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

Atypical antipsychotic agent (neuroleptic), also has antidepressant and antiemetic effect. Neuroleptic effect is associated with antidopaminergic 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. An increase in the amount of dopamine in the central nervous system is associated with an improvement in mood, 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.

In small doses sulpiride can be used as an auxiliary in the treatment of psychosomatic diseases, in particular, it is effective in stopping the negative mental symptoms of peptic ulcer and duodenal ulcer. In irritable bowel syndrome, the drug reduces the intensity of abdominal pain and leads to an improvement in the clinical state of the patient.

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

Pharmacokinetics:After intramuscular (IM) administration of 100 mg, the maximum concentration is 2.2 mg / L after 30 minutes. Connection with plasma proteins - no more than 40%. Quickly penetrates into the liver and nights, more slowly - into the brain tissue (the main amount of the drug accumulates in the pituitary gland). In the human body sulpiride only to a small extent is metabolized: 92% of the intramuscular dose administered is excreted unchanged in urine, by glomerular filtration. Full clearance 126 ml / min. The half-life of the drug is 7 hours. With breast milk, 0.1% of the daily dose is excreted.

Indications:

As a monotherapy or in combination with other psychotropic drugs:

- Acute and chronic schizophrenia;

- acute delirious states;

- Depression of various etiologies.

Contraindications:

- Acute poisoning with alcohol, hypnotics, analgesics;

- hypersensitivity to sulpiride or other ingredient of the drug,

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

- pheochromocytoma,

- manic psychosis, convulsive seizures, hyperprolactinaemia, affective disorders, aggressive behavior.

Contraindicated in combination with sultopride, dopaminergic receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropipirol), except for patients suffering from Parkinson's disease. 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).

Carefully:Epilepsy, arterial hypertension, dysmenorrhea, severe heart disease, angina pectoris, renal and / or hepatic insufficiency, a history of malignant neuroleptic syndrome, glaucoma, prostatic hyperplasia, urinary retention, and advanced 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 is contraindicated.

Dosing and Administration:

In acute and chronic psychoses, treatment is started with intramuscular injections at a dose of 400-800 mg / day and continues in most cases for 2 weeks. The goal of therapy is to achieve a minimally effective dose.

Depending on the clinical picture of the disease, intramuscular injections of sulpiride are prescribed 1-3 times a day, which allows you to quickly soften or numb the symptoms. As soon as the patient's condition allows, you should move on to taking the drug inside. The course of treatment is determined by the doctor.

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

From 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!

From the side of the cardiovascular system - tachycardia, it is possible to increase or decrease blood pressure, in rare cases, it is possible to develop orthostatic hypotension, fibrillar arrhythmias (ventricular arrhythmias of the "torsade de pointes" type).

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

Overdose:Symptoms: dyskinesia (spasm of chewing musculature, spasmodic torticollis), extrapyramidal disorders. In some cases - pronounced parkinsonism, coma.

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 Mg2 + and / or A13 +, reduce bioavailability by 20-40%. In extrapyramidal syndrome, induced by neuroleptics, do not use dopaminergic receptor agonists, but use anticholinergic drugs.

The risk of developing ventricular arrhythmias of the "torsade de pointes" type with simultaneous use with: antiarrhythmic drugs 1a class (quinidine, Dizopira-mid) and III class (amiodarone, sotalol, dofetilide, ibutilide), some neuroleptics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, tiapride, haloperidol, droperidol, pimozide), drugs that cause brady cardia (diltiazem, verapamil, beta-blockers, clonidine, guanfacine, preparations of digitalis, donepezil, rivastigmine, tacrine, ambenonium chloride, galantamine, pyridostigmine bromide, neostigmine bromide), drugs that cause hypokalemia (potassium-leading 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:

When prescribing the drug in patients with epilepsy before the start of treatment, a preliminary clinical and electrophysiological examination is necessary, since the drug reduces the threshold of convulsive activity.

With simultaneous treatment with drugs that increase the risk of developing ventricular arrhythmias, regular monitoring of the electrocardiogram is recommended. Elongation of the QT-interval is a dose-dependent effect.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Solution for intramuscular injection 50 mg / ml.

Packaging:2 ml per ampoule. 10 ampoules with instruction for use and a vial ampoule or scarifier ampullum are placed in a box of cardboard box.

Storage conditions:List B. In dry the dark place at a temperature of no higher than 30 0 С. Store in a place inaccessible to children.

Shelf life:3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-009306/08

Date of registration:24.11.2008

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

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp26.08.2015

Illustrated instructions

Instructions

Sulpiride (Sulpiride)