Sulpiride, 100 mg 2 ml 10 pcs

Sulpiride is an atypical neuroleptic from the group of substituted benzamides.
Sulpiride has moderate neuroleptic activity in combination with stimulant and thymoanaleptic (antidepressant) effects.

The neuroleptic effect is associated with antidopaminergic action. In CNS, sulpiride blocks mainly dopaminergic receptors of limbic system, and it has little effect on neostriatal system, it has antipsychotic effect and causes a small number of side effects.

The peripheral effects of sulpiride are based on inhibition of presynaptic receptors. An increase in dopamine in the CNS is associated with an improvement in mood, and a decrease is associated with the development of symptoms of depression.

The antipsychotic effects of sulpiride are seen in doses greater than 600 mg/day, with stimulant and antidepressant effects predominating in doses less than 600 mg/day.

Sulpiride has no significant effect on adrenergic, cholinergic, serotonin, histamine and gamma-aminobutyric acid receptors (GABA receptors).

In low doses, sulpiride may be used as an adjunctive agent in the treatment of psychosomatic diseases, in particular, it is effective in relieving the negative psychiatric symptoms of gastric and duodenal ulcer disease. In irritable colon syndrome sulpiride reduces the intensity of abdominal pain and leads to improvement of the clinical condition of the patient.

Low doses of sulpiride (50-300 mg/day) are effective in dizziness, regardless of etiology. Sulpiride stimulates prolactin secretion and has a central antiemetic effect (inhibition of the vomiting center).

Pharmacokinetics

After oral administration, Cmax in plasma is reached after 1.5-3 hours. Bioavailability of sulpiride is 27%. Sulpiride binding to plasma proteins is less than 40%. Concentration of sulpiride in CNS is 2-5% of plasma concentration. Sulpiride is excreted with breast milk. Sulpiride is not metabolized in the human body and is excreted almost unchanged through the kidneys. T1/2 is 6-8 h. T1/2 is significantly increased in patients with moderate to severe renal impairment up to 20-26 h after IV administration. Such patients should reduce the dose of sulpiride and/or increase the interval between doses of the drug.

Indications

As monotherapy or in combination with other psychotropic drugs.

• acute and chronic schizophrenia
• acute delirium
• depressions with various etiologies
• depressions of various etiologies
• neurotic disorders.
• depressions of various etiology;
• neurotic disorders;
• dizziness of various etiologyDizziness of various etiologies (vertebro-basilar insufficiency, vestibular neuritis, Meniere’s disease, the state after craniocerebral trauma, otitis media);
• accompanitory therapy for gastric and duodenal ulcers and irritable bowel syndrome.

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Active ingredient

Sulpiride

Composition

1 ml of solution for intramuscular injection contains:

acting substances:

sulpiride 50 mg;

auxiliary substances:

Sodium chloride, 0.38 mg;

sulfuric acid (0.2 M solution) – to pH 4-6;

water for injection – up to 1 ml

How to take, the dosage

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

Depending on the clinical picture of the disease, intramuscular injections of sulpiride are administered 1-3 times a day, which allows rapid relief or resolution of symptoms. As soon as the patient’s condition allows, it is necessary to switch to taking the drug orally. The course of treatment is determined by the doctor.

Interaction

Simultaneous administration of sulpiride and CNS depressant drugs (narcotic analgesics, antihistamines, barbiturates, benzodiazepines and other anxiolytics) may increase the sedative effect of these drugs.
Combination of sulpiride with alcohol may also increase the sedative effect of alcohol.
Concomitant administration with levodopa should be avoided because of mutual antagonism of levodopa and sulpiride.
There is an increased risk of orthostatic hypotension when sulpiride and antihypertensive agents are taken concurrently.
Sucralfate, antacids containing Mg2+and/or Al3+ reduce bioavailability by 20-40%.

Antagonism with dopaminergic receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, pyribedil, pramipexole, quinagolide, ropinirole) and neuroleptics. In extrapyramidal syndrome induced by neuroleptics, dopaminergic receptor agonists are not used but anticholinergic medications are. If it is necessary to treat patients with Parkinson’s disease against the background of using dopaminergic receptor agonists, the dose of the latter should be gradually reduced until complete withdrawal (abrupt withdrawal may lead to the development of malignant neuroleptic syndrome).

