Eglonil 200 instructions for use. Eglonyl. International non-proprietary name

3D images

Composition and form of release

in a blister 10 pcs.; in a box of 3 blisters.

in a blister 12 pcs.; in a box 1 blister.

in a blister 6 ampoules; in a box 1 blister.

in glass bottles of 200 ml.

pharmachologic effect

Blocks dopamine receptors.

Pharmacodynamics

In small doses, acting at the level of central dopaminergic receptors, it has a disinhibitory effect. In doses above 600 mg / day, it reduces productive symptoms (the actual antipsychotic effect).

Pharmacokinetics

After parenteral administration of 100 mg C max (2.2 mg / l) is determined after 30 minutes, after oral administration of 200 mg (0.73 mg / l) - after 4.5 hours. Bioavailability after oral administration is 25-35% ( may vary significantly among individual patients). It easily penetrates into all organs, especially quickly into the liver and kidneys, more slowly into the brain tissue (the main amount is concentrated in the pituitary gland). Plasma protein binding - 40%. T 1/2 is about 7 hours. Virtually no biotransformation. Total Cl - 126 ml / min. Excretion occurs mainly by the kidneys (92% of the administered dose) by glomerular filtration and secretion; a small part (about 1% of the daily dose) is excreted in breast milk.

Eglonil ® indications

Acute and chronic psychoses (lethargy, delirium, confusion, agrammatism, abulia), schizophrenia; neurotic states accompanied by lethargy; psychosomatic symptoms (especially with peptic ulcer of the stomach and duodenum and hemorrhagic rectocolitis).

Contraindications

Hypersensitivity, suspicion of pheochromocytoma.

Use during pregnancy and lactation

With prolonged use of high doses (over 200 mg / day), extrapyramidal syndrome was sometimes noted in newborns. Therefore, if necessary, treatment in pregnant and lactating women is recommended to lower the dose and reduce the duration of treatment.

Side effects

With prolonged use in high doses, lethargy, drowsiness, hyperprolactinemia, amenorrhea, galactorrhea, gynecomastia, impotence, frigidity, weight gain, early (spastic, torticollis, oculomotor disorders, spasm of masticatory muscles) and tardive dyskinesia, extrapyramidal disorders, orthostatic hypotension are sometimes possible , neuroleptic malignant syndrome (hyperthermia).

Interaction

Weakens the effect of levodopa, enhances the severity of lowering blood pressure against the background of antihypertensive drugs; incompatible with alcohol and other drugs that depress the central nervous system (mutual enhancement of sedative properties).

Dosage and administration

Psychoses: i/m- 200-800 mg / day for 2 weeks; inside- with negative symptoms - 200-600 mg / day, with productive symptoms - 800-1600 mg / day, with motor inhibition and psychosomatic disorders - 100-200 mg / day, with peptic ulcer of the stomach and duodenum - 150 mg / day for 4-6 weeks. Children (preferably in the form of a solution for oral administration) - 5-10 mg / kg / day (1 teaspoon - 25 mg; 4 drops - 1 mg).

Precautionary measures

Be wary appoint patients with renal insufficiency, epilepsy, parkinsonism, the elderly and newborns; during work, drivers of vehicles and people whose profession is associated with increased concentration of attention.

Storage conditions of the drug Eglonil ®

Keep out of the reach of children.

Expiration date of the drug Eglonil ®

Do not use after the expiry date stated on the packaging.

Synonyms of nosological groups

Antipsychotic drug (neuroleptic)

Active substance

Release form, composition and packaging

Capsules hard gelatinous, size No. 4, opaque, white or white with a yellowish-grayish tint; the contents of the capsules are a homogeneous yellowish-white powder.

Excipients: lactose monohydrate - 66.92 mg, methylcellulose - 580 mcg, talc - 1.3 mg, magnesium stearate - 1.2 mg.

The composition of the capsule shell: gelatin - 98%, titanium dioxide (E171) - 2%.

15 pcs. - blisters (2) - packs of cardboard.

Tablets white or white with a yellowish tint, scored on one side, engraved with "SLP200" on the other side and chamfered on both sides.

Excipients: potato starch - 53.36 mg, lactose monohydrate - 23 mg, methylcellulose - 2.64 mg, colloidal silicon dioxide - 15 mg, talc - 2 mg, magnesium stearate - 4 mg.

12 pcs. - blisters (1) - packs of cardboard.
12 pcs. - blisters (5) - packs of cardboard.

Solution for intramuscular injection transparent, colorless or almost colorless, odorless or almost odorless.

Excipients: sulfuric acid - 14.36 mg, - 9.5 mg, water for injection - up to 2 ml.

2 ml - ampoules with a break point and two rings (6) - contour plastic packaging (1) - cardboard packs.

pharmachologic effect

Sulpiride is an atypical neuroleptic from the group of substituted benzamides.

Sulpiride has a moderate antipsychotic activity in combination with a stimulating and thymoanaleptic (antidepressant) action.

