Sulpiride - instructions for use, dose, side effects, contraindications

auxiliary substances: lactose monohydrate (sugar milk) -63.2 mg or 95.0 mg, potato starch - 22.5 mg or 64.0 mg, microcrystalline cellulose - 6.5 mg or 20.0 mg, gelatin -4, 0 mg or 5.0 mg, talc (magnesium hydrosilicate) 2.3 mg or 12.0 mg, magnesium stearate -1.5 mg or 4.0 mg.

Description:Round flat cylindrical tablets white or white with a weak yellowish tint of color with a bevel. Tablets with a dosage of 200 mg are at risk.

Pharmacotherapeutic group:Antipsychotic agent (antipsychotic).

ATX: & nbsp

N.05.A.L Benzamides

Pharmacodynamics:Atypical antipsychotic agent (neuroleptic), also has antidepressant and antiemetic effect. Neuroleptic effect is associated with antidophaminergic action. In the central nervous system sulpiride blocks predominantly dopaminergic receptors of the limbic system, affects the neostriatic system only slightly, has an antipsychotic effect. The peripheral action of sulpiride is based on oppression of presynaptic receptors. With an increase in the amount of dopamine in the central nervous system (hereinafter referred to as the CNS), the improvement in mood is associated with a decrease in the development of symptoms of depression.

Antipsychotic effect of sulpiride is manifested in doses of more than 600 mg per day, in doses up to 600 mg per day, a stimulating and antidepressant effect predominates. Sulpiride has no significant effect on adrenergic, cholinergic, serotonin, histamine, and gamma-aminobutyric acid receptors. Sulpiride stimulates the secretion of prolactin and has a central antiemetic effect (suppression of the emetic center) due to blockade of dopamine D2 receptors in the trigger zone of the vomiting center.

Pharmacokinetics:Bioavailability - 27%. The binding to plasma proteins is less than 40%. Concentration of the drug in the central nervous system is 2-5% of the concentration in the plasma. Excreted in breast milk. In the human body is not exposed to metabolism and is excreted almost unchanged through the kidneys. The half-life period (T1 / 2) is 6-8 hours. T1 / 2 is significantly increased in patients with moderate and severe renal insufficiency. Such patients should reduce the dose and / or increase the interval between taking the drug.

Indications:

Tablets 200 mg:

Acute psychotic disorders in adults; chronic psychotic disorders in adults (schizophrenia, chronic non-schizophrenic delusions: paranoid nonsense, chronic hallucinatory psychosis).

Tablets 50 mg:

Alarming conditions in adults (short-term symptomatic treatment with ineffectiveness of conventional methods of treatment).

Severe behavioral disorders (agitation, self-mutilation, stereotypes) in children older than 6 years, especially with autism.

Contraindications:

Children under 18 years (for tablets 200 mg).

Children under 6 years (for tablets 50 mg).

- Acute poisoning with alcohol, hypnotics, analgesics;

- hyperprolactinemia;

- Galactosemia, glucose malabsorption / galactose syndrome or lactase deficiency;

- hypersensitivity to sulpiride or other ingredient of the drug;

- prolactin-dependent tumors (eg, pituitary prolactinoma and breast cancer);

- pheochromocytoma;

- acute porphyria;

- simultaneous administration of levodopa (see section "Interaction with other drugs");

- concomitant therapy with dopamine receptor agonists (cabergoline, quinagolide, ropinirole, rotigotine) (see section "Interaction with other drugs").

Carefully:Epilepsy, arterial hypertension, dysmenorrhea, severe heart disease, angina, renal and / or hepatic insufficiency, a history of malignant neuroleptic syndrome, glaucoma, prostatic hyperplasia, my delay, old age.

Pregnancy and lactation:

It is not recommended to prescribe sulpiride to pregnant women, except when the doctor, having estimated the ratio of benefit and risk to the pregnant and fetus, decides that the use of the drug is necessary.

The use of the drug during lactation (breastfeeding) is contraindicated.

Dosing and Administration:

Tablets are taken orally, squeezed with a small amount of liquid, regardless of food intake.

In all cases, use the minimum effective dose of the drug. If the patient's clinical condition allows, treatment should begin with low doses. The minimum effective dose is selected by gradually increasing the dose until the desired effect is achieved.

Acute psychotic disorders in adults; chronic psychotic disorders in adults: The daily dose is divided into several doses and ranges from 200 to 1000 mg. It is not recommended to take the drug in the afternoon (after 16 hours) due to the possible activating action of the drug.

