Expiration date: 08/2028

Structure and Composition:

Tablets. One tablet contains 50 or 200 mg sulpiride

Excipients: lactose, potato starch monohydrate, colloidal silicon dioxide, hypromellose K4M K15M hypromellose (200 mg tablet), magnesium stearate, talc

in blister 10 pcs. In the paper cartons 3 blisters.

Description pharmaceutical form:

Round flat tablets white white or almost scored on one side

Pharmacokinetics:

When inside designation Cmax plasma levels achieved after 3-6 hours and 0.73 mg / l while taking one tablet containing 200 mg, and 0.25 mg / L for a tablet containing 50 mg.

The bioavailability of dosage forms intended for oral administration, is about 25-35% and is characterized by a large individual variability. Sulpiride has linear kinetics after administration of doses ranging from 50 to 300 mg.

Sulpiride quickly diffuses into the tissues of the body: the apparent Vss - 0,94 l / kg. Binding to plasma proteins - about 40%. It penetrates into erythrocytes by passive diffusion, the concentration in plasma and erythrocyte comparable. Sulpiride concentration in cerebrospinal fluid is low and, on average, about 13% (4-29%) serum. Quickly penetrates the liver and kidneys, slowly - in brain tissue (basic amount of drug accumulated in the pituitary gland). Sulpiride concentration in the CNS is 2-5% of plasma concentrations. It penetrates through the placental barrier. Minor amounts of sulpiride appear in breast milk.

Sulpiride in humans only marginally metabolized and excreted by the kidneys virtually unchanged by glomerular filtration (92%) and the residue is eliminated with the feces. Plasma T1 / 2 of 7 hours. With breast milk is allocated 0.1% of the daily dose. The total plasma clearance of sulpiride reaches 90-126 ml / min and the renal clearance of up to several magnitudes smaller than the total plasma clearance.

Description of the pharmacological actions:

Sulpiride is the most prominent representative of the benzamide antipsychotics group. It has a moderate antipsychotic activity combined with a stimulating and timoanalepticheskim (antidepressant) effect.

Neuroleptic dofaminoblokiruyuschim effect is associated with the action. In the CNS, sulpiride blocks predominantly dopaminergic receptors of the limbic system, as the system acts on neostriatnuyu slightly. It has an antipsychotic effect. Peripheral effects of sulpiride based on the inhibition of presynaptic receptors. With the increase in the content of dopamine in the central nervous system associated improvement in mood, with a decrease - the development of depressive symptoms.

Antipsychotic effect of sulpiride manifested at doses over 600 mg / day, in doses up to 600 mg / day is dominated by stimulating and antidepressant effects.

Culpirid no significant effects on adrenergic, cholinergic, serotonin, histamine and GABA receptors.

Indications:

As monotherapy or in combination with other psychotropic drugs:

• acute and chronic schizophrenia
  
• acute delirious state
  
• Depression different etiology
  
• neuroses and anxiety in adults after failure of conventional therapies (for tablets of 50 mg)
  
• severe behavioral disorders (agitation, self-mutilation, stereotypes) in children older than 6 years, especially in combination with the syndrome of autism (for tablets of 50 mg).
  

Contraindications:

• Hypersensitivity to sulpiride or any other component of the drug
  
• prolaktinzavisimye tumors (eg pituitary gland prolactinomas and breast cancer)
  
• hyperprolactinemia
  
• acute poisoning with alcohol, hypnotics, narcotic analgesics
  
• affective disorders, aggressive behavior, mania, psychosis
  
• pheochromocytoma
  
• breastfeeding
  
• Children up to age 18 years (for tablets of 200 mg)
  
• Children under 6 years (for tablets of 50 mg)
  

in combination with:

• sultopride
  
• Antagonists of dopamine receptors: amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole (see "Interactions" section.).
  

Carefully

Not recommended for pregnant sulpiride purpose, except in cases when a doctor to weigh the risks and benefits for the pregnant woman and the fetus, decides that the use of the drug is needed.

Not recommended the appointment of sulpiride in combination with alcohol, levodopa, drugs capable of causing ventricular arrhythmias such as «torsade des pointes»: antiarrhythmics class Ia (quinidine, gidrohinidin, disopyramide) and class III (amiodarone, sotalol, dofetilide, Ibutilide) some antipsychotics ( thioridazine, chlorpromazine, Levomepromazine, trifluoperazine, tsiamemazin, amisulpride, tiaprid, pimozide, haloperidol, droperidol), other medications such as bepridil, cisapride, difemanil, I / erythromycin, mizolastine, I / vincamine, halofantrine, pentamidine, sparfloxacin, moxifloxacin etc.

Due to the presence of lactose drug, sulpiride is contraindicated in congenital deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.

Care should be exercised in the appointment of sulpiride in patients with renal and / or hepatic insufficiency, neuroleptic malignant syndrome (NMS), a history of epilepsy or seizures in history, severe heart disease, hypertension, Syndrome / Parkinson's disease, dysmenorrhea, in the elderly .

