agonists and neuroleptics.
Domperidone
There is an increased risk of developing ventricular arrhythmias, in particular torsades de pointes.
Hydroxyzine
There is an increased risk of developing ventricular arrhythmias, in particular torsades de pointes.
There is an increased risk of developing ventricular arrhythmias, in particular torsades de pointes.
Undesirable combinations (see section "Special precautions for use").
Antiparasitic (drugs that can cause the development of paroxysmal ventricular tachycardia (torsades de pointes) (chloroquine, halofantrine, lumefantrine, pentamidine)
Increased risk of ventricular arrhythmias, particularly torsades de pointes. If possible, one of these two drugs should be discontinued.
If concomitant use cannot be avoided, the QT interval should be checked before starting treatment and ECG should be monitored during treatment.
Antiparkinsonian dopamine agonists (amantadine, apomorphine, bromocriptine, entacapone, lisuride, pergolide, piribedil, pramipexole, ropinirole, rasagiline, rotigotine, selegiline)
There is mutual antagonism between dopamine agonists 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).
Other drugs that may induce torsades de pointes (class Ia (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, dronedarone, sotalol, dofetilide, ibutilide) antiarrhythmics and other drugs such as arsenic compounds, diphemanil, intravenous dolasetron, domperidone, intravenous erythromycin, hydroxychloroquine, levofloxacin, mechitazine, mizolastine, prucalopride, intravenous vincamine, moxifloxacin, intravenous spiramycin, toramifene and vandetanib).
High risk of ventricular arrhythmias, particularly torsades de pointes.
Other neuroleptics that may cause the development of torsades de pointes (amisulpride, chlorpromazine, cyamemazine, droperidol, flupentixol, fluphenazine, haloperidol, levomepromazine, pimozide, pipamperon, pipothiazide, sultopride, tiapride, zuclopenthixol)
High risk of ventricular arrhythmias, in particular paroxysmal ventricular tachycardia of the "pirouette" type (torsades de pointes).
Alcohol (drink or excipient).
Potentiation of the sedative effects of neuroleptics.
Due to impaired ability to concentrate, driving vehicles and operating other machinery may be dangerous.
Patients should avoid drinking alcoholic beverages or using medications that contain alcohol.
Levodopa
There is mutual antagonism between levodopa and neuroleptics.
Patients with Parkinson's disease treated with dopamine agonists and neuroleptics should be prescribed the minimum effective doses of both drugs.
Methadone
Increased risk of ventricular arrhythmias, in particular torsades de pointes.
Combinations requiring caution
Anagrelide
Increased risk of ventricular arrhythmias, especially torsades de pointes. ECG monitoring and clinical monitoring are required during concomitant use.
Azithromycin
Increased risk of ventricular arrhythmias, especially torsades de pointes. ECG monitoring and clinical monitoring are required during concomitant use.
Beta-blockers used in patients with heart failure (bisoprolol, carvedilol, metoprolol, nebivolol)
Increased risk of ventricular arrhythmias, including torsades de pointes. Clinical and ECG monitoring is required.
Agents that cause bradycardia (such as class Ia antiarrhythmics, beta-blockers, some class III antiarrhythmics, some calcium channel blockers, crizotinib, digitalis glycosides, pasireotide, pilocarpine, anticholinesterase agents).
Increased risk of ventricular arrhythmias, including torsades de pointes. Clinical and ECG monitoring is required.
Ciprofloxacin, levofloxacin, norfloxacin
Increased risk of ventricular arrhythmias, especially torsades de pointes. ECG monitoring and clinical monitoring are required during concomitant use.
Clarithromycin
Increased risk of ventricular arrhythmias, especially torsades de pointes. ECG monitoring and clinical monitoring are required during concomitant use.
Potassium-sparing drugs (potassium-sparing diuretics, alone or in combination, stimulant laxatives, glucocorticoids, tetracosactide and amphotericin B for intravenous use).
Increased risk of ventricular arrhythmias, in particular torsades de pointes.