The neuroleptic effect is associated with antidopaminergic action. In the central nervous system, sulpiride mainly blocks the dopaminergic receptors of the limbic system, and has little effect on the neostriatal system, it has an antipsychotic effect. The peripheral action of sulpiride is based on the inhibition of presynaptic receptors. An increase in the amount in the central nervous system is associated with an improvement in mood, 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, stimulating and antidepressant effects predominate.

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 stopping the negative mental symptoms of gastric and duodenal ulcers. 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 vertigo, regardless of etiology. Sulpiride stimulates the secretion of prolactin and has a central antiemetic effect (inhibition of the vomiting center) due to the blockade of dopamine D2 receptors in the trigger zone of the vomiting center.

Pharmacokinetics

With the / m administration of 100 mg of the drug C max sulpiride in the blood is reached after 30 minutes and is 2.2 mg / l.

When administered orally, Cmax of sulpiride in plasma is reached after 3-6 hours and is 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 doses ranging from 50 to 300 mg.

Sulpiride rapidly diffuses into the tissues of the body: the apparent V d in the equilibrium state is 0.94 l / kg.

Plasma protein binding is approximately 40%.

Small amounts of sulpiride appear in breast milk and cross the placental barrier.

In the human body, sulpiride is only slightly metabolized: 92% of the administered intramuscular dose is excreted in the urine unchanged.

Sulpiride is excreted mainly through the kidneys, by glomerular filtration. Total clearance 126 ml/min. T 1/2 of the drug is 7 hours.

Indications

As monotherapy or in combination with other psychotropic drugs:

• acute and chronic schizophrenia;
• acute delirious states;
• depression of various etiologies;
• neurosis and anxiety in adult patients, with the ineffectiveness of conventional methods of treatment (only for 50 mg capsules);
• severe behavioral disorders (agitation, self-mutilation, stereotypy) in children over the age of 6 years, especially in combination with autism syndromes (only for 50 mg capsules).

Contraindications

• prolactin-dependent tumors (eg, pituitary prolactinomas and breast cancer);
• hyperprolactinemia;
• acute intoxication with ethanol, hypnotics, opioid analgesics;
• affective disorders, aggressive behavior, manic psychosis;
• pheochromocytoma;
• breastfeeding period;
• children's age up to 18 years (for tablets and solution for intramuscular injection);
• children's age up to 6 years (for capsules);
• in combination with sultopride, dopaminergic receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, kinagolid, ropinirole);
• hypersensitivity to sulpiride or another ingredient of the drug.

Due to the presence of lactose in the preparation, it is contraindicated in congenital galactosemia, glucose / galactose malabsorption syndrome or lactase deficiency.

It is not recommended to prescribe sulpiride in combination with ethanol, levodopa, drugs that can cause ventricular arrhythmias of the "torsade de pointes" type (antiarrhythmic drugs of class 1a (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, difemanil, intravenous erythromycin, mizolastine, intravenous vincamine, halofantrine, pentamidine, moxifloxacin, moxifloxacin etc.

Precautions must be observed when prescribing sulpiride to patients with renal and / or hepatic insufficiency, a history of neuroleptic malignant syndrome, a history of epilepsy or seizures, severe heart disease, arterial hypertension, patients with parkinsonism, dysmenorrhea, in the elderly.

Dosage

Solution for intramuscular injection

At acute and chronic psychosis treatment begins with intramuscular injections at a dose of 400-800 mg / day and continues in most cases for 2 weeks. The goal of therapy is to achieve the lowest effective dose.

With the / m administration of sulpiride, the usual rules for i / m injections are observed: deep into the outer upper quadrant of the gluteal muscle, the skin is pre-treated with an antiseptic.

Depending on the clinical picture of the disease, intramuscular injections of sulpiride are prescribed 1-3 times / day, which allows you to quickly alleviate or stop the symptoms. As soon as the patient's condition allows, you should proceed to taking the drug inside. The course of treatment is determined by the doctor.

Tablets and capsules take 1-3 times / day with a small amount of liquid, regardless of the meal.

The goal of therapy is to achieve the lowest effective dose.

Tablets

Acute and chronic schizophrenia, acute delirious psychosis, depression: the daily dose is from 200 to 1000 mg, divided into several doses.

Capsules

neurosis and anxiety adults patients: the daily dose is 50 to 150 mg for a maximum of 4 weeks.

Severe behavioral disorders children: the daily dose is 5 to 10 mg/kg of body weight.

Doses for elderly people: the initial dose of sulpiride should be 1/4-1/2 of the adult dose.

Doses at patients with impaired renal function

Due to the fact that sulpiride is excreted from the body mainly through the kidneys, it is recommended to reduce the dose of sulpiride and / or increase the interval between the administration of individual doses of the drug, depending on the CC parameters:

Side effects

Adverse events that develop as a result of taking sulpiride are similar to those caused by other psychotropic drugs, but the frequency of their development is generally less.

From the endocrine system: it is possible to develop reversible hyperprolactinemia, the most common manifestations of which are galactorrhea, amenorrhea, menstrual irregularities, less often gynecomastia, impotence and frigidity. During treatment with sulpiride, there may be increased sweating, weight gain.

