Sulpiride

Sulpiride refers to non-typical neuroleptics, which have a regulating effect on the central nervous system.

The drug has a weak antipsychotic effect, mixed with the psycho-stimulating process. It is also a moderate antidepressant. The chemical composition of sulpiride refers to benzamides, which are replaced by their structure. Such a group usually includes various drugs of psychotropic action.

When using a large dosage of the drug (about 600 mg), it has the effect of an antipsychotic, small dosages lead to the development of an antidepressant and stimulating therapeutic effect. Very low dosages help reduce the severity of dizziness.

Clinical and pharmacological group

Antipsychotic agent (antipsychotic) from the group of substituted benzamides.

Terms of sale from pharmacies

Can buyby prescription.

Price

How much does Amaryl cost in pharmacies? The average price is at the level of120 rubles.

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Composition and form of release

Tablets have a white color, a round shape and a flat-cylindrical surface.

• 1 tablet of the preparation Sulpiride contains 50 or 200 mg of the same active substance.

It also includes auxiliary substances, which include:

• Potato starch.
• Magnesium stearate.
• Lactose.
• Microcrystalline cellulose.
• Gelatin.
• Talc.

Tablets are packaged in a blister for 10 pieces. Cardboard pack contains 3 blisters (30 tablets), as well as instructions for the use of the drug.

pharmachologic effect

Among the main effects of the drug are:

• anti emetic effect;
• protection of the gastric mucosa;
• treatment of delusions and sleeplessness;
• treatment of depressive, as well as inhibited states.

Sulpiride has a moderate neuroleptic effect in combination with an activating and antidepressant effect. Neuroleptic effect is associated with an antidopaminergic effect. In the nervous system, Sulpirid inhibits only limbic dopaminergic receptors, and on the neostriatic the system has almost no effect; has an antipsychotic effect and causes a small number of adverse reactions. Peripheral action is based on the suppression of presynaptic receptors. With the increase in the amount of dopamine in the nervous system, the improvement of the psychoemotional state and mood is usually associated, with a decrease - the appearance of symptoms of depression.

1. Small doses of the drug, about 50-300 mg per day, are effective in dizziness, independent of causes, stimulate the release of prolactin and have an anti-emetic effect (central suppression of the center vomiting).
2. In small doses can be used as an additional tool in the therapy of psychosomatic diseases, for example, in the relief of undesirable mental reactions in peptic ulcer. With irritated intestines reduces the severity of abdominal pain and improves the patient's condition.
3. In a dose of up to 600 mg per day, the antidepressant and stimulating effect of the drug predominates, and in doses of 600 mg per day, its antipsychotic effect is manifested.

Does not affect adrenergic, serotonin, cholinergic, histamine receptors and GABA receptors (gamma-aminobutyric acid).

Pharmacokinetics

When administered orally, the maximum concentration of sulpiride in the plasma is reached after 3-6 hours. Bioavailability of the substance with oral administration is 25-35%, binding to plasma proteins is less than 40%. Concentration in the central nervous system is 2-5% of the concentration in the plasma. In the human body, when administered orally, sulpiride is not metabolized and is excreted through the kidneys almost unchanged (approximately 95%).

The half-life after oral administration is from 6 to 8 hours. In patients with moderate and severe renal failure, this indicator is significantly increased, so there is a need to reduce the dose and / or increase the interval between doses.

When intramuscular injection of sulpiride in a dose of 100 mg, the maximum concentration (mg / l) is reached after, hour. The substance quickly penetrates into the kidneys and liver, more slowly - into the brain tissue (accumulates mainly in the pituitary gland). Connection with plasma proteins - no more than 40%. The intramuscularly administered sulpiride is practically not metabolized: 92% of the dose is excreted unchanged in urine (by glomerular filtration). The half-life of sulpiride is 7 hours. The total clearance is 126 ml / min.

Sulpirid penetrates into breast milk (with intramuscular injection % of daily dose).

Indications for use

The drug is prescribed for such diseases:

• Phobias.
• Asthenic neurosis or neurasthenia.
• Obsessive-compulsive disorder - obsessive thoughts or actions.
• Dissociative disorders - dissociative disorders of movements and sensations.
• Somatoform disorders - physical disorders on moral grounds: VSD, neurosis of the heart, etc.
• Depression.
• Acute obscuration of consciousness.
• Acute schizophrenia.
• Static psychosis.
• Chronic schizophrenia.
• Neutrality of neuritis and neuralgia.
• Neurotic disorders:
• Dizziness or changes in stability associated with the work of the vestibular apparatus or caused by the following diseases:
• Neuritis of the vestibular nerve, craniocerebral lesions or Meniere's disease. otitis media, vertebrobasilar insufficiency.
• As an auxiliary preparation, sulpiride is prescribed for ulcers of the gastrointestinal tract or irritation of the duodenum.

