Composition 1 capsule contains: active ingredient: sulpiride 50 mg, excipients: lactose monohydrate, methylcellulose, talc, magnesium stearate, gelatin, titanium dioxide
Sulpiride is an atypical neuroleptic from the group of substituted benzamides. Sulpiride has moderate neuroleptic activity in combination with stimulating and thymoanleptic (anti-depressive) effects. Neuroleptic effect is associated with anti-dopaminergic action. In the central nervous system, sulpiride mainly blocks the dopaminergic receptors of the limbic system, while the non-striated system has little effect, it has an antipsychotic effect. The peripheral action of sulpiride is based on the inhibition of presynaptic receptors. With an increase in the amount of dopamine in the CNS, an improvement in mood is associated with a decrease in the development of symptoms of depression. The antipsychotic effect of sulpiride is manifested in doses of more than 600 mg / day, in doses up to 600 mg / day, a stimulating and antidepressant effect prevails. Sulpiride has no significant effect on adrenergic, cholinergic, serotonin, histamine and GABA receptors. In small doses, sulpiride can be used as an additional agent in the treatment of psychosomatic diseases, in particular, it is effective in relieving negative mental symptoms of gastric ulcer and duodenal ulcer. In irritable bowel syndrome, sulpiride reduces the intensity of abdominal pain and leads to an improvement in the patient's clinical condition. Low doses of sulpiride (50-300 mg / day) are effective for dizziness, regardless of etiology. Sulpiride stimulates the secretion of prolactin and has a central antiemetic effect (inhibition of the emetic center) due to the blockade of the dopamine D2 receptors of the trigger zone of the emetic center.
When i / m injection of 100 mg of the drug Cmax sulpiride in the blood plasma is reached after 30 minutes and is 2.2 mg / l. When administered orally, Cmax sulpiride in plasma is reached after 3-6 hours and amounts to 0.73 mg / l when taking 1 tablet containing 200 mg and 0.25 mg / ml for 1 capsule containing 50 mg.The bioavailability of dosage forms intended for oral administration is 25-35% and is characterized by significant individual variability. Sulpiride has a linear kinetics after administration of doses in the range from 50 to 300 mg. Sulpiride diffuses rapidly into body tissues: visible Vd in an equilibrium state of 0.94 l / kg. Plasma protein binding is approximately 40%. Small amounts of sulpiride appear in breast milk and cross the placental barrier. In humans, sulpiride is only metabolized to a small extent: 92% of the IV dose is excreted unchanged in the urine. Sulpiride is excreted mainly through the kidneys, by means of bulb-like filtration. Full clearance of 126 ml / min. T1 / 2 of the drug is 7 hours.
As monotherapy or in combination with other psychotropic drugs: acute and chronic schizophrenia, acute delirious states. Depression of various etiologies, neuroses and anxiety in adult patients, with the failure of conventional treatment methods (only 50 mg capsules), severe behavioral disorders (agitation, self-mutilation) , stereotype) in children over the age of 6 years, especially in combination with autism syndromes (50 mg capsules only).
Hypersensitivity to sulpiride or other components of the drug. Prolactin-dependent tumors (for example, pituitary prolactinomas and breast cancer). Hyperprolactinemia. Acute intoxication with ethanol, hypnotics, opioid analgesics. Affective disorders, aggressive behavior, manic psychosis. Pheochromocytoma. Breastfeeding period. Infants up to 18 years old (for pills and solution for i / m administration). Children's age up to 6 years (for capsules). In combination with sultopride, dopaminergic receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lizurid, pergolide, piribedil, pramipexol, kinagolide, ropinirole). Because of the presence of lactose in the composition of the preparation, it is contraindication, and the application is applied to the lactose application, the lactose is applied, and the lactose is applied to the nodal pattern, lactose, pramipexol, kinagolide, ropinirole. / galactose or lactase deficiency. With caution: it is not recommended to assign Eglonyl to pregnant women, unless the doctor, having assessed the balance between benefits and risks for the pregnant woman and the fetus, decidesthat the use of the drug is necessary. It is not recommended to administer sulpiride in combination with ethanol, levodopa, drugs that can cause ventricular arrhythmias such as torsade de pointes (class 1a antiarrhythmic drugs (quinidine, hydroquinidine, disopyramide) and class iii (amiodarone, sotalol, dofetilide, ibutilide) ), some neuroleptics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, Tiapride, pimozide, haloperidol, droperidol) and other drugs, such as: bepridil, cisapride, diphemanil, intravenous e rithromycin, mizolastine, intravenous vincamine, halofantrine, pentamidine, sparfloxacin, moxifloxacin, etc. Care should be exercised in the appointment of Eglonyl patients with renal and / or hepatic insufficiency, neuroleptic malignant syndrome, a history of seizures epilepsieyili a history of severe heart disease, hypertension, patients with Parkinson's disease, dysmenorrhea, in old age.