Doses in patients with impaired renal function: due to sulpiride is excreted primarily through the kidneys, it is recommended to reduce the dose and / or increase the interval between the administration of individual doses of the drug depending on the creatinine clearance: when creatinine clearance is 30-60 ml / min, the dose of sul-pyrid should be reduced by 30%and the intervals between receptions should be increased by 1.5 times; with a creatinine clearance of 10-30 ml / min, the dose of sulpiride should be reduced 2-fold, and the interval between doses of the drug should be increased 2-fold; with creatinine clearance less than 10 ml / min, the dose of sulpiride should be reduced by 70%, and the interval between doses of the drug should be increased 3 times.

Short-term symptomatic treatment of anxiety states with ineffectiveness of conventional methods of treatment: The daily dose is 50 - 150 mg for no more than 4 weeks.

Severe behavioral disorders (agitation, self-mutilation, stereotypes) in children older than 6 years, especially with autism syndrome: The daily dose is 5-10 mg / kg body weight.

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

Side effects:Undesirable phenomena that develop as a result of taking sulpiride are similar to undesirable phenomena caused by other psychotropic drugs, but their frequency of development is, in general, less.

From the endocrine system: it is possible to develop reversible hyperprolactinemia, the most frequent manifestations of which are galactorrhea, menstrual cycle disorder, less often - gynecomastia, impotence and frigidity; increased sweating, weight gain.

From the digestive system: dry mouth, heartburn, nausea, vomiting, constipation, increased activity of transaminases and alkaline phosphatase in the blood serum.

From the side of the central nervous system: sedation, drowsiness, dizziness, headache, tremor, rarely - extrapyramidal syndrome, early and late dyskinesias, akatizatsiya, oral automatism, aphasia. When used in small doses, there may be psychomotor agitation, anxiety, irritability, sleep disorder, visual acuity. With the development of hyperthermia, the drug should be discarded. an increase in body temperature may indicate the development of neuroleptic malignant syndrome (NZS)!

From the side of the cardiovascular system - tachycardia, it is possible to raise or lower blood pressure, in rare cases, the development of orthostatic hypotension, prolongation of the QT-interval, rarely, arrhythmia of the "torsade de pointes" type is possible.

Allergic reactions: possible skin rash, itching, eczema.

Overdose:

Symptoms: dyskinesia (spasm of chewing musculature, spasmodic torticollis), extrapyramidal disorders. In some cases - pronounced parkinsonism, coma.Can be observed: blurred vision, hypertension, sedation, nausea, dry mouth, vomiting, increased sweating and gynecomastia, the development of NZS.

Treatment: symptomatic. Holinoblokatory central action.

Interaction:

With simultaneous application: with levodopa the effectiveness of sulpiride decreases; with hypotensive drugs, their hypotensive effect is increased and the risk of orthostatic hypotension increases.

With drugs that depress the central nervous system (narcotic analgesics, sleeping pills and anxiolytic drugs (tranquilizers), clonidine, antitussive drugs (central action), their oppressive effect is intensified.

Sucralfate, antacids containing magnesium ions and / or aluminum, reduce bioavailability by 20-40%.

Antagonism with dopaminergic receptor agonists (amantadine, apomorphine, riptin bromide, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ro-pinirol) and neuroleptics. In extrapyramidal syndrome, induced by neuroleptics, do not use dopaminergic receptor agonists, but use anticholinergic drugs.If it is necessary to treat patients with Parkinson's disease when dopaminergic receptor agonists are used, the dose of the latter should be gradually reduced to a total cancellation (sudden cancellation can lead to the development of malignant neuroleptic syndrome).

Sulpiride increases the risk of developing ventricular arrhythmias (including atrial fibrillation).

The risk of developing ventricular arrhythmias of the "torsade de pointes" type with simultaneous use with: antiarrhythmic drugs 1a class (quinidine, disopyramide) and III class (amiodarone, sotalol, dofetilide, ibutilide), some neuroleptics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, tiapride, haloperidol, droperidol, pimozide), drugs that cause bradycardia (diltiazem, verapamil, beta-blockers, clonidine, guanfacine, preparations of digitalis, donepezil, rivastigmine, tacrine, ambenonium chloride, galantamine, pyridostigmine bromide, neostigmine bromide), drugs that cause hypokalemia (potassium-withdrawing diuretics, some laxatives, amphotericin B intravenously (iv), glucocorticosteroids, tetracosactide) and others (including bepridil, cisapride, dipemanyl methyl sulfate, erythromycin in / in, misolastine, wincamine in / in, halofantrine, pentamidine, sparfloxacin, moxifloxacin).