Contraindications

Contraindications to taking the drug:

• galactosemia;
• pheochromocytoma;
• Acute poisoning with alcohol, analgesics or hypnotics;
• hypersensitivity to the components of the drug;
• Prolactin-dependent tumors (prolactinoma of the pituitary gland, breast cancer);
• deficiency of lactase or malabsorption syndrome of galactose / glucose;
• manic psychosis;
• convulsive seizures;
• aggression;
• affective disorders;
• hyperprolactinemia;
• pregnancy and lactation period;
• age to 14 years.

Sulpiride should be taken with caution to elderly patients, and also to those who suffer from the following diseases:

• epilepsy;
• angina pectoris;
• dysmenorrhea;
• glaucoma;
• malignant neuroleptic syndrome;
• arterial hypertension;
• hepatic / renal insufficiency;
• severe heart disease;
• hyperplasia of the prostate;
• retention of urine.

Intended use for pregnancy and lactation

Studies on animals have not revealed embryotoxic or fetotoxic effects of the drug, human experience shows similar results. However, due to the inadequacy of some data obtained during the study in humans, the use of sulpiride in pregnancy is recommended only with strict indications. After delivery, newborns should be further examined, since there are individual cases of extrapyramidal side effects.

Sulpirid penetrates into the milk of lactating women. Because the consequences are unclear, women should not breast-feed during treatment with this drug.

Dosage and route of administration

As indicated in the instructions for use, the dosage of Sulpirid and the method of use depends on the form of release.

Pills

Tablets are taken orally with a sufficient amount of liquid, regardless of food intake, in the first half (no later than 16 hours) of the day.

Treatment should begin with the appointment of a low dose of the drug, corresponding to the clinical condition of the patient. Then, gradually increasing, it is brought to the minimum effective dose.

Recommended dosing:

• chronic and acute psychotic disorders: adults - 200-1000 mg per day, divided into several receptions;
• anxiety conditions (symptomatic short-term therapy in the absence of the effect of conventional methods of treatment): 50-150 mg per day for 4 weeks;
• severe behavioral disorders in children older than 6 years, especially with autism syndrome (self-mutilation, agitation, stereotypes): at a rate of 5-10 mg per 1 kg of weight per day.

Solution for oral administration

The solution is taken orally, preferably in the morning, after shaking the contents of the vial.

Recommended dosing:

• chronic and acute schizophrenia, acute delirious psychosis: the initial dose (depending on the clinical indications) - 600-1200 mg per day, divided into several receptions. The maintenance dose may range from 300 to 800 mg per day;
• depression: 150-600 mg per day, divided into several doses;
• dizziness: 150-200 mg per day, to achieve the desired effect in severe conditions, the dose can be increased to 300-400 mg per day. Duration of treatment - 2 weeks or more;
• auxiliary therapy for irritable bowel syndrome, peptic ulcer of stomach and duodenum: 100-300 mg per day, the frequency of reception is 1-2 times.

The daily intake for adults should not exceed 1600 mg of sulpiride.

If the kidney function is impaired, you should lower the dose and / or increase the interval between taking the drug.

For children older than 14 years, the standard dose of the drug is 3-5 mg per 1 kg of body weight.

Capsules

Capsules are taken orally no later than 1 hour before and no earlier than 2 hours after eating.

Recommended daily dosing:

• schizophrenia: depending on the symptoms - 200-1200 mg divided into 2 doses, the maximum daily dose - 1200 mg;
• neurosis, psycho-functional disorders: 150-300 mg;
• Migraine, dizziness (Meniere's syndrome): 50-200 mg, course - not less than 2 weeks.

With peptic ulcer as an auxiliary therapy, the drug is taken at 50-100 mg 3 times daily for 2 months.

The dose for children from 6 years is 5-10 mg per 1 kg of body weight per day.

Older patients do not need to adjust the dosing.

Duration of treatment the doctor appoints individually, taking into account the patient's condition.

Side effect

Sulpiride is usually well tolerated, producing few side effects. In more than 1% of patients there are:

• hyperprolactinemia - increase in plasma levels of the hormone prolactin, which, in turn, leads to sexual dysfunction, galactorrhea, amenorrhea, gynecomastia and similar phenomena;
• nausea;
• vomiting;
• nasal congestion;
• anticholinergic side effects, such as: dry mouth, constipation, blurred vision;
• excited state;
• dizziness;
• headache;
• Extrapyramidal side effects: tremor, dystonia, akathisia - an increased sense of inner anxiety, parkinsonism.
• drowsiness - is manifested very smooth, given the lack of effect of the drug on alpha-1-adrenergic, histamine and muscarinic receptors;
• insomnia;
• increase or decrease in weight;
• violation of concentration and attention.

