Expiration date: 08/2027

Structure and Composition:

Tablets. One tablet contains 50 or 200 mg sulpiride

Excipients: milk sugar (lactose), gelatin, potato starch MCC talc magnesium stearate (magnesium stearate) - sufficient to produce tablets weighing 0.15 g or 0.4

in blisters of 10 pieces. in a stack of cardboard 3 packaging or in a dark glass banks to 30 pc. In the paper cartons 1 bottle.

A solution for intramuscular injection. 1 ml contains 50 mg sulpiride

Excipients: sodium chloride, sulfuric acid, 0.2 M solution Water for Injection

in 2 ml ampoules, complete with knife ampulnam in paper cartons of 10 vials.

Description pharmaceutical form:

Tablets: white or white with a slight yellowish tint.

Solution for i / m injection: clear, colorless or slightly colored liquid.

Pharmacokinetics:

When ingestion bioavailability is 27%. Binding to plasma proteins - less than 40%. The concentration of drug in the CNS - 2-5% of plasma concentrations.

The human body is not metabolized and excreted virtually unchanged through the kidneys. T1 / 2 is 6-8 hours.

T1 / 2 is significantly increased in patients with moderate to severe renal insufficiency. Such patients should reduce the dose and / or increase the interval between doses of the drug.

After the / m at a dose of 100 mg Cmax is reached after 30 min and was 2.2 mg / l. Quickly penetrates the liver and kidneys, slowly - in brain tissue (basic amount of drug accumulated in the pituitary gland). In humans, sulpiride only marginally subject to metabolism: 92% of the administered / m dose is excreted in the urine in unchanged form by glomerular filtration. Complete clearance - 126 ml / min. T1 / 2 of the drug is 7 hours. 0.1% of the daily dose is excreted in breast milk.

Description of the pharmacological actions:

Atypical antipsychotic (neuroleptic) also has antidepressant and antiemetic effect. Adjunct effect associated with antidofaminergicheskim action (mostly blocks dopaminergic receptors of the limbic system, the system acts on neostriatnuyu slightly).

Antipsychotic effect of sulpiride manifested at doses over 600 mg / day, in smaller doses (up to 600 mg / day) is dominated by stimulating and antidepressant effects. Sulpiride has no significant effect on the adrenergic, cholinergic, serotonin, histamine and GABA receptors.

In small doses sulpiride can be used as an adjunct in the treatment of psychosomatic diseases, in particular, it is effective in relieving the negative mental symptoms in gastric ulcer and duodenal ulcer. The syndrome Irritable bowel preparation reduces the intensity of abdominal pain and leads to an improvement of the clinical condition of the patient.

Low doses (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 vomiting center).

Indications:

As monotherapy or in combination with other psychotropic drugs in the following diseases and conditions:

• schizophrenia
  
• acute delirious state
  
• Depression different etiology.
  

Contraindications:

• sulpiride hypersensitivity to the drug or other ingredient
  
• acute poisoning with alcohol, hypnotics, analgesics
  
• manic psychosis
  
• seizures
  
• hyperprolactinemia
  
• affective disorder
  
• aggressive behavior
  
• prolactin-dependent tumors (eg pituitary gland prolactinomas and breast cancer)
  
• pheochromocytoma
  
• used in conjunction with sultopride, dopamine receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole), except in patients suffering from Parkinson's disease (see., "Interaction" field)
  
• pregnancy (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 necessary)
  
• lactation
  
• Children up to age 14 years.
  

For tablets additionally:

• galactosemia
  
• malabsorption syndrome glucose / galactose or lactase deficiency.
  

Carefully:

• epilepsy
  
• arterial hypertension
  
• dysmenorrhea
  
• severe heart disease
  
• angina
  
• renal and / or hepatic impairment
  
• neuroleptic malignant syndrome history
  
• glaucoma
  
• prostatic hyperplasia
  
• urinary retention
  
• elderly age.
  

Side effect:

Adverse events, developing as a result of receiving sulpiride, like adverse events caused by other psychotropic drugs, but some of them are less pronounced.

From endocrine system: may develop reversible hyperprolactinemia, which is the most common manifestations are galactorrhoea, menstrual disorders, rarely - gynecomastia, impotence and frigidity increased sweating, increased body mass index.

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

CNS: sedation, drowsiness, dizziness, headache, tremor, rarely - extrapyramidal syndrome, early and late dyskinesia, akathisia, oral automatism, aphasia. When used in small doses may agitation, anxiety, irritability, sleep disorders, visual acuity. With the development of hyperthermia, the drug should be discontinued, since increased body temperature may indicate the development of neuroleptic malignant syndrome (NMS).