From the digestive system: increased activity of liver enzymes.

From the side of the central nervous system: sedation, drowsiness, dizziness, tremor, early dyskinesia (spastic torticollis, oculogeric crises, trismus), which disappears when an anticholinergic antiparkinsonian drug is prescribed, rarely - extrapyramidal syndrome and related disorders (akinesia, sometimes combined with muscle hypertonicity and partially eliminated when prescribed anticholinergic antiparkinsonian drugs, hyperkinesia-hypertonicity, motor agitation, akatsia). 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 during the course of treatment with all antipsychotics: the use of antiparkinsonian drugs is ineffective or may cause worsening of symptoms. With the development of hyperthermia, the drug should be discontinued, because. an increase in body temperature may indicate the development of neuroleptic malignant syndrome (NMS).

From the side of the cardiovascular system: tachycardia, possibly an increase or decrease in blood pressure, in rare cases, the development of orthostatic hypotension, prolongation of the QT interval, very rare cases of the development of the "torsade depointes" syndrome.

Allergic reactions: possible skin rash.

Overdose

Experience with overdose of suilpiride is limited. Specific symptoms absent, may be observed: 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, NMS may develop. Some patients have Parkinson's syndrome.

Treatment: Sulpiride is partially excreted by hemodialysis. Due to the absence of a specific antidote, symptomatic and supportive therapy should be used, with careful monitoring of respiratory function and constant monitoring of cardiac activity (risk of prolongation of the QT interval), which should continue until the patient has completely recovered, centrally acting anticholinergics are prescribed with the development of a pronounced extrapyramidal syndrome.

drug interaction

Contraindicated combinations

Dopaminergic receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, kinagolid, ropinirole), except for patients suffering from Parkinson's disease: there is mutual antagonism between dopaminergic receptor agonists and antipsychotics. In extrapyramidal syndrome induced by antipsychotics, dopaminergic receptor agonists are not used; in such cases, anticholinergics are used.

Sultopride: the risk of ventricular arrhythmias, in particular atrial fibrillation, increases.

Drugs that can cause ventricular arrhythmias such as "torsade de pointes": class Ia antiarrhythmics (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, sotalol, dofetilide, ibutilide), some antipsychotics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, tiapride, haloperidol, droperidol, pimozide) and other drugs such as: bepridil, cisapride, diphemanil, 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 machines. You should avoid the consumption of alcoholic beverages and the use of medicines containing.

Levodopa: there is mutual antagonism between levodopa and antipsychotics. Patients with Parkinson's disease should be given the lowest effective dose of both drugs.

Dopaminergic receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, kinagolide, ropinirole) in patients with Parkinson's disease: there is mutual antagonism between dopaminergic receptor agonists and antipsychotics. The above drugs can cause or exacerbate psychosis. If treatment with a neuroleptic is necessary in a patient suffering from Parkinson's disease and receiving a dopaminergic antagonist, the dose of the latter should be gradually reduced until withdrawal (abrupt withdrawal of dopaminergic agonists can lead to the development of neuroleptic malignant syndrome).

Halofantrine, pentamidine, sparfloxacin, moxifloxacin: increased risk of ventricular arrhythmias, in particular "torsade de pointes". If possible, the antimicrobial drug that causes ventricular arrhythmia should be discontinued. If the combination cannot be avoided, the QT interval should first be checked and the ECG should be monitored.

Combinations requiring caution

Drugs that cause bradycardia (with bradycardic action: diltiazem, verapamil, beta-blockers, clonidine, guanfacine, digitalis alkaloids, cholinesterase inhibitors: donepezil, rivastigmine, tacrine, ambenonium chloride, galantamine, pyridostigmine, neostigmine): increased risk of ventricular arrhythmias, in particular "torsade de pointes". Clinical and ECG monitoring is recommended.

Drugs that reduce the level of potassium in the blood (potassium-releasing diuretics, stimulant laxatives, amphoteric B (iv), glucocorticoids, tetracosactide): increased risk of ventricular arrhythmias, in particular "torsade de pointes". Before prescribing the drug, hypokalemia should be eliminated and clinical, cardiographic control, as well as control of electrolyte levels should be established.

Combinations to consider:

: 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 histamine H 1 receptor antagonists, centrally acting antihypertensives, baclofen, thalidomide - CNS depression, impaired attention poses a danger to driving transport and work on machines.

Sucralfate, antacids containing Mg2+ and/or A13+, reduce the bioavailability of oral dosage forms by 20-40%. Sulpiride should be prescribed 2 hours before taking them.

special instructions

Malignant neuroleptic syndrome: with the development of hyperthermia of undiagnosed origin, sulpiride should be discontinued, as this may be one of the signs of a malignant syndrome described with the use of neuroleptics (pallor, hyperthermia, autonomic dysfunction, impaired consciousness, muscle rigidity).

Signs of autonomic dysfunction, such as increased sweating and labile blood pressure, may precede the onset of hyperthermia and therefore represent early warning signs.

Although this action of antipsychotics may be idiosyncratic in origin, it appears that certain risk factors may predispose to it, such as dehydration or organic brain damage.