Rare, less than 1% of cases, side effects:

• Malignant neuroleptic syndrome is rare. The frequency of side effects increases with the concomitant use of drugs based on lithium salts.
• Late dyskinesia is rare. Often the disorder manifests itself in the form of early disorders, expressed in a constant disorder of the motor, but not more often than with antipsychotic drugs. The clinic is expressed by involuntary, repetitive and aimless movements of mimic muscles.
• Pathological changes in the blood system are rare. Sometimes life-threatening complications in this area arise in the case of a complex use of a number of different antipsychotics, especially clozapine.

Changes in the blood picture include, in this case:

• neutropenia;
• leukopenia;
• leukocytosis;
• convulsions;
• agranulocytosis - a significant drop in the number of leukocytes in the blood, increasing the risk of life-threatening opportunistic infections.

Extremely rare side effects include:

• depression;
• catatonia;
• palpitation;
• sweating without the condition of the preceding factor, for example, increased ambient temperature or physical stress;
• hypotension - low blood pressure;
• hypertension - high blood pressure;
• QTc prolongation interval on the ECG, which can lead to potentially fatal arrhythmias;
• cholestatic jaundice;
• increased serum levels of liver enzymes;
• primary biliary cirrhosis;
• allergic reactions;
• photosensitivity;
• skin rashes;
• venous thromboembolism.

Overdose

In case of an overdose, blurred vision, arterial hypertension, sedation, nausea, extrapyramidal symptoms, dry mouth, vomiting, increased sweating and gynecomastia, development of NZS. Symptomatic and supportive therapy is used.

special instructions

Before starting treatment, read the special instructions:

1. Use with caution in children.
2. During the treatment period, do not drink alcohol.
3. In the case of hyperthermia, which is one of the elements of the NSA, sulpiride should be immediately withdrawn.
4. With caution apply in patients with Parkinsonism, the elderly. In severe renal failure, a dose reduction or intermittent course of treatment is recommended.
5. In patients with epilepsy, a preliminary clinical and electrophysiological examination is necessary before starting therapy. Sulpiride lowers the threshold of convulsive readiness.
6. During the period of treatment, one should refrain from engaging in potentially dangerous activities requiring increased attention and rapid psychomotor reactions.

Interaction with other drugs

When prescribing the drug, it is necessary to take into account interactions with other drugs:

1. With simultaneous use with levodopa, the effectiveness of sulpiride decreases.
2. With simultaneous application with fluoxetine, extrapyramidal symptoms and dystonia may develop.
3. Cases of the development of severe extrapyramidal reactions are described with simultaneous application of sulpiride with lithium carbonate.
4. With the simultaneous use of drugs, oppressive central nervous system (opioid analgesics, hypnotics, tranquilizers, clonidine, antitussive drugs of central action), the oppressive effect on the central nervous system.
   With simultaneous use with antihypertensive drugs, antihypertensive effect is increased and the risk of orthostatic hypotension increases.

Reviews

We offer you to read reviews of people who used the drug:

1. Artem. He took the drug due to the fact that he suspected an exacerbation of stomach ulcers. I'll describe how I felt. After taking 50 mg 2 times a day in the morning and at lunch, you become emotionally more stable, what before could cause the excessive effect, (the child could fail because of his provocation), not so emotional become. Also noted the improvement in appetite, increases the potential for energy efficiency without emotional and motor arousal. Often I apply in clinical practice in patients who have undergone heart surgery, with short-term depressive episodes in the context of adaptation disorders.
2. Veronica. I used this drug to treat delirium, which arose in the daughter during the heat. Well, what can I say... People, this is a quiet horror! Even loud! Have you ever read the composition? How can I prescribe such a child? I believe that such a remedy acts very aggressively, as it provoked vomiting, and delirium did not take away either a little

Analogues

Structural analogs for the active substance:

• Betamax;
• Prosulfin;
• Sulpirid Belupo;
• Eglek;
• Eglonyl.

Before buying an analogue, consult your doctor.

Shelf life and storage conditions

Shelf life of Sulpirid tablets is 4 years. The preparation should be stored in the whole factory packaging, dark, dry, inaccessible to children at an air temperature of not more than +20 ° C.

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