Cardio-vascular system: tachycardia, increased or decreased blood pressure, rarely - the development of orthostatic hypotension, QT-interval lengthening rare - arrhythmia type «torsade de pointes».

Allergic reactions: possible skin rash, itching, eczema.

Drug Interactions:

Together with the application:

• Levodopa - reduced efficacy of sulpiride
  
• Antihypertensive drugs - enhanced their hypotensive effect and increased risk of orthostatic hypotension
  
• Drugs, CNS depressants (opioids, hypnotics and antianxiety drugs), clonidine, antitussive drugs of the central action - enhanced their inhibitory effect on the central nervous system.
  

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

Antagonism of dopamine receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole), and neuroleptics.

When extrapyramidal syndrome, neuroleptic induced without use of dopaminergic receptor agonists and anticholinergic drugs are used. If necessary, the treatment of patients with Parkinson's disease during treatment with agonists of dopaminergic receptors, the latter should reduce the dose gradually to a complete cancellation (abrupt withdrawal may lead to the development of neuroleptic malignant syndrome).

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

The risk of developing ventricular arrhythmias such as torsade de pointes, while the application:

• With antiarrhythmic drugs of class Ia (quinidine, disopyramide), and Class III (amiodarone, sotalol, dofetilide, Ibutilide)
  
• Some antipsychotics (thioridazine, chlorpromazine, Levomepromazine, trifluoperazine, tsiamemazin, amisulpride, tiaprid, haloperidol, droperidol, pimozide)
  
• Drugs that cause bradycardia (diltiazem, verapamil, beta-blockers, clonidine, guanfacine, digitalis drugs, donepezil, rivastigmine, tacrine, ambenonium chloride, galantamine, pyridostigmine, neostigmine bromide)
  
• Drugs that cause hypokalemia (kaliyvyvodyaschie diuretics, some laxatives, amphotericin B with a / in the introduction, the GCS tetrakozaktid)
  
• Bepridilom, cisapride, difemanila methyl sulfate, erythromycin (in / in the introduction), mizolastine, vincamine (in / in the introduction), halofantrine, pentamidine, sparfloxacin, moxifloxacin.
  

Dosage and administration:

Pills. Inside.

Acute and chronic schizophrenia, acute delirious psychosis: initial dose depending on the clinical picture of the disease and constitute 600-1200 mg / day, divided into several times maintenance doses - 300-800 mg / day.

Depression, from 150-200 mg to 600 mg / day, divided into several times.

Dizziness: 150-200 mg / day in heavy conditions the dose can be increased to 300-400 mg. Duration of treatment - at least 14 days.

Adjuvant therapy for stomach ulcers and duodenal ulcers, irritable bowel syndrome: 100-300 mg / day in 1 or 2 divided doses.

Dose in patients with impaired renal function

Due to the fact that sulpiride excreted primarily through the kidneys, it is advisable to reduce the dose and / or increase the interval between administration of the individual doses, depending on the performance of creatinine clearance:

Creatinine clearance ml / min	sulpiride dose compared to the standard,%	Increasing the interval between doses of sulpiride
30–60	70	1.5 times
10–30	50	2 times
less than 10	30	3 times

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

Doses for children: the standard dose for children over 14 years is 3-5 mg / kg body weight.

The solution for intramuscular injection

In acute and chronic psychoses: treatment starts with a dose of 400-800 mg / day / m and injection in most cases continued for 2 weeks. The goal of therapy - to reach the minimum effective dose.

Depending on the clinical picture of the disease in / m injection of sulpiride administered 1-3 times a day, allowing you to quickly mitigate or arrest the symptoms. As soon as the patient's condition allows, should move to the ingestion of the drug. The course of treatment is determined by the doctor.

Overdose:

Symptoms (common to both dosage forms): dyskinesia (spasm of the masticatory muscles, spasmodic torticollis), extrapyramidal disorders. In some cases - marked parkinsonism, coma.

When using the tablets may occur: blurred vision, hypertension, sedation, nausea, dry mouth, vomiting, excessive sweating, and gynecomastia, the CSN development.

Treatment: symptomatic. Appointment of centrally acting anticholinergics.

Special instructions:

In appointing the drug to patients with epilepsy before treatment is necessary to pre-clinical and electrophysiological examination, as the drug reduces the threshold for seizure activity.

With the simultaneous use of the drug with the medicines that increase the risk of ventricular arrhythmias is recommended that regular monitoring of the ECG. QT-interval lengthening - a dose-dependent effect.

Effects on ability to drive and operate machinery. During the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions.

Drinking alcohol while taking the drug is contraindicated.