Prolongation of the QT interval: Sulpiride prolongs the QT interval in a dose dependent manner. This action, which is known to increase the risk of developing serious 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 prolongation of the QT interval).

• bradycardia with a number of beats less than 55 beats / min,
• hypokalemia,
• congenital prolongation of the QT interval,
• simultaneous treatment with a drug that can cause severe bradycardia (less than 55 beats / min), hypokalemia, slowing of intracardiac conduction or prolongation of the QT interval.

Except in cases of urgent intervention, patients who require treatment with antipsychotics are recommended to conduct an ECG during the status assessment.

Except in exceptional cases, this drug should not be used in patients suffering from Parkinson's disease.

In patients with impaired renal function, reduced doses should be used and monitoring should be strengthened; in severe forms of renal failure, intermittent courses of treatment are recommended.

Control during treatment with sulpiride should be strengthened:

• in patients with epilepsy, since the convulsive threshold may be lowered;
• in the treatment of elderly patients who are more sensitive to postural hypotension, sedation and extrapyramidal effects.

The consumption of alcohol or the use of medicines containing ethyl alcohol during treatment with the drug is strictly prohibited.

Influence on the ability to drive vehicles and control mechanisms

During treatment with Eglonil, it is forbidden to drive vehicles and work with mechanisms that require increased attention, as well as drinking alcohol.

Pregnancy and lactation

Animal experiments did not reveal teratogenic effects. In a small number of women who took low doses of sulpiride (about 200 mg / day) during pregnancy, there was no teratogenic effect. There are no data on the use of higher doses of sulpiride. There are also no data on the potential effect of neuroleptic drugs taken during pregnancy on fetal brain development. 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 to limit the dose and duration of treatment as far as possible. In newborns whose mothers received long-term treatment with high doses of antipsychotics, gastrointestinal symptoms (bloating, etc.) associated with the atropine-like action of certain drugs (especially in combination with antiparkinson drugs), as well as extrapyramidal syndrome, were rarely observed.

With prolonged treatment of the mother, or when using high doses, as well as in the case of prescribing the drug shortly before childbirth, it is reasonable to monitor the activity of the nervous system of the newborn.

The drug passes into breast milk, so you should stop taking the drug during breastfeeding.

Application in childhood

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

List B. Store at a temperature not exceeding 30 ° C, out of the reach of children. Shelf life - 3 years. Do not use after the expiry date stated on the package.

Antipsychotic drug (neuroleptic)

Active substance

Release form, composition and packaging

Capsules hard gelatinous, size No. 4, opaque, white or white with a yellowish-grayish tint; the contents of the capsules are a homogeneous yellowish-white powder.

Excipients: lactose monohydrate - 66.92 mg, methylcellulose - 580 mcg, talc - 1.3 mg, magnesium stearate - 1.2 mg.

The composition of the capsule shell: gelatin - 98%, titanium dioxide (E171) - 2%.

15 pcs. - blisters (2) - packs of cardboard.

Tablets white or white with a yellowish tint, scored on one side, engraved with "SLP200" on the other side and chamfered on both sides.

Excipients: potato starch - 53.36 mg, lactose monohydrate - 23 mg, methylcellulose - 2.64 mg, colloidal silicon dioxide - 15 mg, talc - 2 mg, magnesium stearate - 4 mg.

12 pcs. - blisters (1) - packs of cardboard.
12 pcs. - blisters (5) - packs of cardboard.

Solution for intramuscular injection transparent, colorless or almost colorless, odorless or almost odorless.

Excipients: sulfuric acid - 14.36 mg, - 9.5 mg, water for injection - up to 2 ml.

2 ml - ampoules with a break point and two rings (6) - contour plastic packaging (1) - cardboard packs.

pharmachologic effect

Sulpiride is an atypical neuroleptic from the group of substituted benzamides.

Sulpiride has a moderate antipsychotic activity in combination with a stimulating and thymoanaleptic (antidepressant) action.

The neuroleptic effect is associated with antidopaminergic action. In the central nervous system, sulpiride mainly blocks the dopaminergic receptors of the limbic system, and has little effect on the neostriatal system, it has an antipsychotic effect. The peripheral action of sulpiride is based on the inhibition of presynaptic receptors. An increase in the amount in the central nervous system is associated with an improvement in mood, 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, stimulating and antidepressant effects predominate.

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 stopping the negative mental symptoms of gastric and duodenal ulcers. 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 vertigo, regardless of etiology. Sulpiride stimulates the secretion of prolactin and has a central antiemetic effect (inhibition of the vomiting center) due to the blockade of dopamine D2 receptors in the trigger zone of the vomiting center.

Pharmacokinetics

With the / m administration of 100 mg of the drug C max sulpiride in the blood is reached after 30 minutes and is 2.2 mg / l.

When administered orally, Cmax of sulpiride in plasma is reached after 3-6 hours and is 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 doses ranging from 50 to 300 mg.

Sulpiride rapidly diffuses into the tissues of the body: the apparent V d in the equilibrium state is 0.94 l / kg.