Application of pregnancy and breastfeeding:

Animal studies have not revealed teratogenic effects. A small number of women taking during pregnancy low dose sulpiride (approximately 200 mg / day), there was no teratogenic effect. With regard to the use of higher doses sulpiride data are not available. There is also the potential effect of these neuroleptic drugs taken during pregnancy on the development of the fetal brain. Hence, as a precaution sulpiride preferably not used during pregnancy.

However, when using this drug during pregnancy is recommended whenever possible to limit the dose and duration of treatment. Neonates whose mothers have received long-term treatment with high doses of neuroleptics, rarely observed gastrointestinal symptoms (bloating, etc.) associated with the m-anticholinergic effect of some drugs, especially in combination with antiparkinsonian agents and extrapyramidal syndrome.

In long-term treatment of the mother or the use of high doses, as well as in the case of the appointment of the drug shortly before delivery, reasonable control over the activity of the nervous system of both mother and newborn.

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

Side effect:

CNS: sedation, somnolence, dizziness, tremor, early dyskinesia (spasmodic torticollis, oculogyric crises, lockjaw), passing in the appointment of the central m-holinoblokatorov rarely - extrapyramidal syndrome and related disorders: akinesia, sometimes combined with muscle hypertonicity and It is partially eliminated in the appointment of the central m-anticholinergics, hyperkinesia, hypertonicity, motor agitation, akathisia.

Cases of tardive dyskinesia, characterized by involuntary rhythmic movements mainly language and / or persons with long courses of treatment that can be observed during the course of treatment by all antipsychotic drugs: the use of antiparkinsonian drugs is not effective or may cause worsening of symptoms.

With the development of hyperthermia, the drug should be discontinued, since increased body temperature may indicate the development of neuroleptic malignant syndrome.

From endocrine system: may develop reversible hyperprolactinemia, the most common manifestations of which are galactorrhea, amenorrhea, dysmenorrhea rarely - impotence and frigidity.

During treatment with sulpiride may experience excessive sweating, increased body mass index.

From the digestive system: increased activity of liver enzymes.

From the CCC: tachycardia may increase or decrease blood pressure in rare cases may develop orthostatic hypotension, QT prolongation very rare cases of the syndrome «torsade des pointes».

From the circulatory and lymphatic systems: hemolytic anemia, aplastic anemia, leukocytosis, thrombocytopenia purpura, granulocytosis.

Allergic reactions: possible skin rash.

Drug Interactions:

contraindicated combinations

Dopamine receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole), except for patients with Parkinson's disease

Between the dopamine receptor agonists and neuroleptics there is mutual antagonism. When extrapyramidal syndrome, neuroleptic induced not dopamine receptor agonists used in these cases use anticholinergics.

Sultoprid

Increased risk of ventricular arrhythmias, particularly atrial fibrillation.

Not recommended combinations

Drugs that can cause ventricular arrhythmias such as «torsade des pointes»: antiarrhythmics class Ia (quinidine, gidrohinidin, disopyramide) and class III (amiodarone, sotalol, dofetilide, Ibutilide), some antipsychotics (thioridazine, chlorpromazine, Levomepromazine, trifluoperazine, tsiamemazin, amisulpride, tiapride, haloperidol, droperidol, pimozide) and other drugs such as bepridil, cisapride, difemanil in / from erythromycin, mizolastine, in / etc vincamine

Alcohol

Alcohol increases the sedative effect of neuroleptics. Violation of attention creates a danger for driving and using machinery that require attention. consumption of alcoholic beverages should be avoided and the use of medicinal products containing alcohol.

Levodopa

Mutual antagonism between levodopa and neuroleptics. Patients with Parkinson's disease should be prescribed the lowest effective dose of both drugs.

Dopamine receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole) in patients with Parkinson's disease

Between the dopamine receptor agonists and neuroleptics there is mutual antagonism. The above drugs can cause or exacerbate psychosis. If you need neuroleptic treatment of the patient with Parkinson's disease and dopamine receptor antagonist receives, the latter should gradually reduce the dose until canceled (abrupt withdrawal of dopamine agonists may lead to the development of neuroleptic malignant syndrome).

Halofantrine, pentamidine, sparfloxacin, moxifloxacin

There is a growing risk of ventricular arrhythmias, in particular, «torsade des pointes». If possible, you should cancel the antimicrobial agent, causing ventricular fibrillation. If the combination is unavoidable, pre-check the QT interval and monitor ECG.

Combinations requiring caution

Drugs associated with bradycardia (BPC with bradycardic action: diltiazem, verapamil, beta-blockers, clonidine, guanfacine, cardiac glycosides cholinesterase inhibitors: donepezil, rivastigmine, tacrine, ambenonium chloride, galantamine, pyridostigmine, neomycin metilsulfat

There is a growing risk of ventricular arrhythmias, in particular, «torsade des pointes». It is recommended that clinical and cardiographic control.