Before administration, correction of existing hypokalemia should be performed and clinical monitoring and control of electrolytes and ECG should be performed.
Risk of neuropsychiatric changes suggestive of neuroleptic malignant syndrome or lithium toxicity. Regular clinical and laboratory monitoring is indicated, especially at the beginning of concomitant use. At the first signs of neurotoxicity, it is recommended to discontinue one of the two drugs.
Ondansetron
Increased risk of ventricular arrhythmias, especially torsades de pointes. ECG monitoring and clinical monitoring are required during concomitant use.
Roxithromycin
Increased risk of ventricular arrhythmias, especially torsades de pointes. ECG monitoring and clinical monitoring are required 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) between the administration of sucralfate and sulpiride.
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) between the administration of these agents and sulpiride.
Combinations to consider
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.
Antihypertensives
Increased risk of arterial hypotension, especially orthostatic.
Beta-blockers used in patients with heart failure (bisoprolol, carvedilol, metoprolol, nebivolol)
For beta-blockers used in heart failure, see “Combinations requiring caution”. Vasodilatory effect and risk of hypotension, particularly postural (additive effect).
Dapoxetine
Risk of increased incidence of adverse effects, especially dizziness or syncope.
Orlistat
Risk of treatment failure when used concomitantly with orlistat.
Application features
In patients with diabetes mellitus or with risk factors for developing diabetes mellitus, adequate blood glucose control should be performed at the beginning of sulpiride therapy.
Except in special cases, this medicine should not be prescribed to patients with Parkinson's disease.
For patients with renal insufficiency, reduced dosage and increased monitoring are recommended; in case of severe renal insufficiency, intermittent courses of treatment are advisable.
During treatment with sulpiride, closer monitoring is necessary for:
patients with epilepsy, as sulpiride may lower the seizure threshold; there have been reports of seizures in patients treated with sulpiride (see section "Adverse reactions");
elderly patients who are more susceptible to the development of postural hypotension, sedation, and extrapyramidal effects of the drug.
Leukopenia, neutropenia and agranulocytosis have been reported with antipsychotics, including Eglonil®. Unexplained infections or fever may be signs of leukopenia (see section 4.8): in such cases, a blood test should be performed immediately.
Potentially fatal neuroleptic malignant syndrome. Neuroleptic malignant syndrome, a potentially fatal complication reported with neuroleptic therapy, is characterized by hyperthermia, pallor, autonomic nervous system disorders, impaired consciousness, muscle rigidity, rhabdomyolysis, elevated serum creatine phosphokinase, and autonomic dystonia. Cases with atypical features such as fever without muscle rigidity or hypertonia have been reported. In the event of an unexplained fever that may be considered an early sign/symptom of neuroleptic malignant syndrome or atypical neuroleptic malignant syndrome, sulpiride and all other neuroleptics should be discontinued immediately under medical supervision.
Signs of autonomic nervous system dysfunction, such as increased sweating and changes in blood pressure, may develop before the onset of hyperthermia and should therefore be considered as 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.
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 are to receive treatment with a neuroleptic drug.
Stroke
In randomized, placebo-controlled clinical trials, an increased risk of stroke has been observed in elderly patients with dementia treated with some atypical antipsychotics. The mechanism of this increased risk is unknown. An increased risk cannot be excluded with other antipsychotics or in other patient populations. This drug should be prescribed with caution to patients with risk factors for stroke.
Elderly patients with dementia
The risk of death is increased in elderly patients with dementia-related psychosis who are treated with antipsychotics.
An analysis of data from 17 placebo-controlled trials (with a median duration of 10 weeks) conducted in patients who were generally taking atypical antipsychotics showed that the risk of death was increased 1.6–1.7 times in patients taking these drugs compared with placebo.
After a median treatment period of 10 weeks, the risk of death was 4.5% in the treated group compared with 2.6% in the placebo group.
Although the causes of death during clinical trials with atypical antipsychotics varied, the majority of deaths were due to either cardiovascular (such as heart failure, sudden death) or infectious diseases (such as pneumonia).