Plasma protein binding is approximately 40%.

Small amounts of sulpiride appear in breast milk and cross the placental barrier.

In the human body, sulpiride is only slightly metabolized: 92% of the administered intramuscular dose is excreted in the urine unchanged.

Sulpiride is excreted mainly through the kidneys, by glomerular filtration. Total clearance 126 ml/min. T 1/2 of the drug is 7 hours.

Indications

As monotherapy or in combination with other psychotropic drugs:

• acute and chronic schizophrenia;
• acute delirious states;
• depression of various etiologies;
• neurosis and anxiety in adult patients, with the ineffectiveness of conventional methods of treatment (only for 50 mg capsules);
• severe behavioral disorders (agitation, self-mutilation, stereotypy) in children over the age of 6 years, especially in combination with autism syndromes (only for 50 mg capsules).

Contraindications

• prolactin-dependent tumors (eg, pituitary prolactinomas and breast cancer);
• hyperprolactinemia;
• acute intoxication with ethanol, hypnotics, opioid analgesics;
• affective disorders, aggressive behavior, manic psychosis;
• pheochromocytoma;
• breastfeeding period;
• children's age up to 18 years (for tablets and solution for intramuscular injection);
• children's age up to 6 years (for capsules);
• in combination with sultopride, dopaminergic receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, kinagolid, ropinirole);
• hypersensitivity to sulpiride or another ingredient of the drug.

Due to the presence of lactose in the preparation, it is contraindicated in congenital galactosemia, glucose / galactose malabsorption syndrome or lactase deficiency.

It is not recommended to prescribe sulpiride in combination with ethanol, levodopa, drugs that can cause ventricular arrhythmias of the "torsade de pointes" type (antiarrhythmic drugs of class 1a (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, difemanil, intravenous erythromycin, mizolastine, intravenous vincamine, halofantrine, pentamidine, moxifloxacin, moxifloxacin etc.

Precautions must be observed when prescribing sulpiride to patients with renal and / or hepatic insufficiency, a history of neuroleptic malignant syndrome, a history of epilepsy or seizures, severe heart disease, arterial hypertension, patients with parkinsonism, dysmenorrhea, in the elderly.

Dosage

Solution for intramuscular injection

At acute and chronic psychosis treatment begins with intramuscular injections at a dose of 400-800 mg / day and continues in most cases for 2 weeks. The goal of therapy is to achieve the lowest effective dose.

With the / m administration of sulpiride, the usual rules for i / m injections are observed: deep into the outer upper quadrant of the gluteal muscle, the skin is pre-treated with an antiseptic.

Depending on the clinical picture of the disease, intramuscular injections of sulpiride are prescribed 1-3 times / day, which allows you to quickly alleviate or stop the symptoms. As soon as the patient's condition allows, you should proceed to taking the drug inside. The course of treatment is determined by the doctor.

Tablets and capsules take 1-3 times / day with a small amount of liquid, regardless of the meal.

The goal of therapy is to achieve the lowest effective dose.

Tablets

Acute and chronic schizophrenia, acute delirious psychosis, depression: the daily dose is from 200 to 1000 mg, divided into several doses.

Capsules

neurosis and anxiety adults patients: the daily dose is 50 to 150 mg for a maximum of 4 weeks.

Severe behavioral disorders children: the daily dose is 5 to 10 mg/kg of body weight.

Doses for elderly people: the initial dose of sulpiride should be 1/4-1/2 of the adult dose.

Doses at patients with impaired renal function

Due to the fact that sulpiride is excreted from the body mainly through the kidneys, it is recommended to reduce the dose of sulpiride and / or increase the interval between the administration of individual doses of the drug, depending on the CC parameters:

Side effects

Adverse events that develop as a result of taking sulpiride are similar to those caused by other psychotropic drugs, but the frequency of their development is generally less.

From the endocrine system: it is possible to develop reversible hyperprolactinemia, the most common manifestations of which are galactorrhea, amenorrhea, menstrual irregularities, less often gynecomastia, impotence and frigidity. During treatment with sulpiride, there may be increased sweating, weight gain.

From the digestive system: increased activity of liver enzymes.

From the side of the central nervous system: sedation, drowsiness, dizziness, tremor, early dyskinesia (spastic torticollis, oculogeric crises, trismus), which disappears when an anticholinergic antiparkinsonian drug is prescribed, rarely - extrapyramidal syndrome and related disorders (akinesia, sometimes combined with muscle hypertonicity and partially eliminated when prescribed anticholinergic antiparkinsonian drugs, hyperkinesia-hypertonicity, motor agitation, akatsia). 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 during the course of treatment with all antipsychotics: the use of antiparkinsonian drugs is ineffective or may cause worsening of symptoms. With the development of hyperthermia, the drug should be discontinued, because. an increase in body temperature may indicate the development of neuroleptic malignant syndrome (NMS).

From the side of the cardiovascular system: tachycardia, possibly an increase or decrease in blood pressure, in rare cases, the development of orthostatic hypotension, prolongation of the QT interval, very rare cases of the development of the "torsade depointes" syndrome.