Drugs that decrease in blood potassium concentration (kaliyvyvodyaschie diuretics, laxatives stimulating character, amphotericin B (w / w), corticosteroids, tetracosactide

There is a growing risk of ventricular arrhythmias, in particular, «torsade des pointes». Before the appointment of the drug should be removed hypokalemia, establish clinical and cardiographic control, and monitoring the concentration of electrolytes.

Combinations to be taken into account

antihypertensive drugs

Increased hypotensive action and increased the possibility of postural hypotension (additive effect).

Other means, CNS depressants: morphine derivatives (narcotic analgesics, antitussives and substitution therapy), barbiturates, benzodiazepines and other anxiolytics, hypnotics, sedatives, antidepressants, sedatives blocker of H1-histamine receptors, antihypertensives central action, baclofen, thalidomide

Inhibition of the CNS. Violation of attention creates a danger for driving and using machinery that require attention.

Sucralfate, antacids containing Mg2 + and / or A13 +, reduce bioavailability of dosage forms for oral administration of 20-40%. Sulpiride should be administered 2 hours prior to their admission.

Dosage and administration:

Inside, 1-3 times a day, drinking a small amount of liquid, regardless of the meal. It is not recommended to take the drug in the second half of the day (after 16 hours) due to the increased level of activity.

The goal of therapy - to reach the minimum effective dose.

200 mg Tablets

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

50 mg Tablets

Anxiety neurosis and in adults: the daily dose is from 50 to 150 mg for 4 weeks maximum.

Severe behavioral disorders in children older than 6 years: the daily dose is from 5 to 10 mg / kg body weight.

Dosages for the elderly: the initial dose should be 1 / 4-1 / 2 the adult dosage.

Doses for patients with impaired renal function. Due to the fact that up to 92% sulpiride excreted through the kidneys, it is advisable to reduce the dose sulpiride and / or increase the interval between the reception of individual doses, depending on the creatinine clearance rates (see Table..):

Creatinine clearance ml / min	The dose of sulpiride% standard	Increasing the interval between doses
30–60	70	1.5 times
10–30	50	2 times
<10	34	3 times

Overdose:

Symptoms. Experience with overdose is limited sulpiride. Specific symptoms are absent, can be observed: dyskinesia with spastic torticollis, and tongue protrusion lockjaw, blurred vision, increased blood pressure, sedation, nausea, extrapyramidal symptoms, dry mouth, vomiting, excessive sweating, and gynecomastia may develop CSN. In some patients - parkinsonism.

Treatment. Sulpiride partly removed by hemodialysis. In the absence of a specific antidote should be used symptomatic and supportive care with careful monitoring of respiratory function and constant monitoring of cardiac activity (risk of QT interval prolongation), which should continue until the full recovery of the patient holinoblokatory central action is prescribed for the development of extrapyramidal syndrome.

Special instructions:

Neuroleptic malignant syndrome: should cancel the development of hyperthermia of unknown etiology sulpiride, because this may be one of the symptoms of neuroleptic malignant syndrome, as described in the application of neuroleptics (pallor, hyperthermia, autonomic dysfunction, impaired consciousness, muscle rigidity).

Signs of autonomic dysfunction, such as sweating and labile blood pressure may precede the onset of hyperthermia and, therefore, represent the early warning signs. Although such action may have idiosyncratic neuroleptics origin, apparently certain risk factors can predispose to it, such as dehydration or organic brain damage.

Increased QT interval: QT interval lengthens sulpiride, depending on the dose. This action, which is known to increase the risk of developing a serious ventricular arrhythmia as «torsade des pointes», is more pronounced in the presence of bradycardia, hypokalemia, or congenital or acquired prolongation of the interval QT (combination with a drug that causes QT interval prolongation). If the clinical situation allows, it is recommended before prescribing the drug to ensure that there are no factors that could contribute to the development of this type of arrhythmia:

• Bradycardia with a heart rate less than 55 beats / min.
  
• hypokalemia
  
• Congenital long QT
  
• Simultaneous treatment of drug that can cause severe bradycardia (less than 55 beats / min.), Hypokalaemia, slowing of intracardiac conduction, or prolongation of the interval the QT.
  

Except for urgent intervention, patients who require treatment with neuroleptics, it is recommended to conduct the process of evaluating the status of the ECG. Apart from exceptional cases, this drug should not be used in patients with Parkinson's disease.

In patients with impaired renal function should use lower doses of sulpiride and strengthen control conducting intermittent courses of treatment is recommended in severe renal insufficiency.

Control the treatment of sulpiride should be strengthened:

• In patients with epilepsy, because the seizure threshold may be lowered
  
• In the treatment of elderly patients showing a greater sensitivity to postural hypotension, sedation and extrapyramidal effects.
  

During drug treatment Prosulpin prohibited from driving and operating machinery that require attention, as well as the use of alcohol or use medicines that contain alcohol.