Observational studies suggest that treatment with standard antipsychotics may increase mortality in the same way as with atypical antipsychotics.
The respective role of antipsychotic drug and patient characteristics in increasing mortality rates in observational studies remains uncertain.
Venous thromboembolism: Cases of venous thromboembolism (VTE) have been reported with antipsychotic drugs. Since patients taking antipsychotics often have acquired risk factors for VTE, all potential risk factors for VTE should be identified and preventive measures taken before and during treatment with Eglonil® (see section 4.8).
Breast cancer. Sulpiride may increase prolactin levels. Therefore, it should be used with caution. Regardless of gender, patients with a personal or family history of breast cancer require close monitoring during sulpiride therapy.
Slowing of intestinal peristalsis. Cases of intestinal obstruction have been reported in patients receiving antipsychotics. Rare cases of ischemic colitis and intestinal necrosis, sometimes fatal, have also been reported. Most of these patients were receiving concomitant treatment with one or more medicinal products known to reduce intestinal motility (including medicinal products with anticholinergic properties). Particular attention should be paid to the appearance of abdominal pain with vomiting and/or diarrhoea. It is very important to recognise constipation in time and treat it actively. The development of paralytic or mechanical intestinal obstruction requires urgent treatment.
It is not recommended to take this medicine simultaneously with alcohol, levodopa, dopamine receptor agonists, antiparasitic drugs that may cause torsades de pointes, methadone, other neuroleptics and drugs that may cause torsades de pointes, see section "Adverse reactions".
When using the drug even at low doses, the risk of developing tardive dyskinesia should be considered, particularly among elderly patients.
Since the efficacy and safety of sulpiride in children have not been fully studied, precautions should be taken when using this drug (see section "Method of administration and dosage"). Due to the effect of the drug on cognitive function, it is recommended to conduct an annual clinical examination to assess learning ability. The dose of the drug should be adjusted periodically, taking into account the clinical status of the child. The use of tablets and hard capsules in children under 6 years of age is contraindicated, as this may lead to airway obstruction.
Eglonil® should be used with caution in patients with arterial hypertension, especially in elderly patients, due to the risk of hypertensive crisis. Careful monitoring of the patient's condition is necessary.
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 diseases).
Use during pregnancy or breastfeeding
Pregnancy. In animals, a decrease in fertility was observed, associated with the pharmacological properties of the drug (prolactin-mediated effect). There is very limited data on the use of sulpiride during pregnancy. The safety of sulpiride during pregnancy has not been established. Sulpiride crosses the placental barrier. Animal studies have shown reproductive toxicity. Sulpiride is not recommended for use in pregnant women and women of childbearing potential not using effective contraception, except in cases where the expected benefits of sulpiride justify the potential risks. Newborns whose mothers received antipsychotics (including Eglonil®) during the third trimester of pregnancy are at risk of developing undesirable effects, including extrapyramidal symptoms and/or withdrawal symptoms, of varying severity and duration, after birth. The following adverse reactions have been reported: agitation, hypertonia, hypotension, tremor, drowsiness, respiratory distress and feeding problems. Therefore, neonates should be closely monitored.
Breastfeeding. Sulpiride is excreted in breast milk in relatively large quantities. In some cases, the concentration exceeds 10% of the dose adjusted for the mother's body weight. However, the concentration in the blood of breastfed infants has not been determined. There is insufficient data on the effects of sulpiride on newborns and infants.
A decision must be made whether to discontinue breast-feeding or to discontinue sulpiride therapy taking into account the benefit of breast-feeding for the child and the benefit of continued therapy for the woman.
Ability to influence reaction speed when driving vehicles or other mechanisms
Patients, especially those who drive or operate machinery, should be warned that taking this medicinal product may cause drowsiness (see section "Adverse reactions"). Driving and operating machinery is contraindicated during treatment with this medicinal product.
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.
Adults: Short-term symptomatic treatment of anxiety disorders when conventional therapeutic measures have failed: daily dose is 50-150 mg for no more than 4 weeks.