Allergic reactions: possible skin rash.

Overdose

Experience with overdose of suilpiride is limited. Specific symptoms absent, may be observed: 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, NMS may develop. Some patients have Parkinson's syndrome.

Treatment: Sulpiride is partially excreted by hemodialysis. Due to the absence of a specific antidote, symptomatic and supportive therapy should be used, with careful monitoring of respiratory function and constant monitoring of cardiac activity (risk of prolongation of the QT interval), which should continue until the patient has completely recovered, centrally acting anticholinergics are prescribed with the development of a pronounced extrapyramidal syndrome.

drug interaction

Contraindicated combinations

Dopaminergic receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, kinagolid, ropinirole), except for patients suffering from Parkinson's disease: there is mutual antagonism between dopaminergic receptor agonists and antipsychotics. In extrapyramidal syndrome induced by antipsychotics, dopaminergic receptor agonists are not used; in such cases, anticholinergics are used.

Sultopride: the risk of ventricular arrhythmias, in particular atrial fibrillation, increases.

Drugs that can cause ventricular arrhythmias such as "torsade de pointes": class Ia antiarrhythmics (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, sotalol, dofetilide, ibutilide), some antipsychotics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, tiapride, haloperidol, droperidol, pimozide) and other drugs such as: bepridil, cisapride, diphemanil, 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 machines. You should avoid the consumption of alcoholic beverages and the use of medicines containing.

Levodopa: there is mutual antagonism between levodopa and antipsychotics. Patients with Parkinson's disease should be given the lowest effective dose of both drugs.

Dopaminergic receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, kinagolide, ropinirole) in patients with Parkinson's disease: there is mutual antagonism between dopaminergic receptor agonists and antipsychotics. The above drugs can cause or exacerbate psychosis. If treatment with a neuroleptic is necessary in a patient suffering from Parkinson's disease and receiving a dopaminergic antagonist, the dose of the latter should be gradually reduced until withdrawal (abrupt withdrawal of dopaminergic agonists can lead to the development of neuroleptic malignant syndrome).

Halofantrine, pentamidine, sparfloxacin, moxifloxacin: increased risk of ventricular arrhythmias, in particular "torsade de pointes". If possible, the antimicrobial drug that causes ventricular arrhythmia should be discontinued. If the combination cannot be avoided, the QT interval should first be checked and the ECG should be monitored.

Combinations requiring caution

Drugs that cause bradycardia (with bradycardic action: diltiazem, verapamil, beta-blockers, clonidine, guanfacine, digitalis alkaloids, cholinesterase inhibitors: donepezil, rivastigmine, tacrine, ambenonium chloride, galantamine, pyridostigmine, neostigmine): increased risk of ventricular arrhythmias, in particular "torsade de pointes". Clinical and ECG monitoring is recommended.

Drugs that reduce the level of potassium in the blood (potassium-releasing diuretics, stimulant laxatives, amphoteric B (iv), glucocorticoids, tetracosactide): increased risk of ventricular arrhythmias, in particular "torsade de pointes". Before prescribing the drug, hypokalemia should be eliminated and clinical, cardiographic control, as well as control of electrolyte levels should be established.

Combinations to consider:

: 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 histamine H 1 receptor antagonists, centrally acting antihypertensives, baclofen, thalidomide - CNS depression, impaired attention poses a danger to driving transport and work on machines.

Sucralfate, antacids containing Mg2+ and/or A13+, reduce the bioavailability of oral dosage forms by 20-40%. Sulpiride should be prescribed 2 hours before taking them.

special instructions

Malignant neuroleptic syndrome: with the development of hyperthermia of undiagnosed origin, sulpiride should be discontinued, as this may be one of the signs of a malignant syndrome described with the use of neuroleptics (pallor, hyperthermia, autonomic dysfunction, impaired consciousness, muscle rigidity).

Signs of autonomic dysfunction, such as increased sweating and labile blood pressure, may precede the onset of hyperthermia and therefore represent early warning signs.

Although this action of antipsychotics may be idiosyncratic in origin, it appears that certain risk factors may predispose to it, such as dehydration or organic brain damage.

Prolongation of the QT interval: Sulpiride prolongs the QT interval in a dose dependent manner. This action, which is known to increase the risk of developing serious 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 prolongation of the QT interval).

• bradycardia with a number of beats less than 55 beats / min,
• hypokalemia,
• congenital prolongation of the QT interval,
• simultaneous treatment with a drug that can cause severe bradycardia (less than 55 beats / min), hypokalemia, slowing of intracardiac conduction or prolongation of the QT interval.

Except in cases of urgent intervention, patients who require treatment with antipsychotics are recommended to conduct an ECG during the status assessment.

Except in exceptional cases, this drug should not be used in patients suffering from Parkinson's disease.

In patients with impaired renal function, reduced doses should be used and monitoring should be strengthened; in severe forms of renal failure, intermittent courses of treatment are recommended.

Control during treatment with sulpiride should be strengthened:

• in patients with epilepsy, since the convulsive threshold may be lowered;
• in the treatment of elderly patients who are more sensitive to postural hypotension, sedation and extrapyramidal effects.