Special instructions:

Patients with epilepsy

Due to the fact that neuroleptics can lower the epileptogenic threshold, when sulpiride is prescribed to patients with epilepsy, the latter should be under strict medical supervision.

QT interval extension

Sulpiride can induce prolongation of the QT interval. It is known that this effect increases the risk of developing severe ventricular arrhythmias, such as ventricular tachycardia of the "torsade de pointes" type (see "Side effect" section).

Older patients with dementia

In elderly patients with psychoses associated with dementia, in the treatment with antipsychotic drugs, there was an increase (1.6-1.7 times) in the risk of death in most cases due to heart failure or an infectious disease (pneumonia). When sulpiride was used, the risk of death in the elderly with dementia was 4.5%, with placebo 2.6%. As far as the increase in mortality is associated with the drug, and not with the characteristics of the patient itself is not clear.

Malignant neuroleptic syndrome

Malignant neuroleptic syndrome is characterized by pallor, hyperthermia, muscle stiffness, autonomic nervous system dysfunction, such as increased sweating, lability of blood pressure and pulse may precede the onset of hyperthermia and, therefore, be early warning signs. In the case of an unexplained increase in body temperature, treatment with sulpiride should be stopped. The genesis of malignant neuroleptic syndrome remains unclear: it is assumed that the blockade of dopamine receptors in the striatum and hypothalamus plays a role in its mechanism, and congenital predisposition (idiosyncrasy) is not ruled out. The development of the syndrome can be facilitated by intercurrent infection, dehydration or ortho-

Ganic brain damage.

Extrapyramidal syndrome

With extrapyramidal syndrome caused by neuroleptics, m-cholin blocking drugs (and not dopamine receptor agonists) should be prescribed (see "Interaction with Other Drugs").

Stroke

In randomized clinical trials, compared with some atypical antipsychotics with placebo performed in elderly patients with dementia, there was a triple increase in the risk of developing cerebrovascular events. The mechanism of this risk is unknown. It can not be ruled out that this risk increases with other neuroleptics or in other patient populations, so sulpiride should be used with caution in patients with risk factors for stroke.

Venous thromboembolic complications

When using antipsychotic drugs, there have been cases of venous thromboembolic complications, including pulmonary embolism, sometimes fatal; deep vein thrombosis. Therefore, all possible risk factors for venous thromboembolic complications must be identified before and during drug therapy; it is also necessary to take appropriate preventive measures.

Patients with Parkinson's disease receiving dopamine receptor agonists

In exceptional cases, this drug should not be used in patients with Parkinson's disease.If there is an urgent need for treatment with neuroleptics of patients with Parkinson's disease receiving dopamine receptor agonists, a gradual reduction in the doses of the dopamine receptors should be performed (abrupt withdrawal of dopamine receptor agonists may increase the risk of developing a malignant neuroleptic syndrome in the patient) (see "Interaction with other medicinal preparations ").

Patients with impaired renal function

Use reduced dosages (see section "Method of administration and dose").

Patients with diabetes mellitus or with risk factors for diabetes mellitus

Since there is information about the development of hyperglycemia in patients taking atypical antipsychotics, patients with an established diagnosis of diabetes mellitus or with risk factors for its development who are prescribed sulpiric-house treatment should monitor blood sugar levels.

Hemorrhage disorders

With prolonged use of antipsychotics, it is recommended to regularly monitor the composition of peripheral blood, especially if a fever occurs or an infection of an unexplained etiology is established (the possibility of developing leukopenia and agranulocytosis).In case of significant hematological changes in the peripheral blood, treatment with sulfirid should be stopped. The use of alcohol on the background of taking the drug is contraindicated.

Effect on the ability to drive transp. cf. and fur:During the treatment period, it is prohibited to drive vehicles and work with mechanisms that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets of 50 mg and 200 mg.

Packaging:

10 tablets per contour cell packaging made of polyvinylchloride film and aluminum foil.

For 30 tablets in a can of light-protective glass.

Each jar or 3 contour squares, together with the instructions for use, are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006863/08

Date of registration:22.08.2008

The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp31.08.2015

Illustrated instructions

Instructions

Sulpiride (Sulpirid)