Children aged 6 years and over. Serious behavioral disorders (agitation, self-harm, stereotypy) in children aged 6 years and over, especially in patients with autistic syndromes:
5−10 mg/kg body weight per day.
Children. The use of hard capsules in children under 6 years of age is contraindicated.
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.
Fatal cases were recorded mainly when used in combination with other psychotropic drugs.
Sulpiride is partially removed by hemodialysis. There is no specific antidote for sulpiride.
Treatment should be symptomatic, resuscitation with careful monitoring of cardiac activity 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.
Side effects
From the blood and lymphatic system.
Uncommon: leukopenia.
Frequency unknown: neutropenia, agranulocytosis.
Immune system disorders.
Frequency unknown: anaphylactic reactions: urticaria, anaphylactic shock.
Endocrine disorders.
Common: hyperprolactinemia.
Mental disorders.
Common: insomnia.
Frequency unknown: confusion.
Nervous disorders.
Common: sedation or drowsiness; extrapyramidal syndrome, which is partially reversible with anticholinergic antiparkinsonian agents; parkinsonism; tremor; akathisia.
Uncommon: hypertonicity, dyskinesia, dystonia.
Rare: oculogyric crisis.
Frequency not known: potentially fatal neuroleptic malignant syndrome (see section "Special warnings and precautions for use"), hypokinesia.
Tardive dyskinesia, which can occur during long-term treatment with all neuroleptics; in this case, antiparkinsonian drugs are ineffective and may worsen clinical manifestations.
Metabolic and nutritional disorders.
Frequency unknown: hyponatremia, syndrome of inappropriate antidiuretic hormone secretion.
Cardiological disorders.
Rare: ventricular arrhythmias, including torsades de pointes and ventricular tachycardia, which may lead to ventricular fibrillation or cardiac arrest.
Frequency unknown: QT prolongation, sudden death (see section "Special warnings and precautions for use").
Vascular disorders.
Uncommon: orthostatic hypotension.
Frequency unknown: venous thromboembolism, pulmonary embolism, deep vein thrombosis (see section "Special warnings and precautions for use"), increased blood pressure (see section "Special warnings and precautions for use").
Disorders of the respiratory system, chest organs and mediastinum.
Frequency unknown: aspiration pneumonia (mainly in the case of simultaneous use of sulpiride with other CNS depressants).
Gastrointestinal disorders.
Common: constipation.
Uncommon: salivary hypersecretion.
On the part of the hepatobiliary system.
Common: increased liver enzymes.
Frequency unknown: hepatocellular, cholestatic or mixed liver damage.
Musculoskeletal and connective tissue disorders.
Frequency unknown: rhabdomyolysis.
Pathology of the skin and subcutaneous tissue.
Common: maculopapular rash.
Pregnancy, postpartum and perinatal periods.
Frequency not known: withdrawal syndrome in newborns (see section "Use during pregnancy or breastfeeding").
Disorders of the reproductive system and mammary glands.
Often: galactorrhea.
Uncommon: amenorrhea, impotence or frigidity.
Frequency unknown: gynecomastia.
General disorders.
Common: weight gain.
Frequency unknown: increased body temperature (see section "Special warnings and precautions for use").
Laboratory and instrumental studies.
Frequency unknown: increased blood creatine phosphokinase levels.
Reporting of suspected adverse reactions.
Post-marketing adverse reaction reporting is an important measure. It allows monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals should report any adverse reactions using the adverse reaction reporting system in Ukraine.
Expiration date
3 years.
Storage conditions
Keep out of reach of children. Store in original packaging at a temperature not exceeding 30 °C.
Packaging
No. 30 (15 × 2): 15 capsules in a blister; 2 blisters in a cardboard box.
No. 30 (30 × 1): 30 capsules in a blister; 1 blister in a cardboard box.
Vacation category
According to the recipe.
Producer
DELPHARM DIJON.
Location of the manufacturer and its business address
6 Boulevard de l'Europe, QUETIGNY, 21800, France.