The consumption of alcohol or the use of medicines containing ethyl alcohol during treatment with the drug is strictly prohibited.

Influence on the ability to drive vehicles and control mechanisms

During treatment with Eglonil, it is forbidden to drive vehicles and work with mechanisms that require increased attention, as well as drinking alcohol.

Pregnancy and lactation

Animal experiments did not reveal teratogenic effects. In a small number of women who took low doses of sulpiride (about 200 mg / day) during pregnancy, there was no teratogenic effect. There are no data on the use of higher doses of sulpiride. There are also no data on the potential effect of neuroleptic drugs taken during pregnancy on fetal brain development. 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 to limit the dose and duration of treatment as far as possible. In newborns whose mothers received long-term treatment with high doses of antipsychotics, gastrointestinal symptoms (bloating, etc.) associated with the atropine-like action of certain drugs (especially in combination with antiparkinson drugs), as well as extrapyramidal syndrome, were rarely observed.

With prolonged treatment of the mother, or when using high doses, as well as in the case of prescribing the drug shortly before childbirth, it is reasonable to monitor the activity of the nervous system of the newborn.

The drug passes into breast milk, so you should stop taking the drug during breastfeeding.

Application in childhood

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

List B. Store at a temperature not exceeding 30 ° C, out of the reach of children. Shelf life - 3 years. Do not use after the expiry date stated on the package.

A medicine that helps with neurotic disorders is Eglonil. Instructions for use suggest taking pills for depression and migraines.

Forms of release and composition

1. Solution for intramuscular injection (injections in ampoules for injection).
2. Capsules 50 mg.
3. Oral solution (preferably for children) 0.5%.
4. Tablets "Eglonil" 200 mg.

One tablet contains 0.2 g or 0.05 g of the active ingredient sulpiride and additional substances (potato starch, methylcellulose, talc, lactose monohydrate, silicon dioxide, magnesium stearate).

In a solution for internal use per 100 ml of sulpiride 0.5 g + excipients. The solution for intramuscular injection (1 ampoule) of sulpiride contains 0.1 g + sodium chloride, water and sulfuric acid.

The second name of the drug "Eglonil" - Sulpiride.

Pharmacological properties

The active substance of the drug "Eglonil", instructions for use explains this - Sulpiride is an atypical antipsychotic from the group of substituted benzamides. It has a moderate antipsychotic activity in combination with a stimulating and thymoanaleptic (antidepressive) action. The neuroleptic effect is associated with antidopaminergic action.

In the central nervous system, the substance mainly blocks the dopaminergic receptors of the limbic system, and has little effect on the neostriatal system, it has an antipsychotic effect. The peripheral effect of the drug is based on the inhibition of presynaptic receptors.

An increase in the amount of dopamine in the CNS is associated with an improvement in mood, with a decrease in the development of symptoms of depression. The antipsychotic effect of sulpiride is manifested in doses of more than 600 mg per day, in doses up to 600 mg per day, stimulating and antidepressant effects predominate.

Sulpiride has no significant effect on adrenergic, cholinergic, serotonin, histamine and GABA receptors. In small doses, the drug can be used as an additional remedy in the treatment of psychosomatic diseases, in particular, it is effective in stopping the negative mental symptoms of gastric and duodenal ulcers. With irritable bowel syndrome, Eglonil reduces the intensity of abdominal pain and leads to an improvement in the patient's clinical condition.

Low doses of sulpiride (50 - 300 mg per day) are effective for dizziness, regardless of etiology. Sulpiride stimulates the secretion of prolactin and has a central antiemetic effect (inhibition of the vomiting center) due to the blockade of dopamine D2 receptors in the trigger zone of the vomiting center.

Injections, tablets "Eglonil": what helps

Indications for use include:

• confusion and delirium;
• sluggish schizophrenia;
• psychosomatic diseases;
• abulia;
• neuroses;
• lethargy and other psychoses;
• agrammatism.

Why is Eglonil prescribed yet? Also an indication for the use of "Eglonil" is a stomach ulcer and duodenal ulcer.

Instructions for use

"Eglonil" (tablets)

Acute and chronic schizophrenia, acute delirious psychosis, depression: the daily dose is from 200 to 1000 mg, divided into several doses. Capsules Neurosis and anxiety in adult patients: the daily dose is 50 to 150 mg for a maximum of 4 weeks. Severe behavioral disorders in children: the daily dose is 5 to 10 mg/kg body weight.

Solution for intramuscular injection in ampoules (injections)

In acute and chronic psychosis, treatment begins with intramuscular injections at a dose of 400-800 mg per day and continues in most cases for 2 weeks. The goal of therapy is to achieve the lowest effective dose. With intramuscular administration of sulpiride, the usual rules for intramuscular injections are observed: deep into the outer upper quadrant of the gluteus muscle, the skin is pre-treated with an antiseptic.