The prescription of sulpiride to pregnant women is not recommended, unless the doctor, having assessed the ratio of benefits and risks to the pregnant woman and the fetus, decides that the use of the drug is necessary. The administration of sulpiride in combination with ethanol, levodopa, drugs capable of inducing ventricular arrhythmias such as torsade de pointes (class 1a antiarrhythmic drugs (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, sotalol, dofetilide, ibutilide), some neuroleptics ( thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, Tiapride, pimozide, haloperidol, droperidol) and other drugs, such as: bepridil, cisapride, diphemanil, intravenous erythromycin, intravenous erythromycin, intravenous Vincamine, halofantrine, pentamidine, sparfloxacin, moxifloxacin, etc. Care should be exercised in the appointment of sulpiride in patients with renal and / or hepatic insufficiency, neuroleptic malignant syndrome, a history of epilepsy or seizures in history, severe heart disease, hypertension, patients with Parkinson's disease, dysmenorrhea, in old age.
Use during pregnancy and lactation
Animal experiments revealed no teratogenic effects. A small number of women taking low doses of sulpiride (approximately 200 mg / day) during pregnancy had no teratogenic effect. With regard to the use of higher doses of sulpiride, no data are available. There is also no data on the potential effect of antipsychotic drugs taken during pregnancy on the development of the fetal brain. Therefore, as a precautionary measure, it is preferable not to use sulpiride during pregnancy. However, in the case of the use of this drug during pregnancy, it is recommended, as far as possible, to limit the dose and duration of treatment. Newborns whose mothers received long-term treatment with high doses of neuroleptics rarely observed gastrointestinal symptoms (abdominal distension, etc.) associated with the atropine-like effect of certain drugs (especially in combination with anti-parkinson drugs), as well as extrapyramidal syndrome. With prolonged treatment of the mother, or with the use of high doses, as well as in the case of the appointment of the drug shortly before delivery, control over the activity of the nervous system of the newborn is justified. The drug enters the breast milk, so you should stop taking the drug during breastfeeding.
Dosage and administration
Capsules are taken 1-3 times a day, washed down with a small amount of liquid, regardless of the meal. It is not recommended to take the drug in the afternoon (after 16 h) due to the increased level of activity. Acute and chronic schizophrenia, acute delirious psychosis, depression: the daily dose ranges from 200 to 1000 mg, divided into several doses. Neurosis and anxiety in adult patients: the daily dose ranges from 50 to 150 mg for 4 weeks maximum. Severe behavioral disorders in children: the daily dose is from 5 to 10 mg / kg body weight. Doses for the elderly: the initial dose of sulpiride should be 1 / 4-1 / 2 doses for adults.
On the part of the endocrine system, it is possible to develop reversible hyperprolactinemia, the most frequent manifestations of which are galactorrhea, amenorrhea, menstrual disorders, less often, gynecomastia, impotence and frigidity.During treatment with sulpiride, heightened bodyliness, weight gain can be observed. From the digestive system, liver enzymes are increased. rarely, extrapyramidal syndrome and related disorders (akinesia, sometimes combined with muscle hypertonus and partially eliminated when prescribing cholinergic antiparkinson agents, hyperkinesia, hypertonicity, motor excitation akataziya). There have been cases of tardive dyskinesia characterized by involuntary rhythmic movements, mainly of the tongue and / or face during long courses of treatment, which can be observed in the course of treatment with all neuroleptics, the use of antiparkinson preparations is ineffective or may cause worsening of symptoms. With the development of hyperthermia, the drug should be canceled, because increase in body temperature may indicate the development of malignant neuroleptic syndrome (ZNS). On the cardiovascular system, tachycardia, it is possible to increase or decrease arterial suppression, in rare cases it is possible to develop orthostatic hypotension, prolongation of the QT interval, very rare cases of development of torsade syndrome depointes. Allergic reactions are possible skin rash.
Experience overdose suilpirida limited. There are no specific symptoms, there may be: dyskinesia with spastic torticollis, protrusion of the tongue and trismus, blurred vision, arterial hypertension, sedation, nausea, extrapyramidal symptoms, dry mouth, vomiting, increased sweating and gynecomastia; In some patients - Parkinson's syndrome. Treatment: Sulpiride is partially excreted by hemodialysis. In the absence of a specific antidote, symptomatic and supportive therapy should be used, with careful monitoring of the respiratory function and constant monitoring of cardiac activity (risk of prolonged QT interval), which should continue until the patient recovers completely, centrally acting holinoblockers develop an extrapyramidal syndrome.