The risk of ventricular arrhythmias such as “torsade de pointes” when used simultaneously with: Class 1a (quinidine, hydroquinidine, disopyramide) and Class III (amiodarone, sotalol, dofetil, ibutilide) antiarrhythmic drugs, some neuroleptics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, thiapride, haloperidol, droperidol, pimozide), bradycardia-inducing drugs (diltiazem, verapamil, beta-blockers, clonidine, guanfacine foxglove drugs, donepizil, rivastigmine, tacrine, ambenonium chloride, galantamine, pyridostigmine, neostigmine), drugs causing hypokalemia (potassium withdrawing diuretics, some laxatives, Amphotericin B w/v, GCS, tetracosactide) and others (including bepridil, cisapride, difemanil, erythromycin intravenously, misolastin, vincamine w/v, halofantrine, pentamidine, sparfloxacin, moxifloxacin).

Special Instructions

If hyperemia occurs during treatment with Sulpiride Belupo should be discontinued. Hyperemia may be a sign of malignant neuroleptic syndrome (manifested by hyperthermia, dyskinesia, autonomic disturbances) described during treatment with neuroleptics. Although there are no data on the development of the syndrome during treatment with Sulpiride Belupo, caution is necessary, especially when prescribing high doses of the drug.

When Sulpiride Belupo is prescribed to patients with epilepsy, a prior clinical and electrophysiologic evaluation should be performed before starting treatment, because the drug reduces the seizure threshold.

Impact on driving and operating machinery

During treatment, driving and operating machinery requiring increased attention and drinking alcohol are prohibited.

Contraindications

• acute alcohol poisoning, sleeping pills, analgesics;
• sensitivity to sulpiride; pheochromocytoma;
• epilepsy;
• prolactin-dependent tumors (including breast cancer);
• hyperprolactinemia;
• period of breastfeeding;
children under 14 years of age;
• Parkinson’s disease;
• galactosemia;
• glucose/galactose malabsorption syndrome or lactase deficiency.

With caution: precautions should be taken when prescribing sulpiride to patients with impaired renal function because up to 95% of sulpiride is excreted through the kidneys. It is recommended to reduce the dose of sulpiride in these patients; precautions should also be observed when prescribing sulpiride in patients with heart disease, blood vessel disease, angina pectoris, arterial hypertension, hepatic failure, history of malignant neuroleptic syndrome, epilepsy, glaucoma, prostatic hyperplasia, urinary retention, young women with irregular menstrual cycle, elderly patients.

Side effects

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

Endocrine system disorders: reversible hyperprolactinemia may develop, the most frequent manifestations of which are galactorrhea, menstrual cycle disorders, less frequent – gynecomastia, impotence, and frigidity.

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

CNS disorders: sedative effect, somnolence, dizziness, dizziness, headache, tremor, rarely – extrapyramidal syndrome, early and late dyskinesia, akathisia, oral automatism, aphasia. When used in low doses, psychomotor agitation, anxiety, irritability, sleep disturbance, visual acuity may occur. If hyperthermia develops, the drug should be discontinued, because increased body temperature may indicate the development of neuroleptic malignant syndrome (NMS).

Cardiovascular system disorders: tachycardia, possible increase or decrease of blood pressure, in rare cases development of orthostatic hypotension, prolongation of the QT interval, rarely, “pirouette”-type arrhythmia.

Allergic reactions: skin rash, itching, eczema are possible.

During treatment with sulpiride increased sweating and weight gain may be noted.

Overdose

Symptoms (common for both dosage forms): dyskinesia (spasm of masticatory muscles, spastic torticollis), extrapyramidal disorders. In some cases – pronounced parkinsonism, coma.

Treatment: symptomatic. Administration of choline blockers of central action.

Pregnancy use

Prescribing sulpiride to pregnant women is not recommended unless the physician, after assessing the balance of benefits and risks for the pregnant woman and the fetus, decides that the use of the drug is necessary.

Breastfeeding should be stopped during treatment with the drug.

Similarities

Eglonil, Sulpiride, Sulpiride-Belupo