Depending on the clinical picture of the disease, intramuscular injections of sulpiride are prescribed 1-3 times a day, which allows you to quickly alleviate or stop the symptoms. As soon as the patient's condition allows, you should proceed to taking the drug inside. The course of treatment is determined by the doctor.

Tablets and capsules are taken 1-3 times a day with a small amount of liquid, regardless of the meal. The goal of therapy is to achieve the lowest effective dose. It is not recommended to take the drug in the afternoon (after 4 p.m.) due to increased activity levels. Doses for the elderly: the initial dose of sulpiride should be 1 / 4-1 / 2 doses for adults.

Contraindications

According to the instructions "Eglonil" can not be used in case of individual intolerance, tumors of the adrenal medulla - pheochromocytoma, with high blood pressure, in a state of psychomotor agitation. Caution in the use of "Eglonil" is required during pregnancy, breastfeeding, in old age, with epilepsy, renal failure.

Side effects

Side effects occur infrequently, subject to dosage. Observed:

• hyperthermia;
• various types of dyskinesias;
• orthostatic hypotension;
• galactorrhea;
• frigidity and impotence;
• gynecomastia;
• drowsiness and lethargy;
• amenorrhea;
• the occurrence of excess weight;
• hyperprolactinemia.

Analogues of the drug "Eglonil"

Full analogues for the active element:

1. Vero Sulpiride.
2. Betamax.
3. Sulpiride.
4. Prosulpin.
5. Eglek.

Price, vacation conditions

The average price of "Eglonil" in pharmacies (Moscow) is 320 rubles for 12 tablets of 200 mg. The cost of injections reaches 310 rubles. In Minsk, there is no medicine for sale, pharmacies offer an analogue of Betamax for 7.6 - 19 bel. rubles. Price in Kyiv - 117 hryvnia, in Kazakhstan - 1890 tenge. Implemented according to the recipe.

One tablet of the drug contains 0.2 g or 0.05 g of the active ingredient and additional substances ( potato starch, methylcellulose, talc, lactose monohydrate, silicon dioxide, magnesium stearate ).

In solution for intramuscular injection (1 ampoule) sulpiride contains 0.1 g + sodium chloride, water and sulphuric acid .

In a solution for internal use per 100 ml sulpiride 0.5 g + excipients.

Release form

The drug is available in the form of gelatin capsules, solid, yellow-gray shade, white-yellow powder inside. Packs of 15 or 30 capsules.

in the form of yellowish tablets, with a line on one side and the inscription “SLP200” on the other, packs of 12, 60 pieces.

in the form of a colorless solution for injection, odorless in ampoules. Packs of 6 ampoules.

pharmachologic effect

Antipsychotic.

Pharmacodynamics and pharmacokinetics

The drug has a fairly moderate neuroleptic effect. The active substance selectively blocks dopamine receptors , while not exerting a strong sedative effect . To a small extent, the drug acts as antidepressant and stimulant .

Depending on the dose, it can eliminate rave and or just increase the tone and reduce anhedonia . In very significant doses, a sedative effect occurs.

After half an hour (for intramuscular) or 5 hours (inside), the effect of the drug occurs. The output is carried out by the kidneys, is not metabolized, the half-life is about 7 hours.

Indications for use Eglonil

• and rave ;
• agrammatism ;
• retardation and others psychoses ;
• sluggish;
• psychosomatic diseases .

Also an indication for the use of Eglonil is duodenum .

Contraindications

Pheochromocytoma , into components.

Side effects of Eglonil

Side effects occur infrequently, subject to dosage.

Possible:

• and lethargy ;
• gynecomastia ;
• different kinds dyskinesia ;
• galactorrhea ;
• frigidity and ;
• hyperthermia ;
• orthostatic hypotension ;
• the occurrence of excess weight.

Instructions for Eglonil (Method and dosage)

Dosage, method of administration and duration should be prescribed by a specialist.

When using tablets, the daily dose can be about 0.2 - 1 gram, capsules - 0.05-0.15 g. The dose is divided into 3 doses, the course is about a month.

To achieve a quick effect or to relieve acute symptoms, injections of the drug are prescribed. intramuscularly .

According to the instructions for the use of Eglonil, when using the drug in ampoules, the daily dose is 0.4-0.8 g. Injections are carried out three times a day, for 2 weeks, then they switch to tablets or capsules.

Overdose

May occur: dyskinesia,, , visual disturbances, arterial hypertension, nausea and dry mouth, sweating and weakness extrapyramidal effect .

Gives partial relief. Therapy - according to symptoms, closely monitor breathing and heart rate . Application possible anticholinergic central action .

Interaction

Simultaneous reception is contraindicated , kinagolide, levodopa and Eglonyla .

Should not be combined with others sedative means and ethanol , to avoid mutual amplification of the effects.

Combine with caution with blood pressure lowering drugs.

Medicines, in the side effects of which there is a risk of occurrence, should not be combined with Eglonil.

Simultaneous reception is not recommended with: pentamidine, lumefantrine, halofantrine, antifungals, apomorphine, bromocriptine, entacapone, lisuride, selegiline, disopyramide, quinidine, sotalol, ibutilide, dofetilide, with ethanol,