Interaction with other drugs
Contraindicated combinations: Dopaminergic receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lizurid, pergolide, piribedil, pramipexol, kinagolide, ropinirol), except for those who suffer from Parkinson's; In extrapyramidal syndrome induced by neuroleptics, dopaminergic receptor agonists are not used, in such cases anticholinergic agents are used. Sultoprid: the risk of ventricular arrhythmias increases, in particular atrial fibrillation. Non-recommended combinations: Preparations that can cause ventricular arrhythmias such as torsade de pointes: anti-rhythmic agents with Class Ia (quinidine, hydroquinidine, disipyramide) and Class III (amiodarone, sotalol, dofetilide, ibutilide), some neuroleptics (thiordazine, chlorpromazine, Thiordidazine, chlorpromazine, ibutylide), some neuroleptics (thiordazine, chlorpromazine, ibutilide) , amisulpride, Tiapride, haloperidol, droperidol, pimozide) and other drugs such as: bepridil, cisapride, difemanil, intravenous erythromycin, mizolastine, intravenous vincamine, etc. Ethanol: enhances the sedative effect of neuroleptics. Violation of attention creates a danger to driving vehicles and working on machine tools. Consumption of alcoholic beverages and the use of medications containing ethyl alcohol should be avoided. Levodopa: there is mutual antagonism between levodopa and neuroleptics. Patients suffering from Parkinson's disease, it is necessary to prescribe the minimum effective dose of both drugs. Dopaminergic receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lizurid, pergolide, piribedil, pramipexol, kinagolide, ropinirole), in patients with Parkinson's disease: between dopaminergic receptors, in a human body, and in a human body, between the dopaminergic receptor receptors and the ritinol, nopolycon, ramiphenol) The above drugs can cause or intensify psychosis. If treatment with a neuroleptic patient suffering from Parkinson's disease and receiving a dopaminergic antagonist is necessary, the dose of the latter should be gradually reduced to cancellation (abrupt cancellation of dopaminergic agonists may lead to the development of a malignant neuroleptic syndrome).Halofantrine, pentamidine, sparfloxacin, moxifloxacin: the risk of ventricular arrhythmias increases, in particular torsade de pointes. If possible, you should cancel the antimicrobial drug that causes ventricular arrhythmia. If the combination cannot be avoided, you should first check the QT interval and ensure that the ECG is monitored. Combinations requiring a brave effect: preparations of bradycardia (calcium channel blockers with a brachitis): diltiazem, verapamil, beta-blockers, clonidine, guanfacine, alkaloids, digitalis, cholinesterase inhibitors: donepezil, rivastimine, ethereal therapy, dystrophagous, cholinesterase inhibitors; : The risk of ventricular arrhythmias is increasing, in particular torsade de pointes. It is recommended to conduct clinical and ECG monitoring. Drugs that reduce the level of potassium in the blood (potassium diuretics, stimulant laxatives, amphoteric B (IV), glucocorticoids, tetrakozaktid): increases the risk of ventricular arrhythmias, in particular torsade de pointes. Before prescribing the drug, one should eliminate hypokalemia and establish clinical, cardiographic control, as well as control of the level of electrolytes. Combinations to be taken into account: Antihypertensive drugs: increased hypotensive effect and increased possibility of postural hypotension (additive effect). Other CNS depressants: morphine derivatives (analgesics, antitussives and substitution therapy), barbiturates, benzodiazepines and other anxiolytics, hypnotics, sedative antidepressants, sedative antagonists of histamine H1-receptors, centrally acting hypotensive drugs, baclofen, talidomide treatment. danger to driving vehicles and working on machine tools. Sucralfate, antacids containing Mg2 + and / or A13 +, reduce the bioavailability of oral dosage forms by 20-40%. Sulpiride should be administered 2 hours before they are taken.
Malignant neuroleptic syndrome: when hyperthermia develops, the undiagnosed origin of sulpiride should be canceled, as this may be one of the signs of the malignant syndrome described with the use of neuroleptics (pallor, hyperthermia, autonomic dysfunction, impairment of consciousness, muscle rigidity).Signs of autonomic dysfunction, such as increased sweating and labile blood pressure, may precede the onset of hyperthermia and, therefore, are early warning signs. Although this neuroleptic effect may be of idiosyncratic origin, it appears that some risk factors may predispose to it, such as dehydration or organic brain damage. Increased QT interval: sulpiride extends the QT interval depending on the dose. This action, which is known to increase the risk of developing severe ventricular arrhythmias, such as torsade de pointes, is more pronounced in the presence of bradycardia, hypokalemia, or congenital or acquired prolonged QT interval (combination with a drug that causes a prolongation of the QT interval). If the clinical situation allows, it is recommended to ensure the absence of factors that may contribute to the development of this type of arrhythmia before the administration of the drug: bradycardia with the number of strokes less than 55 bpm, hypokalemia, congenital lengthening of the QT interval, simultaneous treatment with a drug capable of causing marked bradycardia (less 55 beats / min), hypokalemia, slowing of intracardiac conduction or prolongation of the QT interval. With the exception of cases of urgent intervention, patients who require treatment with neuroleptics are recommended to conduct an ECG in the status assessment process. Except in exceptional cases, this drug should not be used in patients with Parkinson's disease. In patients with impaired renal function, reduced doses should be used and control should be strengthened, in case of severe forms of renal insufficiency, intermittent treatment is recommended. Control with treatment with sulpiride should be strengthened: in patients with epilepsy, since the convulsive threshold can be lowered when treating elderly patients who are more sensitive to postural hypotension, sedation and extrapyramidal effects. Consumption of alcohol or the use of medicines containing ethyl alcohol during the course of drug treatment is strictly prohibited. Impact on the ability to drive motor vehicles and control mechanisms: During treatment with Eglonyl, it is prohibited to drive vehicles and work with mechanisms that require increased attention, as well as alcohol intake.